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Cyanidin-3-O-galactoside chloride (Ideain chloride) is a component from extract peel of hawthorn fruit (EPHF) with the value of 179.4 mg/g. EPHF exhibits strong AChEinhibitoryactivity .
Transketolase-IN-3 is a potent transketolase (TK)inhibitor. Transketolase-IN-3 has herbicidal activity and has inhibitory effects against Digitaria sanguinalis (DS) and Amaranthus retroflexus (AR). Transketolase-IN-3 can be used for the research of herbicides .
BChE-IN-19 (Compound 7b) is a para-substituted derivative of indone (7b) with inhibitoryactivity of butyryl cholinesterase (BChE) (IC50=0.04 μM). BChE-IN-19 improves cholinergic scheduling in the nervous system. BChE-IN-19 can be used against Alzheimer's disease .
Schiarisanrin A (Kadsulignan J) is a lignan with inhibitoryactivity on NO production. Schiarisanrin A inhibits NO production in BV-2 cells with an IC50 of 9.6 μM .
Withanoside V (Standard) is the analytical standard of Withanoside V. This product is intended for research and analytical applications. Withanoside V, a withanolide glycoside, exhibits inhibitoryactivity for tachyphylaxis to Clonidine in isolated guinea-pig ileum .
Kadsulignan H (compound 13) is a lignan with inhibitoryactivity on NO production. Kadsulignan H inhibits NO production in BV-2 cells with an IC50 of 14.1 μM .
Methyl 4-O-caffeoylquinate is an extract naturally
derived from the leaf ofIlex paraguariensis. Methyl
4-O-caffeoylquinate has human neutrophilic elastase (HNE) inhibitoryactivity
.
Cyanidin-3-O-galactoside (chloride) (Standard) is the analytical standard of Cyanidin-3-O-galactoside (chloride). This product is intended for research and analytical applications. Cyanidin-3-O-galactoside chloride (Ideain chloride) is a component from extract peel of hawthorn fruit (EPHF) with the value of 179.4 mg/g. EPHF exhibits strong AChE inhibitoryactivity .
Danshenol B is a diterpenoid. Danshenol B has strong aldose reductase (AR) inhibitoryactivity with IC50 value of 0.042μM. Danshenol B can be used for the research of diabetic related complication resulted by metabolic abnormality, such as cataracts, retinopathy, neuropathy, and nephropathy .
3,4,5-Trihydroxycinnamic acid decyl ester is an excellent inhibitor of lipid absorption and accumulation, with anti-obesity properties. 3,4,5-Trihydroxycinnamic acid decyl ester is a pancreatic lipase inhibitor, with an EC50 of approximately 0.9 μM .
Antitumor agent-55 (compound 5q) is a potent antitumor agent. Antitumor agent-55 effectively inhibits PC3, with an IC50 of 0.91 μM. Antitumor agent-55 effectively inhibits the colony formation, suppresses the cell migration in PC3. Antitumor agent-55 induces G1/S phase arrest and apoptosis in PC3 .
Benzisothiazolone is an isothiazolone fungicide. Benzisothiazolone has growth inhibitingactivity against E. coli ATCC 8739 and saccharornyces pombe NCYC 1354. Benzisothiazolone can be used in the study of growth inhibition model .
Benzisothiazolone (Standard) is the analytical standard of Benzisothiazolone. This product is intended for research and analytical applications. Benzisothiazolone is an isothiazolone fungicide. Benzisothiazolone has growth inhibitingactivity against E. coli ATCC 8739 and saccharornyces pombe NCYC 1354. Benzisothiazolone can be used in the study of growth inhibition model .
Tuberculosis inhibitor 10 shows moderate inhibitory effect on the enzymatic activity of MSMEG_6649. Tuberculosis inhibitor 10 enhances the inhibitoryactivity of PAS against mycobacteria .
(S)-PF 03716556 is a K+-competitive acid blocker with gastric acid pump inhibitoryactivity. (S)-PF 03716556 can be used to inhibit disease states mediated by acid pump inhibitoryactivity .
FR-202306 is a compound with antibacterial and peptide deformylase inhibitoryactivities, isolated from microorganisms, which has an inhibitory effect on the peptide deformylase of Staphylococcus aureus and also has antibacterial activity.
Licoagrochalcone C, a flavonoid, reveals efficacious inhibitoryactivity on NF-κB transcription. Licoagrochalcone C shows significant inhibitoryactivity on LPS (HY-D1056)-induced NO production .
ARM1 (4BSA) is a potent aminopeptidase and epoxide hydrolaseinhibitor. ARM1 shows aminopeptidase inhibitoryactivity with an IC50 7.61 µM and epoxide hydrolase inhibitoryactivity with an IC50 12.4 µM .
JAK2/TYK2-IN-2 is a potent and selective TYK2inhibitor with IC50 values of 9 and 157 nM for TYK2 and JAK2, respectively. JAK2/TYK2-IN-2 has anti-inflammatory activity .
Necroptosis-IN-4, a potent necroptosisinhibitor, is a RIP kinase 1 (RIPK1)inhibitor. Necroptosis-IN-4 has no inhibitoryactivity against RIPK3 and weak inhibitoryactivity against VEGFR1/2 and PDGFR-α .
Gastric Inhibitory Polypeptide (1-30), porcine lacks the C-terminal 12 amino acid residues of natural gastric inhibitory polypeptide (GIP), exhibits biologic activity by potentiating the release of insulin and somatostatin .
Fusion Inhibitory Peptide (Z-D-Phe-Phe-Gly-OH, FIP, Virus Replication Inhibitory Peptide) is a potent inhibitor of the virus replication, by inhibiting the membrane fusing activity of a viral glycoprotein .
NE58018 is a compound with bone resorption inhibitoryactivity. NE58018 exerts its effect by affecting the action of Farnesyl pyrophosphate synthase (FPPS). The structural features of NE58018 combined with aminophosphonates significantly enhance its inhibitoryactivity. NE58018 affects the roles of Thr201 and Tyr204 residues in substrate binding and catalysis. The interaction of NE58018 enhances the inhibitory effect on the target enzyme .
Artanin is a coumarin, has biological activities related to Alzheimer’s disease. Artanin exerts function including AChEinhibitory and AChE- and self-induced amyloid beta (Aβ) aggregation inhibitoryactivities, with IC50s of 51 μM, 98 μM, and 124 μM, respectively .
BTK-IN-7 is a potent and selective inhibitor of BTK (IC50=4.0 nM). BTK-IN-7 has high selectivity in both enzymatic (ITK >250-fold, EGFR >2500-fold) and cellular levels (ITK >227-fold, EGFR 27-fold). BTK-IN-7 also has potent antitumor activity .
HDAC8-IN-8 (15a) is an HDAC8 inhibitor, with IC50 values of 23.9 μM and 268.2 μM for hHDAC8 and smHDAC8 respectively. And for hHDAC1 and hHDAC6, the IC50 values are 12.1 μM and 2.9 μM respectively. HDAC8-IN-8 can be used in schistosomiasis-related research .
Calceolarioside B is a natural product isolated from Akebia quinata leaves. Calceolarioside B exhibits significant inhibitoryactivity against rat lens aldose reductase (RLAR) with an IC50 of 23.99 μM. Calceolarioside B displays inhibitory effect on DPPH radical scavenging activity with an IC50 of 94.60 μM .
(S)-KT109 is an inhibitor of diacylglycerol lipase β (DAGLβ) with low inhibitoryactivity (IC50 = 39.81 nM). (S)-KT109 has relatively low inhibitoryactivity against DAGLα-mediated hydrolysis of 1-stearoyl-2-arachidonoyl-sn-glycerol (IC50 = 794.3 nM). (S)-KT109 also has relatively low inhibitoryactivity against α/β-amidase domain-containing 6 (ABHD6) (IC50 = 630.9 nM) .
Licopyranocoumarin is an isoflavonoid that shows CYP3A4inhibitoryactivity with an IC50 of 32 μM. Licopyranocoumarin has potent neuroprotective activities .
Ethybenztropine hydrochloride (Ponalid hydrochloride) is an anticholinergic drug with antiparkinsonian activity. Ethybenztropine hydrochloride may also have dopamine reuptake inhibitory effects. Ethybenztropine hydrochloride is used to improve motor symptoms in patients with Parkinson's disease. Ethybenztropine hydrochloride exerts its inhibitory effects by regulating the balance of neurotransmitters .
A variety of compounds were designed and synthesized by modifying cap groups. The enzyme inhibition test showed that compound 12C had broad-spectrum enzyme inhibitoryactivity, and compounds 9m and 9q were more inclined to inhibit HDAC6, showing a certain selective inhibitoryactivity among the representative subtypes.
Cryptosporiopsin A, a polyketide with antifungal activity, exhibits motility inhibitory and lytic activities against zoospores of the grapevine downy mildew pathogen Plasmopara viticola .
Ro 18-5364 is an inhibitor of gastric (H? + K?)-ATPase, which has the effect of inhibiting the activity of the enzyme. Ro 18-5364 has a very strong inhibitory effect on gastric mucosal (H? + K?)-ATPase, and the inhibitory effect is more significant at low pH. At the same time, there is no selectivity difference between the two enantiomers of (H? + K?)-ATPase, and its inhibitory effect can be studied and verified by a variety of experimental methods, including inhibition of enzyme activity, proton transport, and studies on its binding.
4-Nitrobenzofuroxan is an antiviral compound with HIV-1 inhibitoryactivity. 4-Nitrobenzofuroxan also exhibits an inhibitory effect on IDO1. The application potential of 4-Nitrobenzofuroxan lies in its ability to be used to inhibit viral infection .
Hoquizil hydrochloride is a novel bronchodilator with oral activity, demonstrating phosphodiesterase inhibitory effects and potential for modulation of smooth muscle contraction.
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ)inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitoryactivity against other phosphatases, with only modest inhibitoryactivity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration .
STAT3-IN-19 (compound 31) is a BRAF(V600E) inhibitor that has the function of inhibiting BRAF(V600E) activity. Its inhibitory mode and activity were determined through relevant screening and structural studies, and it has an inhibitory effect on MAPK signaling in melanoma cells.
Polyphemusin II-Derived Peptide (T140), a CXCR4inhibitor, shows high inhibitoryactivity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4 .
(+)-Nipecotic acid ((+)-β-Homoproline) is a GABA transport inhibitor with potential antidepressant and anxiolytic activities. (+)-Nipecotic acid can increase the concentration of GABA in the synaptic cleft, thereby enhancing inhibitory neurotransmission. The research on (+)-Nipecotic acid provides a possible direction for the development of new inhibitory compounds for psychiatric diseases .
Microginin 527 is a linear cyanobacterial peptide with potent angiotensin-converting enzyme (ACE) inhibitoryactivity. Microginin 527 also exhibits inhibitory effects on protein phosphatases and leucine aminopeptidase. With an IC50 value of 31 μM, Microginin 527 is the most active component in this class of compounds .
Phenazoviridin is a free radical scavenger. Phenazoviridin shows strong inhibitoryactivity against lipid peroxidation in rat brain homogenate and exhibits antihypoxic activity in mice .
Anguinomycin A is an antibiotic that exhibits good inhibitoryactivity against G. boninense with an MIC value of 5 µg/disk. Anguinomycin A has antitumor activity .
Antimalarial agent 46 (Compound 42a) is an antimalarial agent with antimalarial activity. Antimalarial agent 46 shows inhibitoryactivity against P. falciparum lines .
Streptovitacin A is a compound with antibacterial and antiproliferative activities isolated from microorganisms, which has inhibitory effects on a variety of bacteria and tumor cells.
Antibiotic AC4437 is a compound with antimicrobial activity isolated from specific soil microorganisms and has an inhibitory effect on Bacillus subtilis.
CM026 is a selective aldehyde dehydrogenase 1A1 inhibitor with submicromolar inhibitoryactivity against aldehyde dehydrogenase 1A1. Its inhibitory mechanism is related to binding to the aldehyde binding pocket and utilizing a unique glycine residue. It can be used as a chemical tool to study the role of this enzyme in disease.
Vormatrigine is an orally active sodium channelinhibitor with anti-epileptic activity. Vormatrigine has a specific inhibitory effect on overactive NaV channels in vitro and has a good inhibitory effect in the maximal electroconvulsive seizure (MES) model. Vormatrigine can be used to study human focal and generalized epilepsy .
LF 1695 is an immunomodulator. LF 1695 enhances the proliferative response of T cells by increasing the production of IL2 (interleukin-2) or the expression of the IL2 receptor. LF 1695 also increases CONA-induced inhibitoryactivity in human lymphocytes. LF 1695 can be used to study the proliferative and inhibitoryactivity of T cell subpopulations, as well as their role in immune regulation .
Tyropeptin A-4 (TP-101) is a potent proteasome inhibitor with the ability to inhibit mammalian 20S proteasome activity. Tyropeptin A-4 exerts its inhibitory effect by binding to the site responsible for trypsin-like activity. Tyropeptin A-4 derivative TP-104 has a 20-fold increase in inhibitoryactivity over Tyropeptin A. TP-110 specifically inhibits trypsin-like activity without affecting PGPH and trypsin-like activity .
1,3-Dipalmitoleoyl glycerol (DG(16:1/0:0/16:1)) is a compound isolated from sea cucumber viscera, which has α-glucosidase inhibitoryactivity and has different degrees of inhibitory effects on α-glucosidase from different sources.
GK241 (compound 31a-c) is a 2-oxoamide-based compound that has inhibitoryactivity against human and mouse group IIA secretory phospholipase A2 (GIIA sPLA2) (IC50 of 143 nM and 68 nM, respectively), and its inhibitory mechanism was studied by molecular dynamics simulation.
Valiolamine is an aminocyclitol. Valiolamine has potent alpha-glucosidase inhibitoryactivity against porcine intestinal sucrase, maltase and isomaltase .
PHYLPA-8 is an inhibitor for DNA polymerase-α, which exhibits weak inhibitoryactivity for the stereochemistry of the fatty acid moiety and the cyclic phosphate .
Saptomycin D is an antibiotic with antitumor activity isolated from the Streptomyces sp. HP530 strain. Saptomycin D exhibits potent inhibitory effects against Gram-positive bacteria, while demonstrating weaker inhibitoryactivities against certain Gram-negative bacteria and yeasts. Saptomycin D also displays remarkable antitumor properties. Saptomycin D is applicable in research within the field of oncology .
Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR)inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment .
Methylpiperic acid is a piperine alkaloid with significant MAO inhibitoryactivity (IC503.6 μM). Methylpiperic acid is less effective against MAO-B (IC 501.6 μM) than MAO-A (IC5027.1 μM) has a bidirectional inhibitory effect. Methylphenidate is used to treat mental disorders .
Apterin is a natural compound with anti-inflammatory activity. Apterin shows significantly inhibitoryactivity on NO production in RAW264.7 cells with an IC50 value of 41.8 μM .
Arcapillin is a flavonoid that can be isolated from Artemisia capillaris Thunb. Arcapillin has antispasmodic activity. Arcapillin also has moderate PTP1Binhibitoryactivity .
Aculene D, a fungal metabolite, shows quorum sensing (QS) inhibitoryactivity against Chromobacterium violaceum CV026, and could significantly reduce violacein production in N-hexanoyl-l-homoserine lactone (C6-HSL) induced C. violaceum CV026 cultures at sub-inhibitory concentrations .
Antibacterial agent 175 (compound Y40), a ML346 (HY-18669) analog, is a Sortase A (SrtA)inhibitor. Antibacterial agent 175 shows inhibitoryactivity on Staphylococcus aureus SrtA and shows inhibitory effects on biofilm formation. Antibacterial agent 175 is an antivirulence agent against S. aureus infections .
Camellianin B, a flavonoid compound, is a Camellianin A metabolite. Camellianin B has antioxidant and angiotensin converting enzyme (ACE)inhibitoryactivities .
Rubinaphthin A is a naphthohydroquinone that can be found in the roots of Rubia yunnanensis. Rubinaphthin A exhibits inhibitoryactivity against tobacco mosaic virus (TMV) .
Lyciumin A, a cyclic octapeptide, exhibits inhibitoryactivity on proteases, renin and angiotensin-converting enzyme. Lyciumin A can be used for the research of hypertension .
Tinospinoside C is a bioactive?clerodane diterpene glycoside compound. Tinospinoside C shows inhibitoryactivities of NO production with an IC50 value of 218 μM .
(+)-Epieudesmin is an antineoplastic agent. (+)-Epieudesmin has marginal cancer cell line inhibitoryactivities. (+)-Epieudesmin inhibits the growth of Gram-negative pathogen .
FaX-IN-1 (compound 11A) is an intermediate in the preparation of FaXinhibitors and was used to study the inhibitoryactivity against venous thrombosis in rats .
Quipazine maleate is a 5-HT agonist that causes behavioural changes such as hyperactivity. Quipazine maleate also shows a weak reversible MAOinhibitoryactivity .
(+)-Xylariamide A (compound 6b) is a mycobacterial and fungal carbonic anhydrase probe with inhibitoryactivity against pathogen β-carbonic anhydrases .
Hellicoside is a natural product that can be obtained from plantain. Hellicoside has inhibitoryactivity against cAMP phosphodiesterase and 5-lipoxygenase .
Calceolarioside B (Standard) is the analytical standard of Calceolarioside B. This product is intended for research and analytical applications. Calceolarioside B is a natural product isolated from Akebia quinata leaves. Calceolarioside B exhibits significant inhibitoryactivity against rat lens aldose reductase (RLAR) with an IC50 of 23.99 μM. Calceolarioside B displays inhibitory effect on DPPH radical scavenging activity with an IC50 of 94.60 μM .
Sinulatumolin E (compound 6), a terpenoid, displays significant TNF-αinhibitoryactivity with an IC50 of 3.6 μM. Sinulatumolin E (compound 6) exhibits anti-inflammatory activity .
MBX2329, a potent influenza virus inhibitor, specifically inhibits hemagglutinin (HA)-mediated viral entry with HIV/HA(H5) displaying IC90 of 8.6 μM. MBX2329 inhibits a wide spectrum of influenza A viruses, which includes the 2009 pandemic influenza virus A/H1N1/2009, highly pathogenic avian influenza (HPAI) virus A/H5N1, and oseltamivir-resistant A/H1N1 strains .
Enocyanin is an anthocyanin extracted from grapes. Enocyanin shows inhibitory effect on the leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase and esterase activity .
Osmanthuside B can be isolated from Pseuderanthemum carruthersii (Seem.) Guill. var. atropurpureum (Bull.) Fosb and has weak acetylcholinesterase inhibitoryactivity .
Psychotridine is a natural alkaloid isolated from Psychotria colorata, reveals an analgesic activity in nervous system and an inhibitory efficacy towards platelet aggregation .
Massarigenin C is a compound that can be isolated from Massarina tunicata. Massarigenin C has inhibitoryactivity against Bacillus subtilis (ATCC 6051) .
Decarestrictine D exhibits inhibitoryactivity against cholesterol levels. Decarestrictine D is utilized as receptor for glycosylation reactions to synthesize novel hybrid antibiotics .
Napitane (A 75200) is a groundbreaking catecholamine uptake inhibitor that exhibits inhibitory effects on α-adrenergic receptors and shows promise for antidepressant activity in depression research.
Leucosceptoside A is a phenylethanoid glycoside with anti-hyperglycemic and anti-hypertensive activities. Leucosceptoside A shows inhibitoryactivity against α-glucosidase and PKCα (IC50 of 19.0 μM) .
JANEX-1 (WHI-P131) is a potent and specific JAK3inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitoryactivity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
Limochromin is a pigment produced by Streptomyces limosus that strongly inhibits the reverse transcriptase of avian myeloid leukemia virus (AMV). The inhibitoryactivity of limochromin is not affected by changes in the concentration of template-primer, substrate or carrier protein, but its inhibitory effect is significantly reduced when the concentration of AMV reverse transcriptase increases. Limochromin can be used to develop antiviral treatments .
Chlorambucyl-proline is a chloroplatinyl amino acid derivative with inhibitoryactivity against bovine pulmonary vasoconstrictor enzyme. Chlorambucyl-proline reacts with the convertase in a 1:1 ratio, and the removal of its radiolabel indicates that the compound has an irreversible inhibitory effect on the enzyme activity. Chlorambucyl-proline binds to the aspartic acid or glutamic acid side chain of the enzyme by forming an ester bond, resulting in irreversible inactivation of the enzyme. The inactivation rate constant of chlororambucyl-proline increases in the pH range of 5-8, indicating that its effect on the enzyme activity is affected by the pH environment .
(+)-Medioresinol Di-O-β-D-glucopyranoside is a lignan glucoside with strong inhibitoryactivity of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterase .
Diplacol ia a natural compound from from Mimulus clevelandi and shows potent inhibitoryactivities against lipopolysaccharide (LPS)-induced nitric oxide production .
Scirpusin B (compound 5) is a dimeric antioxidant isolated from Scirpus maritimus L.. Scirpusin B exhibits antitumor, antifungal, insecticidal, and plant growth inhibitoryactivities.
PD 140248 hydrochloride is a quinolone broad-spectrum antibacterial agent with good in vitro bacteriostatic activity, especially having a significant inhibitory effect on Gram-positive bacteria .
Deschloro-Zopiclone is an impurity of Zopiclone. Zopiclone is the first non-benzodiazepine compound, which can enhance the activity of inhibitory neurotransmitter gamma amino butyric acid in the brain .
Benzamidine is a reversible competitive trypsininhibitor with a Ki of 19 μM . Benzamidine shows inhibitoryactivity against homogeneous boar sperm acrosin with a Ki of 4 μM .
Trifolirhizin is a pterocarpan flavonoid isolated from the roots of Sophora flavescens. Trifolirhizin possesses potent tyrosinaseinhibitoryactivity with an IC50 of 506 μM . Trifolirhizin exhibits potential anti-inflammatory and anticancer activities .
Rabelomycin is antibiotic, which exhibits antimicrobial activity against gram positive bacteria. Rabelomycin exhibits inhibitoryactivity against inducible nitric oxide synthase (iNOS) with an IC50 of 63.9 μM .
Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitoryactivities.
RK-286D is an antibiotic and a PKCinhibitor with antimicrobial activity. RK-286D shows inhibitoryactivities against bleb formation induced by PDBu (HY-18985) and in vitro PKCactivity .
Ofloxacin (Hoe-280) is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase. Ofloxacin shows inhibitoryactivity against vaccinia virus (VV).
Terphenyllin is a naturally abundant p-terphenyl metabolite isolated from the coral derived fungus Aspergillus candidus, has significant α-glucosidaseinhibitoryactivity .
Cefepime hydrochloride is a cephalosporin antibiotic agent. Cefepime hydrochloride has inhibitoryactivity against human serum paraoxonase-1 (hPON1) with an IC50 value of 21.115 mM .
Minimolide F is a sesquiterpene lactone. Minimolide F has inhibitoryactivity against human nasopharyngeal cancer cells. Minimolide F can be used for the research of cancer .
Phebestin is a compound with antimalarial activity that has an inhibitory effect on Plasmodium and has shown good results in in vitro and in vivo experiments. It can also bind to related enzymes of Plasmodium.
(S,S)-Dehydroemetine is an antispasmodic compound with inhibitoryactivity on smooth muscle. (S,S)-Dehydroemetine can be used to inhibit diseases related to smooth muscle contraction .
Bovinic acid sodium is a fatty acid (FA) extracted from the Indonesian coix seed (C. lacryma-jobi) variety Agrotis. Bovinic acid sodium is an insecticide with inhibitoryactivity against Leptinotarsa ??decemlineata .
Luotonin A is an antiviral and antiphytopathogenic fungus agent. Luotonin A has good antiviral activity against tobacco mosaic virus (TMV). Luotonin A also has certain inhibitoryactivity on topoisomerase I and topoisomerase II. Luotonin A shows antitumor activity .
These compounds have strong hdac and hsp90inhibitoryactivities. Compound 20 (HDAC ic50 = 194 nm; Hsp90 α < b> Ic50 = 153 nm) and compound 26 ((HDAC ic50= 360 nm; Hsp90 α < b> Ic50 = 77 nm) shows the strongest HDAC and HSP90 α Inhibitoryactivity. Both compounds can induce hsp90 expression and down regulate hsp90 client proteins, which play an important role in regulating the survival and invasion of cancer cells.
mTOR inhibitor-25 is an enzyme inhibitor that is more selective than PI3K and has good anticancer activity. mTOR inhibitor-25 shows strong inhibitory effects on mTOR and may be used to study leukemia, skin cancer, breast cancer, lung cancer and colon cancer. mTOR inhibitor-25 showed excellent activity in cell proliferation experiments, but its inhibitory ability on PI3K was relatively weak .
Kushenol B is an isoprenoid flavonoid isolated from S. flavescens, has antimicrobial, anti-inflammatory and antioxidant activities . Kushenol B has inhibitoryactivity against cAMP phosphodiesterase (PDE), with an IC50 of 31 µM .
HDAC/BET-IN-1 displays submicromolar inhibitoryactivity against HDAC1 and 6 (IC50 = 0.163 μM and 0.067 μM), and BRD4 (Ki = 0.076 μM), and possess potent antileukemia activity.
FtsZ-IN-2 (Compound 19) is an inhibitor of the bacterial cell division protein FtsZ with GTPase inhibitoryactivity. FtsZ-IN-2 exhibits anti-staphylococcal activity with MIC values of 2 µg/ml for MSSA and MRSA .
MurA-IN-3 is a reversible pyrrolidinedione-based MurAinhibitor. MurA-IN-3 has inhibitoryactivity for MurA with an IC50 value of 4.5 μM. MurA-IN-3 also has antibacterial activity .
Strictamine (compound 2) is an alkaloid with antiviral activity. Strictamine has significant inhibitoryactivity against herpes simplex virus (HSV) and adenovirus (ADV), with EC50 values ??of 0.36 μg/mL and 0.28 μg/mL, respectively .
1-Docosanol (Behenyl alcohol) is a saturated fatty alcohol with reported inhibitoryactivity against lipid-enveloped viruses, including herpes simplex virus (HSV) .
Escin IB is a saponin isolated from skin and the endosperm of seeds of horse chestnut (Aesculus hippocastanum). Escin IB shows inhibitory effect on pancreatic lipaseactivity .
N-Caffeoyl O-methyltyramine is a class of alkaloid isolated from Cuscuta reflexa with strong inhibitoryactivity against α-glucosidase (IC50 of 103.58 μM) .
Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitoryactivity toward methicillin-resistant Staphylococcus aureus (MRSA) .
Lonicerin is an anti-algE (alginate secretion protein) flavonoid with inhibitoryactivity for P. aeruginosa. Lonicerin prevents inflammation and apoptosis in LPS-induced acute lung injury .
Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities .
Neochlorogenic acid methyl ester (5-O-Caffeoylquinic acid methyl ester) is an HBVinhibitor. Neochlorogenic acid methyl ester can be isolated from L. japonica flower buds with potent HBV inhibitoryactivity .
DNA polymerase-IN-3 (Compd 5b) is a coumarin derivative that exhibits inhibitoryactivity against Taq DNA polymerase and can be used in proliferative disease research .
6',7'-Epoxybergamottin is a metabolism of Penicillium digitatum. 6',7'-Epoxybergamottin can be used in study the cytochrome P450 3A4inhibitoryactivity .
Thiolopyrrolone A (compound 1) exhibits antibacterial activities against BCG, M. tuberculosis and S. aureus with minimum inhibitory concentrations (MIC) of 10, 10 and 100 μg/mL, respectively .
Sodium iodoacetate is a specific inhibitor of GAPDH and has glycolysis inhibitoryactivity. In addition, sodium iodoacetate can induce osteoarthritis and related pain models in experimental animals .
15-epi-Danshenol A is a diterpenoid with an immune-modulating activity. 15-epi-Danshenol A shows inhibitory effect on B lymphoblasts cells in a concentration-dependent manner .
Bassianin is a compound isolated from fungi that has the activity of inhibiting erythrocyte membrane ATPase and causing cell lysis. Its inhibitory effect on ATPase may be due to membrane disruption.
YAP/TAZ inhibitor-4 (Compound 45) is an inhibitor of YAP/TAZ, exhibiting TEAD transcriptional activation inhibitoryactivity by suppressing the binding of YAP or TAZ to TEAD .
Antimycin A2 is the component of the antibiotic antimycin A. Antimycin A is an antibiotic, that exhibits inhibitoryactivity against fungi and some insects through inhibition of respiration and cytochrome b reoxidation .
1650-M15 is an inhibitor of lipoteichoic acid synthase (LtaS). It has inhibitoryactivity against Gram-positive bacteria but has no significant inhibitory effect against Gram-negative bacteria. The IC50s of 1650-M15 against MRSA and MSSA are 62.44 μM and 66.42 μM, respectively, and the MICs are both 200 μM .
Brevianamide F (Cyclo(L-Pro-L-Trp)) is a mycotoxin isolated from Colletotrichum gloeosporioides, with antibacterial activity. Brevianamide F shows potent PI3Kαinhibitoryactivity with an IC50 of 4.8 μM .
5-Hydroxyoxindole is a structural analog of uric acid. 5-Hydroxyoxindole has DPPH radical scavenging activities and lipid peroxidation-inhibitoryactivities. 5-Hydroxyoxindole can be used for the research of oxidative stress-mediated disorders .
Talaromycesone A is an oxaphenalenone dimer compound. Talaromycesone A exhibits potent antibacterial activities with an IC50 of 3.70 μM, against human pathogenic Staphylococcus strains. Talaromycesone A displays potent acetylcholinesterase inhibitoryactivities with an IC50 of 7.49 μM .
(R)-tert-OMe-byakangelicin is a kind of furanocoumarin, which has inhibitoryactivity to liver drug metabolizing enzyme (DME) activity. (R)-tert-OMe-byakangelicin can be isolated from immature fruits of Angelica sinensis .
Lucidadiol is a natural compound isolated from Ganoderma lucidum. Lucidadiol exhibits acetylcholinesterase-inhibitory activity, with IC50 values of 31 μM. Lucidadiol shows antiviralactivity against influenza virus type A and HSV type 1 .
Makaluvamine A is a member of Makaluvamines. Makaluvamines can be isolated from Fijian sponges of the genus Zyzzya, and possess inhibitoryactivity toward topoisomerase II along with cytotoxic activity against HCT-116 human colon cancer cells .
Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinaseactivity. Taxifolin exhibits significant inhibitoryactivity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Eperezolid(PNU-100592) is a oxazolidinone antibacterial agent, Eperezolid demonstrated good in vitro inhibitoryactivity, regardless of methicillin susceptibility for staphylococci(MIC90= 1-4 mg/ml).
Monobehenin, an bacterial biofilm formation inhibitor, has strong inhibitoryactivity toward bacterial biofilm formation of S. mutans, X. oryzae, and Y. enterocolitica in a strain specific manner .
Quercetin 3-O-(6''-O-galloyl)-β-D-glucoside (Tellimoside) is a flavonol glycoside with strong inhibitoryactivity against the growth of Microcystis aeruginosa .
Considerable studies confirmed that BRD4 inhibition ameliorated kidney injury and fibrosis ，and ZLD2218 exhibited the most potent inhibitoryactivity against BRD4, with the IC50 value of 107 nM
Herpotrichone A shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.41 μM.
NOSO-502 is an inhibitor of bacterial translation. NOSO-502 exhibits inhibitoryactivity against Enterobacteriaceae. NOSO-502 has good safety and antibacterial properties .
Dalbergioidin, a well-known anthocyanin, ameliorates doxorubicin-induced renal fibrosis by suppressing the TGF-β signal pathway. Dalbergioidin exhibits tyrosinase inhibitoryactivity with an IC50 of 20 mM .
Persiconin is a tyrosinase Inhibitor. Persiconin can be isolated from Prunus persica. Persiconin has tyrosinase inhibitoryactivity of 46% at 500 μM. Persiconin can be used in whitening research .
Drechslerine A has neuraminidaseinhibitoryactivity (IC50: 0.79 μM). Drechslerine A is a terpene that can be isolated from endophytic Cochliobolus. Drechslerine A can be used for research of Influenza Virus .
Pisiferic acid is an antibacterial agent with inhibitoryactivity against Gram-negative/positive bacteria such as P. vulgaris, S. aureus and B. subtilis. Pisiferic acid can be used to study bacterial infections .
Carbonic anhydrase inhibitor 16 (compound 1) is a dengue protease inhibitor with inhibitoryactivity against carbonic anhydrasehCA I and hCA II (Ki: 28.5 nM, 2.2 nM) .
Crocapeptin C is a cyclic depsipeptide that can be extrated from Melittangium boletus. Crocapeptin C exhibits potent inhibitoryactivity against chymotrypsin with an IC50 value of 0.5 µM .
Plipastatin A1 is a lipopeptide with enzyme inhibitory and immunosuppressive activities. Plipastatin A1 is found in Bacillus cereus and inhibits phospholipase A2 (PLA2), PLC, and PLD .
Firefly luciferase-IN-4 (CID: 3987260) is an inhibitor of ATP-dependent luciferase (Firefly luciferase). It has nM-level inhibitoryactivity (pIC< sub>50=6.5) .
Hyalodendrin ((+)-Hyalodendrin) is a fungal growth inhibitor with inhibitoryactivity against wood decay fungi. Hyalodendrin has low phytotoxicity, with an acute toxicity (LD50) of 75 mg/kg in mice .
Methylsticin (Standard) is the analytical standard of Methylsticin. This product is intended for research and analytical applications. Methylsticin is a kavalactone isolated from the Piper methysticum . Methylsticin exhibit osteoclast formation inhibitoryactivity .
Militarine (Standard) is the analytical standard of Militarine. This product is intended for research and analytical applications. Militarine, a glycosidic compound isolated from Bletilla striata, exhibits plant growth-inhibitoryactivity .
Stemoninine is a lycoris alkaloid that can be used as an antitussive. Stemoninine has significant inhibitoryactivity against human acetylcholinesterase (AChE) (IC50=5.52 μM) .
Flavanone (Standard) is the analytical standard of Flavanone. This product is intended for research and analytical applications. Flavanone is a naturally occurring flavone. Flavanone has inhibitoryactivity for human estrogen synthetase (aromatase) .
Antibiotic SF-2132 is a peptide antibiotic identified in Nocardiopsis sp., which exhibits inhibitoryactivity against β-lactam antibiotic-resistant strains, such as Pseudomonas and Escherichia .
LY-99335 is an anesthetic antagonist with behavioral inhibitoryactivity. LY-99335 exhibits large dose separation at specific doses, indicating its potential in anesthetic antagonism .
Topiroxostat (Standard) is the analytical standard of Topiroxostat. This product is intended for research and analytical applications. Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR)inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment .
Lagunamycin is a 5-lipoxygenase inhibitor isolated from the culture medium of Streptomyces sp. AA0310. Lagunamycin has a significant inhibitoryactivity against rat 5-lipoxygenase with an IC50 value of 6.08 μM. Lagunamycin can effectively inhibit 5-lipoxygenase without causing lipid peroxidation, indicating that it has an effective inhibitory effect without causing side effects.
4'-Methoxy-S-trityl-L-cysteinol is an allosteric inhibitor of vertebrate Kinesin Spindle Protein (KSP). 4'-Methoxy-S-trityl-L-cysteinol significantly enhances its inhibitoryactivity against NCI60 tumor cells by modifying the trityl and cysteine groups. Its EC50 for bipolar spindle formation is 28 μM, showing stronger inhibitory potency than the parent molecule and monastrol.
KN-92 hydrochloride is an inactive derivative of KN-93, without CaM kinase inhibitoryactivity. KN-92 hydrochloride is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93 .
LSN 3213128 is a selective, nonclassical, orally bioavailable antifolate with potent and specific inhibitoryactivity for aminoimidazole-4-carboxamide ribonucleotide formyltransferase (AICARFT), with IC50 of 16 nM for AICARFT enzyme inhibiton and 19 nM in cells. Anti-tumor activity .
Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitoryactivity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria .
Pectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is a dual inhibitor of COX-2/5-LOX. Anti-inflammatory activity . Pectolinarigenin has potent inhibitoryactivities on melanogenesis .
Nocardicin A is a beta-lactam antibiotic with selective antibacterial activity. Nocardicin A has moderate antibacterial activity against a broad spectrum of Gram-negative bacteria including Proteus and Pseudomonas; it has no inhibitory effect on Staphylococcus, Mycobacterium, fungi, and yeast .
ORG 33628 is a potent and selective progesterone receptor modulator. ORG 33628 shows anti-progestational and anti-glucocorticoid activity. ORG 33628 shows ovulation-inhibitoryactivity. ORG 33628 has the potential for the research of breast and endometrium .
Dihydrodiol-Ibrutinib (PCI-45227) is a dihydrodiol active metabolite of Ibrutinib (HY-10997), has inhibitoryactivity towards BTK approximately 15 times lower than that of ibrutinib .
Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis. Enrofloxacin monohydrochloride shows inhibitoryactivity against vaccinia virus (VV).
Herpotrichone B shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.11 μM.
Phaeosphaone D is a thiodiketopiperazine alkaloid compound isolated from Phaeosphaeria fuckelii, an endophytic fungus. Phaeosphaone D displays mushroom tyrosinase inhibitoryactivity with an IC50 value of 33.2 μM .
Sorbifolin, a flavone glucoside, can be isolated from the Pterogyne nitens. Sorbifolin has myeloperoxidase inhibitory and radical scavenging activities. Sorbifolin is also a MPOinhibitor with an IC50 value of 19.2 nM .
4-Chlorocinnamic acid has inhibitory effects on tyrosinase. 4-Chlorocinnamic acid has antibacterial activity. 4-Chlorocinnamic acid also inhibitsColletotrichum gloeosporioides growth .
Acetyl-binankadsurin A (compound 5) is a lignan isolated from Kadsura longipedunculata. Acetyl-binankadsurin A has low inhibitoryactivity against HIV-1 protease, with IC50 >100 μg/mL .
Aloveroside A is a triglucosylnaphthalene derivative isolated from ethanolic extract of aloe vera. Aloveroside A has weak bACE inhibitoryactivity (inhibition rate at a dose of 100 μg/mL is approximately 18.68%) .
Kagimminols A is a cembrene-type diterpenoids and can be isolated from an Okeania sp. marine cyanobacterium. Kagimminols A shows selective growth-inhibitoryactivity against the causative agent of human African trypanosomiasis .
Hippeastrine hydrobromide is an active alkaloid that exhibits a good dose-dependent inhibitory effect on topoisomerase I (Top I) with an IC50 of 7.25 μg/mL. Hippeastrine hydrobromide exhibits antiproliferative and anticancer activities.
(S)-Ladostigil (TV-3279), the S-enantiomer of TV 3326 (HY-10399), is a ChEinhibitor with poor MAO-B inhibitoryactivity. (S)-Ladostigil has neuroprotective effect
Ro 24-6392 is an ester-linked co-drug combining Ciprofloxacin (HY-B0356) and Desacetylcefotaxime (HY-126129) with inhibitoryactivity against a variety of aerobic bacteria in vitro.
Benzenesulphonamide (Standard) is the analytical standard of Benzenesulphonamide. This product is intended for research and analytical applications. Benzenesulphonamide (compound 1) is a potent carbonic anhydrase inhibitor. Benzenesulphonamide shows CA II inhibitoryactivity .
Saframycin S is an antibiotic with a racemomycin group that exhibits inhibitoryactivity against Ehrlich ascites tumors. The LD50 of Saframycin S in ddY mice is 3.2 mg/kg (i.p.) .
(±)-Taxifolin ((±)-Dihydroquercetin) is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinaseactivity. Taxifolin exhibits significant inhibitoryactivity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
8-Methylsulfinyloctyl isothiocyanate, an isothiocyanate, has antimicrobial activity and remarkable inhibitoryactivity against plant growth . 8-Methylsulfinyloctyl isothiocyanate impair COX-2 mediated inflammatory responses in LPS stimulated raw macrophages .
CNX-500 is a probe consisting of a covalent Btkinhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitoryactivity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn .
(-)-Taxifolin is the less active enantiomer of Taxifolin. Taxifolin exhibits important anti-tyrosinaseactivity. Taxifolin exhibits significant inhibitoryactivity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Mulberroside F is one of the main bioactive constituents in mulberry (Morus alba L.) . Mulberroside F shows inhibitory effects on tyrosinaseactivity and on the melanin formation. Mulberroside F also exhibits superoxide scavenging activity that is involved in the protection against auto-oxidation .
Nopol is a quinoline derivative based on nopol that has inhibitoryactivity against the asexual blood stage of Plasmodium falciparum. Derivatives with different structures have different activities against different Plasmodium strains, and some derivatives have submicromolar EC50 values in specific strains.
Dihydrofuran-3(2H)-one (3-Oxotetrahydrofuran) can be used to synthesize cyclic ketone inhibitors that inhibit the serine protease plasmin and increase its inhibitoryactivity .
T-705RMP, a phosphorylated metabolite of T-705, exhibits a very weak inhibitory effect on the IMP dehydrogenase (IMPDH) activities of the host cells, with an IC50 of 601 μM .
Ilexoside O is a triterpene saponin isolated from the roots of Ilex pubescens. Ilexoside O exhibits weak xanthine oxidase (XOD)inhibitoryactivity (IC50=53.05 μM) .
3-Methylcarbazole is an carbazole alkaloid compound with anticancer effects. 3-Methylcarbazole shows growth inhibitoryactivity (IC50 of 25 μg/mL) on human fibrosarcoma HT-1080 cells .
Bim-IN-1 is a potent Bim expression inhibitor. Bim-IN-1 reduces Bim expression levels and has little inhibitory effect upon protein kinase A activity and minimal toxicity .
4'-Deoxyphlorizin is an inhibitor of the glucose transport system. 4'-Deoxyphlorizi has good phlorizin hydrolaseinhibitoryactivity with the Km value of 0.59 nM and the Ki value of 0.33 nM, respectively .
Curcolonol is a furan type sesquiterpene. Curcolonol can be isolated from several medical herbs. Curcolonol has inhibitoryactivity for LIM kinase 1. Curcolonol can be used for the research of breast cancer .
Bradykinin potentiator B (Bradykinin potentiating peptide B) is venom of Agkistrodon halys blomhoffi. Bradykinin potentiator B is a potent ACEinhibitor. Bradykinin potentiator inhibits the activity of bradykinin inhibitory peptidase .
BRD0476 is an inhibitor of pancreatic β-cell apoptosis with an EC50 value of 0.78 μM and a maximal inhibitoryactivity of 99%. BRD0476 can be used in diabetes-related research .
Aranciamycin (Compound 1) is an anthracycline antibiotic with collagenase inhibitoryactivity (IC503.7*10-7M). Aranciamycin can be used to inhibit DNA synthesis in tumor cells .
Kanshone B (Compound 5) is isolated from the
natural Nardostachys chinensis. Kanshone B shows inhibitoryactivity against LPS-induced NO production (IC50=11.5 μM)
.
Chloramultilide B is a lindenane dimer that can be isolated from Chloranthus serratus. Chloramultilide B has inhibitoryactivities against Candida albicans and C.parapsilosis with a MIC value of 0.068 μM .
Indanomycin is an antibiotic of the pyrroloketoindane class, which includes an unusual indane ring structure. It has bactericidal activity against Gram-positive bacteria, with minimum inhibitory concentration (MIC) values of ≤0.2 μg/mL.
Firefly luciferase-IN-3 (CID: 17087944) is an inhibitor of ATP-dependent luciferase (Firefly luciferase) and has nM-level inhibitoryactivity against NanoLuc (pIC50=7.5) .
JM 1397 is an antibacterial agent that exhibits potent antibacterial activity against both methicillin-susceptible and methicillin-resistant Staphylococcus aureus with a minimum inhibitory concentration (MIC90) of 1 μg/mL . .
Araloside A (Standard) is the analytical standard of Araloside A. This product is intended for research and analytical applications. Araloside A (Chikusetsusaponin IV) is a component of Panax japonicus, with low-renin-inhibitoryactivity, with an IC50 of 77.4 μM .
DL-Homocysteine thiolactone (hydrochloride) (Standard) is the analytical standard of DL-Homocysteine thiolactone (hydrochloride). This product is intended for research and analytical applications. DL-Homocysteine thiolactone hydrochloride is a cyclic amino acid derivative that exhibits root-growth inhibitoryactivity.
ICI 186756 is a compound that inhibits the activity of human neutrophil elastase, has a competitive inhibitory effect on the enzyme, can inhibit enzyme-induced lung changes, and can also modulate hamster lung lesions.
Bromperidol decanoate (Standard) is the analytical standard of Bromperidol decanoate. This product is intended for research and analytical applications. Bromperidol decanoate (R46541) is a compound used for the inhibition of schizophrenia and has certain clinical inhibitoryactivity.
ts-SA is a carbonic anhydrase (CA) inhibitor with activity against seven human CA homologues. ts-SA can bind to the Zn(II) ion in the enzyme active site in a deprotonated form. The organic skeleton of ts-SA extends in the enzyme cavity and participates in multiple interactions with amino acid residues and water molecules. Due to its structural differences, the inhibitory performance of ts-SA is significantly better than that of another pyridine derivative. ts-SA exhibits low nanomolar inhibitoryactivity and is a multi-target CA inhibitor .
Sandosaponin A (Soyasaponin Bd) is a saponin with inhibitoryactivity against human recombinant aldehyde reductase (hAKR1B1). Sandosaponin A can inhibit the reduction of l-idose and 4-hydroxynonenal to varying degrees. The presence of Sandosaponin A reveals the challenges posed by the masking effect of conventional aldehyde reductase inhibitors in mixtures when exploring differential aldehyde reductase inhibitors. The inhibitory mechanism of Sandosaponin A may be related to its mode of action on different substrates .
TANDEM (Des-N-tetramethyltriostin A) is a synthetic antibiotic drug that has the activity of inhibiting the growth of tumor cells. TANDEM can be used in combination with chemotherapy to enhance the inhibitory effect. TANDEM has shown significant inhibitory effects on a variety of cancer cell lines in in vitro experiments. The structure of TANDEM allows it to effectively target tumor cells during the inhibition process. TANDEM's mechanism of action involves interfering with cell proliferation and survival pathways .
Evodol is a natural product isolated from the dried and nearly ripe fruits of Euodia rutaecarpa. Evodol shows inhibitoryactivity against NO production . Evodol possesses larvicidal activity against the Asian tiger mosquitoes with a LC50 value of 32.43 μg/ml .
Norchelerythrine is an alkaloid isolated from the roots of Zanthoxylum capense with antibacterialactivity against gram-positive and gram-negative bacteria. Norchelerythrine exhibits inhibitoryactivity against Staphylococcus aureus, Pseudomonas aeruginosa, and Enterococcus faecalis and Escherichia coli with MIC values >50 µg/mL .
Procaine benzylpenicillin (Penicillin G procaine) is an antimicrobial agent. Procaine benzylpenicillin shows inhibitoryactivity against gram-positive bacteria and synergistic activity with Neomycin (HY-B0470). Procaine benzylpenicillin can be used in the study of bovine mastitis in animal husbandry .
ACHN-975 is a selective LpxCinhibitor and exhibits a subnanomolar LpxC inhibitoryactivity. ACHN-975 is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL) .
Acetyllovastatin, a acetate of Lovastatin, presentes a moderate inhibitory effect against the enzyme acetylcholinesterase with an IC50 of 79 μg/mL. Lovastatin has been found to display antifungal activity, and suppresses proliferation of a number of transformed cell lines .
Chlormidazole hydrochloride is an antifungal agent and has inhibitoryactivity against many fungi and some gram-positive cocci. Chlormidazole hydrochloride can be applied in fungal and bacterial infections of nails and skin, including interdigital and periungual mycoses .
Cassiaside C (Toralactone 9-O-β-D-gentiobioside) is a naphthopyrone isolated from the seed of Cassia tora and has inhibitoryactivity on advanced glycation end products (AGE) formation in vitro .
MsbA-IN-3 (compound 31) is a potent and highly selective MsbAinhibitor with an IC50 value of 2 nM. MsbA-IN-3 has inhibitoryactivity against Escherichia coli with a MIC of 35 μM .
MsbA-IN-4 (compound 32) is a potent and highly selective MsbAinhibitor with an IC50 value of 3 nM. MsbA-IN-4 has inhibitoryactivity against Escherichia coli with a MIC of 12 μM .
Ar524 has higher inhibitoryactivity than the known transgenic inhibitor kifunensine. At the same time, ar524 inhibited low concentration (10 μ M) Spheroid formation of human malignant cells.
Urease-IN-5 is an inhibitor of urease with an IC50 value of 1.473 µM. Urease-IN-5 has low cytotoxicity and inhibitoryactivity on P. vulgaris with an IC50 value of 17.78 µg/mL .
Ganoderenic acid K is a natural product, that can be isolated from fruiting bodies of Ganoderma lucidum. Ganoderenic acid K shows strong inhibitoryactivity against HMG-CoA reductase (HMGCR) with IC50 of 16.5 μM .
BMAP-27 is an antimicrobial peptide capable of disrupting the membrane integrity of microorganisms. Due to its membrane permeability, MAP-27 has inhibitoryactivity against both bacteria and cancer cells .
Acantrifoside E (Compound 8) is a nature compound. Acantrifoside E can be isolated from the 90% ethanol extract of Salacia cochinchinensis. Acantrifoside E has none α-glucosidase inhibitoryactivity .
N-cis-Feruloyl tyramine (cis-N-(4-Hydroxyphenethyl) ferulamide) is a natural phenolic compound, exhibits modest inhibitoryactivity on LPS-activated NO production in RAW 264.7 cells .
Low molecular weight protamine is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitoryactivity. Low molecular weight protamine can inhibit tumor growth and is used in cancer research .
Dehydroperilloxin is a natural compound isolated from the dichloromethane extract of the stems of Perilla frutescens var. acuta. Dehydroperilloxin possesses inhibitoryactivity against cyclooxygenase-1, with the IC50 value of 30.4 μM .
Kagimminol B, a cembrene-type diterpenoid, can be isolated from an Okeania sp. marine cyanobacterium. Kagimminol B shows selective growth-inhibitoryactivity against the causative agent of human African trypanosomiasis .
Tetrahydrobostrycin is a secondary metabolite from Aspergillus sp., which exhibits a weak inhibitoryactivity against Staphylococcus aureus and Escherichia coli (100 mg/disc with the inhibition zones of 15 and 9.2 mm in diameter) .
Hippeastrine hydrobromide is an active alkaloid that exhibits a good dose-dependent inhibitory effect on topoisomerase I (Top I) with an IC50 of 7.25?μg/mL. Hippeastrine hydrobromide exhibits antiproliferative and anticancer activities .
S-(+)-Marmesin (Standard) is the analytical standard of S-(+)-Marmesin. This product is intended for research and analytical applications. S-(+)-Marmesin is a natural coumarin, exhibiting COX-2/5-LOX dual inhibitoryactivity.
Fmoc-D-Thi-OH (Fmoc-D-2-Thienylalanine) is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize AS-Z-P with thrombin inhibitoryactivity .
Fmoc-5-Ava-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize fatty acid-based dimeric peptides with PSD-95 inhibitoryactivity .
HMGB1-IN-3 (compound E) is a glycyrrhizic acid derivative with strong inhibitoryactivity against HMGB1 (high mobility group protein 1) and can be used in the study of intracerebral hemorrhage .
FBPase-IN-3 (compound 45) is a FBPase (fructose-1,6-bisphosphatase)inhibitor with an IC50 of 2.08 μM. FBPase-IN-3 exhibits potent inhibitoryactivity of gluconeogenesis .
3'-Fluorobenzylspiperone maleate is a ligand for dopamine D2 receptors with activity in improving behavioral disorders. 3'-Fluorobenzylspiperone maleate showed better inhibitory effects than placebo, especially in reducing behavioral disorders .
(S)-3'-Aminoblebbistatin is the derivative of Blebbistatin (HY-13813). (S)-3'-Aminoblebbistatin exhibits inhibitoryactivity against myosin II with an IC50 of 14.1 µM .
ABT-518 is a matrix metalloproteinaseinhibitor with anti-tumor activity. ABT-518 has potent inhibitory effects on gelatinase A and gelatinase B, which can inhibit tumor growth and metastasis .
IST-622 (6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin) is an anti-tumor agent with significant growth inhibitoryactivity. IST-622 exhibits significant anti-tumor effects against a variety of mouse tumors such as P388 and L1210 leukemias, B16 melanoma, Lewis lung carcinoma, Colon 26 and Colon 38 adenocarcinomas, and M5076 reticulum cell sarcoma. IST-622 was orally administered and the results showed efficacy in different tumor types. In addition, IST-622 provided significant inhibitory effects against two human tumor xenograft models: large cell lung carcinoma (Lu-116) and gastric adenocarcinoma (St-4). IST-622 also exhibited significant growth inhibitoryactivity against P388 leukemia in vitro, with a half inhibitory concentration (IC50) more than 20 times lower than CT .
Antifungal agent 66 (compound 10) has antifungal activity. Antifungal agent 66 has a broad-spectrum antifungal activity against seven phytopathogenic fungal mycelia. Antifungal agent 66 has pronounced inhibitoryactivity against the spore of B. cinerea with an IC50 value of 47.7 μg/mL .
Rawsonol is a brominated diphenylmethane derivative obtained from the green alga Avrainuika rawsoni. Rawsonol exhibits inhibitoryactivity against 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, with activities related to cholesterol biosynthesis inhibition or other metabolic pathways involving HMG-CoA reductase activity .
Kaempferol 3-O-gentiobioside is a flavonoid isolated from C. alata leaves with antidiabetic activity. Kaempferol 3-O-gentiobioside possesses activity against α-glucosidase and displays carbohydrate enzyme inhibitory effect with an IC50 of 50.0 µM .
Hamaudol is a chromone isolated from Saposhnikovia divaricata. Hamaudol shows significant inhibitoryactivity on cyclooxygenase (COX)-1 and COX-2activities with IC50 values of 0.30, 0.57 mM, respectively, and has potent analgesia and anti-inflammary effects .
Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitoryactivity on β-secretion (BACE) (IC50=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release.
Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A)inhibitor. Didesmethylrocaglamide has potent growth-inhibitoryactivity with an IC50 of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity .
MAPK-IN-1 (Compound 2) is a MAPK signaling pathwayinhibitor. MAPK-IN-1 exhibits AChEinhibitoryactivity with an IC50 of 23.84 μM. MAPK-IN-1 shows anti-neuroinflammatory and neuroprotective activity and can be used for Alzheimer's disease research .
Carazostatin (DC118), an antioxidant, can be isolated from Streptomycs chromofuscus. Carazostatin (DC118) exhibits strong inhibitoryactivity against free radical-induced lipid peroxidation and shows stronger antioxidant activity in liposomal membranes than α-tocopherol (VE) .
VCC234718 is a molecule with mycobacterial growth inhibitoryactivity, specifically targeting Mycobacterium tuberculosis (Mtb). The primary molecular target of VCC234718 is inosine monophosphate dehydrogenase (GuaB2), and it inhibits the growth of Mtb by affecting the function of this enzyme. VCC234718 inhibits GuaB2 with a K value of 100 nM and exhibits non-competitive inhibition with IMP and NAD+. VCC234718 exerts its inhibitory effect by directly interacting with IMP and binding at the NAD+ site .
Phenethyl ferulate is a major constituent ofQianghuo, shows inhibitoryactivity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively .
653-47 hydrochloride, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB)inhibitoryactivity of 666-15. 653-47 hydrochloride is also a very weak CREB inhibitor with IC50 of 26.3 μM .
653-47, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB)inhibitoryactivity of 666-15. 653-47 is also a very weak CREB inhibitor with IC50 of 26.3 μM .
Tetrahydroamentoflavone (Amentoflavanone) is a potent xanthine oxidase (XO)inhibitor. Tetrahydroamentoflavone has inhibitoryactivity for XO with IC50 and Ki values of 92 nM and 0.982 μM, respectively. Tetrahydroamentoflavone can be used for the research of inflammatory disorders and gout .
Clausine E, is a alkaloid which can be isolated from Clausena excavata, is a inhibitor of fat mass and obesity-associated protein (FTO) demethylase. Clausine E shows inhibitoryactivities against proliferation of synoviocytes and cancer cells.
Mortatarin G (compound 3) is a prenylated flavonoid, that can be isolated from mulberry leaves. Mortatarin G exhibits good α-glucosidaseinhibitoryactivity, with an IC50 of 20.4±1.4 μM .
6β-Hydroxyipolamiide can be isolated from the methanolic extract of S. jamaicensis leaves. 6β-Hydroxyipolamiide has α-glucosidaseinhibitoryactivity with an IC50 of 539.17 μg/mL .
HPSE1-IN-1 (compound 16) is a selective inhibitor of Heparanase-1 (HPSE1) with moderate inhibitoryactivity against exo-β-d-glucuronidase (GUSβ) and glucocerebrosidase (GBA) .
3-Tosylimidazolidine-2,4-dione (compound 2C) is a hydantoins derivative, and exhibits inhibitoryactivity against the Pf3D7 strain, with an IC50 value of 3.97 nM .
PPO-IN-12 (Compound E-Ic) an inhibitor for nicotiana tabacum protoporphyrinogen IX oxidase (NtPPO), with the Ki of 3 nM. Antibacterial agent 208 exhibits a board herbicide spectrum, with good inhibitoryactivity against broadleaf weeds .
Simocyclinone D8 is an anthracycline antibiotic with antibacterial and antitumor activity against Gram-positive bacteria. Simocyclinone D8 inhibitsDNA gyrase and thus has an inhibitory effect on a variety of tumor cell lines .
5-Feruloylquinic acid (Standard) is the analytical standard of 5-Feruloylquinic acid. This product is intended for research and analytical applications. 5-Feruloylquinic acid (5-FQA) possesses antioxidative effects and tyrosinase inhibitoryactivities .
YKAs3003 is a potent inhibitor of Escherichia coli KAS III (ecKAS III) with antibacterial activity. The minimum inhibitory concentrations (MICs) of YKAs3003 against a variety of bacteria ranged from 128 to 256 μg/mL .
Parogrelil (NT-702 free base) is a compound with intermittent claudication inhibitoryactivity that inhibits PDE3, inhibits platelet aggregation and vasoconstriction, and improves walking distance and plantar surface temperature in a rat experimental model.
Nolatrexed (AG 337 free base) is a compound with antifolate activity, high oral bioavailability, and major toxicity at inhibitory doses is gastrointestinal reactions. It can be safely taken orally at specific doses for inhibition, with effects on platelets and neutrophils.
Antitumor agent-188 (compound C6) exerts α-glucosidaseinhibitoryactivity, and antitumor effects.Antitumor agent-188 induces excessive production of ROS to trigger oxidative stress .
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibitsDNA polymeraseactivity in melanoma cells . 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitoryactivity in melanoma cell lines with varying degrees of tyrosinase activity .
aPKC-IN-2 is a small molecule inhibitor that inhibits aPKC activity. aPKC-IN-2 can effectively block vascular endothelial permeability in cell culture and in vivo experiments. aPKC-IN-2 shows biological activity in interfering with NFκB-driven gene transcription and is associated with inflammatory responses. aPKC-IN-2 has a significant inhibitory effect on vascular endothelial permeability induced by VEGF and TNF, and its EC50 value is in the low nanomolar range. The structural characteristics of aPKC-IN-2 reveal key elements of its inhibitoryactivity, providing the possibility for further development of small molecule aPKC inhibitors .
QC6352 is an orally active KDM4inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivoinhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibitsKDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitoryactivity against KDM5 with an IC50 of 750 nM (KDM5B) .
Protorubradirin is an antibiotic that can be isolated from Streptomyces achromogenes var. rubradirin together with Rubradirin. Protorubradirin has inhibitoryactivity against HIV reverse transcriptase. In vitro studies have shown that Protorubradirin also inhibits Staphylococcus aureus strains and Streptococci. In infected mice, subcutaneous injection of Protorubradirin showed in vivo inhibitory efficacy against antibiotic-resistant Staphylococcus aureus strains. However, oral administration may result in a significant reduction in the activity of Protorubradirin, possibly due to faster cleavage of its C-nitroso sugar in the acidic gastric environment compared to Rubradirin .
PD-L1-IN-4 (Compound X18) is an orally active PD-L1inhibitor that exhibits remarkable inhibitoryactivity against the PD-1/PD-L1 interaction (IC50 = 1.3 nM) and enhances PD-L1 inhibitory effect on T cells (EC50 = 152.8 nM). PD-L1-IN-4 can be used for the research of cancer .
Purpurogallin is a naturally phenol extracted from the plants of Quercus spp, has potent xanthine oxidase (XO)inhibitoryactivity with an IC50 of 0.2 µM. Purpurogallin has antioxidant and anti-inflammatory effects .
Velutin is an aglycone extracted from Flammulina velutipes, with inhibitoryactivity against melanin biosynthesis. Velutin reduces osteoclast differentiation and down-regulates HIF-1α through the NF-κB pathway .
ACHN-975 TFA is a selective LpxCinhibitor and exhibits a subnanomolar LpxC inhibitoryactivity. ACHN-975 TFA is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL) .
Triptoquinone B ((+)-Triptoquinone B), a sesquiterpene alkaloid, is an interleukin-1inhibitor. Triptoquinone B shows potent inhibitoryactivities against interleukin 1α and β releases for human peripheral mononuclear cells .
Chaetosemin J, an antifungal metabolite, exhibits inhibitoryactivity against plant pathogenic fungi Botrytis cinerea, Alternaria solani, Magnaporthe oryzae, and Gibberella saubinettii, with MIC values ranging from 12.5-25 μM .
Urease-IN-4 is an effective inhibitor of urease with an IC50 value of 1.64 µM. Urease-IN-4 has low cytotoxicity and shows inhibitoryactivity on P. vulgaris with an IC50 value of 15.27 µg/mL .
18A (HIV-1 inhibitor 18A) is a reversible broad-spectrum HIV-1inhibitor. 18A exhibits broad inhibitoryactivity against multiple HIV-1 strains by blocking the function of Env .
ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity .
DNA polymerase-IN-2 (Compd 3c), a coumarin derivative, exhibits inhibitoryactivity against Taq DNA polymerase with IC50 of 48.25 μM , which can be used in value-added disease research .
Cryptomeridiol is a platelet-activating factor (PAF) receptor binding inhibitor. Cryptomeridiol has melanogenesis inhibitoryactivity in the α-MSH (HY-P0252)-stimulated B16 melanoma cells .
Aloeresin G is a chromone glycoside that can be isolated from Aloe. Aloeresin G has a weak inhibitory effect on TNFα-induced NF-κB transcriptional activity, with an IC 50 value of 40.02 μM .
Hyperelamine A (compound 5) is a polycyclic polyprenylated acylphloroglucinols (PPAPs). Hyperelamine A exhibits inhibitoryactivity against LPS-activated NO production in BV-2 cells via TLR-4/NF κB signaling .
HKI12134085 (compound 3) is an orally available antibacterial nitrobenzothiazinone (BTZ) derivative with activity against Mycobacterium tuberculosis. HKI12134085 has in vivo inhibitory potency in a BALB/c mouse model of Mycobacterium tuberculosis infection .
Talaroderxine D (compound 4) has biofilm inhibitory effect. Talaroderxine D shows antimicrobial activities against Bacillus subtilis and Staphylococcus aureus with MIC values of 2.1 and 8.3 μg/mL .
Urease-IN-14 (compound 15) is an ureaseinhibitor and antioxidant. Urease-IN-14 shows DPPH radical scavenging and urease inhibitoryactivities with IC50 values 151.7 μM and 41.6 μM, respectively .
GS-7682 is an antiviral compound. GS-7682 has inhibitoryactivity against pneumoviruses and picornaviruses. GS-7682 can be used in the study of respiratory diseases such as asthma and chronic obstructive pulmonary disease .
Fmoc-Phe(4-tBu)-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize rOicPaPhe(p-Me)-NH(2) with platelet aggregation activation inhibitoryactivity .
TYT-1 is a sulfonamide-thiourea compound that has inhibitoryactivity against West Nile virus replication with a 50% effective concentration of 0.7 microM, blocking a post-entry, pre-assembly step of viral replication.
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase .
Glyurallin B is a flavonoid, that can be isolated from licorice (Glycyrrhiza inflata and Glycyrrhiza uralensis). Glyurallin B shows ABTS + radical scavenging activity and the inhibitoryactivity on lipid peroxidation, with EC50 values of 11.9 ± 0.58 μM and 15.3 ± 1.26 μM, respectivley .
Trifolirhizin (Standard) is the analytical standard of Trifolirhizin. This product is intended for research and analytical applications. Trifolirhizin is a pterocarpan flavonoid isolated from the roots of Sophora flavescens. Trifolirhizin possesses potent tyrosinase inhibitoryactivity with an IC50 of 506 μM . Trifolirhizin exhibits potential anti-inflammatory and anticancer activities .
Lentinellic acid is an antimicrobial and cytotoxic diterpenoid with biological activity. Lentinellic acid exerts its antimicrobial activity by inhibiting the growth of microorganisms. Lentinellic acid also shows inhibitory effects on tumor cells and has potential anticancer properties. The structure of lentinellic acid was determined by spectroscopic methods and single crystal X-ray analysis .
Tioconazole (UK-20349) is an antifungal imidazole derivative with broad spectrum activity. Tioconazole has inhibitory active aginst several dermatophytes and several yeasts with MIC50s <3.12 mg/L and <9 mg/L, respectively .
Prunin is a potent inhibitor of human enterovirus A71 (HEVA71). Prunin shows strong inhibitoryactivity against protein tyrosine phosphatase 1B (PTP1B), with an IC50 of 5.5 μM .
Cyclofenil is a selective estrogen receptor modulator and an ovulation-inducing agent. Cyclofenil shows an inhibitory effect on dengue virus replication in Vero cells with an EC50 of 1.62 μM. Cyclofenil has anti-dengue-virus activity .
15a-Hydroxy-3,11,23-trioxo-lanost-8,20-dien-26-oic acid, a Lanostane triterpenoid, possesses NO production inhibitoryactivities of LPS-induced microglia .
Cap-dependent endonuclease-IN-12 (EXP-35) is a potent Cap-dependent endonuclease inhibitor with low cytotoxicity. Cap-dependent endonuclease-IN-12 shows inhibitoryactivity against H1N1 .
19-O-Acetylchaetoglobosin A, a cytochalasan alkaloid, is a fungal metabolite originally isolated from C. globosum that has actin polymerization inhibitory and cytotoxic activities. 19-O-Acetylchaetoglobosin A is cytotoxic to HeLa cervical cancer cells .
ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitoryactivity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis .
ARN5187 is a lysosomotropic REV-ERBβ ligand with a dual inhibitoryactivity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomotropic potency and cytotoxicity. ARN5187 induces apoptosis .
VU0410425 is an mGlu1 negative allosteric modulator. VU0410425 exhibits potent inhibitoryactivity for rat mGlu1 with an IC50 value of 140 nM. VU0410425 can be used for the research of central nervous system disorders .
Isodonal is a N-pentane diterpene compound with potential cytotoxic, antitumor, inhibitory oxidative phosphorylation and antiingestion activities. Isodonal can be isolated from the leaves of Isodon wikstroemioides and is used in the study of gastrointestinal diseases, anti-tumor and anti-inflammatory .
Antitumor agent-106 (compound 42) is an anticancer agent that exhibits good inhibitoryactivity (IC50=4.2-6.6 µM) against both lung cancer and colon cancer cell lines .
Chamigrenol is a Na +/K +-ATPaseinhibitor with an IC50 value of 15.9 μg/mL. Chamigrenol shows strong inhibitoryactivities against Gram-positive and Gram-negative bacteria except Escherichia coli, with MIC values of 50 µg/mL .
7-O-Methylaloesinol is a chromone derivative. 7-O-Methylaloesinol shows significant inhibitory effects against TNFα-induced NF-κB transcriptional activity with an IC50 value of 29.07 μM .
Human enteropeptidase-IN-3 is an enteropeptidase inhibitor. Human enteropeptidase-IN-3 exhibits enteropeptidase activity and long duration of inhibitory state. Human enteropeptidase-IN-3 can be used for intetinal digestive related diseases research .
3,3′-Bisdemethylpinoresinol, lignin, is a nature product and has MMP-1 inhibitoryactivity in UVA-irradiated human dermal fibroblasts. 3,3′-Bisdemethylpinoresinol can be isolated from the seeds of Morinda citrifolia .
PB17-026-01 is a potent SHP2 allosteric inhibitor and shows the highest inhibitoryactivity with an IC50 value of 38.9?nM. PB17-026-01 can be used for the research of tumor .
DHFR-IN-17 (compound j9) is an oral active SaDHFRinhibitor with the IC50 of 0.97 nM. DHFR-IN-17 shows antibacterial activity against S. aureus with the minimum inhibitory concentration of 0.031 μg/mL .
Cetamolol hydrochloride is classified as a potent β1-blocker with intrinsic sympathomimetic activity and cardioselectivity. Low and medium doses of Cetamolol and Atenolol produce a more prolonged inhibitory effect than the same doses of Propranolol and Dexpropranolol.
STING18 (Stimulator of interferon genes 18) is a compound that inhibits STING protein by utilizing a small molecule active site dimer, with good oral exposure, slow binding kinetics, and functional inhibitoryactivity on STING-mediated cytokine release.
Tylocrebrine is a compound with anticancer activity. Its clinical research was interrupted due to toxicity issues. By making it into targeted nanoparticles, its inhibitory index can be improved, the killing effect on tumor cells can be enhanced and brain penetration can be reduced.
AA863 is a 5-lipoxygenase inhibitor with activity in inhibiting the proliferation of human glioma cells. AA863 exhibits significant and dose-dependent inhibitory effects in monolayer cultured glioma cells with an IC50 of 9.0 micromolar .
Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitoryactivity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities .
Carbonic anhydrase inhibitor 12 is a potent CA IIinhibitor, also has inhibitoryactivity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines .
Taxiphyllin (2R-Taxiphyllin) is a plant cyanogenic glycoside, which exhibits inhibitoryactivity for tyrosinase . Taxiphyllin exhibits cytotoxicity in BRL-3A cellls with an IC50 of 18.75 μm and antimicrobial activities against Staphylococcus aureus with an EC50 of 0.96 μM .
CRAMP-18 (mouse) is an antibiotic peptide without hemolytic activity. CRAMP-18 (mouse) has good inhibitoryactivity against Gram-negative bacteria, such as S. typhimurium and P. aeruginosa. CRAMP-18 (mouse) has the potential to study antifungal, antibacterial and antitumor .
Adechlorin (2'-Chloropentostatin) is an adenosine deaminase inhibitor isolated from actinomycete culture, with potent inhibitoryactivity against calf intestinal adenosine deaminase, a Ki value that is comparable to other known inhibitors, and can enhance the antiviral activity of Ara-A, and has lower acute toxicity in mice than other analogs.
Taxifolin (Standard) is the analytical standard of Taxifolin. This product is intended for research and analytical applications. Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitoryactivity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Methyl gallate (Standard) is the analytical standard of Methyl gallate. This product is intended for research and analytical applications. Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitoryactivities.
YZ51 is a derivative of Osalmid (HY-B2116) with stronger ribonucleotide reductase (RR) inhibitoryactivity and HBV replication inhibition ability than Osalmid. The IC50 of YZ51 against recombinant RRactivity is 0.6 μM, and the IC50 against HepG2.2.15 cell RRactivity is 23.7 μM .
Radamide is an inhibitor of Grp94 with anti-migratory activity. Radamide is used to inhibit Grp94-related diseases such as glaucoma, cancer metastasis, and multiple myeloma. Radamide exhibits selective inhibitoryactivity by acting on the specific structure of Grp94. Radamide derivatives show better potency and selectivity in improved structure-activity relationship studies .
NDV-IN-1 is an antiviral agent with high neuraminidaseinhibitoryactivity. NDV-IN-1 exhibits in vitro inhibitoryactivity against Newcastle disease virus (NDV). NDV-IN-1 significantly inhibits NDV infection of Vero cells by preventing the release of virus particles from infected cells . Neuraminidase-IN-12 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
p18SMI-21 is a novel INK4C inhibitor that specifically blocks the biological activity of p18 protein. p18SMI-21 exerts its anti-gastric acid effect through direct contact, and the intensity of this effect varies with the dose. p18SMI-21 can significantly reduce the proteolytic activity of pepsin under certain conditions. The inhibitory effect of p18SMI-21 is best achieved in direct contact with the substrate. If it contacts the substrate first, the inhibitory effect will be lost .
MoTPS1/2-IN-1 (Compound A1-4 ) is a bispecific inhibitor of MoTps1 and MoTps2. MoTPS1/2-IN-1 has antifungalactivity and showed good inhibitoryactivity against the growth and virulence of B. cinerea and F. graminearum .
Cinosulfuron is a selective herbicide with excellent inhibitoryactivity against a variety of broadleaf weeds and is widely used in crop fields to protect the growth of crops. Cinosulfuron can effectively manage weed problems by inhibiting specific enzyme activity. Cinosulfuron is used in agriculture to increase crop yield and quality and ensure efficient use of farmland.
LY2334737 is an nucleoside analog and is an orally active proagent of Gemcitabine. LY2334737 exhibits inhibitoryactivity against enterovirus A71 (EV-A71) infection. LY2334737 has antiviral and anticancer effects .
JMJD7-IN-1 is a potent JMJD7inhibitor, with an IC50 of 6.62 μM. JMJD7-IN-1 shows good inhibitoryactivity against cells expressing a high level of JMJD7 .
5,7-Diacetoxy-8-methoxyflavone is a natural product that could come from scutellaria genus plants. 5,7-Diacetoxy-8-methoxyflavone has inhibitoryactivity for cAMP phosphodiesterase .
L-Adenosine is a metabolically stable enantiomeric analog and also is a potential probe. L-Adenosine has weakly inhibitoryadenosine deaminase (ADA)activity with an Ki value of 385 μM. L-Adenosine can be used for the research of adenosine uptake and accumulation .
Protosappanin A dimethyl acetal is a homoisoflavonoid. Protosappanin A dimethyl acetal can be isolated from Caesalpinia sappan. Protosappanin A dimethyl acetal is also a competive inhibitor with significant xanthine oxidaseinhibitoryactivity (IC50=50.7 μM) .
Vibralactone D (Compound 1) is a metabolite isolated and cultured from natural basidiomycetes Boreostereum vibrans. Vibralactone D shows weak inhibitoryactivity against isoenzymes of 11b-hydroxysteroid dehydrogenase (HSD) (IC50 85.7 μM).
Anti-inflammatory agent 63 is an anti-inflammatory agent that shows optimal inhibitoryactivity (EC50 = 5.33±0.57 μM) against the production of nitric oxide (NO) induced by lipopolysaccharide (LPS) in RAW264.7 cells .
CSNK2A-IN-2 (compound 6c) is a selective CSNK2Ainhibitor with antiviral activity. CSNK2A-IN-2 exhibits an inhibitory effect on viral replication and is selective for PIM3 .
nNOS-IN-1(Compound 14) is an inhibitor for nitric oxide synthases (NOS), that exhibits inhibitoryactivities against neuroal, inducible and endothelial NOS, with IC50s of 2.5, 5.7 and 13 μM, respectively .
Detoxin D1 is a compound with antihistamine activity and a new type of H1 antagonist. In the suppression of seasonal allergic rhinitis, a daily dose of 10-30 mg has an equivalent and highly effective inhibitory effect compared with placebo and has good safety.
HU 331 (HU 331) is a highly specific Topoisomerase IIinhibitor with anticancer activity. HU 331 has shown promising inhibitory effects on human cancer cell lines in vitro and human tumor xenografts in nude mice in vivo .
Antimicrobial agent-2 (compound V-a) is a broad-spectrum antimicrobial agent, possessing inhibitoryactivity against various Gram-positive and -negative bacteria. Antimicrobial agent-2 has excellent inhibitory effect on Methicillin-resistant Staphylococcus aureus (MRSA) with a MIC of 1 μg/mL. Antimicrobial agent-2 can effectively damage the membrane and lead to the leakage of protein, also can induce the generation of ROS. Antimicrobial agent-2 exhibits low toxicity, no obvious resistance and good bioavailability .
EPZ033294 is an inhibitor of SYMD2 (IC50 is 3.9 nM). SYMD2 itself has catalytic activity and can methylate the lysine residue of BTF3 to BTF3me1, which was experimentally demonstrated by detecting an IC50 of 2.9 nM for inhibition of BTF3ME1 by SYMD2, indicating an active inhibition of SYMD2 by EPZ033294. EPZ033294 (0-50 µM) has an inhibitory effect on SYMD2 and a concentration-dependent inhibitory effect in 293T .
PF-05150122 is a novel potent and selective human Nav1.7 channel blocker with the activity of inhibiting human pain signaling. PF-05150122 exhibited favorable biopharmacokinetic parameters in microdose studies, providing a basis for exploring its application in acute or chronic pain inhibition. The pharmacokinetic model of PF-05150122 predicted that at the corresponding oral dose, it could effectively reduce the 50% inhibitory concentration (IC50) of Nav1.7, demonstrating its inhibitory potential .
Bruceine D is a Notchinhibitor with anti-cancer activity and induces apoptosis in several human cancer cells. Bruceine D is an effective botanical insect antifeedant with outstanding systemic properties, causing potent pest growth inhibitoryactivity . Bruceine D has strong anthelminticactivity against D. intermedius with an EC50 value of 0.57 mg/L .
Macropin (MAC-1 peptide) is an antimicrobial peptide found in the venom of the solitary bee Macropis fulvipes. Macropin has antibacterial activity against both Gram-positive and Gram-negative bacteria, and also exhibits inhibitoryactivity against fungi and moderate hemolytic activity against human erythrocytes. Macropin can be used in research on anti-infective therapy .
KN-92 is an inactive derivative of KN-93, without CaM kinase inhibitoryactivity. KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
KN-92 phosphate is an inactive derivative of KN-93, without CaM kinase inhibitoryactivity. KN-92 phosphate is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
Tribuloside is a flavonoid that can be isolated from Tribulus terrestris L . Tribuloside exhibits anti-mycobacterialactivity against the non-pathogenic Mycobacterium species with a minimum inhibitory concentration (MIC) of 5.0 mg/mL. Tribuloside has 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity .
Solidagonic acid inhibitsHSET motor activity by promoting the conversion from abnormal monopolar to bipolar spindles. Solidagonic acid suppresses fission yeast cell death and enables reversion of the mitotic spindles from a monopolar to bipolar morphology. Solidagonic acid showed the growth inhibitoryactivity on the seedlings of Lactuca sativa L. and Lolium multiflorum Lam .
SIQ17 is an EGFRinhibitor that inhibits its activity by occupying the ATP-binding site, with IC50 of 0.62 nM. SIQ17 shows more effective EGFR-TK inhibitoryactivity compared to the known inhibitor Erlotinib (HY-50896) (IC50 of ∼20 nM). SIQ17 can be used for cancer research
TIM-098a is a selective AAK1inhibitor with an IC50 of 0.24 µM. TIM-098a has no inhibitoryactivity against CaMKK isoforms. TIM-098a inhibits AAK1-regulated endocytosis by suppressing AAK1 kinase activity .
Oligomycin E is a antitumor antibiotic that can be isolated from Streptomyces. Oligomycin E has significant antifungal activity, showing minimal inhibitory concentrations (MICs) values between 2 and 75μg/mL. Oligomycin E has strong antitumor activity against HeLa cells, with an IC50 of 0.014 μg/mL .
Gypenoside XLVI is one of the major dammarane-type triterpenoid saponins from Gynostamma pentaphallum . Gypenoside XLVI has a tetracyclic triterpene structure and possess potent non-small cell lung carcinoma A549 cell inhibitoryactivity .
WAY-213613 (hydrochloride) is a potent and selective human EAAT2inhibitor. WAY-213613 has potent EAAT2 inhibitoryactivity with an IC50 value of 85 nM. WAY-213613 can be used for the research of central nervous system .
Oroxylin A-7-O-glucuronide (Oroxyloside; Oroxylin A-7-O-β-D-glucuronide) is a flavonoid glucuronide isolated from the dried root of Scutellaria baicalensis, with prolyl oligopeptidase (POP)inhibitoryactivity .
Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa .
TASP0415914 is a potent and orally active PI3Kγinhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Aktinhibitoryactivities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research .
Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitoryactivity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively .
STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitoryactivity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3 .
AXKO-0046 dihydrochloride, indole derivative, is an uncompetitive Lactate dehydrogenase B (LDHB) selective inhibitor. AXKO-0046 dihydrochloride has LDHB inhibitoryactivity with an EC50 value of 42 nM. AXKO-0046 dihydrochloride can be used for the research of cancer metabolism .
Cholesteryl n-butyrate is a cholesterol ester composed of cholesterol and butyrate, two naturally occurring substances. Cholesteryl n-butyrate can be used to synthesize solid lipid nanoparticles (SLNs) with inhibitoryactivity on the adhesion and migration of colon cancer cells, providing a delivery system for the anticancer drug butyrate .
HDAC-IN-68 (hydrochloride) (Compound 29) has inhibitoryactivity against HDACs (IC50=0.04 μM) and fragments microtubules by activating katanin, a microtubule-severing protein. HDAC-IN-68 (hydrochloride) can be used in cancer research .
AS-2077715 is an antifungal agent that shows inhibitoryactivity against the Trichophyton species. AS-2077715 can be obtained from the fermentation broth of Capnodium sp. 339855. AS-2077715 can be used to study fungal infections .
Ofloxacin (Standard) is the analytical standard of Ofloxacin. This product is intended for research and analytical applications. Ofloxacin (Hoe-280) is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase. Ofloxacin shows inhibitoryactivity against vaccinia virus (VV).
KWWCRW is a Holliday linker inhibitory peptide with anticancer activity. KWWCRW inhibits homologous recombination repair (HDR) during DNA repair by binding to the reactive Holliday linker intermediate and preventing its degradation, and inhibits site-specific recombination by bacteriophage in vitro .
Prudomestin (Standard) is the analytical standard of Prudomestin. This product is intended for research and analytical applications. Prudomestin, isolated from the heartwood of Prunus domestica, shows potent xanthine oxidase (XO) inhibitoryactivity (IC50≈6?μM) .
Kayaflavone is an amentoflavone type biflavonoid. Kayaflavone has an inhibitoryactivity against amyloid-β42 cytotoxicity in PC-12 cells with an EC50 value of 5.29 μΜ. Kayaflavone is promising for research of Alzheimer’s disease .
RDEA 806 is an orally active non-nucleoside reverse transcriptaseinhibitor (NNRTI) that exhibits potent in vitroinhibitoryactivity against both wild-type HIV-1 (EC50 = 3.05 nM) and NNRTI-resistant HIV-1 .
DNS-pE is a vinyl sulfone-based fluorescent probe that has the activity to selectively label 3-phosphoglycerate dehydrogenase (PHGDH) in living mammalian cells and generate fluorescence after labeling, while having inhibitory properties comparable to those of known inhibitors.
Langkamide is a novel hypoxia-inducible factor-2 (HIF-2) inhibitory pyrrolidone alkaloid isolated from the roots and stems of Piper sarmentosum, which inhibits HIF-2 transcriptional activity with an EC?? value of 14.0μM.
FR 106969 (A26771E) is a platelet activating factor antagonist with anti-inflammatory activity. FR 106969 can be used to alleviate inflammatory responses. FR 106969 has shown potential inhibitory effects on inflammation-related diseases in studies .
CID 2011756 is an ATP competitive PKDinhibitor, with an IC50 of 3.2 μM for PKD1 in cell free assay, and also shows cellular pan-PKD inhibitoryactivity against PKD2 and PKD3 (IC50, 0.6 and 0.7 μM, respectively). CID 2011756 also has antitumor activity.
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitoryactivity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population .
IR415 is a potent anti-HBV agent and inhibitsHBV replication by blocking the HBx activity. IR415 selectively interacts with HBx (Kd=2 nM) and blocks HBV-mediated RNAi suppression, reverses the inhibitory effect of HBx protein on the activity of the dicer endoribonuclease . HBx: hepatitis B virus X protein.
3-O-Methylellagic acid is a nature product that can be isolated from Myrciaria cauliflora, with anti-inflammatory activity. 3-O-Methylellagic acid shows an inhibitory effect on glucose transport assay. 3-O-Methylellagic acid has antibacterial activity, with a MIC of 32 μg/mL for Staph. Aureus ATCC 25923 .
MtTMPK-IN-5 (compound 17) is a potent M. tuberculosis thymidylate kinase (MtbTMPK)inhibitor with an IC50 value of 34 μM. MtTMPK-IN-5 combines favorable enzyme inhibitoryactivity with significant activity against M. tuberculosis (MIC = 12.5 μM). MtTMPK-IN-5 can be used for researching tuberculosis .
6-Benzoylheteratisine is an Aconitum alkaloid with potential neuroprotective activity. 6-Benzoylheteratisine can antagonize tetrodotoxin, inhibit the increase of [Na +]i, [Ca 2+]i and glutamate release, and block sodium channels. 6-Benzoylheteratisine has an inhibitory effect on the neuronal activity underlying epileptiform burst discharge .
(±)-ε-Viniferin is a racemate of ε-Viniferin (HY-N3841). (±)-ε-Viniferin exhibits P450inhibitory antioxidants, as well as hepato-protective and antimicrobial activities. (±)-ε-Viniferin has antibacterial and antibiofilm activity against Gram-positive bacteria Streptococcus pneumoniae with a MIC of 20 μM .
Viquidacin (NXL 101) is an antibiotic with inhibitoryactivity against topoisomerase IV and DNA gyrase. Viquidacin exhibits antibacterial activity against gram positive bacterial by inhibiting the supercoiling, decatenation and relaxation in strains Staphylococcus aureus and Escherichia coli in micromolar levels. Viquidacin inhibitsS. aureus wildtype and mutants with MIC of 2-128 mg/L .
WEE1-IN-10 (compound 77) is a Wee1 kinase inhibitor. WEE1-IN-10 shows inhibitoryactivity on LOVO cell growth, with an IC50 of 0.524 μM. WEE1-IN-10 can be used for the research of diseases caused by abnormal activity of Wee1 .
DDCPPB-Glu (compound 3a) is a compound with anti-tumor activity, which has the activity of inhibiting tumor cell growth and prolonging survival. DDCPPB-Glu has growth inhibition effect on various tumor cell lines, can increase the survival time of leukemia mice, and has inhibitory effect on tumors such as colon cancer and lung cancer.
Cedefingol is an antitumor compound with α-glucosidase inhibitoryactivity. Cedefingol was identified together with other compounds in fermented dark tea samples. The biotransformation of cedefingol is related to enzymatic hydrolysis, hydrolysis and biosynthesis. Cedefingol exhibited different bioactivities in samples with different fermentation times. The antioxidant properties of cedefingol showed certain activity in the DPPH model .
CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitoryactivity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.
WAY-213613 is a potent and selective human EAAT2inhibitor. WAY-213613 has potent EAAT2 inhibitoryactivity with an IC50 value of 85 nM. WAY-213613 can be used for the research of central nervous system
Epibetulinic acid exhibits potent inhibitory effects on NO and prostaglandin E2 (PGE2) production in mouse macrophages (RAW 264.7) stimulated with bacterial endotoxin with IC50s of 0.7 and 0.6 μM, respectively. Anti-inflammatory activity .
GRL-0496 is a potent chloropyridyl ester-derived SARS-CoV 3CLproinhibitor, with an IC50 of 30 nM in both enzyme inhibitory and antiviral assays. GRL-0496 shows SARS-CoV antiviral activity, with an EC50 of 6.9 μM .
ACG416B (compound 18) is a potent inhibitor of ChoK (choline kinase) with an IC50 of 0.4 μM. ACG416B renders higher ChoKinhibitory and antiproliferative activities against the HT-29 human colon cancer cell .
AXKO-0046, indole derivative, is an uncompetitive Lactate dehydrogenase B (LDHB) selective inhibitor.AXKO-0046 has LDHB inhibitoryactivity with an EC50 value of 42 nM.AXKO-0046 can be used for the research of cancer metabolism .
4-(Benzo[d]oxazol-2-yl)aniline is a potent antitumor agent. 4-(Benzo[d]oxazol-2-yl)aniline has inhibitoryactivity against mammary carcinoma cell lines .
Debromohymenialdisine (10Z-Debromohymenialdisine) is a pyrrole alkaloid. Debromohymenialdisine has moderate inhibitoryactivity with an IC50 value of 881 nM in the initial Raf/MEK-1/MAPK signaling cascade assay. Debromohymenialdisine can be used for the research of proliferation and differentiation .
Xanthine oxidoreductase-IN-4 is an orally active xanthine oxidoreductase (XOR)inhibitor. Xanthine oxidoreductase-IN-4 has inhibitoryactivity against XOR with an IC50 value of 29.3 nM. Xanthine oxidoreductase-IN-4 can be used for the research of hyperuricemia .
MET kinase-IN-4 is an orally active Met kinaseinhibitor. MET kinase-IN-4 has potent Met kinase inhibitoryactivity with an IC50 value of 1.9 nM. MET kinase-IN-4 can be used for the research of cancer .
BA 41899 is a purely calcium-sensitizing agent. BA 41899 is completely devoid of phosphodiesterase (PDE) III inhibitoryactivity or any other known inotropic mechanism. BA 41899 can be used for the research of cardiovascular diseases, such as congestive heart failure (CHF) .
Limonianin (Atalantoflavone) is a flavone, that can be isolated from Erythrina sigmoidea and the root bark of Citrus limonia. Limonianin presents inhibitory effect against P. gingivalis. Limonianin shows cytotoxic activity against multidrug-resistant (MDR) cancer cell lines .
NSC89641 inhibits MERS-CoV M pro, with an IC50 value < 3.5 μM. NSC89641 exhibits the high inhibitory potency against SARS-CoV-2 M pro enzymatic activity, with an IC50 of 3.05 μM .
Mollicellin I (compound 1) is a depsidone. The growth inhibitoryactivity of Mollicellin I on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines is not significant, with GI50s >10 μg/mL .
Antitumor agent-120 (compound 1) is a flavonoid compound isolated from Kudzu root.Antitumor agent-120 has no significant inhibitoryactivity against LNCaP and PC3 cancer cells, with IC50s >50 μM .
α-Glucosidase-IN-37 (Compound 11) moderately inhibits LPS-induced NO production with an IC50 value of 23.7 μM in macrophages. α-Glucosidase-IN-37 has weak inhibitoryactivity against α-Glucosidase .
Antibacterial agent 169 (Compound 28) is a pyrrolamide-type GyrB/ParE inhibitor with antibacterialactivity. Antibacterial agent 169 has an inhibitory effect on Gyrase and Topo IV of Staphylococcus aureus, with IC50 values of 49 nmol/L and 1.513 μmol/L respectively .
Trypanothione synthetase-IN-5 (compound 9) is a trypanothione reductase (TR)inhibitor, with an IC50 of 20.5 μM for Leishmania infantum TR. Trypanothione synthetase-IN-5 also has inhibitoryactivity for human glutathione reductase (hGR), with an IC50 of 62.4 μM .
CARM1-IN-6 (iCARM1) is an effective and selective inhibitor of CARM1 with an IC50 value of 12.3 μM. CARM1-IN-6 exhibits cell growth inhibitoryactivity and can be used in cancer research .
Lantic acid is a triterpenoid compound possessing antimicrobial activity. Lantic acid exhibits inhibitory effects on a broad range of both Gram-positive and Gram-negative bacteria, with particular potency against Escherichia coli and Bacillus subtilis. Lantic acid is utilized in the research and development of antimicrobial agents .
LCRF-0004 is a potent inhibitor of RON kinase, with the IC50 value of 10 nM. and a surprising result is also obtained regarding its c-Metinhibitoryactivity, with the IC50 value of 12 nM. LCRF-0004 plays an important role in cancer research .
5,10-Dideazafolic acid is a 5,10-dideaza-5,6,7,8-tetrahydrofola analogue, which exhibits some inhibitoryactivity against glycine amide ribonucleotide formyltransferase (GARFT) (Ki=13 μM) .
COX-2-IN-46 (compound 5m) is an anti-inflammatory agent with potent analgesic activity. COX-2-IN-46 exhibits a significant inhibitory effect on COX-2 (IC50=87.74 nM) .
Lonicerin (Standard) is the analytical standard of Lonicerin. This product is intended for research and analytical applications. Lonicerin is an anti-algE (alginate secretion protein) flavonoid with inhibitoryactivity for P. aeruginosa. Lonicerin prevents inflammation and apoptosis in LPS-induced acute lung injury .
COX-1-IN-2 (compound 5h) is an anti-inflammatory agent with potent analgesic activity. COX-1-IN-2 exhibits a significant inhibitory effect on COX-1 (IC50=38.76 nM) .
PDE4-IN-21 (Compound L19) is a poetent PDE4inhibitor, with an IC50 of 0.48 μM. PDE4-IN-21 exhibits good inhibitoryactivity and remarkable metabolic stability in rat liver microsomes .
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasomeinhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitoryactivity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity .
Ianthelliformisamine A TFA is an antibiotic enhancer with activity against resistant Gram-negative bacteria. Ianthelliformisamine A TFA exhibits bactericidal activity against Staphylococcus aureus with an IC50 value of 3.8 μM (minimum inhibitory concentration = 25 μM). The biological activity of Ianthelliformisamine A TFA is derived from the structural variation of its synthetic derivatives and its coupling reaction with different amino ester derivatives .
hAChE-IN-7 (compound 5s) is a mixed inhibitor affecting both the catalytic active site (CAS) and peripheral anionic site (PAS) of hAChE. hAChE-IN-7 displays the balanced inhibitory effect on hAChE (IC50=69.8 nM) and hBuChE (IC50=68.0 nM), and exhibits inhibitoryactivity against β-secretase-1 (BACE-1) (IC50=3.6 μM). hAChE-IN-7 has the potential for Alzheimer's disease (AD) research .
CYP51-IN-20 (compound 5b) is an inhibitor of CYP51 and has antifungal activity. CYP51-IN-20 has a significant inhibitory effect on Candida albicans ATCC 10231, downregulates ERG11 (Cyp51) gene expression, and significantly reduces the yeast-to-hyphae morphological transition. CYP51-IN-20 can synergize with Voriconazole (HY-76200) to occupy the entire CYP51 binding site and exert a synergistic inhibitory effect in the Glechoma moth model .
EF-1502 is a potent and selective GABA transporter inhibitor with GAT1 and BGT1 inhibitoryactivity. EF-1502 produces a synergistic anti-epileptic effect when used in combination with Tiagabine (HY-B0696), a compound used to suppress epileptic seizures. The dosing combination of EF-1502 exhibited reduced anti-epileptic efficacy and dyskinesia when used with THIP (HY-10232). The mechanism of EF-1502 differs significantly from Tiagabine, suggesting a unique role in the inhibitory strategy .
9-Hydroxycalabaxanthone (Xanthone I) is a known xanthone isolated from Garcinia mangostana Linn. 9-Hydroxycalabaxanthone has quorum-sensing inhibitory, anti-microbial, and anti-malarial activities (IC50=1.2-1.5 μM) .
Ursonic acid methyl ester is an esterified derivative of Ursolic acid (HY-N0140). Ursonic acid methyl ester shows growth inhibitoryactivity against four tumor cell lines, HL-60, BGC, Bel-7402 and Hela with ED50 values of >100 µg/ml .
MERS-CoV-IN-1 exhibits excellent inhibitoryactivity against coronavirus. MERS-CoV-IN-1 is useful as a pharmaceutical composition for preventing coronavirus-induced diseases (MERS-CoV and SARS) (extracted from patent WO2018174442A1, compound 1) .
AChE-IN-24 is a potent AChEinhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitoryactivity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD) .
Antitrypanosomal agent 9 (compound 1) is a potent antitrypanosomal agent. Antitrypanosomal agent 9 shows inhibitoryactivity against T. b. brucei, with an IC50 of 1.15 μM. Antitrypanosomal agent 9 can be used for human African trypanosomiasis (HAT) research .
N-Methylcalycinine is a nature product with AChE inhibitoryactivity. N-Methylcalycinine can be isolated from the roots of Stephania epigaea. N-Methylcalycinine can be used for the research of asthma, cancer, dysentery, fever, hyperglycemia, intestinal complaints, inflammation, sleep disturbances, tuberculosis and so on .
Antiparasitic agent-20 (Compound 1p) is a parasiteinhibitor with broad antiparasitic activity. Antiparasitic agent-20 has inhibitory effects on T. brucei and T. cruzi with EC50 values of 0.09 μM and 14.1 μM respectively .
Eupenicisirenin C (compound 1) is a sirenin derivative. Eupenicisirenin C has strong NF-κBinhibitoryactivities. Eupenicisirenin C suppresses effects on cGAS-STING pathway. Eupenicisirenin C inhibits RANKL-induced osteoclast differentiation in bone marrow macrophage cells .
Tachioside inhibits nitric oxide production in lipopolysaccharide (HY-D1056)-stimulated RAW 264.7 cells with IC50 value of 12.14 μM. Tachioside has anti-obesity, antioxidant and α-glucosidaseinhibitoryactivities .
4-Ethyloctanoic acid- 13C2 is 13C labeled Cuminaldehyde (HY-Y0790). Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity .
Firefly luciferase-IN-5 (CID: 16031203) is an inhibitor of ATP-dependent luciferase (Firefly luciferase). It has nM-level inhibitoryactivity against GRLuc, RLuc8, and RLuc respectively (pIC50=8.5,7.5,5.5) .
Kopsoffinol, a bisindole alkaloid, shows in vitro growth inhibitoryactivity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells .
ABT-299 is a prodrug of a platelet-activating factor (PAF) antagonist that exhibits significant inhibitoryactivity on PAF-induced β-platelet globulin release in vitro after in vivo administration in humans, an effect that may be partially attributed to the pyridine-N-oxide metabolite.
PARP1-IN-31 (compound 11f) is a phthalazinone-based compound, an anti-lung adenocarcinoma compound with inhibitoryactivity against PARP-1 (IC50 value of 97 nM), inducing apoptosis and inhibiting cell proliferation in lung cancer cell lines.
Ametantrone acetate (NSC 196473 acetate) is an antineoplastic drug with topoisomerase II inhibitoryactivity. Ametantrone acetate causes covalent cross-linking of DNA. The pharmacokinetic profile of Ametantrone acetate has been confirmed in clinical trials, and its elimination pathway in the body indicates the existence of a major metabolic pathway .
Antifungal agent 33 (compound 4e) is a potent antifungal agent. Antifungal agent 33 exhibits remarkable antifungal activity against C. albicans, with a MIC of 16 μg/mL. Antifungal agent 33 shows potent inhibitoryactivity against Lanosterol 14α-demethylase (CYP51), with an IC50 of 0.19 μg/mL .
Chitin synthase inhibitor 11 is a chitin synthaseinhibitor. Chitin synthase inhibitor 11 shows excellent chitin synthase inhibitoryactivity with an IC50 value of 0.10 mM. Chitin synthase inhibitor 11 has broad-spectrum antifungal activity in vitro. Chitin synthase inhibitor 11 can be used for the research of invasive fungal infections (IFIs) .
Sm4 is a SOX18inhibitor. Sm4 shows SOX18-DNA binding inhibitoryactivity. Sm4 selectively affects SOX18 transcriptional output in vitro. Sm4 blocks SoxF transcriptional activity in vivo. Sm4 can be used for cancer metastasis and vascular cancers research .
XMU-MP-2 is a BRKinhibitor with significant inhibitoryactivity on BRK-positive cells. XMU-MP-2 inhibits oncogenic BRK-driven tumor growth in a mouse xenograft model. XMU-MP-2 also synergizes with HER2inhibitors or endoplasmic reticulum (ER) blockade to exert antiproliferative activity .
Hp1404 is a novel cationic antimicrobial peptide. Hp1404 has specific inhibitoryactivity against Gram-positive bacteria, including Staphylococcus aureus (MRSA) resistant to Laburnetin (HY-N7382). Hp1404 has antimicrobial activity, low toxicity, and is not prone to drug resistance, and can be used in the research of antimicrobial agents .
Isoscoparin-7-O-glucoside is a flavonoid compound found in barley leaves. The total phenolic content (TPC) of isoscoparin-7-O-glucoside is positively correlated with COX-2 inhibitoryactivity, indicating anti-inflammatory activity. Isoscoparin-7-O-glucoside can be used in the study of inflammation .
Cephalandole B is an indigo alkaloid that has the activity of inhibiting IL-17A gene expression. Cephalandole B significantly inhibited the activity of IL-17A luciferase reporter gene in Jukat cells, and this inhibitory effect was dose-dependent. Cephalandole B may have important application prospects in inflammation-related research .
HIV-1 inhibitor-16 (compound 7a) is a highly potent HIV-1inhibitor with an EC50 value of 1.3 nM for HIV-1 WT. HIV-1 inhibitor-16 also has certain inhibitoryactivity against HIV-1 K103N, E138K, Y181C and L100I strains with EC50s of 5.4 nM, 9.2 nM, 22 nM and 35 nM. HIV-1 inhibitor-16 has favorable solubility and liver microsome stability, and does not exhibit apparent CYP enzymatic inhibitoryactivity or acute toxicity .
HDAC6/8/BRPF1-IN-1 is a dual inhibitor of both HDAC6/8 and the bromodomain and PHD finger containing protein 1 (BRPF1). HDAC6/8/BRPF1-IN-1 has inhibitoryactivity for HDAC1, HDAC6 and HDAC8 with IC50 values of 797 nM, 344 nM and 908 nM, respectively. HDAC6/8/BRPF1-IN-1 has inhibitoryactivity for BRPF1 with an Kd value of 175.2 nM. HDAC6/8/BRPF1-IN-1 can be used for the research of cancer .
Betamethasone 17-Propionate is a compound used to study its effects on endotoxin-induced uveitis in rats. It has the activity of inhibiting the infiltration of cells into the aqueous humor in endotoxin-induced uveitis by eye drops and systemic administration at a certain dose. However, its inhibitory effect is relatively weak compared with some other compounds. At the same time, the dose for systemic administration is 1mg/kg. In addition, Betamethasone 17-Propionate has a weaker inhibitory effect on the release of IL-8 from rat peritoneal exudate cells in an in vitro interleukin-8 (IL-8) release assay than betamethasone. Moreover, the simultaneous addition of betamethasone dipropionate and betamethasone 17-Propionate reduces the inhibitory effect of betamethasone on cell infiltration and IL-1β gene expression.
DY3002 is a selective and highly potent EGFR inhibitor with activity in overcoming T790M-mediated drug resistance in non-small cell lung cancer. DY3002 exhibited superior inhibitory effects against EGFR T790M mutants in kinase assays (IC50 = 0.71 nM), compared to weaker inhibitory effects against wild-type EGFR (IC50 = 448.7 nM). DY3002 was significantly superior to rociletinib and osimertinib in selectivity, showing an extremely high selectivity index (SI = 632.0). In cell experiments, DY3002 had an IC50 value of 0.037 μM against H1975 cells, showing enhanced inhibitory potency. In addition, DY3002 was superior to other alternative compounds in terms of biological properties and did not cause hyperglycemia .
11-oxo-mogroside V is a natural sweetener that exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2-, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitoryactivity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation. H-151 can be used for the research of autoinflammatory disease .
Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes . Medicagenic acid (Castanogenin) has low enzyme inhibitoryactivities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE .
Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa .
Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitoryactivity on human aromatase (IC50=0.92 μM) .
Plantanone B is a moderate antioxidant-agent with an IC50 of 169.8±5.2 μM. Plantanone B shows significant ovine COX-1 and moderate COX-2 inhibitoryactivities. Plantanone B has the potential for inflammation-related diseases research .
Moclobemide N-Oxide (Ro 12-5637) is N-oxide metabolite of Moclobemide. Moclobemide N-Oxide retains certain MAO-A (monoamine oxidase) inhibitoryactivity, but is generally present in low concentrations. Moclobemide N-Oxide can be detected by UV absorption at 240 nm .
PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes .
CAY10746 is a selective Rho kinase (ROCK)inhibitor. CAY10746 has inhibitoryactivity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR) .
RTI 336 is a phenyltropane analog, as well as a potent and selective dopamine transporter (DAT)inhibitor. RTI 336 inhibits addictive agent induced locomotor activity and self-administration in Lewis rats. RTI 336 exhibits inhibitory effects depending on inherent NAc DAT levels .
11-O-β-D-glucopyranosyl thamnosmonin, a coumarin glucosides, can be isolated from the roots of Angelica apaensis. 11-O-β-D-glucopyranosyl thamnosmonin has weak inhibitoryactivity on the aggregation of rabbit platelets induced by PAF, AA, and ADP .
alpha-CEHC is a water-soluble metabolite of alpha-tocopherol (α-TOH) with potential antioxidant activity. alpha-CEHC slightly inhibits macrophage-induced low-density lipoprotein (LDL) oxidation, and its inhibitory potency is concentration-dependent .
hCAIX/XII-IN-10 (compound DK-8) is a carbonic anhydrase inhibitor. hCAIX/XII-IN-10 has potent inhibitoryactivity against tumor-associated membrane-bound isoforms hCA IX and XII, with Ki values of 32.5 nM and 29.2 nM .
HIV-1 inhibitor-66 is an orally active non-nucleoside reverse transcriptioninhibitor (NNRTI). HIV-1 inhibitor-66 shows inhibitoryactivity against wild-type HIV-1 reverse transcriptase with an IC50 of 40 nM .
Escin IB (Standard) is the analytical standard of Escin IB. This product is intended for research and analytical applications. Escin IB is a saponin isolated from skin and the endosperm of seeds of horse chestnut (Aesculus hippocastanum). Escin IB shows inhibitory effect on pancreatic lipase activity .
ONCOII is an Mps1inhibitor with an IC50 of 10.8 nM. The inhibitoryactivity of ONCOII against Mps1 is affected by naturally occurring mutations in the Mps1 gene, and cells with Mps1 mutations exhibit increased resistance to ONCOII. ONCOII can be used in cancer research .
LP-130 is a statin-based inhibitor that is a universal inhibitor with nanomolar inhibitoryactivity against all tested retroviral proteases. Crystal structure studies of its binding to different retroviral proteases have shown that it can adapt to different active site regions to achieve inhibition.
(R,R)-Ethambutol is an antituberculosis compound with tuberculosis inhibitoryactivity. (R,R)-Ethambutol is often used in combination with other antituberculosis compounds to enhance the efficacy. (R,R)-Ethambutol can also be used to inhibit Mycobacterium avium complex infection and Mycobacterium kansasii infection .
Linaprazan mesylate can inhibit H+,K+ -ATPase in the stomach through K+ competitive binding. (IC 50: 1.0 ± 0.2 μM), it has a strong inhibitory effect on acid. Linaprazan (AZD0865) mesylate can be used for research on reflux esophagitis with oral activity .
Laninamivir TFA (R 125489 TFA) is an antiviral compound with inhibitory and prophylactic activity against influenza A and B viruses. Laninamivir TFA is a long-acting neuraminidase inhibitor administered by nasal inhalation. Laninamivir TFA has shown good safety and efficacy in the inhibition of influenza viruses .
WAY-260022 is a selective norepinephrine reuptake inhibitor with potent inhibitoryactivity on norepinephrine reuptake. WAY-260022 exhibits excellent selectivity in inhibiting serotonin and dopamine transporters. WAY-260022 also showed oral efficacy in a rat model of thermoregulatory dysfunction .
Pyriftalid is a new type of insecticide with strong inhibitoryactivity against a variety of pests. Pyriftalid is widely used in agriculture to effectively control pests on crops, thereby improving crop yield and quality. Pyriftalid is also being studied for improving plant resistance to resist attacks by pests and diseases.
2-Methyl-3-phenylquinoxaline (compound 38) is a potent platelet-derived growth factor receptor tyrosine kinase (PDGF-RTK) inhibitor with modest inhibitoryactivity against PDGFR kinase in intact cells (IC50 greater than 100 μM) .
SKF 104976 is a 3,2-carboxylic acid derivative with potent 14-alpha-demethylase (14 alpha DM) inhibitoryactivity. SKF 104976 inhibited 14 alpha DM activity by 50% at 2 nM in Hep G2 cell extracts. SKF 104976 inhibited the incorporation of [14C]acetate into cholesterol in intact cells at similar concentrations, accompanied by accumulation of lanosterol, and resulted in a 40-70% decrease in 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) activity. SKF 104976 did not affect the uptake and degradation of low-density lipoprotein in Hep G2 cells, indicating that HMGR and low-density lipoprotein receptor activities are not coordinately regulated under these conditions. The inhibitory effect of SKF 104976 on HMGR activity remained unchanged even when the flux of carbon units in the sterol synthesis pathway was reduced by 80%. SKF 104976 did not inhibit HMGR activity under conditions where sterol synthesis was almost completely blocked by lovastatin .
CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC90=270 nM) and improved liver microsomal stability. CHIKV-IN-2 shows inhibitoryactivity against a cellular target Dihydroorotate Dehydrogenase (DHODH), which interacts with various viruses and regulate their replication via depleting intracellular pyrimidine pools .
DPP-IV-IN-5 is isolated from the fruits of Lycium barbarum. DPP-IV-IN-5 exerts moderate agonistic activities for peroxisome proliferator-activated receptor (PPARγ) with EC50 values of 10.09 - 44.26 μM and also presents inhibitoryactivity on dipeptidyl peptidase-4 (DPPIV) with an IC50 value of 47.13 μM .
MMP-9-IN-8 (Compound 3) is an MMP-9 inhibitor with inhibitoryactivities of 42.16% and 58.28% at 10 μM and 50 μM concentrations, respectively. MMP-9-IN-8 has anti-cancer activity and can induce apoptosis in MCF-7 cells with an IC50 value of 23.42 μM .
KR-27370 (compound 7f) is an antiviral agent and selective PI4KIIIβ/PI4KIIIαinhibitor (IC50: 3.1 nM/15.8 nM), against hRV, Ke Saatchivirus and other enteroviruses have inhibitoryactivity[1].br/ .
Aldose reductase-IN-7 (Compound 6k) targets Aldose reductase. Aldose reductase-IN-7 exhibits potent enzyme inhibitoryactivity (Ki = 0.186 ± 0.020 μM), showing superiority to Epalrestat (HY-66009), which is currently in clinical use. Aldose reductase-IN-7 is less cytotoxic and possesses potent anticancer activity .
IDE-IN-3 (Compound 4) is an inhibitor for insulin-degrading enzyme. IDE-IN-3 is predicted to have CYP3A4, CYP2C19, hERG, NADP+, HIF1α and histidine kinase inhibitoryactivities, and has potential biological activity in anti-diabetic, anti-tumor, anti-bacterial aspects, according to the in silico prediction .
Anticancer agent 240 (compound 9b) is an 8-quinolinesulfonamide derivative with a cytotoxicity activity. Anticancer agent 240 shows inhibitoryactivity in Caco-2, SNB-19, A-549, and SKOV-3 cell line IC50 values of 0.26, 0.38, 0.40 and 4.16 μM .
HBV-IN-47 (compound 4a) is a capsid assembly regulator with inhibitoryactivity against hepatitis B virus (HBV). HBV-IN-47 exhibits strong anti-HBVactivity in HepAD38 cells with low toxicity (EC50=0.24 μM). HBV-IN-47 can be used for the study of chronic hepatitis B (CHB) .
LBM-415 (NVP-PDF 713) is a peptide deformylase (PDF) inhibitor that exhibits inhibitoryactivity against various antimicrobial-resistant gram-positive cocci, with a MIC90 range of 0.12-8 µg/ml. Additionally, inhibiting efflux pump activity can enhance bacterial sensitivity to LBM415, thereby improving its antibacterial efficacy .
SR14150 is a partial agonist of the NOP receptor with high affinity. The biological activity of SR14150 makes it potentially useful for the development of a new generation of multi-target opioids designed to simultaneously improve analgesia and reduce side effects. The activity of SR14150 and its interaction with other opioid receptors may provide new inhibitory options for the management of chronic pain .
Dehydrozingerone (Compound 10), a structural half analogue of Curcumin (HY-N0005), is a phenolic compound with antibacterial, anticancer, antioxidant, anti-Alzheimer’s and antifungal activity, which is isolated from ginger (Zingiber officinale) rhizomes. Dehydrozingerone shows moderate inhibitoryactivities on the secretion of HBsAg in HepG 2 cells with an IC50 value of 0.50 mM .
YM-58790 is a potent antagonist of mAChR. YM-58790 binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 exhibits potent inhibitoryactivity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .
Grape seed extract is a natural product, with anti-inflammatory and anti-proliferative effects. Grape seed extract shows inhibitoryactivity on the fat-metabolizing enzymes pancreatic lipase and lipoprotein lipase. Grape seed extract induces apoptotic in human colorectal cancer cells .
DNA crosslinker 4 (dihydrochloride) is a potent DNA minor groove binder. DNA crosslinker 4 (dihydrochloride) has certain inhibitoryactivity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 4 (dihydrochloride) can be used for researching anticancer .
Quercetin 3-O-rutinoside-7-O-glucoside (compound 8) is an antioxidant agent that canbe found in Hemerocallis fulva. Quercetin 3-O-rutinoside-7-O-glucoside shows strong lipid peroxidation inhibitoryactivities .
4-Nitrophenyl-N-acetyl-β-D-galactosaminide has inhibitoryactivity against GlcNAc and GalNAc with Kis of 1.15 mM and 0.51 mM, respectively. 4-Nitrophenyl-N-acetyl-β-D-galactosaminide is extracted from Trichomonas foetus (T. foetus)
BACE1-IN-11 is a BACE1inhibitor. BACE1-IN-11 has the BACE1 inhibitoryactivity with an IC50 value of 72 μM. BACE1-IN-11 can be used for the research of Alzheimer’s disease (AD) .
Angelol G, a coumarin, can be isolated from Campylotropis hirtella. Angelol G shows inhibitoryactivity for prostate specific antigen (PSA)IC50 value of 152.1μM. Angelol G can be used for the research of benign prostate hyperplasia (BPH) .
Artocarpin is an isoprenoid-substituted flavonoid, that can be isolated from the wood of Artocarpus heterophyllus. Artocarpin inhibits melanin biosynthesis in B16 melanoma cells without inhibiting tyrosinase. The presence of the isoprenoid-substituted moiety enhanced the inhibitoryactivity on melanin production in B16 melanoma cells .
BuChE-IN-8 (compound 19c) is a butyrylcholinesterase (BuChE)inhibitor with an IC50 of 559 nM. BuChE-IN-8 possesses human β-secretase (BACE1) and Aβ40 aggregation inhibitoryactivities. BuChE-IN-8 has significant antiamnesic properties .
Kapurimycin A1 is an anbitiotic that can be isolated from Streptomyces. Kapurimycin A1 has a significant inhibitory effect on Gram-positive bacteria, exhibits cytotoxicity to cultured mammalian cells, and shows strong antitumor activity against the mouse leukemia P388 cell line .
IDX375 is a novel non-nucleoside inhibitor with selective inhibitoryactivity against HCV NS5B. IDX375 has good selectivity for genotypes 1a and 1b. The structure and binding site of IDX375 were confirmed by X-ray cocrystal studies .
DF 461 is a sterol synthase inhibitor with significant inhibitoryactivity. DF 461 shows high selectivity for the liver and can effectively inhibit cholesterol synthesis in rat liver. DF 461 has shown the effect of lowering plasma lipids in repeated dosing studies in non-rodents .
Atecegatran TFA (AR-H067637 TFA) is an anticoagulant with selective direct thrombin inhibitoryactivity. Atecegatran TFA is commonly used to inhibit cardiovascular diseases. The biotransformation product of Atecegatran TFA, AR-H067637, is its active form and participates in the anticoagulation process .
Guanoxyfen (N-(3-Phenoxypropyl)guanidine) nitrate is a compound that exhibits potent inhibitoryactivity against the serine protease enzyme TMPRSS2, which plays a crucial role in the infectivity of coronaviruses. Guanoxyfen nitrate is also an effective inhibitor of vasoconstrictor responses to sympathetic nerve stimulation.
Anti-Trypanosoma cruzi agent-6 (Compound 8) exhibits inhibitoryactivity against Trypanosoma cruzi, that inhibits the epimastigote, trypomastigote and amastigote form of T. cruzi with IC50s of 24.7 µM, 1.8 µM and 1.6 µM, respectively .
PHOP is a fatty acid amide hydrolase (FAAH) inhibitor used to assess inhibitoryactivity in a fluorometric assay. PHOP can determine FAAH activity by measuring the amount of 4-pyridin-1-ylbutyric acid released by the enzyme in rat brain microsomes. PHOP demonstrates potential as a FAAH inhibitor and can directly measure FAAH activity by reversed-phase HPLC and fluorescence detection, providing a basis for the development of new inhibitors.
Lascufloxacin (KRP-AM1977) hydrochloride is a potent antibacterial compound candidate with broad-spectrum activity against various clinical isolates. Lascufloxacin hydrochloride shows the most potent activity against Gram-positive bacteria compared to other tested quinolones. Lascufloxacin hydrochloride demonstrates incomplete cross-resistance against existing quinolone-resistant strains. Lascufloxacin hydrochloride has potent inhibitoryactivity against both wild-type and mutated target enzymes.
Linaprazan (AZD0865) can inhibit H+,K+ -ATPase in the stomach through K+ competitive binding, (IC50: 1.0 ± 0.2 μM), it has a strong inhibitory effect on acid. Linaprazan (AZD0865) can be used for research on reflux esophagitis with oral activity .
OTS514 hydrochloride is a highly potent TOPKinhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells . OTS514 hydrochloride induces cell cycle arrest and apoptosis .
Meleagrin is a roquefortine C-derived alkaloid produced by fungi of the genus Penicillium and has antimicrobial and anti-proliferative activities. Meleagrin is a class of FabIinhibitor. Meleagrin is a lead c-Metinhibitory entity useful for the control of c-Met-dependent metastatic and invasive breast malignancies .
NADH-IN-1 has NADH:ubiquinone oxidoreductaseinhibitoryactivity with an IC50 value of 27 μM. NADH-IN-1 can effectively stimulate glucose uptake in vitro. NADH-IN-1 is readily metabolised by the liver. NADH-IN-1 can be used for researching diabetes .
HIV-1 inhibitor-44 (compound 11l) is a HIV-1 reverse transcriptase inhibitor. HIV-1 inhibitor-44 shows inhibitoryactivity against wild-type HIV-1 strain with an EC50 value of 0.209 μM .
CSNK1-IN-1 is a CSNK1A1inhibitor. CSNK1-IN-1 has inhibitoryactivity for CSNK1A1 kinase with IC50 values of 21 μM. CSNK1-IN-1 can be used for the research of proliferative disorders .
NoxaBH3 is a cysteine-based cross-linked peptide with increased cell permeability and higher inhibitoryactivity against Mcl-1. NoxaBH3 binds to the endogenous CXCR4 ligand to produce ubiquitin-Noxabh3 conjugate. NoxaBH3 is then delivered to cancer cells .
PARP-1-IN-4 is a PARP-1inhibitor. PARP-1-IN-4 has inhibitoryactivity against PARP-1 with IC50 value of 302 μM. PARP-1-IN-4 can be used for the research of lung adenocarcinoma .
Z57346765 is a PGK1-specific inhibitor that reduces the activity of metabolic enzymes in PGK1 glycolysis and inhibits PGK1-dependent cell proliferation. Z57346765 exerts inhibitory effects against clear cell renal cell carcinoma (KIRC) .
JNJ-26990990 is a broad-spectrum antiepileptic agent with oral activity. JNJ-26990990 can inhibit voltage-gated Na + channels and N-type Ca 2+ channels, but has a very weak inhibitory effect on human carbonic anhydrase-II (IC50 = 110 μM) .
1-Docosanol (Standard) is the analytical standard of 1-Docosanol. This product is intended for research and analytical applications. 1-Docosanol (Behenyl alcohol) is a saturated fatty alcohol with reported inhibitoryactivity against lipid-enveloped viruses, including herpes simplex virus (HSV) .
Propioxatin B is a tricyclic sesquiterpenoid compound isolated from the root of vetiver grass. It has anti-tuberculosis activity and inhibitory effects on a variety of drug-resistant mutants of Mycobacterium tuberculosis. In computer simulation docking studies, it showed binding affinity with bacterial DNA gyrase and has a certain safety in vivo.
(S)-Pomalidomide ((S)-CC-4047) is an angiogenesis-inhibiting drug with growth-inhibitoryactivity against B-cell tumors. (S)-Pomalidomide can induce complete tumor regression in BurKitt lymphoma cells. (S)-Pomalidomide serves as an immunomodulator with potential applications in inhibiting hematological malignancies .
Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS .Tilorone dihydrochloride exhibits an inhibitoryactivity with EC50 of 230 nM against Ebola virus (EBOV) .
ent-Toddalolactone is a natural compound with anti-inflammatory and anticancer activities. Ent-Toddalolactone has shown inhibitory effects on phosphodiesterase-4 (PDE4) in vitro and is a potential drug target for inhibiting asthma and chronic obstructive pulmonary disease. The activity of ent-Toddalolactone is related to its unique chemical structure, and some of its derivatives showed IC50 values below 10 μM in inhibition experiments, showing high biological activity .
Amcasertib (BBI503) is an orally active and small-molecule multi-kinase inhibitor. Amcasertib exhibits inhibitoryactivity against the NANOG and CD133 expression and cell viability in PC-9/GR cells. As an orally available cancer cell stemness kinase inhibitor with potential antineoplastic activity, it is currently being studied in phase I clinical trials in a number of cancers.
Pyropheophorbide-a (Ppa) is a photosensitizer used in photodynamic therapy (PDT) for tumors. Pyropheophorbide-a exhibits phototoxic effects on tumor cells, such as cervical cancer cells, and also has anti-lipogenesis activity. Pyropheophorbide-a shows potential for research in the fields of cancer and age-related macular degeneration (AMD). Pyropheophorbide-a derivatives also demonstrate inhibitoryactivity against tumor cells .
2-Hydroxycinnamic acid is a phenolic acid with antimicrobial and antioxidant properties. 2-Hydroxycinnamic acid has antimicrobial activity against Staphylococcus aureus and is not susceptible to drug resistance. 2-Hydroxycinnamic acid shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC50 of 0.3 mM. In addition, 2-Hydroxycinnamic acid has neuroprotective and antitumor activity .
Calphostin C is a potent and specific inhibitor of protein kinase C. Calphostin C is an antitumor antibiotic. Calphostin C has 1000 times more inhibitory to protein kinase C with an IC50 of 0.05 μM than other protein kinases. Calphostin C induces apoptosis in some tumor cell lines. Calphostin C has potent cytotoxic activity and antitumor activity .
TP0480066 is a selective topoisomerase IIinhibitor with IC50s of 1.10 and 62.89 nM for DNA gyrase and topo IV, respectively. TP0480066 shows good activity of againsting various bacterial species including drug-resistant strains. TP0480066 also exhibits potent inhibitoryactivity to N. gonorrhoeae, can be used in study of gonorrhea .
6-Prenylquercetin-3-Me ether is a natural product that can be extracted from G. uralensis leaves.
6-Prenylquercetin-3-Me ether has radical scavenging activity toward DPPH. 6-Prenylquercetin-3-Me ether also has inhibitoryactivity against α-glucosidase .
HPPD-IN-1 (compound II-3) is a HPPDinhibitor. HPPD-IN-1 shows inhibitoryactivity of Arabidopsis thaliana HPPD (AtHPPD) with an IC50 value of 0.248 μM, which was superior to that of mesotrione (HY-12853) (0.283 μM) in vitro. HPPD-IN-1 shows excellent herbicidal activity against broadleaf and monocotyledonous weeds .
3-Hydroxybakuchiol can be isolated from Otholobium mexicanum J. W. Grimes. 3-Hydroxybakuchiol is an electron transport chain (ETC)inhibitor. 3-Hydroxybakuchiol has antitumor activity, and induces tumor cell apoptosis. 3-Hydroxybakuchiol also has moderate inhibitoryactivity against α-glucosidase (IC50: 345 μM) .
Antibacterial agent 162 trifluoromethanesulfonate (compound 7) is an antibacterial agent that exhibits potent inhibitoryactivity against Staphylococcus aureus, including MRSA. Antibacterial agent 162 trifluoromethanesulfonate is also an anticancer agent and exhibits antiproliferative activity against colon cancer and non-small cell lung cancer cells. Antibacterial agent 162 trifluoromethanesulfonate can be used in anticancer and antibacterial research .
Cirsimarin (Standard) is the analytical standard of Cirsimarin. This product is intended for research and analytical applications. Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase .
AZD1897 is a PIM1, PIM2, and PIM3inhibitor with IC50 values of less than 3 nM for these three PIM kinases. AZD1897 exhibits anticancer activity and synergistically inhibits the activity of acute myeloid leukemia (AML) cells in combination with Capivasertib (HY-15431). This synergistic inhibitory effect is achieved through the inhibition of the mTOR and MCL1 pathways .
Guanfu base A hydrochloride is an antiarrhythmic alkaloid with the ability to inhibit CYP2D6 enzyme activity. Guanfu base A hydrochloride can be used to inhibit arrhythmia-related diseases. Guanfu base A hydrochloride exhibits inhibitory effects on CYP2D6 in different species of organisms, including humans, monkeys, and dogs. The biological activity of Guanfu base A hydrochloride makes it have potential clinical application value .
BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitoryactivity with an IC50 of 39.9 nM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses .
Apiin, a major constituent of Apium graveolens leaves with anti-inflammatory properties. Apiin shows significant inhibitoryactivity on nitrite (NO) production (IC50 = 0.08 mg/mL) in-vitro and iNOS expression (IC50 = 0.049 mg/ mL) in LPS-activated J774.A1 cells .
Pogostone is isolated from patchouli oil with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml . Pogostone induces cell apoptosis and autophagy .
Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer .
Slingshot inhibitor D3 is a potent, selective, reversible and competitive inhibitor of Slingshot. The IC50 value for Slingshot 1 is 3 μM and the Ki value for Slingshot 2 is 3.9 μM. Slingshot inhibitor D3 has similar inhibitoryactivities toward both Slingshot 1 and Slingshot 2 .
Cymarin, a cardiac glycoside, potently inhibits the Palytoxin (PTX)-induced K + release (IC50=0.42 μM). Cymarin reveals an antitumor activity against breast cancer and pancreatic cancer. Cymarin exhibits antifeedant and growth inhibitory effects as crop protectant .
Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitoryactivity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia .
CSNK1-IN-2 is a CSNK1A1inhibitor. CSNK1-IN-1 has inhibitoryactivity for CSNK1A1 kinase with IC50 values of 2.52 μM. CSNK1-IN-2 can be used for the research of proliferative disorders .
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA) is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
cis-Ferulic acid 4-O-β-D-glucopyranoside (compound 7) is a phenolic glycosid, which can be isolated from Nitraria sibirica.. cis-Ferulic acid 4-O-β-D-glucopyranoside exhibits antioxidant activity and potent inhibitory effect on Phosphatase PTP1B .
Hedycoronen A has inhibitoryactivity on the IL-6, IL-12 p40, and TNF-α production in LPS-Stimulated BMDCs, with IC50s of 9.1 μM, 5.6 μM, and 46.0 μM. Hedycoronen A can be isolated from Hedychium coronarium .
Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer .
(2E)-Eicosenoic acid is an inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase A (PtpA). (2E)-Eicosenoic acid exhibits strong inhibitoryactivity against PtpA with an IC50 value in the low micromolar range. (2E)-Eicosenoic acid can be used for research on Mycobacterium tuberculosis infection .
CS-722 is a centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex[1]. CS-722 inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents .
SEP-227900 is an orally active and potent DAAO (DAO) inhibitor with potential inhibitory applications. The biological activity of SEP-227900 may show benefits in diseases associated with vitamin D or sunlight exposure. SEP-227900 is expected to play an important role in improving cancer prognosis .
Alvimopan metabolite is a μ opioid receptor antagonist with activity that selectively interacts with μ peripheral receptors. Alvimopan metabolite can be used as a potential inhibitory drug to alleviate the side effects caused by opioids. Alvimopan metabolite was identified as a highly selective μ opioid receptor antagonist during research and development .
Benz[g]isoquinoline-5,10-dione, an active component isolated from the ethanolic extract of the aerial parts of Mitracarpus scaber, demonstrates notable in vitro inhibitoryactivity against AIDS-related pathogens, along with significant antibacterial and antifungal properties, as evidenced by the agar well-diffusion assay.
FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
(±)-Taxifolin-13C3 ((±)-Dihydroquercetin-13C3) is a derivative of (±)-Taxifolin, labeled with 13C3. (±)-Taxifolin is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitoryactivity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
NBD-556, a CD4 mimetic, is a potent HIV-1 entry inhibitor that blocks the gp120-CD4 interaction. NBD-556 shows potent cell fusion and virus-cell fusion inhibitoryactivity at low micromolar levels .
Alisol F is a triterpene isolated from Alisma orinentale, has immunosuppressive and anti-virus functions. Alisol F exhibits inhibitoryactivity in vitro on hepatitis B virus (HBV) surface antigen (HBsAg) secretion of the HepG2.2.15 cell line with an IC50 of 0.6 μM .
Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses the potential anti-tumor bioactivity, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitoryactivity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM .
Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 17.38 μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products .
CGP7930 (3-(3’,5’-Di-tert-butyl-4’-hydroxy) phenyl-2, 2-dimethylpropanol) is a positive metabotropic GABAB receptor allosteric modulator. CGP7930 enhances the inhibitory effect of l-baclofen on the oscillatory activity of cultured cortical neurons .
TbPTR1 inhibitor 1 (compound 5d) is a potent kinetoplastid pteridine reductase 1 (PTR1)inhibitor with an IC50<0.1 nM for TbPTR1. TbPTR1 inhibitor 1 has inhibitoryactivity against Trypanosoma brucei (EC50=0.66 μM) .
L2H2-6OTD, containing one to four G-quadruplex binding loops, is a telomeric inhibitor analogue. l2H2-6OTD has telomeraseinhibitoryactivity with an IC50 value of 15 nM .
Aromatase-IN-3 (compound 7d) is an aromataseinhibitor with an IC50 of 54 nM. Through suppressing the conversion of androstenedione to oestrogen caused by aromatase, Aromatase-IN-3 exerts an appreciable tumor growth inhibitoryactivities against breast cancer cell lines, suggesting its usage for ER+ cancer research .
SDH-IN-11 (compound A7) is a SDHinhibitor, and shows inhibitory effect on nematode feeding, reproductive ability, and egg hatching. SDH-IN-11 promotes the oxidative stress of nematodes and causes intestinal damage to nematodes. SDH-IN-11 inhibits the activity of succinate dehydrogenase (SDH) in nematodes .
Ebelactone A is a mycolic acid β-lactone, which exhibits inhibitoryactivity for esterase, lipase, fMet aminopeptidase (fMet AP) and PNBase, with IC50s of 56, 3, 8 and 7.5 μM, respectively . Ebelactone A inhibitscutinase, exhibits plants protective potency against Erysiphe graminis .
InhA-IN-7 (Compound 11) is a Triclocan (HY-B1119) derivative with inhibitoryactivity towards enoyl-acyl carrier protein reductase (InhA) with an IC50 of 96 nM. InhA-IN-7 inhibits proliferations of Mycobacterium tuberculosis wildtype and mutant strains with MICs ranging from 19 to 75 μM .
L2H2-6OTD acetate contains one to four G-quadruplex binding loops and is a telomere inhibitor analog. L2H2-6OTD acetate has telomerase inhibitoryactivity with an IC50 value of 15 nM .
SHP2-IN-29 (Compound 3) is a potent SHP2inhibitor with an IC50 value of 0.18 μM. SHP2-IN-29 also has inhibitoryactivity against PTP1B and TCPTP, with IC50 values of 4.27 and 4.74 μM, respectively.
Scirpusin A is a naturally occurring compound extracted from the legume plant Caragana rosea Turcz, exhibiting anti-HIVactivity. Scirpusin A demonstrates significant inhibitory effects against HIV-1 (EC50=7 μg/mL). Scirpusin A is utilized in research towards the development of anti-HIV therapeutics .
N-Caffeoyl O-methyltyramine (Standard) is the analytical standard of N-Caffeoyl O-methyltyramine. This product is intended for research and analytical applications. N-Caffeoyl O-methyltyramine is a class of alkaloid isolated from Cuscuta reflexa with strong inhibitoryactivity against α-glucosidase (IC50 of 103.58 μM) .
Antitumor agent-107 (compound 5h) is an anticancer agent that shows excellent inhibitoryactivity against leukemia cell lines (GI50=0.32-1.34 μM). Antitumor agent-107 also shows antitumor activity against various other human cancer cell lines (GI50 range 0.35-9.43 μM) .
Aloenin (Standard) is the analytical standard of Aloenin. This product is intended for research and analytical applications. Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitoryactivity on β-secretion (BACE) (IC50=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release .
BVT173187 is a selective inhibitor of the neutrophil formyl peptide receptor FPR1, with activity that inhibits FPR1 activation. BVT173187 inhibits FPR1 agonist-induced activation in neutrophils, reduces adhesion molecule mobilization and superoxide anion production, and has inhibitoryactivity on FPR1 similar to that of earlier described peptide antagonists, but also has effects on C5aR and CXCR signaling.
SNAP-7941 is a selective antagonist with anxiolytic, antidepressant and appetite suppressant activities. SNAP-7941 showed promising biological activity in initial animal studies. SNAP-7941 targets the melanin concentrating hormone receptor MCH1 and has significant inhibitory potential. SNAP-7941 was shown to inhibit the centrally induced MCH-induced drinking effect in in vivo studies .
Dibenzylideneacetone (DBA) is a fruit antifungal agent with inhibitoryactivity against Botrytis cinerea Chitinase with an IC50 of 13.10 μg/mL. Dibenzylideneacetone has an MIC of 32 μg/mL against B. cinerea and EC50 values of 16.29 and 14.64 μg/mL in inhibiting mycelial growth and spore germination, respectively. Dibenzylideneacetone can overcomes Botrytis cinerea infection in cherry tomatoes by inhibiting chitinase activity .
MLEB-22043 is a synthetic siderophore-monobactam conjugate that is taken up into bacteria via its synthetic siderophore component by TonB-dependent transporters. Once inside the bacteria, it exerts antibacterial activity through its β-lactam component. MLEB-22043 is a broad-spectrum antibiotic with significant inhibitoryactivity against Klebsiella pneumoniae, Escherichia coli, Acinetobacter baumannii, and Pseudomonas aeruginosa .
Cinosulfuron (Standard) is the analytical standard of Cinosulfuron. This product is intended for research and analytical applications. Cinosulfuron is a selective herbicide with excellent inhibitoryactivity against a variety of broadleaf weeds and is widely used in crop fields to protect the growth of crops. Cinosulfuron can effectively manage weed problems by inhibiting specific enzyme activity. Cinosulfuron is used in agriculture to increase crop yield and quality and ensure efficient use of farmland.
D-AP7 is a specific NMDA receptor antagonist with inhibitoryactivity against epileptiform activity. D-AP7 attenuated neuronal activation in spot activity by reducing the duration and number of exogenously induced bursts. D-AP7 also increased the amplitude of secondary action potentials, which may restore neuronal activity in some epileptiform bursts. D-AP7 showed anxiogenic effects and impaired memory consolidation in passive avoidance learning .
INF55 is a NoA multidrug resistance pump inhibitor with the activity of inhibiting the NoA pump. The heterocomplex formed by INF55 combined with berberine shows the potential to combat the resistance of bacterial compounds. INF55 can enhance the antibacterial activity of berberine by reducing its efflux. The structural variants of INF55 can show different NoA inhibitoryactivities, thereby affecting the antibacterial effect of its corresponding heterocomplexes. Different derivatives of INF55 show similar activity in terms of antibacterial dose and effectiveness .
Chroman 1 is a highly potent and selective ROCKinhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitoryactivity against MRCK, with an IC50 of 150 nM .
Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities .
Domatinostat tosylate (4SC-202) is a selective class I HDACinhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitoryactivity against Lysine specific demethylase 1 (LSD1).
Chroman 1 dihydrochloride is a highly potent and selective ROCKinhibitor. Chroman 1 dihydrochloride is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM).
Chroman 1 dihydrochloride also has inhibitoryactivity against MRCK, with an IC50 of 150 nM .
Anti-MRSA agent 2 (compound 14) has highly inhibitoryactivity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and relatively low cytotoxicity in normal cells. Anti-MRSA agent 2 has strong ability to destroy bacterial membrane and bind to genomic DNA .
CDK7-IN-11 is an orally active CDK7inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitoryactivity with IC50 value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7 .
HDAC6-IN-15 is a selective histone deacetylase 6 (HDAC6)inhibitor. HDAC6-IN-15 has potent inhibitoryactivity for HDAC6 with IC50 value of 38.2 nM. HDAC6-IN-15 can be used for the research of cancer and neurodegenerative diseases .
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA ) TFA is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA TFA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
SRI 37892 is a small molecule compound inhibitor of Frizzled protein 7 (Fzd7) with inhibitoryactivity against cancer cell proliferation (IC502μM). SRI 37892 significantly blocks Wnt/Fzd7 signaling. SRI 3789 can be used in the research of developing cancer therapeutic agents [1].
Antibacterial agent 156 (Compound 57) is a selective and potent bactericidal against C. difficile and targets cell-wall synthesis. Antibacterial agent 156 exhibits bactericidal activity with the minimal inhibitory concentration of 0.5 μg/mL and 1 μg/mL against MIMIC50 (101 strains) and MIC90 (101 strains) .
5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl (compound 8) can be isolated from Dendrobium infundibulum (D. infundibulum). 5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl has no inhibitoryactivity against α-glucosidase and pancreatic lipase .
Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs) .
Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy .
BTK-IN-28 (compound PID-4) is a potent BTKinhibitor with anticancer activity. BTK-IN-28 has inhibitory effects on BTK and downstream signaling cascades and selectively inhibits Burkitt lymphoma RAMOS proliferation. BTK-IN-28 has no significant cytotoxicity towards non-tumor cells .
hUP1-IN-1 is a hUP1inhibitor with Kii and Kis Urd of 375 and 635 nM. hUP1-IN-1 showes inhibitoryactivities over hUP1 catalyzed reaction with 70% at 1 μM. hUP1-IN-1 can be used for the research of cancer.
J-1149 is a potent ALK5inhibitor, with an IC50 value of 0.017 μM. J-1149 also shows weak p38α MAP kinase inhibitoryactivity, with an IC50 value of 0.435 μM. J-1149 can be used for liver fibrosis research .
Tioconazole (Standard) is the analytical standard of Tioconazole. This product is intended for research and analytical applications. Tioconazole (UK-20349) is an antifungal imidazole derivative with broad spectrum activity. Tioconazole has inhibitory active aginst several dermatophytes and several yeasts with MIC50s <3.12 mg/L and <9 mg/L, respectively .
ADL-5859 is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of 0.84 and 20 nM, respectively. ADL-5859 also shows inhibitoryactivity to hERG channel with an IC50 value of 78 μM. ADL-5859 can be used for the research of pain .
Cyclofenil (Standard) is the analytical standard of Cyclofenil. This product is intended for research and analytical applications. Cyclofenil is a selective estrogen receptor modulator and an ovulation-inducing agent. Cyclofenil shows an inhibitory effect on dengue virus replication in Vero cells with an EC50 of 1.62 μM. Cyclofenil has anti-dengue-virus activity .
Necroptosis-IN-5 (Compound 26) is an orally active necroptosisinhibitor. Necroptosis-IN-5 also exhibits potent inhibitoryactivity against receptor-interacting protein kinase 1 (RIPK1). Necroptosis-IN-5 can be used to study necroptosis-related inflammatory diseases, neurodegenerative diseases, and cancers .
Boc-β-Ala-ol (3-(Boc-amino)-1-propanol) is an alanine derivative with a Boc protecting group at the N-terminus, which can be used to synthesize bioactive peptide mimics, such as Nα-Benzoyl-α-azaornithine phenyl ester, which has trypsin inhibitoryactivity .
Ro 18-3981 is a dihydropyridine that inhibits cardiac Ca 2+ channels. Ro 18-3981 shows higher inhibitoryactivity when the cell membrane is in a depolarized state (Vh=-20 mV: IC50=2.3 nM; Vh=-50 mV: IC50=100 nM) .
Tolciclate (KC 9147) is an antifungal agent with in vitro inhibitoryactivity against dermatophytes, effective at concentrations of 0.01-0.1 μg/mL. Tolciclate is colorless and soluble in well-tolerated excipients, and it is more lipophilic than Tolnaftate (HY-B0370). Tolciclate can be used in research related to antifungal infections .
Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitoryactivity in structure−activity relationship (SAR) study (KD = 0.0029 μM) .
Neptinib (NEP010) is an orally active derivative of Afatinib (HY-10261) that has stronger antitumor activity than Afatinib (HY-10261) by improving pharmacokinetics. Neptinib has a significant inhibitory effect on tumor growth in mouse non-small cell lung cancer models with different EGFR mutations. Neptinib has a certain inhibitory effect on the EGFR kinase family, with IC50 values ??of 0.24 nM, 7.25 nM, 0.46 nM and 1.79 nM for EGFRwt, EGFRL858R/T790M, EGFRL858R and EGFRT790M, respectively .
NGD9002 free base is a new generation of selective corticotropin-releasing factor-1 (CRF-1) receptor antagonist with inhibitoryactivity on CRF-induced colonic function stimulation. NGD9002 free base can reduce CRF-induced fecal output response and show an inhibitory IC50 value of 4.3 mg/kg. NGD9002 free base can effectively block CRF-induced colonic secretory motility stimulation at the highest dose and reduce acute water avoidance-induced defecation. NGD9002 free base can also prevent the occurrence of pain hypersensitivity reactions to repeated colonic distension .
5M038 is an inhibitor of HIV envelope-mediated fusion with potent inhibitoryactivity against gp41-mediated membrane fusion. 5M038 prevents the formation of the gp41 post-fusion conformation and inhibits envelope-mediated membrane fusion in cell-cell fusion and viral infectivity assays. 5M038 has shown broad fusion inhibition in tests against multiple HIV-1 subtypes, including M and T strains. 5M038 targets a highly conserved hydrophobic pocket and binds to the gp41 trimer, thereby exerting its inhibitory effect .
o-Cymen-5-ol is a broad-spectrum antimicrobial agent with direct antimicrobial activity. o-Cymen-5-ol showed effective minimum inhibitory concentrations (MICs) against a variety of bacteria and fungi, such as Streptococcus mutans and Candida albicans. The combination of o-Cymen-5-ol and zinc showed synergistic effects, enhancing the inhibitory effect against oral pathogens. o-Cymen-5-ol was able to inhibit the glycolysis process and co-enhanced this effect with zinc. o-Cymen-5-ol showed a stronger antibacterial effect in toothpaste than placebo .
AKR1C2/3-IN-2 is a potential AKR1C3 inhibitor with selective AKR1C3 activity. AKR1C2/3-IN-2 is able to block AKR1C3-mediated testosterone (T) production and PSA induction, affecting the endocrine activity of prostate cancer cells. AKR1C2/3-IN-2 shows selectivity over other AKR1C enzymes, indicating its potential application in inhibiting drug-resistant prostate cancer. AKR1C2/3-IN-2 has no inhibitoryactivity against COX isomerases, further emphasizing its specificity as a prostate cancer inhibitory compound .
4-Allylcatechol (4-Allylpyrocatechol) is a xylan isolated from the root of Piper taiwanense. 4-Allylcatechol has a strong inhibitoryactivity against collagen-induced platelet aggregation (IC50=5.3 μM). In addition, 4-Allylcatechol has anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv (MIC=27.6 μg/mL) .
SRI 31215 (TFA) is a Matriptase/Hepsin/hepatocyte growth factor activator (HGFA) triplex inhibitor and mimics the activity of HAI-1/2 (endogenous inhibitors of HGF activation). SRI 31215 has potent inhibitoryactivity against matriptase, hepsin and HGFA with IC50 values of 0.69 μM, 0.65 μM and 0.30 μM, respectively. SRI 31215 can be used for the research of cancer .
HDAC6-IN-18 (Compound 4) is a first irreversible HDAC6 isoform selective inhibitor with potent anti-multiple myeloma activity. HDAC6-IN-18 has HDAC6 inhibitoryactivity in RPMI8266, U266 and MM.1S cells with IC50 values of 0.17, 0.7 and 0.42 μM, respectively .
Cap-dependent endonuclease-IN-27 (Compound 8) is an orally active potent cap-dependent endonuclease (CEN) inhibitor. Cap-dependent endonuclease-IN-27, an antiviral agent, shows activity against influenza B virus. Cap-dependent endonuclease-IN-27 has inhibitoryactivity against IFV A/WSN/33 (H1N1) polymerase (EC50 = 12.26 nM) .
Antibacterial agent 202 (compound 45c) is a low cytotoxicity bacterialinhibitor with good activity against Gram-negative bacteria, including Escherichia coli, Klebsiella pneumonia, especially Pseudomonas aeruginosa, (MIC (minimum inhibitory concentration)=7.8-31.25 μM). Antibacterial agent 202 can exert antibacterial activity by destroying the integrity of cell membranes and can be used in the research of bacterial infections .
BMD4503-2 is a quinoxaline derivative with inhibitoryactivity against LRP5/6-sclerostin interactions. BMD4503-2 restores the activity of the Wnt/β-catenin signaling pathway by competitively binding to the LRP5/6-sclerostin complex. BMD4503-2 can be used in the study of Wnt signaling pathways in bone development, maintenance and osteoporosis .
Ilicicolin C exhibits antibacterial activity against Pseudomonas syringae with IC50 of 28.5 µg/mL. Ilicicolin C exhibits weak inhibitoryactivities against acetylcholinesterase (AChE) and β-glucuronidase with IC50 of 30-43 µg/mL. Ilicicolin C exhibits weak cytoxicity in human lung fibroblasts with IC50 of 64-120 µg/mL. Ilicicolin C affects seed germination and root tip growth of lettuce .
ABD-350 is an antiresorptive agent that inhibits osteoclast activity without affecting osteoblast activity and preventing ovariectomy-induced bone loss. ABD-350 inhibits NF-κB ligand-induced inhibitor of NF-κB phosphorylation, leading to osteoclast apoptosis, but has no inhibitory effect on osteoblast function, effectively preventing bone loss in ovariectomized mice, and does not inhibit parathyroid hormone-induced bone formation.
CGP55845 is a potent and selective GABAB receptor antagonist with activity that blocks agonist binding. The IC50 value of CGP55845 is 5 nM, indicating that it exhibits significant activity in inhibiting GABA and glutamate release. The apparent Kd of CGP55845 when forming a complex with the GABAB receptor is 30 nM, indicating its high affinity for this receptor. CGP55845 is as potent as 100 μM CGP 35348 in relieving the inhibitory effect of (R)-(-)-baclofen .
Etoricoxib hydrochloride (MK-0663 hydrochloride) is a synthetic nonsteroidal anti-inflammatory drug with cyclooxygenase-2 inhibitoryactivity. Etoricoxib hydrochloride can inhibit the conversion of arachidonic acid to prostaglandins, thereby reducing inflammation and pain. Etoricoxib hydrochloride is used to inhibit osteoarthritis and has anti-inflammatory and bone remodeling effects. The formulation of etoricoxib hydrochloride is prepared by emulsion solvent evaporation technology and exhibits good cell compatibility and enhanced alkaline phosphatase activity .
ADL-5859 hydrochloride (compound 20) is a selective and orally active δ opioid receptor (DOR) agonist with an Ki and an EC50 value of 0.84 and 20 nM, respectively. ADL-5859 hydrochloride also shows inhibitoryactivity to hERG channel with an IC50 value of 78 μM. ADL-5859 hydrochloride can be used for the research of pain .
Clinafloxacin (AM 1091) is a potent and broad-spectrum fluoroquinolone antibiotic, has inhibitoryactivity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro . Clinafloxacin is against DNA gyrase and topoisomerase IV of?S. aureus with IC50 values of 0.92 μg/ml and 1.62 μg/ml, respectively .
Domatinostat (4SC-202 free base) is a selective class I HDACinhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitoryactivity against Lysine specific demethylase 1 (LSD1).
Milbemycin oxime is an orally active macrolide with broad-spectrum antiparasitic activity. Milbemycin oxime is a mixture of oximes consisting of oxime derivatives corresponding to milbemycin A4 and A3. Milbemycin oxime binds to glutamate-gated chloride channels and has inhibitory potency against intestinal nematodes and lung/heart worms .
CS-722 Free base is a synthesized centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex . CS-722 Free base inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents .
Clinafloxacin hydrochloride (AM 1091 hydrochloride) is a potent and broad-spectrum fluoroquinolone antibiotic, has inhibitoryactivity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro . Clinafloxacin hydrochloride is against DNA gyrase and topoisomerase IV of S. aureus with IC50 values of 0.92 µg/ml and 1.62 µg/ml, respectively .
ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol and can be isolated from Vitis vinifera, displays a potent inhibitory for all the CYPactivities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity .
TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1)inhibitor with an IC50 of 14 nM. The inhibitoryactivities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM) .
Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin Bactivity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis .
Validamycin A, a fungicidal, is an agricultural antibiotic. Validamycin A is originally isolated from Streptomyces hygroscopicus var. limoneus. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL . Validamycin A shows potent inhibitoryactivity against trehalase of Rhizoctonia solani, with an IC50 of 72 μM . Validamycin A is a reversible tyrosinaseinhibitor, with a Ki of 5.893 mM .
HZ-1157 inhibitsHCV NS3/4A protease with an IC50 of 1.0 μmol/L. HZ-1157 (4a) has a high dengue virus inhibitoryactivity (EC50 = 0.15 μM) and is a relatively nontoxic (CC50 > 10 μM) dengue antiviral agent .
Cap-dependent endonuclease-IN-19 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-19 is a spirocyclic pyridone derivative. Cap-dependent endonuclease-IN-19 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN111410661A, compound 1) .
Harringtonolide is a potent RACK1inhibitor (IC50=39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction between FAK and RACK1. Harringtonolide has plant growth inhibitory, antiviral, anti-inflammatory, and antiproliferation activities .
SIRT5 inhibitor 2 (compound 49) is a potent SIRT5inhibitor with an IC50 value of 2.3 μM. SIRT5 inhibitor 2 has inhibitoryactivity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 can be used for researching cancer and neurodegenerative diseases .
DNA Gyrase-IN-1 (compound 42) is a potent and selective DNA gyraseinhibitor with an IC50 value of 2.6 µM. DNA Gyrase-IN-1 has high inhibitoryactivity against Mycobacterium tuberculosis (Mtb) with MIC of 0.49 µM. DNA Gyrase-IN-1 can be used for researching tuberculosis .
MMP2-IN-3 (compound 2) is a potent MMP-2 (matrix metalloproteinases) inhibitor, with an IC50 of 31 μM. MMP2-IN-3 also shows inhibitoryactivity against MMP-9 and MMP-8, with IC50 values of 26.6, and 32 μM, respectively .
DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitoryactivity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells .
YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitoryactivity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .
Magnoloside B is an α-glucosidaseinhibitor (IC50=0.69 mM), which can be obtained from Magnolia officinalis stem bark. Magnoloside B shows moderate inhibitoryactivity against MGC-803 and HepG2 cells. Magnoloside B has the potential to study cancer and diabetes .
JTK-109 is a potent inhibitor of hepatitis C virus NS5B RNA-dependent RNA polymerase. JTK-109 has NS5B inhibitoryactivity with IC50 value of 0.017μM. JTK-109 can be used for the research of hepatitis C virus (HCV) .
Alternaphenol B2 is a selective IDH1inhibitor from the coral-derived fungus Parengyodontium album SCSIO SX7W11. Alternaphenol B2 shows inhibitoryactivity against isocitrate dehydrogenase mutant R132H (IDH1m), with IC50 values of 41.9 μM .
α-Glucosidase-IN-42 (Compound 26) is a 9-O-berberrubine carboxylate derivative. α-Glucosidase-IN-42 has potent α-glucosidase inhibitoryactivities with an IC50 value in the range of 1.61 μM. α-Glucosidase-IN-42 can be used for the research of antidiabetic .
Ro 22-9194 inhibits aggregation and thromboxane Az (TXA2) synthetase activity in rabbit and human platelets. Ro 22-9194 has a potent inhibitory action against various types of model arrhythmias. Ro 22-9194 has non-cholinergic cardiac depressant properties with its vasodilating action .
hUP1-IN-1 potassium (compound 6a) is a hUP1inhibitor with Kii and Kis Urd of 375 and 635 nM. hUP1-IN-1 potassium showes inhibitoryactivities over hUP1 catalyzed reaction with 70% at 1 μM. hUP1-IN-1 potassium can be used for the research of cancer .
SGP8 (IAVPGEVA) is an octapeptide produced by hydrolysis of soybean 11S globulin, which has the effects of regulating lipid metabolism, inflammation and fibrosis. SGP8 (IAVPGEVA) exhibits inhibitoryactivity against DPP4 and inhibits the JNK-c-Jun signaling pathway, and has the ability to inhibit non-alcoholic steatohepatitis (NASH) .
TEAD-IN-10 (compound 15) has good selective activity and inhibitory effect on TEAD1 (IC50=14 nM), TEAD2 (IC50=179 nM) and TEAD3 (IC50=4 nnM) as a covalent inhibitor. TEAD-IN-10 can be used for cancer research .
JANEX-1 (WHI-P131) hydrochloride is a potent and specific JAK3inhibitor (Ki=2.3 μM). JANEX-1 hydrochloride shows potent JAK3inhibitoryactivity (IC50=78 μM), does not inhibitJAK1 and JAK2 .
Sartorypyrone A (20-O-Acetylsartorypyrone D) is a monocyclic terpenoid isolated from the soil fungus Neosartorya fischeri. Sartorypyrone A exhibits in vitro growth inhibitoryactivity against MCF-7, NCI-H460, and A375-C5 cell lines, and has potential anticancer properties.
MeSeI exhibits a weak inhibitoryactivity against monoamine oxidase MAO-A and MAO-B (IC50=198.8 µM). MeSeI regulates dopamine receptor D2 and norepinephrine receptor α2, β1, and exhibits antidepressant-like effect in mice. MeSeI is orally active .
InhA-IN-8 (compound 6c) is an orally active inhibitor of Mycobacterium tuberculosis InhA (enoyl ACP reductase). InhA-IN-8 has good inhibitoryactivity against Mtb UalRv (MIC = 0.5-1 μg/mL). InhA-IN-8 can be used in research on acute tuberculosis model mice .
Isomer-CM 352 is a new antifibrinolytic agent with inhibitoryactivity against matrix metalloproteinases. Isomer-CM 352 effectively reduced hematoma expansion and promoted functional and neurological recovery in a model of intracerebral hemorrhage. Isomer-CM 352 improved neurological function by preventing hematoma growth and showed potential in the suppression of acute neurological diseases .
4-Methylumbelliferyl β-D-mannopyranoside is a substrate that exhibits β-mannosidase activity. 4-Methylumbelliferyl β-D-mannopyranoside can be used to study β-mannosidase deficiency. The reactivity of 4-Methylumbelliferyl β-D-mannopyranoside shows different inhibitory effects on various substrates.
20(R)-Ginsenoside Rg2 (Standard) is the analytical standard of 20(R)-Ginsenoside Rg2. This product is intended for research and analytical applications. 20(R)-Ginsenoside Rg2 shows inhibitory effects on lung cancer NCI-H1650 cells. Anti-cancer activities .
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
JNK-1-IN-3 (Compound 9e) is an inhibitor of JNK1 that downregulates JNK1 gene expression and inhibits the protein levels of its phosphorylated form, concurrently reducing the expression of its downstream targets, c-Jun and c-Fos, in tumors while restoring p53activity. JNK-1-IN-3 exhibits broad-spectrum antiproliferative activity, particularly with high inhibitoryactivity against renal and breast cancer cell lines, demonstrating both in vivo and in vitro anticancer activity .
Cadmium pyrithione is a metal compound that inhibits protein deubiquitinase activity. Cadmium pyrithione treatment results in significant accumulation of ubiquitinated proteins in cancer cells and primary leukemia cells. Cadmium pyrithione strongly inhibits the activity of proteasome deubiquitinase (such as USP14 and UCHL5), but has a smaller inhibitory effect on 20S proteasome activity. The anticancer activity of Cadmium pyrithione is associated with the induction of apoptosis through caspase activation. Furthermore, Cadmium pyrithione inhibition inhibited proteasome function and suppressed tumor growth in animal xenograft models .
Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
Metallo-β-lactamase-IN-5 (compound 5c) is a potent metallo-β-lactamases (MBL)inhibitor. Metallo-β-lactamase-IN-5 shows inhibitoryactivity against MBLs NDM-1 and VIM-1. Metallo-β-lactamase-IN-5 inhibits HUVECs with an IC50 of 45 μg/mL. Metallo-β-lactamase-IN-5 plus Imipenem exhibits synergistic antimicrobial activity .
Chitin synthase inhibitor 12 is a chitin synthaseinhibitor. Chitin synthase inhibitor 12 shows excellent inhibitoryactivity with an IC50 value of 0.16 mM. Chitin synthase inhibitor 12 also is a broad-spectrum antifungal agent and has significantly antifungal activity against drug-resistant fungal variants, such as C. albicans and C. neoformans. Chitin synthase inhibitor 12 can be used for the research of invasive fungal infections (IFIs) .
Chitin synthase inhibitor 10 is a chitin synthaseinhibitor. Chitin synthase inhibitor 10 shows excellent chitin synthase inhibitoryactivity with an IC50 value of 0.11 mM. Chitin synthase inhibitor 10 also is an antifungal agent and has significantly antifungal activity against drug-resistant fungal variants, such as C. albicans and C. neoformans. Chitin synthase inhibitor 10 can be used for the research of invasive fungal infections (IFIs) .
CPUL1 is a TrxRinhibitor, which shows proliferation-inhibitory and anti-metastatic activity against A549 cells. CPUL1 influences EMT (epithelial-mesenchymal transition) via inducing ROS-mediated ERK/JNK signaling by inhibiting TrxR1 enzyme activity. CPUL1 in combination with α-Lipoic Acid (HY-N0492) or Dithiodipropionic acid (HY-W014395) is more effective .
PC-766B is a macrolide antibiotic. PC-766B is active against Gram-positive bacteria, and some fungi and yeasts, but inactive against Gram-negative bacteria. PC-766B shows antitumor activity against murine tumor cells. PC-766B has weak inhibitoryactivity against Na +, K +-ATPase .
AK-HW-90 (compound 2B) is a potent panBcr-Ablinhibitor with significant inhibitoryactivity against Imatinib (HY-15463)-resistant mutants. AK-HW-90 inhibits the resistance mutant Bcr-Abl T315I with an IC50 of 0.65 nM. AK-HW-90 has potential anticancer activity and can be used in the study of chronic myelogenous leukemia (CML) .
Kaempferol 3-O-gentiobioside (Standard) is the analytical standard of Kaempferol 3-O-gentiobioside. This product is intended for research and analytical applications. Kaempferol 3-O-gentiobioside is a flavonoid isolated from C. alata leaves with antidiabetic activity. Kaempferol 3-O-gentiobioside possesses activity against α-glucosidase and displays carbohydrate enzyme inhibitory effect with an IC50 of 50.0 μM .
7ETMC is a cytochrome P450 inhibitor with selective inhibition of human cytochrome P450s 1A1 and 1A2. 7ETMC has inhibitory effects on P450s 1A1 and 1A2 with IC?? values of 0.46μM and 0.50μM, respectively, within the first six minutes, and has no inhibitoryactivity against P450s 2A6 and 2B1. Except for 7-ethynyl-3-methyl-4-phenylcoumarin, the remaining inhibitors show mechanism-based inhibition of P450s 1A1 and 1A2.
Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
AA26-9 is a potent and broad spectrum serine hydrolaseinhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitoryactivity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .
Pterostilbene is a stilbenoid isolated from blueberries and Pterocarpus marsupium . Shows anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic and anti-obesity properties . Pterostilbene blocks ROS production , also exhibits inhibitoryactivity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide .
SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibitsLeishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitoryactivity against cathepsin G .
IM-54 is a selective inhibitor of oxidative stress-induced necrosis. IM-54 shows potent inhibitoryactivity against H2O2-induced necrosis. IM-54 acts as a potential cardioprotective agent and biological tool for investigating the molecular mechanisms of cell death .
MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE V; PDE5)inhibitor with an IC50 of 19 nM. MBCQ lacks inhibitoryactivity toward other PDE isozymes (all IC50s>100 μM). MBCQ dilates coronary arteries via specific inhibition of cGMP-PDE .
Gallocyanine chloride, a synthetic blue dyestuff, blocks DKK1inhibitoryactivity by disrupting DKK1/LRP6 interaction. Its association with LRP6 is weak (IC50 of about 3 μM in the inhibition of DKK1 binding). Gallocyanine dye acts as a potential agent for the research of Alzheimer's disease and related neurodegenerative tauopathies .
Mt KARI-IN-2 (compound 5b) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI)inhibitor with a Ki value of 2.02 μM. Mt KARI-IN-2 has inhibitoryactivity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 86 μg/mL) .
Mt KARI-IN-4 (compound 5c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI)inhibitor with a Ki value of 5.48 μM. Mt KARI-IN-4 has inhibitoryactivity against Mtb H37Rv (MIC = 0.78 μM) and low cytotoxicity (HEK IC50 > 72 μg/mL) .
Mt KARI-IN-5 (compound 6c) is a potent Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI)inhibitor with a Ki value of 4.72 μM. Mt KARI-IN-5 has inhibitoryactivity against Mtb H37Rv (MIC = 1.56 μM) and low cytotoxicity (HEK IC50 > 64 μg/mL)
DNA crosslinker 2 (dihydrochloride) is a potent DNA minor groove binder with DNA binding affinity (ΔTm) of 1.2 °C. DNA crosslinker 2 (dihydrochloride) has certain inhibitoryactivity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 2 (dihydrochloride) can be used for researching anticancer .
Kanamycin (Kanamycin A) is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin shows good inhibitoryactivity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
ALK5-IN-29 is an selective activin receptor-like kinase (ALK)inhibitor. ALK5-IN-29 can inhibit the activity of ALK5 with an IC50 value of ≤10 nM. ALK5-IN-29 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
HSP90-IN-18 is an effective heat shock protein 90 (Hsp90) inhibitor. HSP90-IN-18 has effective Hsp90 inhibitoryactivity with an IC50 value of 0.39 μM. HSP90-IN-18 can be used for the research of viral infection, neurodegenerative disease, and inflammation .
HSP90-IN-19 is an effective heat shock protein 90 (Hsp90) inhibitor. HSP90-IN-19 has effective Hsp90 inhibitoryactivity with an IC50 value of 0.27 μM. HSP90-IN-19 can be used for the research of viral infection, neurodegenerative disease, and inflammation .
LSD1-IN-23 is a competitive/non-competitive mixed inhibitor of lysine specific demethylase 1 (LSD1). LSD1-IN-23 has LSD1 inhibitoryactivity with an IC50 value of 0.58 μM. LSD1-IN-23 can be used for the research of neuroblastoma (NB) .
Estrone O-sulfamate (Estrone 3-O-sulfamate) is a potent steroid sulfatase (STS)inhibitor. Estrone O-sulfamate has inhibitoryactivity for STS in a placental microsomes (P.M.) preparation and in MCF-7 cells with IC50 values of 18 nM and 0.83 nM, respectively. Estrone O-sulfamate can be used for the research of cancer .
AChE-IN-29, 3-OH pyrrolidine derivative, is an cholinesterase (ChE)inhibitor. AChE-IN-29 has cholinesterase inhibitoryactivity for hAChE, eeAChE and eqBChE with IC50 values of 0.25 μM, 0.23 μM and 0.72 μM, respectively. AChE-IN-29 can be used for the research of Alzheimer's disease .
Lyoniside is a lignan glycoside with antioxidant, allelopathic and antifungal activities, which can be isolated from the rhizomes and stems of bilberry (Vaccinium myrtillus L.). Lyoniside exhibits radical scavenging properties with an IC50 value of 23 μg/mL in DPPH assay. Lyoniside inhibits the mycelial growth of Fusarium oxysporum and Mucor hiemalis at 50 μg/mL with inhibitory rates of 78% and 80%, respectively .
CAF-382 (compound B1) is an analog of SNS-032 and a CDKL5 and pan-CDK inhibitor with a weak GSK3α/β affinity (>1.8 μM) and inhibitoryactivity. CAF-382 inhibits CDKL5 and blocks the phosphorylation of the CDKL5 E2 domain .
HMG-CoA Reductase-IN-1 is a HMG-CoA reductaseinhibitor. HMG-CoA Reductase-IN-1has high HMGRinhibitoryactivity and OATP1B1 affinity with pIC50 and pKm values of 8.54 and 1.98, respectively. HMG-CoA Reductase-IN-1 can be used for the research of hypercholesterolemia .
Protoapigenone is an antineoplastic agent isolated from ferns. Protoapigenone has significant inhibitoryactivity against Hep G2, Hep 3B, MCF-7, A549 and MDAMB-231, with IC50s values of 1.60, 0.23, 0.78, 3.88 and 0.27 μg/mL respectively .
Majoranaquinone exhibits a high antibacterial effect against 4 Staphylococcus, 1 Moraxella, and 1 Enterococcus strains. Majoranaquinone shows substantial efflux pump inhibitoryactivity in Escherichia coliATCC 25922 strain. Majoranaquinone is found to be an effective biofilm formation inhibitor on E.coli, ATCC 25922 and E. coli K-12 AG100 bacteria .
RIPK1-IN-13 (compound 28) is a selective inhibitor for receptor-interacting serine/threonine-protein kinase 1 (RIPK1), the inhibitoryactivity is measured by ADP-Glo Kinase Assay with a pKi of 7.66. RIPK1-IN-13 inhibits human leukaemia cells U937 with a pIC50 of 7.2 .
AChE/BuChE-IN-5 (compound 5a) is a dual target inhibitor. AChE/BuChE-IN-5 has excellent nanomolar inhibitoryactivity on acetylcholinesterase (AChE) (IC50=46.9 nM) and butyryl cholinesterase (BuChE) (IC50=3.5 nM). AChE/BuChE-IN-5 can be used for Alzheimer's Disease research .
Altromycin F is an anthraquinone-derived antibiotic produced by the actinomycete AB 1246E-26 isolated from a South African bush soil. Altromycin F has antibacterial activity against Gram-positive bacteria, particularly Streptococcus and Staphylococcus, with a microbial inhibitory concentration (MIC) ranging from 0.2-3.12 μg/mL .
Antibacterial agent 235 (compound thy2I) shows antibacterial activity with minimum inhibitory concentration (MIC) values ranging from 0.5 μg/mL to 8 μg/mL. Antibacterial agent 235 could kill both gram-positive and gram-negative bacteria via a membrane-targeting mechanism of action with a low frequency of resistance .
GSK-3β inhibitor 21 (compound 44) is an ATP-competitive GSK-3βinhibitor (IC50=6.06 μM) with anti-amyloid aggregation and tau phosphorylation inhibitoryactivities. GSK-3β inhibitor 21 can be used in the study of Alzheimer's disease .
Photosensitizer-6 (Compound 4) is a gold (I) complex and exhibits inhibitoryactivity against TrxR. Photosensitizer-6 induces apoptosis in 4T1 cell, targets and eradicates tumors through chemo-phototherapy and immunogenic cell death under light exposure. Photosensitizer-6 can be used for tumor imaging .
U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
APA-APA-MPO dihydrochloride is an inhibitor of PCAF bromodomain/Tat-AcK50 interaction with reduced cytotoxic activity. APA-APA-MPO dihydrochloride can effectively inhibit the binding of PCAF to Tat-AcK50, showing its potential in HIV/AIDS inhibitory strategies. APA-APA-MPO dihydrochloride can be used in studies that hinder HIV replication .
L589420-0-2 (L-420) is a sodium pump inhibitor with inhibitoryactivity in human erythrocytes. L589420-0-2 can regulate the concentration of intracellular sodium ions, thereby affecting the electrophysiological properties of cells. L589420-0-2 may also play an important role in the inhibition of cardiovascular diseases .
Fagaronine chloride is an alkaloid with inhibitoryactivity against reverse transcriptase and topoisomerase I. Fagaronine chloride can effectively inhibit the reverse transcriptase of RSii tumor virus at a concentration of 6-60 μg/mL. Fagaronine chloride rapidly blocks the synthesis of DNA polymerase by interacting with the template primer. Fagaronine chloride has shown anti-tumor potential, especially in the study of retroviral infection .
Lankacidin C 8-acetate is an antibiotic with antibacterial activity. Lankacidin C 8-acetate, as a component of the Lankacidin group (T-2636) antibiotics, shows inhibitory effects against specific bacteria. Lankacidin C 8-acetate can generate other esterates by reacting with different acyl donors, indicating its importance in the synthesis of antibiotics .
ALK5-IN-84 (Compound 23) is an ALK5 inhibitor with a pKi value of 9.35 against hALK5. When administered via inhalation, ALK5-IN-84 exhibits significant ALK5inhibitoryactivity. ALK5-IN-84 is promising for the development of inhaled ALK5inhibitors .
2,5-Dimethylcelecoxib is an analogue of celecoxib (HY-14398) with anticancer activity but without COX-2 inhibitoryactivity. 2,5-Dimethylcelecoxib exerts its anti-cancer cell proliferation effect by inhibiting the core mechanism of the Wnt/β-catenin signaling pathway. 2,5-Dimethylcelecoxib also inhibits T-cell factor-dependent transcriptional activity and inhibits expression of the Wnt/β-catenin target gene products cyclin D1 and survivin .
Tilorone (dihydrochloride) (Standard) is the analytical standard of Tilorone (dihydrochloride). This product is intended for research and analytical applications. Tilorone dihydrochloride is an orally active interferon (IFN) inducer with broad-spectrum antiviral activities. Tilorone dihydrochloride possesses robust anti-Severe fever with thrombocytopenia syndrome virus (SFTSV) activity in vitro and in vivo through stimulation of host innate immunity. Tilorone dihydrochloride can penetrate the blood-brain barrier to activate HIF in the CNS .Tilorone dihydrochloride exhibits an inhibitoryactivity with EC50 of 230 nM against Ebola virus (EBOV) .
SB 239063 is a potent, selective and orally active p38 MAPKinhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitoryactivity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD .
AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals .
Y18501 is a oxysterol-binding protein (OSBPI) inhibitor with a similar structure to Oxathiapiprolin. Y18501 shows strong inhibitoryactivities against Phytophthora spp. and Pseudoperonospora cubensis, with EC50 ranging from 0.0005 to 0.0046 μg/mL. Y18501 shows excellent protective and curative activities against P. cubensis. Y18501 in combination with Chlorothalonil (HY-N6625) can significantly promote the inhibition of P. cubensis .
Talaroterphenyl A (compound 1) is a p-terphenyl derivative present in the mangrove sediment-derived fungus Talaromyces sp. SCSIO 41412, which exhibits phosphodiesterase 4 (PDE4) inhibitoryactivity (IC50=1.2 μM). Talaroterphenyl A also exhibits anti-inflammatory and anti-fibrotic activities, significantly reducing the mRNA levels of pro-inflammatory cytokines IL-6, TNF-α, and IL-1β .
SCH-538415 is a novel acyl carrier protein synthase inhibitor isolated from an unknown bacterial microorganism. The structural elucidation of compound 1 was completed by analyzing spectral data including UV, MS and 2D-NMR spectra. Compound 1 showed inhibitoryactivity in the acyl carrier protein synthase (AcpS) test with an IC50 value of 4.19 μM and exhibited antibacterial activity against Staphylococcus aureus in the agar diffusion test.
Diclofenac deanol (DDNL) is a nonsteroidal anti-inflammatory drug with anti-inflammatory, analgesic and antipyretic activities. Diclofenac deanol has a more potent inhibitory effect on cyclooxygenase (COX)-2 than on COX-1. The solubility of diclofenac deanol is significantly higher than that of other diflunisal salts reported earlier. Diclofenac deanol has a wide range of potential applications in the medical field due to its biological activity and high water solubility .
Doramapimod hydrochloride (BIRB 796 hydrochloride) is an anti-inflammatory compound with biological activity through inhibition of p38 MAPK. Doramapimod hydrochloride can significantly inhibit the activities of TNF-α and IL-1β induced by LPS, LTA and PGN. Doramapimod hydrochloride showed a stronger inhibitory effect on inflammation induced by all three bacterial toxins, which was more significant compared with the effects of other compounds. Doramapimod hydrochloride can be used in the research of autoimmune diseases .
Kanamycin (Kanamycin A) sulfate is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin sulfate shows good inhibitoryactivity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitoryactivities against other MMPs . CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression .
CETP-IN-3 (Compound 13) is an small molecule inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP. CETP-IN-3 for the CETP inhibitoryactivity in the scintillation proximity (SPA) and whole plasma assay (WPA) with IC50s of 0.002 μM and 0.06 μM, respectively .
SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibitsLeishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitoryactivity against cathepsin G .
ONO 1301 (ONO-AP 500-02), a prostaglandin (PG) I2 mimetic, is an orally active, long-acting prostacyclin agonist with thromboxane-synthase inhibitoryactivity. ONO 1301 promotes production of hepatocyte growth factor (HGF) from various cell types and ameliorates ischemia-induced left ventricle dysfunction in the mouse, rat and pig .
MPT0B390 is an arylsulfonamide-based derivative with potent HDACinhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM .
MsbA-IN-5 (compound 40) is a potent and highly selective MsbAinhibitor with an IC50 value of 2 nM. MsbA-IN-5 has inhibitoryactivity against Escherichia coli, Klebsiella pneumoniae, and Enterobacter cloacae with MICs of 12 μM, 12 μM and 25 μM, respectively. MsbA-IN-5 can be used for researching anti-Gram-negative bacteria .
Anti-inflammatory agent 18 (compound 3b) shows NOinhibitoryactivity, with an IC50 of 15.94 μM. Anti-inflammatory agent 18 inhibits HMGB1-induced later inflammation. Anti-inflammatory agent 18 can be used for the research of later inflammation diseases such as coronavirus diseases (COVID-19) and sepsis, etc .
Anti-inflammatory agent 19 (compound 2b) shows NOinhibitoryactivity, with an IC50 of 36.00 μM. Anti-inflammatory agent 19 inhibits HMGB1-induced later inflammation. Anti-inflammatory agent 19 can be used for the research of later inflammation diseases such as coronavirus diseases (COVID-19) and sepsis, etc .
Anti-MRSA agent 3 (compound 18) has highly inhibitoryactivity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and low cytotoxicity in normal cells. Anti-MRSA agent 3 has relatively strong ability to destroy bacterial cell wall and membrane, high binding affinity to bacterial genomic DNA .
SAP2-IN-1 is a secreted aspartic protease 2 (SAP2)inhibitor and has potent SAP2 inhibitoryactivity with an IC50 value of 0.92 μM. SAP2-IN-1 also is a virulence factor inhibitor and is inactive in vitro. SAP2-IN-1 can be used for the research of infection .
SOS1-IN-16 (Comp 54) is a selective inhibitor of SOS1 with an IC50 of 7.2 nM. SOS1-IN-16 has inhibitoryactivity of CYP3A4 when using testosterone as a substrate, with an IC50 of 8.9μM. SOS1-IN-16 can be used for cancer research .
PI3Kδ-IN-17 (Compound S5) is a potent inhibitor of PI3Kδ, with IC50 of 2.82?nM. PI3Kδ-IN-17 shows strong inhibitoryactivity of proliferation in SU-DHL-6 cells (IC50 = 0.035 μM) .
PDM-042 is a potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor. PDM-042 shows potent inhibitoryactivities for human and rat PDE10A with IC50 values of less than 1 nM and more than 1000-fold selectivity against other phosphodiesterases. PDM-042 can be used for the research of schizophrenia .
ABHD antagonist 1 possesses ABHD6 (α/β-Hydrolase domain containing 6) inhibitoryactivity, involving the regulation of biochemical pathways involved in ABHD6, thereby affecting cell function and inflammatory response. ABHD antagonist 1 can be used in pain, neuropathic diseases, inflammatory diseases. Autoimmune diseases, metabolic diseases, and cancer research .
BK-218 is an orally active cephalosporin antibiotic that binds to penicillin-binding proteins (PBPs) and has a greater inhibitory effect than Cephalexin (HY-B0200) and Cefoxitin (HY-B1825). BK-218 has similar antibacterial activity to Cefamandole (HY-B1128) and can be used in the development of antibacterial drugs .
Medicagenic acid (Standard) is the analytical standard of Medicagenic acid. This product is intended for research and analytical applications. Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes . Medicagenic acid (Castanogenin) has low enzyme inhibitoryactivities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE .
(+)-Benalaxyl is a broad-spectrum benzamide fungicide. (+)-Benalaxyl inhibits the growth of the freshwater algae S. obliquus, with an EC50 value of 8.441 mg/L. (+)-Benalaxyl can induce the production of chlorophyll a and b, as well as increase the activity of superoxide dismutase (SOD) and the generation of malondialdehyde (MDA). (+)-Benalaxyl has inhibitory effects on catalase (CAT). (+)-Benalaxyl is effective against diseases caused by oomycetes .
Ro 14-9578 is a tricyclic quinolone analog with antibacterial activity. Ro 14-9578 inhibits DNA biosynthesis (IC50=117 μM) and DNA supercoiling (IC50=66.8 μM) in Escherichia coli. Furthermore, Ro 14-9578 exhibits inhibitory effects against various Gram-negative bacteria and Staphylococcus aureus .
Cilofexor tromethamine (GS-9674 tromethamine) is a nonsteroidal farnesene oxide receptor agonist with activity in improving markers of cholestasis and liver injury. Cilofexor tromethamine was shown to be well tolerated in patients without cirrhosis and resulted in significant improvements in liver biochemical parameters and cholestatic markers. Cilofexor tromethamine offers a potential inhibitory option for the management of primary sclerosing cholangitis .
2-PADQZ is an antiviral compound with activity against influenza viruses. 2-PADQZ specifically binds to the influenza A virus RNA promoter and forms a binding site at the internal loop. 2-PADQZ has a significant inhibitory effect on H1N1 and H3N2 influenza A viruses and influenza B viruses .
(E/Z)-Aureusidin is a flavonoid compound with antioxidant activity. (E/Z)-Aureusidin can inhibit the production of reactive oxygen species and reduce cell damage. (E/Z)-Aureusidin has anti-inflammatory effects and can reduce the expression of inflammatory factors. (E/Z)-Aureusidin has inhibitory effects on a variety of bacteria, indicating its potential antimicrobial properties .
Isothiazole-5-carboxylic acid (8-Isoquinoline-methaneaminedihydrochloride) is an organic compound with antibacterial, anticancer and anti-inflammatory properties. Isothiazole-5-carboxylic acid can be used to develop novel compounds to combat various diseases. Isothiazole-5-carboxylic acid exhibits a wide range of potential pharmacological activities and helps improve existing inhibitory schemes.
2-Azaadamantane-N-oxyl (AZADO) is a compound with antioxidant activity that can effectively scavenge free radicals. 2-Azaadamantane-N-oxyl has been widely studied in compound development and has shown potential inhibitory effects on a variety of diseases. The structure of 2-Azaadamantane-N-oxyl gives it excellent biocompatibility and is suitable for screening innovative compounds.
Pyriftalid (Standard) is the analytical standard of Pyriftalid. This product is intended for research and analytical applications. Pyriftalid is a new type of insecticide with strong inhibitoryactivity against a variety of pests. Pyriftalid is widely used in agriculture to effectively control pests on crops, thereby improving crop yield and quality. Pyriftalid is also being studied for improving plant resistance to resist attacks by pests and diseases.
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitoryactivity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
Medroxyprogesterone (17α-Hydroxy-6α-methylprogesterone) is a synthetic human variant of progesterone that is a progesterone receptor agonist with oral activity. Medroxyprogesterone can induce cell proliferation through the PI3K/Akt signaling pathway. Medroxyprogesterone has an inhibitory effect on atherosclerosis in mice. The progesterone agonist activity of Medroxyprogesterone is less effective than Medroxyprogesterone acetate (HY-B0469) .
DHFR-IN-1 (compound 12) is a potent and selective DHFR (dihydrofolate reductase)inhibitor, with an IC50 of 40.71 nM. DHFR-IN-1 exhibits promising antibacterial activity against gram-positive and gram-negative bacteria. DHFR-IN-1 exhibits moderate antifungal activities. DHFR-IN-1 exhibits a high synergistic effect with Levofloxacin (HY-B0330), where the FIC (fractional inhibitory concentration index) value is 0.249 .
AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitoryactivity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease .
BAY-771, a structurally close pyrimidinedione, is a chemical probe with good lead-like properties and high permeability in Caco-2 cells (no hint of efflux). BAY-771 shows very weak inhibitoryactivity in the BCAT1 biochemical assay and no activity in BCAT2. BAY-771 can be used as a negative control of HY-148242 BAY-069. BAY-771 can be used for the research of tumor metabolism .
2-Hydroxycinnamic acid (Standard) is the analytical standard of 2-Hydroxycinnamic acid. This product is intended for research and analytical applications. 2-Hydroxycinnamic acid is a phenolic acid with antimicrobial and antioxidant properties. 2-Hydroxycinnamic acid has antimicrobial activity against Staphylococcus aureus and is not susceptible to drug resistance. 2-Hydroxycinnamic acid shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC50 of 0.3 mM. In addition, 2-Hydroxycinnamic acid has neuroprotective and antitumor activity .
Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
Ganoderic acid SZ is a natural product with 3-hydroxy-3-methylglutaryl-CoA reductase inhibitoryactivity. Ganoderic acid SZ shows stronger activity than the positive control atorvastatin in inhibiting HMG-CoA reductase. Ganoderic acid SZ exhibits significant inhibition of yeast-derived α-glucosidase with IC50 values achieved at very low concentrations. Ganoderic acid SZ also exhibits cytotoxicity against K562 cells with IC?? values in the range of 10-20 μM .
VEC6 (NSC 11435) is an inhibitor of VEZF1–DNA interaction and has the activity to recapitulate RhoB loss in ischemic retinopathy. VEC6 reduces pathological angiogenesis and promotes lymphangiogenesis. VEC6 plays a unique role in angiogenesis and lymphangiogenesis by regulating the expression of different sets of genes in endothelial cells. VEC6 has an inhibitory effect on VEZF1-mediated transcriptional activity, thereby affecting the proliferation and sprouting of endothelial cells .
AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitoryactivity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing .
T863 is an orally active, selective and potent DGAT1 (acyl-CoA:diacylglycerol acyltransferase 1)inhibitor with an IC50 of 15 nM. T863 has no inhibitoryactivity against human MGAT3, human DGAT2, or human MGAT2. T863 interacts with the acyl-CoA binding site of DGAT1, and inhibits triacylglycerol synthesis in cells .
Varespladib (LY315920) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2)inhibitor with an IC50 of 9 nM. Varespladib exhibits the significant inhibitory effect on sPLA2activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively .
Pseudouridimycin (PUM) is an antibiotic that selectively inhibits bacterial RNA polymerase (RNAP), with an IC50 of about 0.1 μM and a minimum inhibitory concentration (MIC) of 4 - 6 μg/mL. Pseudouridimycin is a C-nucleoside analogue that's effective against both Gram-negative and Gram-positive bacteria. Pseudouridimycin inhibits bacterial growth in vitro and shows activity in a mouse model of purulent streptococcal peritonitis .
Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2)inhibitor with an IC50 of 9 nM. Varespladib sodium exhibits the significant inhibitory effect on sPLA2activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively .
SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitoryactivity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated .
Moracin P is a 2-arylbenzofuran isolated from the Mori Cortex Radicis. Moracin P exhibits potent in vitro inhibitoryactivity against hypoxia-inducible factor (HIF-1). Moracin P reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin P has neuroprotective and anti-inflammatory effects .
Moracin O is a 2-arylbenzofuran isolated from the Morus alba Linn. . Moracin O exhibits potent in vitro inhibitoryactivity against hypoxia-inducible factor (HIF-1). Moracin O reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin O has neuroprotective and anti-inflammatory effects .
CYD19 is a potent Snail/HDAC dual target inhibitor. CYD19 displays potent inhibitoryactivity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. CYD19 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis .
TFC-007, a selective hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, show high inhibitoryactivity against H-PGDS enzyme (IC50 value of 83 nM). TFC-007 can be used for composing H-PGDS degradation inducer PROTAC(H-PGDS)-1 (TFC-007 binds to H-PGDS, and Pomalidomide binds to cereblon) .
Mazaticol is an anticholinergic agent. Mazaticol blocks the muscarinic acetylcholine receptors and cholinergic nerve activity. Mazaticol is a potent 3H-QNB and 3H-PZ binding inhibitor, can bind to the M2 receptors with high affinity. Mazaticol exhibits inhibitory effects on dopamine uptake in the striatal nerve terminal. Mazaticol can be used for parkinsonian syndrome research .
COX-2-IN-18 (Compound 3) is a potent inhibitor of COX-2. COX-2-IN-18 possesses good COX-2 inhibitoryactivity (IC50 = 0.775 μM) compared to the reference agent, Celecoxib (IC50 = 0.153 μM). COX-2-IN-18 has the potential for the research of cancer diseases .
MMP2-IN-2 (compound 42) is a potent and selective MMP-2 (matrix metalloproteinases) inhibitor, with an IC50 of 4.2 μM. MMP2-IN-2 also shows inhibitoryactivity against MMP-13, MMP-9 and MMP-8, with IC50 values of 12, 23.3, and 25 μM, respectively .
1-Methyl-2-nonyl-4(1H)-quinolone, a quinolone alkaloid, is a potent and selective MAO-B (monoamine oxidase) inhibitor. 1-Methyl-2-nonyl-4(1H)-quinolone exhibites inhibitoryactivity on leukotriene biosynthesis, with an IC50 of 12.1 μM .
N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma - .
HDAC-IN-45 (Compound 14) is a small molecule HDACinhibitor and has anticancer activity, also can forms a hydrogen
bond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively .
CDK4/6-IN-12 is a potent cyclin-dependent kinase 4/6 (CDK4/6)inhibitor. CDK4/6-IN-12 has enzymatic inhibitoryactivity for CDK4 and CDK6 with IC50 of 592.3 nM and 3090 nM, respectively. CDK4/6-IN-12 can be used for the research of cancer .
ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK)inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
SENP2-IN-1 (compound 77) is a selective SENP2inhibitor. SENP2-IN-1 shows inhibitoryactivities with IC50s of 1.3, 0.69 and 22.7 μM for SENP1, SENP2 and SENP5, respectively. SENP2-IN-1 can be used for the research of cancer .
hBChE-IN-1 (compound 4), a quinolizidinyl derivative, is a potent hBChEinhibitor (IC50=7 nM) and highly selective over hAChE. hBChE-IN-1 shows inhibitoryactivity against tau and Aβ40 protein aggregation, with IC50 values of 20 and 4.3 μM, respectively. hBChE-IN-1 can be used for Alzheimer's disease research .
Lys-[Des-Arg9]Bradykinin, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin has low inhibitoryactivity on B2 receptors .
2-Hydroxy-3-methylanthraquinone (compound 1) is a natural compound isolated from a water extract of Hedyotis diffusa WILLD. 2-Hydroxy-3-methylanthraquinone shows inhibitoryactivity against protein tyrosine kinases v-src and pp60src, and induces growth arrest and apoptosis in the HepG2 cancer cells .
δ-Viniferin is a resveratrol dehydrodimer, an isomer of ε-Viniferin (HY-N3841) . ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol, displays a potent inhibitory for all the CYPactivities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity.
Tricetin 3',4',5'-trimethyl ether (5,7-Dihydroxy-3',4',5'-trimethoxyflavone) is a flavone glucoside, that can be isolated the flowers of Chrysanthemum sinensea. Tricetin 3',4',5'-trimethyl ether displays xanthine oxidase competitive-type inhibitoryactivity, with an IC50 of 0.51 μM and a Ki of 0.37 μM .
Halociline, a derivative of alkaloids, that can be isolated from the marine fungus Penicillium griseofulvum.
Halociline targets MAPK1, MMP-9, and PIK3CA in gastric cancer cells, potentially mediated by diverse pathways including cancer, lipid metabolism, atherosclerosis, and EGFR tyrosine kinase inhibitor resistance. Halociline possesses antimicrobial, antioxidant and biofilm inhibitoryactivities .
DNA-PK-IN-13 (Compound SK10) is a DNA-PKinhibitor that exhibits potent inhibitoryactivity (IC50= 0.11 nM). DNA-PK-IN-13 regulates tumor cell proliferation by decreasing the expression level of γH2A.X and enhancing the sensitivity of tumor cells to chemotherapeutic agents. DNA-PK-IN-13 is suitable for oncology studies .
Nemonoxacin (Standard) is the analytical standard of Nemonoxacin. This product is intended for research and analytical applications. Nemonoxacin (TG-873870) is an orally active and potent broad-spectrum antibiotic. Nemonoxacin shows good inhibitoryactivity against different species of staphylococci, streptococci, and enterococci, Neisseria gonorrhoeae, and Haemophilus influenza. Nemonoxacin can be used in the study of bacterial infections and community-acquired pneumonia .
Plant 14-3-3-IN-1 (Compound 2) is an inhibitor for 14-3-3 proteins in Arabidopsis thaliana, with an IC50 of 1.21 μM. Plant 14-3-3-IN-1 exhibits different inhibitoryactivities against different 14-3-3 isomers. Plant 14-3-3-IN-1 promotes the closure of stomata on leaves .
Apiin (Standard) is the analytical standard of Apiin. This product is intended for research and analytical applications. Apiin, a major constituent of Apium graveolens leaves with anti-inflammatory properties. Apiin shows significant inhibitoryactivity on nitrite (NO) production (IC50 = 0.08 mg/mL) in-vitro and iNOS expression (IC50 = 0.049 mg/ mL) in LPS-activated J774.A1 cells .
Pogostone (Standard) is the analytical standard of Pogostone. This product is intended for research and analytical applications. Pogostone is isolated from patchouli oil?with anti-bacterial and anti-cancer activities.?Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 μg/ml .?Pogostone induces cell apoptosis and autophagy .
BAY-8040 is a pyrimidopyridazine derivative which has inhibitoryactivity against human neutrophil elastase (HNE). BAY-8040 decreases cardiac remodeling and ameliorates cardiac function in a Monocrotaline (HY-N0750)-induced rat model for pulmonary arterial hypertension. BAY-8040 is promising for research of inflammatory pathologies and cardiopulmonary pathologies .
Mcl1-IN-7 (compound 11) is a reversible covalent inhibitor of Mcl-1 with the activity of inhibiting Mcl-1. By covalently targeting the non-catalytic lysine side chain of Mcl-1, it has higher potency than non-covalent counterparts and can be used to develop Mcl-1 inhibitory compounds and study related biological phenomena.
(Rac)-Ganoderic acid C2 is the racemate of Ganoderic acid C2 (HY-N1517). Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses anti-tumor, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitoryactivity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM[ .
BMS-707035 is a potent orally active HIV-1 integrase strand transferinhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC50 value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1) .
BGT226 (NVP-BGT226 maleate) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ) /mTOR dual inhibitor which displays potent growth-inhibitoryactivity against human head and neck cancer cells .
PCI 29732 is a potent, orally active, reversible BTK inhibitor with Kiapp values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitoryactivity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 .
Sophoflavescenol is a prenylated flavonol, which shows great inhibitoryactivity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
Ilaprazole (IY-81149) is an orally active proton pumpinhibitor. Ilaprazole irreversibly inhibitsH +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitoryactivity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitoryactivity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation .
Lys-[Des-Arg9]Bradykinin TFA, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin TFA has low inhibitoryactivity on B2 receptors .
BGT226 (NVP-BGT226) is a PI3K (with IC50s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitoryactivity against human head and neck cancer cells .
K-975 is a potent, selective and orally active TEADinhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma .
PF-07038124 is a PDE4inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 shows inhibitoryactivities against IL-13, IL4, and IFNγ (IC50=125, 4.1, 1.06 nM, respectively). PF-07038124 can be used for research of atopic dermatitis and plaque psoriasis .
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAFinhibitor, also inhibitsMAPK signaling. Everafenib has inhibitoryactivity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .
2′-Hydroxygenistein is a natural product that can be isolated from Crotalaria pallida and C. assamica. 2′-Hydroxygenistein shows anti-inflammatory activity. 2′-Hydroxygenistein shows significant concentration-dependent inhibitory effects on the release of β-glucuronidase and lysozyme from rat neutrophils, with IC50 values of 5.9 ± 1.4 and 9.7 ± 3.5 μM, respectively .
METTL3-IN-5 (Compound 13) is a METTL3inhibitor. METTL3-IN-5 inhibits MOLM-13 growth with an IC50 less than 2 μM. METTL3-IN-5 has weak hERG inhibitoryactivity (IC50 >30 μM). METTL3-IN-5 can be used for AML research .
NW-1772 (methanesulfonate) (compound 22b) is a potent and selective monoamine oxidase (MAO) B inhibitor. NW-1772 has some advantages, such as rapid blood-brain barrier penetration, short-acting and reversible inhibitoryactivity, slight inhibition of selected cytochrome P450s, and low in vitro toxicity. NW-1772 can be used for the research of neurodegenerative diseases .
anti-TNBC agent-4 (compound 7) exhibits highly inhibitoryactivity against different TNBC cells with IC50s from 0.37 μM to 1.52 μM. anti-TNBC agent-4 inhibitsIKKβ mediated phosphorylation of IκB and p65. anti-TNBC agent-4 induces TNBC cells apoptosis .
Exatecan-amide-bicyclo[1.1.1]pentan-1-ol (Compound 79) is an exatecan (HY-13631) derivative that can be used as a payload in drug conjugates. Exatecan-amide-bicyclo[1.1.1]pentan-1-ol has significant inhibitoryactivity against a variety of tumor cell lines .
Pirfenidone (Standard) is the analytical standard of Pirfenidone. This product is intended for research and analytical applications. Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities .
Waldiomycin is an antibiotic that can be isolated from Streptomyces sp. MK844-mF10 that has inhibitory effects on low GC-content Gram-positive bacteria. Waldiomycin inhibits the activity of WalK kinase by targeting its ATP-binding domain, thereby blocking the WalK/WalR signal transduction system, which plays a role in cell growth and division .
FR 75513 is a 1,1'-biphenyl-2,6-dicarboxylic acid diester series compound that can inhibit the contraction of the detrusor muscle of guinea pig bladder (IC50=3.3 μg/mL). After intravenous injection of FR 75513 into anesthetized rats, it also showed strong inhibitoryactivity on the detrusor contraction (ID50=0.04 mg/kg).
PF-07038124 hydrochloride is a PDE4inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 hydrochloride shows inhibitoryactivities against IL-13, IL4, and IFNγ (IC50=125, 4.1, 1.06 nM, respectively). PF-07038124 hydrochloride can be used for research of atopic dermatitis and plaque psoriasis .
Silydianin (Standard) is the analytical standard of Silydianin. This product is intended for research and analytical applications. Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 17.38?μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products .
GZ4 is a calcium current inhibitor with direct inhibitoryactivity on cell surface channels. GZ4 inhibition reverses mechanical hyperalgesia/hyperalgesia in a spinal nerve ligation-induced neuropathic pain model. The mechanism of action of GZ4 is similar to that of gabapentin, but the time course of its biological effects is more rapid, indicating that GZ4 can directly inhibit calcium channel currents .
BuChE-IN-14 is a novel compound that selectively inhibits acetylcholinesterase (AChE) activity. BuChE-IN-14 showed a concentration-dependent inhibitory effect on AChE in rat brain in vitro experiments. BuChE-IN-14 can increase the extracellular acetylcholine (ACh) concentration in the rat hippocampus and striatum at a certain dose. BuChE-IN-14 may help improve memory impairment caused by cholinergic dysfunction .
MAO-B-IN-35 is a potent, selective, reversible monoamine oxidase B (MAO-B) inhibitor with high inhibitoryactivity. MAO-B-IN-35 can exhibit high selectivity and potency at a small molecule scale. MAO-B-IN-35 is designed and synthesized so that it can be efficiently obtained during standard synthesis procedures and has superior physical and chemical properties .
TGFBR1-IN-2 (Compound AQA) is a TGFBR1inhibitor and an antibacterial agent. TGFBR1-IN-2 is a substrate for cytochrome P450s. TGFBR1-IN-2 contains the pyridyl-6-methyl moiety necessary for Mycobacterium tuberculosis inhibition and has potent inhibitoryactivity against non-replicating and persistent Mycobacterium tuberculosis .
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta .
Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models , has selective inhibitoryactivity towards cyclooxygenase-2 (COX-2) .
Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways .
Zingibroside R1 is dammaranae-type triterpenoid saponin, isolated from rhizomes, taproots, and lateral roots of Panax japonicas C. A. Meyer, shows excellent anti-tumor effects as well as anti-angiogenic activity .
Zingibroside R1 possesses some anti-HIV-1activity.
Zingibroside R1 has inhibitory effects on the 2-deoxy-D-glucose (2-DG) uptake by EAT cells (IC50=91.3 μM) .
N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid (Neu5Ac2en) is a potent neuraminidase (sialidase)inhibitor. N-acetyl-2,3-dehydro-2-Deoxyneuraminic Acid shows inhibitoryactivities against human neuraminidase enzymes with IC50s of 143, 43, 61, and 74 μM for NEU1, NEU2, NEU3, and NEU4, respectively. Anti-influenza virus activity .
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4)inhibitor. BRD4 Inhibitor-20 has inhibitoryactivity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer .
OMS14 is exhibits inhibitoryactivity for phosphoinositide 3-kinase γ (PI3Kγ) and PIK3CD/PIK3R1, which inhibits 19% PI3Kγ and 65% PIK3CD/PIK3R1 activity at 100 μM. OMS14 exhibits anticancer efficacy in various cancer cells .
Alectinib analog (CH5424802 analog) is a selective ALK inhibitor with activity in blocking resistance gating mutations. The synthetic optimization of alectinib analog allows it to be combined with specific peptides to improve the ability to target cancer cells. Alectinib analog exhibits low micromolar IC50 values in antiproliferation and shows good cytotoxic effects. The inhibitoryactivity of alectinib analog is closely related to its stability and release of active ingredients. Alectinib analog demonstrated the ability to inhibit vascular septal length or width in an in vivo zebrafish model .
CP 461 free base (OSI-461 free base) is a novel pro-apoptotic compound with the activity of inhibiting cyclic guanosine monophosphate phosphodiesterase. CP 461 free base exhibits growth inhibitoryactivity against a variety of human tumor cell lines in vitro. CP 461 free base selectively induces apoptosis in cancer cell lines but has no effect on normal cells. CP 461 free base can be used in the study of renal cell carcinoma, prostate cancer and Crohn's disease .
Foretinib phosphate is an orally bioavailable small molecule with potential anti-tumor activity. Foretinib phosphate can selectively inhibit hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), thereby potentially inhibiting tumor angiogenesis, tumor cell proliferation and metastasis. Foretinib phosphate shows different anti-cancer activity from cabozantinib in lung cancer cells and has stronger inhibitory effects on targets such as MEK1/2, FER and AURKB .
CatB-IN-1 is an enzyme inhibitor with significant inhibitoryactivity against tumor invasion. CatB-IN-1 may reduce the invasiveness of tumor cells by regulating intracellular protein metabolism. CatB-IN-1 demonstrates effective anti-invasive ability in cell models and can significantly reduce the invasive ability of MCF-10A neoT cells. The structure-activity relationship study of CatB-IN-1 shows that its design can target multiple functions of cat hepsin B .
CQ-16 is an orally active small molecule drug conjugate (SMDC) targeting prostate-specific membrane antigen (PSMA). CQ-16 exhibits highly selective antiproliferative activity between PSMA-positive and PSMA-negative prostate cells. In addition, CQ-16 also has PARPinhibitoryactivity (IC50=1 nM). (Pink: PSMA Ligand (HY-139840); Black: Linker (HY-W037980); Blue: PARP Inhibitor (HY-10162))
ZXX2-77 is a cyclooxygenase-1 (COX-1) selective inhibitor belonging to the benzenesulfonylanilide class of compounds. It is reported as a novel analgesic that does not cause gastric damage. ZXX2-77 has a weak analgesic effect but exhibits potent COX-1 inhibitoryactivity in vitro. The low oral absorption rate of ZXX2-77 leads to its weak analgesic effect in vivo. At a dose of 30 mg/kg, the maximum plasma concentration of ZXX2-77 (1.2 mM) did not reach its COX-1 IC50 value (3.2 mM). In contrast, its derivative ZXX2-79, although weaker in vitro COX inhibitoryactivity, is better absorbed, exhibits stronger analgesic effect and hardly causes gastric damage. These findings suggest that ZXX2-77 and its derivatives as COX-1 selective inhibitors may become effective analgesics that do not cause gastric damage.
Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide . Telaprevir inhibits SARS-CoV-2 3CL proactivity .
XAV-939 is a Tankyraseinhibitor. XAV-939 has inhibitoryactivity for TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation .
Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro .
FGI-106 is a potent and broad-spectrum inhibitor with inhibitoryactivity against multiple viruses. FGI-106 is active against Ebola, Rift Valley and Dengue Fever viruses with EC50s of 100 nM, 800 nM and 400-900 nM, respectively. FGI-106 also inhibits non-hemorrhagic fever viruses HCV and HIV-1 with EC50s of 200 nM and 150 nM, respectively .
A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitoryactivity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor .
HIV-1 inhibitor-49 is an orally active HIV-1inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptaseinhibitoryactivity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model .
HIV-1 inhibitor-59 (Compound I-5b) is a HIV-1inhibitor, with EC50s of 5.62-171 nM against the wild-type (WT) and mutant HIV-1 strains. HIV-1 inhibitor-59 has moderate RT enzyme inhibitoryactivity (IC50: 0.094-12.0 μM) .
L2H2-6OTD intermediate-1 is an intermediate for the synthesis of L2H2-6OTD (HY-148200) and can be used for ADC preparation. L2H2-6OTD, a telomestatin analog with telomerase inhibitoryactivity (IC50: 15 nM) .
EGFR-IN-95 (compound 5j) is an 2,4-diaminonicotinamide derivative. EGFR-IN-95 has potent inhibitoryactivity against EGFR del19/T790M/C797S and L858R/T790M/C797S .
L2H2-6OTD intermediate-3 is an intermediate for the synthesis of L2H2-6OTD (HY-148200) and can be used for ADC preparation. L2H2-6OTD, a telomestatin analog with telomerase inhibitoryactivity (IC50: 15 nM) .
Clinafloxacin (Standard) is the analytical standard of Clinafloxacin. This product is intended for research and analytical applications. Clinafloxacin (AM 1091) is a potent and broad-spectrum fluoroquinolone antibiotic, has inhibitoryactivity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro . Clinafloxacin is against DNA gyrase and topoisomerase IV of S. aureus with IC50 values of 0.92 µg/ml and 1.62 µg/ml, respectively .
Timcodar mesylate (VX-853-2) and its analog VX-710 are mammalian multidrug-resistant bacterial efflux pump inhibitors that directly inhibit ethidium bromide efflux in Staphylococcus aureus. Timcodar mesylate has the potential to enhance antibiotic activity by inhibiting bacterial efflux pumps, effectively reducing the minimum inhibitory concentration of some antibiotics against Gram-positive pathogens such as Staphylococcus aureus, Enterococcus and Streptococcus pneumoniae .
Pan-rasin-2 (compound 6A) is a molecular glues that targets RAS. Pan-rasin-2 has significant inhibitoryactivity on cell proliferation of RAS mutant cell lines. Pan-rasin-2 can form ternary complexes with cyclophilin A (CYPA) and RAS (ON) proteins and the formation of ternary complexes can block the binding of RAF downstream of RAS, which has anti-tumor effects .
Methyl-L-NIO (compound 2d) hydrochloride is a potential selective inhibitor (IC50: 70 μM) of dimethylarginine dimethylaminohydrolase hDDAH. Methyl-L-NIO also has inhibitoryactivity against NO synthase. The inhibition rates of Methyl-L-NIO on different isoforms of NO synthase at a concentration of 100 μM are 77% (nNOS), 20% (eNOS), and 72% (iNOS) respectively; the inhibition rates at a concentration of 1 mM are 100% (nNOS), 85% (eNOS), 100% (iNOS) .
Validamycin A (Standard) is the analytical standard of Validamycin A. This product is intended for research and analytical applications. Validamycin A, a fungicidal, is an agricultural antibiotic. Validamycin A is originally isolated from Streptomyces hygroscopicus var. limoneus. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL . Validamycin A shows potent inhibitoryactivity against trehalase of Rhizoctonia solani, with an IC50 of 72 μM . Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM .
S-WJM992 (compound 10ahb) is an antiparasitic agent that inhibitsATPaseactivity under high [Na+] conditions. S-WJM992 also has significant inhibitory effects on parasites that have developed PfATP4inhibitor-resistance. S-WJM992 is a potential transmission blocker that effectively inhibits gamete development and prevents parasite transmission to mosquitoes via blood feeding .
RORγt inhibitor 3 is an orally active and potent retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor. RORγt inhibitor 3 shows high binding affinity and inhibitoryactivity of Th17 cell differentiation. RORγt inhibitor 3 also shows efficacy in both mouse experimental autoimmune encephalomyelitis (EAE) and collagen induced arthritis (CIA) models .
AZD 3043 (THRX 918661) is a positive allosteric modulator of GABA(A) receptors with sedative and hypnotic activity. AZD 3043 can enhance GABA(A) receptor-mediated chloride currents in vitro and produce hypnotic and electroencephalographic inhibitory effects in vivo. Due to its esterase-dependent metabolic pathway, it has a short duration of action and can be quickly cleared even after long-term infusion, which may have clinical application potential.
(E)-L-652343 is a compound with potent cyclooxygenase and 5-lipoxygenase inhibitoryactivity. (E)-L-652343 can effectively inhibit the synthesis of products of these two pathways in vivo. (E)-L-652343 showed high sensitivity and specificity in the detection of geometric isomers in canine and human plasma. (E)-L-652343 showed selective metabolism in vivo, and the elimination rate of the E isomer was faster than that of the Z isomer .
Dapivirine hydrochloride is a non-nucleoside reverse transcriptase inhibitor with antitumor activity. Dapivirine hydrochloride attenuates the proliferation of glioblastoma cells and induces apoptosis. Dapivirine hydrochloride modulates autophagy and activates Akt, Bad, and SAPK/JNK signaling pathways. Dapivirine hydrochloride has shown inhibitory effects on glioma cell growth both in vitro and in vivo. Dapivirine hydrochloride is also a promising drug candidate for topical microbial agents for the prevention of sexual transmission of HIV-1 .
SU9518 is a tyrosine kinase inhibitor with specific activity against PDGFRα. SU9518 can inhibit the development of proliferative vitreoretinopathy (PVR) in fibroblast and Muller cell rabbit models. SU9518 showed effective inhibitory effects in these models without toxic effects. Therefore, SU9518 has the potential to be used to inhibit PVR in humans and other proliferative eye diseases involving fibrosis and gliosis .
5'-Ethylcarboxamido-2',3'-isopropylidene adenosine is an adenosine receptor agonist that promotes the activity of A2B adenosine receptors. 5'-Ethylcarboxamido-2',3'-isopropylidene adenosine can be used to study the role of adenosine in physiological processes. 5'-Ethylcarboxamido-2',3'-isopropylidene adenosine is used as a potential inhibitory target in compound development.
(R)-9b is a potent inhibitor of ACK1 tyrosine kinase (IC50=56 nM) with anticancer activity. (R)-9b exhibits selectivity for ACK1 but has inhibitory effects on JAK family kinases JAK2 and Tyk2. (R)-9b can be used in the study of hormone-regulated cancers such as prostate and breast cancer .
iNOS/COX-2-IN-3 (compound 7d) is a dual inhibitor of iNOS and COX-2, with potential anti-inflammatory activity against LPS (HY-D1056)-induced RAW 264.7 cells (IC50=3.48 μM). iNOS/COX-2-IN-3 has good plasma stability, oral activity and gastric safety, and its inhibitoryactivity on iNOS and COX-2 expression is 5.43-fold and 2.37-fold that of Indomethacin (HY-14397), respectively .
PD117588 is a quinolone antibacterial agent with a broad range of antibacterial activity. PD117588 exhibits excellent activity against a variety of Gram-positive and Gram-negative bacteria from cancer patients, especially against all Gram-positive strains, including methicillin-resistant Staphylococcus aureus, coagulase-negative Staphylococci, and Enterococci. PD117588 is also very effective against most Gram-negative bacilli, although ciprofloxacin shows stronger activity against Pseudomonas aeruginosa. Compared with other quinolone antibiotics, the minimum inhibitory concentration of PD117588 outperforms most of the tested microorganisms, including imipenem and ceftazidime .
SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibitingRaf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines .
CL-385319 is an N-substituted piperidine compound with inhibitoryactivity against H5N1 avian influenza A virus infection. CL-385319 exhibited an IC50 of 27.03±2.54 μM against infection of highly pathogenic H5N1 virus in Madin-Darby canine kidney cells (MDCK). CL-385319 had low cytotoxicity with a CC50 of 1.48 mM and was able to inhibit the entry of pseudoviruses carrying H5N1 strains from different sources, but had no inhibitory effect on the entry of VSV-G pseudotyped particles. Pseudoviruses with the M24A mutation in HA1 or the F110S mutation in HA2 were resistant to CL-385319, indicating that these two residues in the cavity region may be critical for the binding of CL-385319 .
Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitoryactivities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor .
Anticancer agent 58 (compound 16) has inhibitoryactivity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinaseinhibitor. Multi-kinase-IN-2 exhibits excellent inhibitoryactivity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity .
BMY-27709 is an influenza virus growth inhibitor with an IC50 value of 3-8 μM against A/WSN/33 virus growth, and also exhibits inhibitoryactivity against some subtypes of influenza viruses. BMY-27709 acts early in the course of H1 and H2 virus infections, and exhibits antiviral activity through inhibition of hemagglutinin proteins. However, BMY-27709 has no effect on H3 subtype viruses and influenza B/Lee/40 viruses .
15(S)-15-methyl Prostaglandin D2 (15(S)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2. In contrast to PGD2, 15(S)-15-methyl PGD2 induces vasoconstriction and increases systemic blood pressure with much reduced inhibitoryactivity on ADP-induced platelet aggregation. It also exhibits strong antifertility activity in hamsters (200-fold more potent than PGD2).
Evoxine (Haplophytin B) is a compound that selectively inhibits CO2-induced immunosuppression and has activity in inhibiting the expression of interleukin-6 and chemokine CCL2 in human THP-1 macrophages. Evoxine shows antimicrobial activity against a wide range of bacteria, especially performing well in minimum inhibitory concentration (MIC) tests against Escherichia coli, Bacillus subtilis, and Staphylococcus aureus. Evoxine extracts may find application in crude drug preparations in West Africa, provided that their in vivo toxicity results are negative .
Adefovir diphosphate is an antiviral compound with activity against hepatitis B virus (HBV). Adefovir diphosphate blocks the replication of HBV by inhibiting reverse transcriptase. Adefovir diphosphate has also shown activity against other viruses such as herpes viruses and human immunodeficiency virus. Adefovir diphosphate is used as an effective inhibitory option in the suppression of chronic hepatitis B. The mechanism of action of Adefovir diphosphate involves blocking the autophosphorylation of growth factor receptors, thereby potentially reducing the risk of hepatocellular carcinoma (HCC) in patients with chronic hepatitis B .
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitoryactivities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC50=300 nM) and CYP1A2 (IC50=3.1 μM). TMS is a methylated derivative of resveratrol and has anti-cancer activity .
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitoryactivities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
11(α)-Methoxysaikosaponin F is a triterpenoid saponin isolated from Bupleurum marginatum Wall.ex DC(ZYCH) which is a promising therapeutic for liver fibrosis. 11(α)-Methoxysaikosaponin F has an IC50 of 387.7 nM with viability of hepatic stellate cells-T6 (HSCs-T6). Triterpenoid saponins have numerous targets, important network positions, and strong inhibitoryactivity .
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitoryactivities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
PF-04577806 is a potent, selective and ATP competitive PKCinhibitor. PF-04577806 shows potent inhibitoryactivity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats .
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitoryactivity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibitsBTK .
CLK1/4-IN-1 (compound 31) is a potent and selective Clk1 and Clk4inhibitor with an IC50 value of 9.7 nM and 6.6 nM, respectively. CLK1/4-IN-1 has growth inhibitoryactivities against T24 cancer cells with GI50 of 1.1 μM. CLK1/4-IN-1 can be used for researching anticancer .
Anticancer agent 59 (compound 11) has inhibitoryactivity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
RAD51-IN-8, a new RAD51 binder, is a RAD51-BRCA2inhibitor that inhibits the RAD51 BRCA2 protein protein interaction. RAD51-IN-8 also is a protein−protein interaction (PPI) inhibitor. RAD51-IN-8 has inhibitoryactivity for H4A4 with an EC50 value of 19 μM .
PCSK9-IN-11 (compound 5r) is a potent and orally active PCSK9inhibitor. PCSK9-IN-11 exhibits PCSK9 transcriptional inhibitoryactivity in HepG2 cells, with an IC50 of 5.7 μM. PCSK9-IN-11 increases LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research .
(4Z)-Lachnophyllum lactone is a enyne derivative. (4Z)-Lachnophyllum lactone shows growth inhibitoryactivity against Lemna paucicostata (IC50=104 μM), which is a problematic and invasive weed . (4Z)-Lachnophyllum lactone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Retro-indolicidin is a biological active peptide. (Reverse peptide of indolicidin (Rev4) is a 13-amino acid residue peptide based on the sequence of indolicidin. Indolicidin, a member of the cathelicidin protein family, is a 13-amino acid residue cationic, antimicrobial peptide-amide isolated from the cytoplasmic granules of bovine neutrophils. The synthetic peptide Rev4 has been shown to possess strong antimicrobial as well as protease inhibitoryactivities in vitro.)
3-Acetyl-11-keto-ursolic acid (Compound 18) is a triterpenoid compound derived from Eriobotrya japonicaleaves. 3-Acetyl-11-keto-ursolic acid has 11B-hydroxysteroid dehydrogenase 1 (11b-HSD1) inhibitoryactivity. 3-Acetyl-11-keto-ursolic acid can be used for anti-diabetes research .
Mollicellin H is a secondary metabolite of the fungus C. brasiliense and has a wide range of biological activities, including immunomodulation, cytotoxicity and anti-tumor effects. The growth inhibitory effects (GI50s) of Mollicellin H on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines are 5.1 μg/mL, 6.5 μg/mL and 2.5 μg/mL respectively .
hCAIX/XII-IN-8 (compound 3g) is a potent human (carbonic anhydrase) CA IX and XIIinhibitor, with Ki values of 8.5 and 6.7 nM, respectively. hCAIX/XII-IN-8 shows particularly strong inhibitoryactivity against the tumor-associated membrane-bound isoforms, hCA IX and XII, while maintaining a high selectivity ratio over cytosolic off-target isoforms hCA I and II .
Laccase-IN-3 (Compound 2b) is a laccaseinhibitor(IC50 = 1.02= μM) with significant antifungalactivity. Laccase-IN-3 shows superior inhibitory effect on Botryosphaeria dothidea (EC50 = 0.17 mg/L). Laccase-IN-3 effectively blocks the catalytic function of laccase by binding to its active center. Laccase-IN-3 also disrupts pathogen cell membrane integrity and increases ROS .
TEAD-IN-11 (compound 38) has a good inhibitory effect on TEAD1 (IC50=8.7 nM), TEAD2 (IC50=3.4 nM), TEAD3 (IC50=5.6 nnM). TEAD-IN-11 has good selective activity against TEAD1-3 as a covalent inhibitor. TEAD-IN-11 can be used for cancer research .
Milbemycin oxime (Standard) is the analytical standard of Milbemycin oxime. This product is intended for research and analytical applications. Milbemycin oxime is an orally active macrolide with broad-spectrum antiparasitic activity. Milbemycin oxime is a mixture of oximes consisting of oxime derivatives corresponding to milbemycin A4 and A3. Milbemycin oxime binds to glutamate-gated chloride channels and has inhibitory potency against intestinal nematodes and lung/heart worms .
Pterostilbene (Standard) is the analytical standard of Pterostilbene. This product is intended for research and analytical applications. Pterostilbene is a stilbenoid isolated from blueberries and Pterocarpus marsupium . Shows anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic and anti-obesity properties . Pterostilbene blocks ROS production , also exhibits inhibitoryactivity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide .
11-oxo-mogroside V (Standard) is the analytical standard of 11-oxo-mogroside V. This product is intended for research and analytical applications. 11-oxo-mogroside V is a natural sweetener that exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2-, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
Oroxylin A-7-O-glucuronide (Standard) is the analytical standard of Oroxylin A-7-O-glucuronide. This product is intended for research and analytical applications. Oroxylin A-7-O-glucuronide (Oroxyloside; Oroxylin A-7-O-β-D-glucuronide) is a flavonoid glucuronide isolated from the dried root of Scutellaria baicalensis, with prolyl oligopeptidase (POP) inhibitoryactivity .
Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .
Phenyl(9H-purin-6-yl)amine is an antibacterial compound with the activity of inhibiting bacterial growth. The application of phenyl(9H-purin-6-yl)amine can be used to develop new antibacterial compounds. Phenyl(9H-purin-6-yl)amine has shown potential inhibitory effects in medical research.
Ganoderic acid C2 (Standard) is the analytical standard of Ganoderic acid C2. This product is intended for research and analytical applications. Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses the potential anti-tumor bioactivity, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitoryactivity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM .
AVN-101 free base is a multi-target drug candidate with the potential to inhibit central nervous system (CNS) diseases. AVN-101 free base exhibits high inhibitoryactivity on 5-HT7 receptors and also has certain activity on 5-HT6, 5-HT2A and 5-HT2C receptors. Due to its anxiolytic and antidepressant activities, AVN-101 free base is also expected to be used in diseases such as general anxiety disorder, depression, schizophrenia and multiple sclerosis .
Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well .
3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidaseinhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL .
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitoryactivity against mushroom tyrosinase with an IC50 of 53.6 μM .
Indirubin-3'-monoxime is a potent GSK-3βinhibitor, and weakly inhibits5-Lipoxygenase, with IC50s of 22 nM and 7.8-10 µM, respectively; Indirubin-3'-monoxime also shows inhibitoryactivities against CDK5/p25 and CDK1/cyclin B, with IC50s of 100 and 180 nM.
BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitoryactivity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves .
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM . Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL . Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM .
FGI-106 tetrahydrochloride is a potent and broad-spectrum inhibitor with inhibitoryactivity against multiple viruses. FGI-106 tetrahydrochloride is active against Ebola, Rift Valley and Dengue Fever viruses with EC50s of 100 nM, 800 nM and 400-900 nM, respectively. FGI-106 tetrahydrochloride also inhibits non-hemorrhagic fever viruses HCV and HIV-1 with EC50s of 200 nM and 150 nM, respectively .
HIV-1 inhibitor-19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-19 maintains its inhibitoryactivity against L100I, K103N and V106A/ F227L mutant strains with EC50s of 7.3 nM, 9.2 nM and 21.0 nM, respectively[1].
HIV-1 inhibitor-14 (compound 14b) is a highly potent and broad-spectrum HIV-1 non-nucleoside reverse transcriptase (RT) inhibitor with an EC50 of 0.14 μM for HIV-1 RT. HIV-1 inhibitor-14 has inhibitoryactivity against HIV-1 WT and resistant strains with EC50s of 5.79 ~ 28.3 nM .
LRRK2/NUAK1/TYK2-IN-1 (conpound 226) shows inhibitoryactivity toward LRRK2 (Wt), LRRK2 (G2019), TYK2 and NUAK1, with IC50 values lower than 10 nM. LRRK2/NUAK1/TYK2-IN-1 can be used for autoimmune disease research .
5,7,3' -tri-O-Methyl (-)-epicatechin (Compound 13) is a phospholipase Cγ1 (PLCγ1) inhibitor. 5,7,3' -tri-o-methyl (-)-epicatechin has a methylene dioxy benzene ring and can express inhibitoryactivity against PLCγ1. 5,7,3' -tri-O-Methyl (-)-epicatechin can be used in the study of chemotherapy and chemopexic agents for cancer .
Angeloylbinankadsurin A (compound 7) is an anti-rheumatoid arthritis (RA) agent that can be isolated from EtOAc and CH2Cl2 extracts of Black Tiger Beard. Angeloylbinankadsurin A exhibits inhibitoryactivity on RA-FLS cells (IC50=11.70 μM). Angeloylbinankadsurin A is slightly toxic to human cancer cell lines (Hela and BGC-823) (IC50=19.9 μM, 21.93 μM) .
(R)-G12Di-7 is a covalent ligand for KRAS-G12D, which selectively labels K-Ras-G12D·GDP and K-Ras-G12D·GppNHp. (R)-G12Di-7 exhibits inhibitoryactivity against G12D mutated cancer cells .
C450-0730 is an antagonist targeting the AHL membrane-bound sensor kinase and is an antagonist of the nine-transmembrane protein LuxN of Vibrio harveyi . C450-0730 competitively binds to the LuxN AI-1 binding site and specifically antagonizes the LuxN/AI-1 quorum sensing signal in Vibrio harveyi. The inhibitoryactivity of C450-0730 against LuxN I209F was not significant .
[Nle20] H4 peptide (16−23) is a peptide with strong inhibitoryactivity against histone methyltransferase SETD8 (Kd=0.14 μM), which inhibitsSETD8's methylation of histone H4 by competing with SETD8's substrate binding site. [Nle20] H4 peptide (16−23) can be used as a lead compound for anticancer therapy .
ε-Viniferin (Standard) is the analytical standard of ε-Viniferin. This product is intended for research and analytical applications. ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol and can be isolated from Vitis vinifera, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity .
8-Deazahomofolic acid is an inhibitor of thymidylate synthase (TS) and other folate-related enzymes. 8-Deazahomofolic acid shows inhibitoryactivity against folate-dependent S. faecium, L. casei, and MTX (HY-14519) resistant strains. 8-Deazahomofolic acid also inhibits the growth of L1210 leukemia cells, with an IC50 value of 87.5 μM. 8-Deazahomofolic acid can be used in research on bacterial infections and tumors .
MRS2802 is a P2Y14 receptor agonist with an EC50 value of 63 nM. MRS2802 can effectively activate the P2Y14 receptor and may play a role in regulating platelet function. The selectivity and activity of MRS2802 are conducive to in-depth research on the biological functions and pharmacological properties of P2Y receptors. The development of MRS2802 provides a potential inhibitory strategy for the search for new antiplatelet compounds .
MR2034 ((R)-UM-1071) is a κ-opioid receptor agonist with activity that stimulates the hypothalamic-pituitary-adrenal axis. MR2034 has shown the potential to promote mood and inhibit addictive behaviors in animal models and can be used to study inhibitory approaches related to mood and addictive disorders. MR2034 is selective for κ-opioid receptors and can effectively modulate biological processes related to stress and mood .
SKF 95601 is a modulator of small conductive Ca2+-activated K+ channels with anti-atrial fibrillation (AF) activity. SKF 95601 may play a role in inhibiting atrial fibrillation by affecting the interaction between intracellular Ca2+ concentration and membrane potential. SKF 95601 has become a potential inhibitory target against atrial fibrillation due to its significant expression in various species, especially human atria .
BI-9627 is potent sodium-hydrogen exchanger isoform 1 (NHE1)inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitoryactivity against the NHE3 isoform. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
SMCypI C31 is a non-peptidic cyclophilininhibitor with potent peptidyl-prolyl cis/trans isomerases (PPIase)inhibitoryactivity (IC50 of 0.1 µM). SMCypI C31 shows pangenotype anti-HCVactivity with EC50s ranging from 1.20 to 7.76 μM for genotype 1a, 1b, 2a, 3a, and 5a HCV subgenomic replicons (HCV-SGRs) and chimeric genotype 2a/4a HCV-SGRs. SMCypI C31 disrupts the cyclophilin A-NS5A interaction .
BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitoryactivity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
3β-Acetoxy-hop-22(29)-ene (compound 1) is a potent anti-inflammatory agent. 3β-Acetoxy-hop-22(29)-ene shows high inhibitoryactivity of yeast α-glucosidase, with an IC50 of 5.74 μM. 3β-Acetoxy-hop-22(29)-ene inhibitsMPO (myeloperoxidase) activity in a dose-dependent manner in mouse ear edema model induced by 12-O-tetradecanoylphorbol acetate (TPA), with an IC50 of 0.23 μmol/ear .
Norartocarpetin is a tyrosinaseinhibitor. Norartocarpetin has strong tyrosinase inhibitoryactivity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitoryactivity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitoryactivity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitoryactivity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
(±)-Aiphanol is a newly discovered stilbenolignan analog. (±)-Aiphanol exhibits significant anti-inflammatory activity, acting through inhibition of COX-1 and COX-2. The inhibitory effect on COX-1 (IC50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC50= 9.9 μM) is relatively weak .(±)-Aiphanol effectively inhibitsVEGFR2 (IC50=0.92 µM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active .
BuChE-IN-11 (Compound 3b-1) is an selective BuChEinhibitor with an IC50 of 0.44 μM for hBuChE. BuChE-IN-11 has high blood-brain barrier permeability and exhibits strong antioxidant activity due to its free radical scavenging properties. BuChE-IN-11 interacts with the choline binding site, acetyl binding site, and peripheral anionic site, exhibiting submicromolar BuChEinhibitoryactivity and preventing β-amyloid (Aβ) self-aggregation. BuChE-IN-11 holds promise for research in the field of Alzheimer's disease .
Esculentoside A (Standard) is the analytical standard of Esculentoside A. This product is intended for research and analytical applications. Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta .
Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models , has selective inhibitoryactivity towards cyclooxygenase-2 (COX-2) .
Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways .
Amb123203 is an antiviral compound with the activity of inhibiting viral budding. Amb123203 exerts its effect by blocking the interaction between mVP40 and Nedd4 proteins. Amb123203 has a significant inhibitory effect on the budding of VP40 virus-like particles (VLPs) of Marburg (MARV) and Ebola viruses. Amb123203 can effectively target RNA viruses that rely on the PPxY L domain for efficient budding, showing broad-spectrum antiviral activity. The discovery of Amb123203 provides an important basis for the development of new broad-spectrum antiviral compounds .
PDE7-IN-4 is a phosphodiesterase 7 (PDE7) inhibitor with activity that increases intracellular cyclic adenosine monophosphate (cAMP) levels. PDE7-IN-4 shows potential inhibitory effects in neurotransmission and anti-inflammatory applications. PDE7-IN-4 exerts its biological activity by acting on the cAMP/cAMP response element binding protein (CREB) pathway. The development of PDE7-IN-4 aims to improve its pharmacokinetic characteristics to more effectively target neurodegenerative diseases and other inflammation-related diseases .
SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitoryactivity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways .
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specificinhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag Olamine owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag Olamine can be used for the research of cardiovascular. Eltrombopag Olamine also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag Olamine can induce apoptosis in hepatocellular carcinomab (HCC) as well .
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitoryactivity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively . Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitoryactivity against HBV replication .
FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibitsmouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitoryactivity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect .
Tropolone is a seven-membered non-benzenoid aromatic compound, which is the precursor of many Azulene derivatives. Tropolone is a potent mushroom tyrosinaseinhibitor with an IC50 value of 0.4 μM. Its inhibitory effect can be achieved by dialysis or excess CU 2+ Reversa. Tropolone exhibits broad anti-viral and anti-fungal activity and is synergistic upon co-treatment with nucleos(t)ide analog drugs. Tropolone is a promising candidate for research in osteosarcoma .
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases .
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitoryactivities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
Eltrombopag- 13C4 (SB-497115- 13C4) is 13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells .
HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has inhibitoryactivity against pre-miR-21 RNA. HOE 33187-O-CONH-PEG4-phenol-thiophenone-NHPh-COOEt has the potential for the research of neoplastic disease such as cancer and especially cancers expressing miR-21 (extracted from patent WO2021087084A1, compound 25) .
Cap-dependent endonuclease-IN-2 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-2 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-2 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent WO2019052565A1, compound 28) .
Cap-dependent endonuclease-IN-9 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-9 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-9 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN112521386A, compound VI-1) .
DNA-PK-IN-6 is a potent inhibitor of DNA-PK. DNA-PK-IN-6 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-6 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021197159A1, compound 6) .
DNA-PK-IN-5 is a potent inhibitor of DNA-PK. DNA-PK-IN-5 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-5 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021204111A1, compound 2) .
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitoryactivity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .
TP0427736 hydrochloride is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50=836 nM). TP0427736 hydrochloride also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 hydrochloride can be used for the research of androgenic alopecia (AGA) .
Atg4B-IN-2 is a potent competitive Atg4Binhibitor with Ki value of 3.1 μM, also possesses declining PLA2inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition .
MtTMPK-IN-2 (compound 15) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK)inhibitor with an IC50 value of 1.1 μM. MtTMPK-IN-2 has inhibitoryactivity against Mtb H37Rv (MIC = 12.5 μM). MtTMPK-IN-2 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC50 = 6.1 μM). MtTMPK-IN-2 can be used for researching tuberculosis .
MtTMPK-IN-3 (compound 25) is a potent Mycobacterium tuberculosis thymidylate kinase (MtTMPK)inhibitor with an IC50 value of 0.12 μM. MtTMPK-IN-3 has inhibitoryactivity against Mtb H37Rv (MIC = 12.5 μM). MtTMPK-IN-3 exhibits certain cytotoxicity in human fibroblast cells MRC-5 (EC50 = 12.5 μM). MtTMPK-IN-3 can be used for researching tuberculosis .
HDAC-IN-38 (compound 13) is a potent HDACinhibitor. HDAC-IN-38 shows similar micro-molar inhibitoryactivity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5) .
HIV-1 inhibitor-35 (compound 74) is a potent HIV-1inhibitor with EC50s of 80 nM and 70 nM for LTR and CMV in HEK293 cells, respectively. HIV-1 inhibitor-35 has inhibitoryactivity against liver cancer cell HepG2 with a CC50 of 40 nM. HIV-1 inhibitor-35 can be used as HIV-1 latency reversing agent .
HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitoryactivity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity .
HDAC6-IN-6 (compound 6a) is a potent and BBB-penetrated HDAC6inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-6 exhibits strong inhibitoryactivity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-6 can enhance neurite outgrowth without significant neurotoxicity .
BACE1-IN-12 (compound 7g) is a potent and BBB-penetrated BACE1inhibitor, with an IC50 of 8.9 µM. BACE1-IN-12 shows selective BuChE (butyrylcholinesterase) inhibitoryactivity with an IC50 of 3.2 µM. BACE1-IN-12 shows effective antioxidant effect with an IC50 of 10.2 μM (DPPH). BACE1-IN-12 might be served as a potential anti-Alzheimer agent .
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibitsEGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitoryactivities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibitsEGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitoryactivities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .
3-IN-PP1 is a protein kinase D (PKD)inhibitor. 3-IN-PP1 has potent pan-PKD inhibitoryactivity for PKD1, PKD2 and PKD3 with IC50 values of 108, 94 and 108 nM, respectively. 3-IN-PP1 also is a broad spectrum anticancer agent and has inhibition of several tumor cells growth. 3-IN-PP1 can be used for the research of cancer .
PBRM1-BD2-IN-7 is a selective and cell-active polybromo-1 (PBRM1) bromodomaininhibitor. PBRM1-BD2-IN-7 has inhibitoryactivity for PBRM1-BD2 with an IC50 value of 0.29 μM. PBRM1-BD2-IN-7 can be used for the research of cancer .
Tubulin/MMP-IN-2 is dual inhibitor of tubulin and matrix metalloproteinases. Tubulin/MMP-IN-2 can strongly inhibit tubulin polymerization and induces cell apoptosis. Tubulin/MMP-IN-2 has inhibitoryactivities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively. Tubulin/MMP-IN-2 can be used for the research of cancer .
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitoryactivity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
(24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid is a potent PTP1Binhibitor, with an IC50 of 0.4 μM. (24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid exhibits potent PTP1Binhibitoryactivity without cytotoxicity .
Defensin HNP-3 human is a cytotoxic antibiotic peptide known as "defensin". Defensin HNP-3 human has inhibitoryactivity against Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Defensin HNP-3 human is initially synthesized as the 94 amino acids preproHNP(1-94), which is hydrolyzed to proHNP(20-94) and converted to mature HNP(65-94) after the removal of anion precursors .
HMGB1-IN-1 (compound 6) displays strong NO inhibitory effect in RAW264.7 cells with IC50 value of 15.9 ± 0.6 μM. HMGB1-IN-1 inhibit the HMGB1/NF-κB/NLRP3 pathway. HMGB1-IN-1 shows good anti-inflammatory activity and good anti-sepsis effects in kidney injury .
(Z)-ONO 1301 is the isomer of ONO 1301 (HY-106961), and can be used as an experimental control. ONO 1301 (ONO-AP 500-02), a prostaglandin (PG) I2 mimetic, is an orally active, long-acting prostacyclin agonist with thromboxane-synthase inhibitoryactivity. ONO 1301 promotes production of hepatocyte growth factor (HGF) from various cell types and ameliorates ischemia-induced left ventricle dysfunction in the mouse, rat and pig .
mHTT-IN-2 (compound 27) is a potent inhibitor (EC50=0.066 μM) of mutant huntingtin (mHTT). mHTT-IN-2 reduces canonical splicing of HTT RNA exons [49-50] and is a splicing regulator of the huntingtin (HTT) gene. mHTT-IN-2 exhibits inhibitoryactivity in vitro and in vivo in human HD stem cells and mouse BACHD models. mHTT-IN-2 may be used in the study of branaplam-related peripheral neuropathy .
Ginsenoside Rb3 (Standard) is the analytical standard of Ginsenoside Rb3. This product is intended for research and analytical applications. Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
SHP1-IN-1 (compound 5p) is a fluorescent probe for the protein tyrosine phosphatase SHP1 containing the Src homology 2 domain. SHP1-IN-1 has SHP1 inhibitoryactivity, selectivity for Fe 3+ ions and good fluorescence properties. SHP1-IN-1 exhibits aggregation post-quenching (ACQ) effect, good interference immunity and low detection limit (5.55 μM) .
Neodidymelliosides A (compound 1)It is a secondary metabolite of fungi and has a significant inhibitory effect on Staphylococcus aureus and Candida albicans biofilms. Neodidymelliosides AIt also has anti-cancer activity and can inhibit KB3.1 (cervix),PC-3 (prostate),MCF-7(breast),SKOV-3 (ovary),A431 (skin )and A549 (lung )Cell viability of cell lines .
Enpp-1-IN-20 (Compound 31) is an ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitor, with an IC50 of 0.09 nM. Enpp-1-IN-20 has strongest inhibitoryactivity in the cell-based assay, with an IC50 of 8.8 nM. Enpp-1-IN-20 has significant potency in both ENPP1 inhibition and STING pathway stimulation in vitro. Enpp-1-IN-20 can be used for the research of cancer .
HER2-IN-19 (Compound 10e) is a potent inhibitor of HER2 and EGFR with IC50 values of 0.87 respectively and 3.5 nM. HER2-IN-19 has potent inhibitoryactivity against tumor cells, IC50NCI-N87 = 1.63 nM, IC50BT474= 15.17 nM, IC50BaF3-HER2YVMA = 1.49 nM .
LRRK2-IN-14 (Compound 8) is an orally active LRRK2inhibitor. LRRK2-IN-14 has an IC50 of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on hERG (IC50=22 μM). LRRK2-IN-14 has blood-brain barrier permeability .
Ilaprazole (Standard) is the analytical standard of Ilaprazole. This product is intended for research and analytical applications. Ilaprazole (IY-81149) is an orally active proton pumpinhibitor. Ilaprazole irreversibly inhibitsH +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitoryactivity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor .
LDN-211904 is an inhibitor of EphB3 receptor tyrosine kinase. LDN-211904 enhances the inhibitoryactivity of EphB3 kinase by maintaining the 2-chloroaniline group and introducing a phenyl or small electron donor substituent to the 5 position of pyrazole and [1,5-a] pyridine. LDN-211904 can be used as a molecular probe to study the function and signaling pathways of EphB3 receptors, especially in the nervous system during neurodevelopment and adulthood .
PQQ-trimethylester (PQQ-TME) is a synthetic compound that is a trimethylester derivative of pyrroloquinoline quinone (PQQ). PQQ-trimethylester has twice the blood-brain barrier permeability of PQQ (HY-100196) in vitro. In addition, PQQ-trimethylester shows strong inhibitoryactivity against α-synuclein, amyloid β1-42 (Aβ1-42) and prion protein fibrillation. PQQ-trimethylester can be used in the study of neurodegenerative diseases .
Enitociclib (VIP152; BAY-1251152) is a selective CDK9 inhibitor. Known for its unique benzyl sulfoxide moiety, VIP152 has demonstrated promising efficacy and tolerability both in vitro and in vivo, including in mouse and rat xenograft models via weekly intravenous infusions Highly effective and well tolerated. VIP152 shows promising long-term single-agent inhibitoryactivity against double-click refractory diffuse large B-cell lymphoma .
VEGFR-2-IN-50 (Compound 10f) is a VEGFR-2inhibitor and apoptosis inducer, with an IC50 value of 0.33 μM. VEGFR-2-IN-50 (Compound 10f) has growth inhibitoryactivity on MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 19.86 μM and 10.88 μM, respectively, which is expected to be used in the study of breast cancer diseases .
Hsp110/sGC-modulator-1 (compound 17i), an orally active Hsp110/sGC dual-target regulator, exhibits optimal Hsp110 and sGC molecular activities as well as remarkable cell malignant phenotypes inhibitory and vasodilatory effects. Hsp110/sGC-modulator-1 (compound 17i) attenuates pulmonary vascular remodeling and right ventricular hypertrophy via Hsp110 suppression .
Daledalin tosylate (UK 3557) has mono-amine oxidaseinhibitoryactivity in vitro, probably by acting as a substrate. Daledalin tosylate also has antidepressant effects. Daledalin tosylate potentiates amphetamine-induced excitation in rats, antagonises Reserpine (HY-N0480)-hypothermia in mice, tetrabenazine-sedation in rats and Reserpine (HY-N0480)- and Tetrabenazine (HY-B0590)-induced ptosis in mice with . Daledalin tosylate is proming for rasearch of depressive illness .
MGS0039 is a type II group mGluR antagonist. MGS0039 has a high affinity for mGluR2 and mGluR3, with Ki values of 2.2 nM and 4.5 nM, respectively. MGS0039 can attenuate the inhibitory effect of glutamate-induced cyclic AMP formation triggered by Forskolin (HY-15371) in CHO cells expressing mGluR2/mGluR3. MGS0039 shows antidepressant-like activity in rats .
Methyl 5-hydroxy-1H-indole-3-carboxylate is a marine natural product with isocitrate lyase inhibitoryactivity. Methyl 5-hydroxy-1H-indole-3-carboxylate is found in Hyrtios erectus. Methyl 5-hydroxy-1H-indole-3-carboxylate can be used to study its interaction with specific biological targets .
SK609 is a selective dopamine D3 receptor agonist with activity that improves dopamine and norepinephrine levels in the cerebral cortex. SK609 has been successfully used to suppress dyskinesias in Parkinson's disease models and alleviated muscle twitches induced by L-dopa. SK609 improved performance in sustained attention tasks by significantly reducing misses and false alarms. SK609 may provide an inhibitory option for suppressing movement and cognitive impairment in patients with Parkinson's disease .
2002-H20 is an inhibitor of Aβ42-induced cytotoxicity, with the activity of reducing the cytotoxicity of Alzheimer's disease Aβ peptide by binding to it. 2002-H20 protects cells and reduces Aβ toxicity by promoting fibril formation, possibly by accelerating Aβ aggregation. The screening method of 2002-H20 effectively identifies compounds that reduce Aβ toxicity and presents potential inhibitory leads .
Zotiraciclib hydrochloride is a novel small molecule multi-target enzyme inhibitor with activity in inhibiting tumor growth. Zotiraciclib hydrochloride exerts its anti-tumor effect by reducing the level of Myc through inhibiting cyclin-dependent kinase 9 (CDK9). Zotiraciclib hydrochloride may be useful for inhibiting cancers that cross the blood-brain barrier. The high protein level of MCL-1 of Zotiraciclib hydrochloride is associated with survival, suggesting that it may serve as a prognostic factor and inhibitory target in further studies .
PDE5-IN-6c is a potent and selective phosphodiesterase 5A1 (PDE5A1) inhibitor with the potential to inhibit Alzheimer's disease (AD). PDE5-IN-6c exhibits an excellent in vitro IC50 (0.056 nM), demonstrating its potent inhibitoryactivity. PDE5-IN-6c has improved water solubility, making it a more attractive drug candidate .
UK-88947 hydrochloride is a protease inhibitor with activity in inhibiting the replication of human immunodeficiency virus HIV-1. UK-88947 hydrochloride can be added to cells before infection to block the early steps of HIV-1 replication. The use of UK-88947 hydrochloride shows its specific inhibitory effect on HIV-1. At the same time, when the virus infects cells, it inhibits the action of viral protease and affects the virus replication process .
ent-Avibactam sodium (AVE1330A) is a new β-lactamase inhibitor with broad-spectrum antibacterial activity. ent-Avibactam sodium, in combination with ceftazidime, exhibits significant inhibitory effects on Enterobacteriaceae that produce Ambler class A and class C beta-lactamases. The IC50 value of ent-Avibactam sodium is much lower than the commonly used β-lactamase inhibitors clavulanic acid and ticarbonitrile, showing its ability to inhibit TEM-1 and P99 enzyme efficiency .
Kanamycin (sulfate) (Standard) is the analytical standard of Kanamycin (sulfate). This product is intended for research and analytical applications. Kanamycin (Kanamycin A) sulfate is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin sulfate shows good inhibitoryactivity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
CP-31398 can stabilize the active conformation of p53 and promote p53activity in cancer cells with either mutant or wild-type p53. In addition, CP-31398 can upregulate p53 target genes, such as p21WAF1/Cip1 and KILLER/DR5. CP-31398 exerts an inhibitory effect on tumor growth .
SARS-CoV-2 Mpro-IN-34 (Compound 26) is an inhibitor for SARS-CoV-2 Mpro with an IC50 of 6 nM. SARS-CoV-2 Mpro-IN-34 exhibits inhibitory efficacy against OC43 Mpro with an IC50 of 33 nM. SARS-CoV-2 Mpro-IN-34 exhibits antiviral activity in SARS-CoV-2 infected Vero E6 cell with an EC50 of 0.103 μM .
HDM-IN-1 (Compound A4) is an inhibitor for fungal histone demethylase (HDM), that inhibits the H3K27me3 in Cryptococcus neoformans and in Candida auris with IC50s of 134 and 12 nM. HDM-IN-1 exhibits inhibitory efficacy against C. neoformans and C. auris with MIC80 of 0.5-2 μg/mL, through inhibition of the biofilm and capsule formation. HDM-IN-1 exhibits antifungal activity in ICR mouse model .
Angiotensin 1-7 (Ang-(1-7)) is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 inhibits purified canine ACEactivity (IC50=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 μM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 μM) . Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis . Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo .
Angiotensin 1-7 (Ang-(1-7)) acetate is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 acetate inhibits purified canine ACEactivity (IC50=0.65 μM). Angiotensin 1-7 acetate acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 acetate blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium .
HDAC-IN-56 ((S)-17b) is an orally active class I histone deacetylase (HDAC)inhibitor with IC50 values of 56.0 ± 6.0, 90.0 ± 5.9, 422.2 ± 105.1, >10000 nM for HDAC1, HDAC2, HDAC3, and HDAC4-11, respectively. HDAC-IN-56 has potent inhibitoryactivity while strongly increasing intracellular levels of acetylhistone H3 and P21 and effectively inducing G1 cell cycle arrest and apoptosis.HDAC-IN-56 has antitumor activity .
Insecticidal agent 9 (Compound I-17) is an insecticide with good insecticidal activity. Insecticidal agent 9 has LC50 values of 93.32 mg/L and 114.79 mg/L against Plutella xylostella and Ostrinia furnacalis respectively, and exhibits a mortality rate of up to 86.1% against Spodoptera frugiperda at a concentration of 500 mg/L. Insecticidal agent 9 can act simultaneously on the ecdysone receptor (EcR) and three chitinases (OfChtI, OfChtII, and OfChi-h), demonstrating good binding activity (to EcR) and inhibitory rates (to the three chitinases). Insecticidal agent 9 can be used in research for pest management .
Fenbufen (Standard) is the analytical standard of Fenbufen. This product is intended for research and analytical applications. Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitoryactivities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor .
RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .
Nifuratel (NF 113) is an orally active broad-spectrum antibiotic with antiprotozoal, antibacterial, anticancer and anti-inflammatory activities, and has good inhibitory effects on Candida and Trichomonas. Nifuratel is also a STAT3inhibitor, which significantly inhibits the growth and proliferation of human gastric cancer cells and induces apoptosis. In addition, Nifuratel also inhibits mast cell-mediated antigen hypersensitivity reactions and can be used in the study of IgE-mediated allergic diseases .
EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2)inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers . EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
GNF-7 is a multikinase inhibitor. GNF-7 is a Bcr-Ablinhibitor, with IC50s of 133 nM and 61 nM for Bcr-Abl WT and Bcr-Abl T315I, respectively. GNF-7 also possesses inhibitoryactivity against both ACK1 (activated CDC42 kinase 1) and GCK (germinal center kinase) with IC50s of 25 nM and 8 nM, respectively. GNF-7 can be used for the research of hematologic malignancies .
EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
Harpagoside can be obtained by Harpagophytum procumbens, which has anti-inflammatory, anti-cancer, protective activity, and efficacy. Harpagoside has an inhibitory effect on COX-1 and COX-2 active, and suppresses NO production. Harpagoside inhibits HepG2 cell lipid polysaccharide, which is a protein that is expressed horizontally and selectively, and has anti-inflammatory and latent pain effects. Harpagoside has the ability to protect the body, and has a degenerative effect on the β-oxidation (Aβ) .
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects . Mulberroside A shows inhibitoryactivity against mushroom tyrosinase with an IC50 of 53.6 μM .
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterialactivity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains .
DNMT3A-IN-1 (compound 1) is an effective and selective DNMT3A inhibitor. DNMT3A-IN-1 exhibits inhibitoryactivity against DNMT3A, with KI values ranging from 9.16 to 18.85 μM (AdoMet) and 11.37 to 23.34 μM (poly dI-dC). DNMT3A-IN-1 can induce apoptosis in acute myeloid leukemia (AML) cell lines (Apoptosis) .
Tau-aggregation and neuroinflammation-IN-1 is a potent tau-aggregation and neuroinflammationinhibitor. Tau-aggregation and neuroinflammation-IN-1 exhibits remarkable inhibitoryactivities against AcPHF6 and full-length tau aggregation. Tau-aggregation and neuroinflammation-IN-1 has a low cytotoxicity and reduced NO release in LPS-stimulated BV2 cells. Tau-aggregation and neuroinflammation-IN-1 can reverse okadaic acid-induced memory impairment in rats .
Influenza virus-IN-3 (compound 9) is a potent and selective influenza virusinhibitor with IC50s of 0.88, 0.10, 5.5, 0.51 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-3 shows antiviral and NA (neuraminidase enzyme)-inhibitoryactivity. Influenza virus-IN-3 shows low cytotoxicity with an CC50 of >200 µM .
14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a KD of 35 µM. 14-3-3η Protein inhibitor 1 shows inhibitoryactivities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cell apoptosis and G1-S cell cycle arrest with good metabolic stability .
DNDI-8219 (compound 58) is a potent selective and orally active trypanocidal agent, possessing inhibitoryactivity against Trypanosoma cruzi (T. cruzi) with an IC50 of 0.4 μM. DNDI-8219 has low cytotoxicity (L6 cells IC50 > 100 μM). DNDI-8219 can effectively cure chronic T. cruzi infection and markedly reduce parasite burdens in mouse model. DNDI-8219 has good solubility, metabolic stability and safety.
PBRM1-BD2-IN-1 is a selective and cell-active polybromo-1 (PBRM1) bromodomaininhibitor. PBRM1-BD2-IN-1 has binding affinity and inhibitoryactivity for PBRM1-BD2 with Kd and IC50 values of 0.7 μM and 0.2 μM, respectively. PBRM1-BD2-IN-1 can be used for the research of cancer .
PBRM1-BD2-IN-2 is a selective and cell-active polybromo-1 (PBRM1) bromodomaininhibitor. PBRM1-BD2-IN-2 has binding affinity and inhibitoryactivity for PBRM1-BD2 with Kd and IC50 values of 9.3 μM and 1.0 μM, respectively. PBRM1-BD2-IN-2 can be used for the research of cancer .
SARS-CoV-2 3CLpro-IN-6 is a reversible covalent inhibitor of SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro-IN-6 has potent inhibitoryactivity for SARS-CoV-2 3CL pro with an IC50 value of 4.9 μM. SARS-CoV-2 3CLpro-IN-6 can be used for the research of coronavirus disease 2019 (COVID-19) .
8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide (compound 3), a sesquiterpene, has anti-LIMK1activity. 8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide has inhibitory property on cell motility .
Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibitsJNK and p38MAPK signals. Lucidone also has inhibitoryactivity against Dengue virus (DENV) (EC50=25 μM) .
Antifungal agent 72 (Compound B8) is a potent antifungal agent. Antifungal agent 72 suppresses the function of efflux pump and down-regulates the resistance-associated genes through blocking the Pdr1-KIX interaction (Ki: 11.7 μM). Antifungal agent 72 is active against Fluconazole (HY-B0101)-resistant with a MIC value of 63 ng/mL, and shows synergistic inhibitoryactivity with Fluconazole. Antifungal agent 72 can be used for C. glabrata infection research .
ALDH3A1-IN-3 (CB29) is a selective inhibitor of ALDH3A1, with a Ki value of 4.7 μM and an IC50 value of 16 μM. ALDH3A1-IN-3 has no inhibitory potential on the in vitroactivity of ALDH1A1, ALDH1A2, ALDH1A3, ALDH1B1, or ALDH2. ALDH3A1-IN-3 can be used in cellular oxidation and cancer research .
Bavachalcone (Standard) is the analytical standard of Bavachalcone. This product is intended for research and analytical applications. Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro .
(R)-(+)-Mequitazine is a histamine H1 receptor antagonist that mainly undergoes bio-transformation via human liver microsomes, resulting in hydroxylated and S-oxidized metabolites. (R)-(+)-Mequitazine competitively binds to the H1 receptors in gastrointestinal, vascular, and respiratory effect cells, thus blocking the endogenous activity of histamine. (R)-(+)-Mequitazine has an inhibitory effect on CYP3A-catalyzed midazolam 1’-hydroxylase. (R)-(+)-Mequitazine can be used in the study of various allergic diseases .
Arcopilin A (compound Arcopilin A(1))is an antibacterial agent. Arcopilin A has weak inhibitory effects on fungal pathogens and Gram-positive bacteria, with IC50 values of 8.9 μg/mL and 14 μg/mL for cells KB-3-1 and L929, but it can effectively destroy preformed biofilms of Staphylococcus aureus. Arcopilin A can enhance the activities of gentamicin (GM; HY-K1050) and vancomycin (Vac; HY-B0671) by 115 and 31 times, respectively .
hCAIX/XII-IN-13 is an inhibitor of human carbonic anhydrases (hCA). hCAIX/XII-IN-13 shows good inhibitoryactivity against the tumor-related CA subtypes IX and XII, with Ki values of 0.08 µM and 0.06 µM, respectively. Under hypoxic conditions, hCAIX/XII-IN-13 can restore the cytotoxicity of Doxorubicin (HY-15142A) on MCF-7 cells, increasing G2/M phase cell cycle arrest and apoptosis .
AZD-3289 is a potent BACE1 inhibitor with potential Alzheimer's disease inhibitoryactivity. The application of AZD-3289 is intended to slow the pathological progression of Alzheimer's disease by inhibiting the production of β-amyloid protein. The development of AZD-3289 responds to the need to reduce neurodegenerative changes associated with Alzheimer's disease. As a BACE1 inhibitor, AZD-3289 can effectively reduce the accumulation of β-amyloid peptide in the brain, which may improve cognitive function .
PDE8B-IN-1 is a selective inhibitor of phosphodiesterase 8B (PDE8B) with the activity of enhancing insulin secretion. PDE8B-IN-1 showed good efficacy in high-throughput screening and optimized its ligand efficiency through rapid deconstruction. PDE8B-IN-1 showed high target selectivity and good bioavailability in preclinical development, providing a basis for exploring its potential inhibitory use .
Milvexian TFA (BMS-986177 TFA) is a factor XIa inhibitor with biological activity to prevent venous thromboembolism. Milvexian TFA was effective in reducing the occurrence of venous thromboembolism in patients undergoing knee replacement surgery. Milvexian TFA has good selectivity and shows significant inhibitory effects on plasma kallikrein and trypsin. Milvexian TFA has a bioavailability of 32%, which means it has a high absorption rate in the body. Milvexian TFA showed a relatively low risk of bleeding in clinical trials .
BCM-599 is a HBV (hepatitis B virus) capsid assembly inhibitor with the activity of inhibiting HBV capsid assembly. BCM-599 showed an IC50 value of 0.88μM and a CC50 value of 144μM in HepG2.2.15 cells. When used in combination with lamivudine, BCM-599 showed a synergistic inhibitory effect on viral concentration. BCM-599 can be used as an effective combined inhibition option for HBV infection .
NDM-1 inhibitor-2 is an inhibitor of New Delhi metallo-β-lactamase-1 (NDM-1) and has the ability to inhibit NDM-1 activity. NDM-1 inhibitor-2 exhibits a good inhibitory effect on drug-resistant bacterial strains that overexpress NDM-1. When NDM-1 inhibitor-2 is used in combination with the carbapenem antibiotic meropenem, a favorable synergistic effect can be produced .
YM-44781 free acid is a non-peptide neuropeptide receptor antagonist with efficient NK(2) and NK(1) receptor antagonist activity. YM-44781 exhibits significant binding affinity on the NK(2) receptor (pKi = 9.94) and also on the NK(1) receptor Higher binding affinity (pKi = 9.09). In addition, YM-44781 also showed significant inhibitory effects on bladder contraction induced by selective NK(1) receptor agonists .
Parethoxycaine hydrochloride is an anesthetic with nerve conduction blocking activity. Parethoxycaine hydrochloride exhibits non-selective inhibitory effects on responses to various stimulants in rat vas deferens and guinea pig ileum muscles. Parethoxycaine hydrochloride has an enhanced effect on the action of norepinephrine, and its methyl bromide derivative also exhibits the same properties on the action of norepinephrine and potassium ions. Derivatives of parethoxycaine hydrochloride have significant effects on calcium dose-response curves, displaying different tissue and stimulant selectivities. The mechanism of action of Parethoxycaine hydrochloride involves the regulation of calcium transport processes .
Telaprevir (Standard) is the analytical standard of Telaprevir. This product is intended for research and analytical applications. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide . Telaprevir inhibits SARS-CoV-2 3CLpro activity .
EHNA is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
T-3364366 is a reversible, slow-binding, thienopyrimidinone delta-5 desaturase (D5D) inhibitor with IC50s of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cells, respectively. T-3364366 exhibits potent D5D (IC500=19 nM) inhibitoryactivity and excellent selectivity away from delta-6 desaturase (D6D, IC50=6200 nM) and delta-9 desaturase (stearoyl-CoA desaturase, SCD,50 >10000 nM) in the enzymatic activity assay .
α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylaseinhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease .
DNA gyrase B-IN-2 (Compound E) is a 2-aminobenzothiazole-based DNA gyrase B inhibitor with promising activity against ESKAPE bacterial pathogens. DNA gyrase B-IN-2 showed low nanomolar inhibition of DNA gyrase (IC50 < 10 nM) and broad-spectrum antibacterial activity against pathogens belonging to the ESKAPE group, with the minimum inhibitory concentration < 0.03 μg/mL for most Gram-positive strains and 4–16 μg/mL against Gram-negative E. coli, Acinetobacter baumannii, Pseudomonas aeruginosa, and Klebsiella pneumoniae.DNA gyrase B-IN-2 can be used for the research of infection .
Poziotinib (HM781-36B) is an orally active, irreversible pan-HERinhibitor, which effectively inhibits EGFR wt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitoryactivities against mutated EGFRs, including EGFR T790M and EGFR L858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity .
MIND4 is a novel thiozoline that was found to inhibit the deacetylase SIRT2 and to have neuroprotective activity in in vitro brain slices and Drosophila models of Huntington's disease (HD). A systems biology approach revealed another SIRT2-independent property of MIND4, namely as an inducer of nuclear factor erythroid 2 p45-derived factor 2 (NRF2) activity. Structure-activity relationship studies further identified a potent NRF2 activator (MIND4-17) that lacks SIRT2 inhibitoryactivity. MIND compounds induce NRF2 activation responses in both neuronal and non-neuronal cells and reduce the generation of reactive oxygen and nitrogen intermediates. These agent-like thiozolines offer exciting opportunities for the development of multi-target agents with potential synergistic therapeutic benefits for HD and related disorders.
Racemomycin B (229-B; Streptothricin D), the main component from Streptomyces lavendulae OP-2, is a streptothricin antibiotic containing three β-lysine groups. RM-B exhibits antimicrobial activity against plant pathogenic microorganisms and effectively inhibits the growth of Brassica rapa L. roots at 50 ppm. RM-B showed a minimum inhibitory concentration (MIC) of 0.4 μg/ml against Pseudomonas syringae pv. tabaci IFO-3508 and a MIC range of 0.1-2.0 μg/ml against six strains of Fusarium oxysporum, showing stronger antimicrobial activity than RM-A and RM-C. The biological activity of racemomycin compounds increases with the increase in the number of β-lysine groups.
8-(3-Chlorostyryl)caffeine (CSC) is an adenosine antagonist with selective activity at the A2a adenosine receptor. 8-(3-Chlorostyryl)caffeine showed 520-fold selectivity in radioligand binding experiments in rat brain. Antagonism of adenylylase by 8-(3-Chlorostyryl)caffeine shows 22-fold selectivity in rat chromaffin cells When 8-(3-Chlorostyryl)caffeine is co-administered with the A1-selective antagonist CPX, It can also further increase exercise activity. 8-(3-Chlorostyryl)caffeine exhibits good MAO-B inhibitoryactivity in primate mitochondria. 8-(3-Chlorostyryl)caffeine also has excellent A2A receptor affinity .
HIV-1 inhibitor-79 (Compound 3k) is an HIVinhibitor that exhibits significant inhibitoryactivity against HIV-1 and its common mutant strains (with IC50 values of 1.9, 1.9, 8.7, and 11 nM against HIV-1, K103, L100I, and E138K, respectively), and has low cytotoxicity and a high selectivity index (CC50 = 21.95 μM, SI = 11478). Additionally, HIV-1 inhibitor-79 also shows antiviral activity against HIV-2, with an EC50 value of 6.14 μM, and significantly inhibits the activity of HIV-1 reverse transcriptase (IC50 = 25 nM) .
EPZ-011989 trifluoroacetate is a potent and orally active Zeste Homolog 2 (EZH2)inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers . EPZ011989 (trifluoroacetate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects.
Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibitsactivities of p38 MAPK and NF-kB [5][6], exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity . Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.
NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC50 of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 0.584 µM, 0.706 µM, and 0.605 µM, respectively. NVP-2 induces cell apoptosis.
Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM . Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively .
Indirubin-5-sulfonate is a cyclin-dependent kinase (CDK)inhibitor, with IC50 values of 55 nM, 35 nM, 150 nM, 300 nM and 65 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, and CDK5/p35, respectively . Indirubin-5-sulfonate also shows inhibitoryactivity against GSK-3β .
ARP-100 is a potent and selective matrix metalloproteinase MMP-2inhibitor (IC50=12 nM). ARP-100 interacts with S1＇ pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitoryactivity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM) .
Bohemine is a purine analogue and is a synthetic and selective CDKinhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibitsERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities .
(±)-Catechin (rel-Cianidanol) This is a green tea polyester. Catechin possesses anti-cancer activity, which has led to its demise. (±)-Catechin 具有两种forms (+)-Catechin and its reflection body (-)-Catechin. (+)-Catechin inhibitory environment-1 (COX-1) IC50 为 1.4 μM. (-)-Catechin has the effect of promoting hBM-MSC adipose cell differentiation, increasing adipose tissue, and PPARγ horizontal. (±)-Catechin has anti-diabetic, anti-hypertrophic, anti-diabetic, anti-cardiovascular, anti-infective, and liver-protecting effects.
AChE-IN-11 (compound 5C) is a triple inhibitor targeting AChE/MAO-B/BACE1 (IC50=7.9 μM, 9.9 μM, 8.3 μM, respectively) and a selective metal ion chelators. AChE-IN-11 exhibits mixed AChE inhibitory effects, binding to both CAS and PAS of AChE. AChE-IN-11 also exhibits good antioxidant activity (ORAC=2.5 eq) and potential neuroprotective effects in Alzheimer's disease .
5-HT1A/5-HT7 receptor antagonist (5-HT1A Ki = 8 nM, Kb = 0.04 nM; 5-HT7 Ki = 451 nM, Kb = 460 nM) with PDE4B/PDE7A inhibitoryactivity (PDE4B IC50 = 80.4 μM; PDE7A IC50 = 151.3 μM) , its antidepressant like effect is stronger than that of escitalopram as a reference agent.
HDAC1-IN-5 is a potent HDAC1inhibitor with IC50 values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitoryactivity against tumor growth in xenograft mice .
KRAS G12D inhibitor 16 is a KRAS G12Dinhibitor. KRAS G12D inhibitor 16 has inhibitoryactivity against KRAS G12D and KRAS G12D mutation with IC50 value of 0.7 nM and 0.35 μM, respectively. KRAS G12D inhibitor 16 can be used for the research of many malignant tumor, such as pancreatic ductal adenocarcinomas (PDAC), colon and rectal carcinomas (CRC), non-small cell lung carcinomas (NSCLC) .
PD07 is an orally active AChEinhibitor (IC50: 0.29 μM for hAChE). PD07 also inhibits ChEs, BACE1 (IC50: 13.42 μM), and Aβ1–42 aggregation in in vitro. PD07 is an antioxidant, and shows DPPH inhibitoryactivity (IC50: 26.46 μM). PD07 improves memory and cognition in Scopolamine (HY-N0296)-induced amnesia rats. PD07 can be used for research of Alzheimer’s disease .
SARS-CoV-2 3CLpro-IN-23 (Compound Cd3) is a compound that can be isolated from Citrus depressa. SARS-CoV-2 3CLpro-IN-23 has good inhibitoryactivity to the SARS-CoV-2 spike protein, with KD of 0.79 μM. SARS-CoV-2 3CLpro-IN-23 can bind to key amino acid residue, disrupting the formation of the spike protein and h-ACE2 complex .
AZD8421 is a selective CDK2 inhibitor (IC50: 9 nM) with selectivity for CDK1, CDK4 and CDK6. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest and senescence. AZD8421 demonstrated promising single efficacy and synergy with CDK4/6 inhibitors such as Palbociclib (HY-50767) in in vivo breast and ovarian models. AZD8421 also has potent single-agent inhibitoryactivity against drug-resistant breast cancer cells.
Eltrombopag (Standard) is the analytical standard of Eltrombopag. This product is intended for research and analytical applications. Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well .
RW3 is a small cationic hexapeptide with amphiphilic properties. RW3 targets the plasma membrane of bacteria and works by inhibiting cell respiration and cell wall synthesis. RW3 shows high biological activity against gram-positive bacteria and does not show significant cytotoxic or hemolytic effects in previous studies. RW3 quickly kills 97% of the initial colony forming units (CFU) within 10 minutes at twice the minimum inhibitory concentration (MIC). RW3 can be used in antimicrobial and antifungal studies .
Cefsulodin (SCE-129) showed potent activity against Pseudomonas aeruginosa and strains susceptible to penicillin and gentamicin, with effectiveness comparable to that of gentamicin and debendazole. However, its effectiveness was diminished against penicillin-resistant strains of P. aeruginosa, particularly strains that were also resistant to gentamicin. For P. aeruginosa maltofila, SCE-129 showed similar minimum inhibitory concentrations to penicillin, gentamicin, and debendazole. Pseudomonas cepacia strains generally showed moderate resistance to SCE-129 and penicillin, and high resistance to gentamicin and debendazole .
Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
Incadronate disodium (YM 175) is a bisphosphonate with strong inhibitoryactivity on bone resorption. Incadronate disodium indirectly stimulates renal 25-hydroxyvitamin D-1-hydroxylase by increasing circulating parathyroid hormone. Incadronate disodium, a cholesterol-lowering agent, is a potent inhibitor of rat liver microsomal squalene synthase (Ki=57 nM). Incadronate disodium inhibits sterol biosynthesis in mouse macrophage J774 cells (IC50=64 μM). Incadronate disodium has the potential for malignant tumors research .
4-Hydroxycanthin-6-one is a novel quinoline alkaloid isolated from the stem bark of the tree Ailanthus altissima. Five other known compounds were also found in the study. The structures of the new compounds were determined by interpretation of physical and spectroscopic data, and their absolute configurations were determined by electronic circular dichroism spectroscopy and quantum chemical calculations. These compounds showed significant inhibitoryactivity against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, showing potential anti-inflammatory properties .
(Rac)-ACT-451840 is an isomer of ACT-451840 that exhibits significant antimalarial effects. (Rac)-ACT-451840 exhibits significant antimalarial activity against P. berghei-infected mice at a dose of 20 mg/kg (ED90=13 mg/kg), and has an inhibitory effect at a dose of 300 mg/kg. The ED90 of (Rac)-ACT-451840 in the P. falciparum humanized immunodeficient mouse model is 3.7 mg/kg. (Rac)-ACT-451840 is similar to artemisinin, with a rapid onset of action but requires repeated high doses.
Curcumin (Standard) is the analytical standard of Curcumin. This product is intended for research and analytical applications. Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
SB-431542 (Standard) is the analytical standard of SB-431542. SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitoryactivity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways .
Mulberroside A (Standard) is the analytical standard of Mulberroside A. This product is intended for research and analytical applications. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitoryactivity against mushroom tyrosinase with an IC50 of 53.6 μM .
A-81282 (Abbott 81282) is an antagonist of angiotensin II's AT1 receptor, with a pA2 value of 9.64 at the AT1 receptor in rabbit aorta. A-81282 also demonstrates significant inhibitory action on the binding of [125i]_Sar1_lle8_Angiotensin_ll to rat liver membranes, with a pKI value of 8.505. A-81282 has antihypertensive activity and can effectively lower blood pressure in renal artery-ligated rats .
BMT-108908 is a negative allosteric modulator with selective activity on the NR2B subtype of the NMDA receptor. BMT-108908 has been shown to damage cognition in research, affecting cognitive functions in multiple areas. BMT-108908 failed to show a significant impact on the γ wave power of the EEG in the experiment, but it had a significant inhibitory and enhancement effect on the β wave and δ wave power. The effects of BMT-108908 differ from those of other NMDA receptor channel blockers such as ketamine and lanimol .
hCAI/II-IN-9 is a carbonic anhydrase inhibitor with inhibitoryactivity against human carbonic anhydrase isoforms I, II, IX, and XII. The inhibition constants (Ki) of hCAI/II-IN-9 for hCA I are in the range of 7.9-894 nM, for hCA II are in the range of 7.5-1645 nM, for hCA IX are in the range of 5.0-240 nM, and for hCA XII are in the range of 0.47-2.83 nM. hCAI/II-IN-9 may have potential applications in inhibiting a variety of pathologies involving these carbonic anhydrase isoforms .
(R)-KT109 is a highly potent inhibitor of diacylglycerol lipase β (DAGLβ) with an IC50 of 0.79 nM and effectively blocks DAGLα-mediated hydrolysis of 1-stearoyl-2-arachidonoyl-sn-glycerol. Additionally, it demonstrates inhibitoryactivity against α/β-hydrolase domain-containing protein 6 (ABHD6) with an IC50 of 2.51 nM, exhibiting greater potency for DAGLβ, DAGLα, and ABHD6 compared to its (S) isomer, (S)-KT109.
PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitoryactivity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability .
KT109 is a potent and an isoform-selective inhibitor of diacylglycerol lipase-β (DAGLβ) with an IC50 of 42 nM. KT109 has ~60-fold selectivity for DAGLβ over DAGLα. KT109 shows inhibitoryactivity against PLA2G7 (IC50=1 µM). KT109 shows negligible activity against FAAH, MGLL, ABHD11, and cytosolic phospholipase A2 (cPLA2 or PLA2G4A). KT109 perturbs a lipid network involved in macrophage inflammatory responses and lowers 2-arachidonoylglycerol (2-AG), arachidonic acid and eicosanoids in mouse peritoneal macrophages .
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitoryactivity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitoryactivity against hAChE and hBACE-1 enzymes (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research .
[D-Ser14]-Humanin is a bioactive peptide in which the Ser14 residue of Humanin (HY-P1928) is changed from L-form to D-form. [D-Ser14]-Humanin has potent inhibitoryactivity against the fibrillation of amyloid-β. Humanin (HY-P1928) inhibits the aging-related death of various cells caused by amyloid fibrils and oxidative stress, and [D-Ser14]-Humanin has better cell protection activity than Humanin (HY-P1928). [D-Ser14]-Humanin can be used in the study of Alzheimer's disease .
BRD4 Inhibitor-37 is a compound with anticancer activity that has inhibitoryactivity against BRD4. BRD4 Inhibitor-37 has an IC50 of approximately 0.05-0.1 μM in binding assays and shows a GI50 of 0.1-0.3 μM in cell-based assays. The effect of BRD4 Inhibitor-37 on c-Myc, a downstream protein of BRD4, has been validated, demonstrating its ability to intervene in this signaling pathway. BRD4 Inhibitor-37 exhibits selectivity among five different bromodomain proteins, enhancing its potential as a BET protein inhibitor .
COX-2/5-LOX-IN-2 (5b) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-2 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-2 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-2 shows potent COX-1, COX-2 and 5-LOX inhibitoryactivity with IC50s of 5.40, 0.01 and 1.78 μM, respectively .
COX-2/5-LOX-IN-1 (compound 3a) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-1 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-1 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-1 shows potent COX-1, COX-2 and 5-LOX inhibitoryactivity with IC50s of 12.13, 0.4 and 4.96 μM, respectively .
AMG 9090 is characterized as a compound that acts as a partial agonist of rat TRPA1 channels, demonstrating pharmacological activity in pain and inflammation models. TRPA1 is pivotal in sensing reactive compounds, triggering pain responses in humans and rodents. AMG 9090, along with other trichloro(sulfanyl)ethyl benzamides (TCEB compounds), shows differential effects on human and rat TRPA1 channels: it acts as a potent antagonist of human TRPA1 activated by AITC and noxious cold, whereas it behaves as a partial agonist at rat TRPA1. This suggests AMG 9090's potential as a therapeutic agent targeting TRPA1-mediated pain and inflammation, with additional inhibitoryactivity against TRPM8 noted .
5,6,7,8-Tetrahydro-8-deazahomofolic acid is a potential thymidylate synthase (TS) inhibitor with inhibitoryactivity against other folate-related enzymes. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed mild growth inhibition against enterococci, lactic acid bacteria, and L1210 cells in culture. 5,6,7,8-Tetrahydro-8-deazahomofolic acid also showed weak inhibition against thymidylate synthase, dihydrofolate reductase, glycyl-ribonucleoside aminotransferase, and aminoimidazole-carboxyacyl-ribonucleoside aminotransferase. 5,6,7,8-Tetrahydro-8-deazahomofolic acid showed low substrate activity for thymidylate synthase .
CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .
ODE-Bn-PMEG is an antiviral compound with strong inhibitoryactivity against HPV-11, -16, and -18. ODE-Bn-PMEG effectively reduced transient amplification of viral DNA in transfected cells at concentrations well below its cytotoxic levels. ODE-Bn-PMEG showed increased uptake in human foreskin fibroblasts and was able to be efficiently converted to the active antiviral metabolite PMEG diphosphate in vitro. The P-chiral enantiomer of ODE-Bn-PMEG showed comparable antiviral activity, indicating its potential application against multiple HPV types. ODE-Bn-PMEG is a promising candidate for local inhibition of HPV-16, HPV-18, and other high-risk types .
4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) is an antioxidant, can be isolated from Gynura divaricata and Laggera alata. 4,5-Dicaffeoylquinic acid reduces islet cell apoptosis and improves pancreatic function in type 2 diabetic mice, and has obvious inhibitoryactivities against yeast α-glucosidase. 4,5-Dicaffeoylquinic acid inhibits prostate cancer cells through cell cycle arrest. 4,5-Dicaffeoylquinic acid also has anti-apoptotic, anti-injury and anti-hepatitis B virus effects .
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Aktinhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitoryactivity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells .
BOP sodium is a potent and selective dual α9β1/α4β1 integrininhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitoryactivity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins .
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1inhibitor. HIV-1 inhibitor-15 has inhibitoryactivity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability .
FGFR4-IN-12 (Compound A34) is a potent inhibitor of FGFR4. FGFR4-IN-12 exhibits improved FGFR4 inhibitory capability and selectivity and excellent anti-proliferative activities against FGFR4-dependent HCC cell lines. FGFR4-IN-12 has the potential for the research of cancer diseases . FGFR4-IN-12 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
NF-κB/MAPK-IN-1 (compound 11a) is a potent inhibitor of NF-κB and MAPK pathway. NF-κB/MAPK-IN-1 shows inhibitoryactivity against NO production, with an IC50 of 6.96 µM. NF-κB/MAPK-IN-1 suppresses LPS-induced iNOS, COX-2, ERΚ and P38 signaling activation. NF-κB/MAPK-IN-1 can prevent LPS induced inflammatory response in macrophages. NF-κB/MAPK-IN-1 can be used for rheumatoid arthritis (RA) research .
JNK3 inhibitor-3 (compound 15g) is a selective, BBB permeable and orally active c-Jun N-terminal kinase 3 (JNK3) inhibitor. JNK3 inhibitor-3 has inhibitoryactivities to JNK1, JNK2 and JNK3 with IC50 values of 147.8, 44.0 and 4.1 nM, respectively. JNK3 inhibitor-3 significantly improves the memory in mouse dementia model. JNK3 inhibitor-3 can be used for the research of Alzheimer’s disease .
PROTAC ERα Degrader-4 is a highly potent and selectivePROTACERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER + breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
PD1-PDL1-IN 2 (ZE132) is a potent and selective PD-1/PD-L1inhibitor, which has robust anti-tumour activity in vivo. PD1-PDL1-IN 2 promotes cytotoxic T-cell tumour infiltration and induces IL-2 expression. In addition, PD1-PDL1-IN 2 elicits strong inhibitory effects on the mRNA expression of TGF-β .
Eltrombopag (Olamine) (Standard) is the analytical standard of Eltrombopag (Olamine). This product is intended for research and analytical applications. Eltrombopag Olamine (Eltrombopag diethanolamine salt) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag Olamine owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag Olamine can be used for the research of cardiovascular. Eltrombopag Olamine also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag Olamine can induce apoptosis in hepatocellular carcinomab (HCC) as well .
MAO-A/B-IN-3 (Compound 12) stands out as a key dual MAO-AChEinhibitor, displaying excellent multi-target efficacy against MAO-A, MAO-B, and AChE with IC50 values of 67 nM, 29 nM, and 1370 nM respectively. MAO-A/B-IN-3 is adept at altering the A site (hydrophobic ring) and C site (semicarbazone chain) within ketone amine-based MTDLs to bolster the inhibitory potential against MAO-A/B while notably diminishing activity against AChE. MAO-A/B-IN-3 is poised for research applications in the field of neurodegenerative diseases .
Antitumor agent-170 (Compound C6) exhibits inhibitoryactivities against PD-1/PD-L1 interaction and PARP7, with IC50 of 0.342 μM and 7.05 nM. Antitumor agent-170 exhibits a high affinity to human PD-L1, with a Ki of 9.31 nM. Antitumor agent-170 restores the T cell function and increases IFN-γ secretion. Antitumor agent-170 exhibits antitumor efficacy against melanoma in mouse models and good pharmacokinetic characteristics .
BMS-284640 is a synthetic sodium hydrogen exchange isomer-1 (NHE-1) inhibitor. BMS-284640 has a more than 380-fold higher NHE-1 inhibitoryactivity (IC50: 9 nM) compared to cariporide (HY-19693) and is more selective for NHE-1 over NHE-2 (IC50: 1.8 μM) and NHE-5 (IC50: 3.36 μM). BMS-284640 and its analogs also exhibit enhanced oral bioavailability and prolonged plasma half-life in rats. .
Anti-MRSA agent 13 (Compound 9b) is an agent against methicillin-resistant Staphylococcus aureus (MRSA), exhibiting a minimum inhibitory concentration (MIC) of 0.5–2 μg/mL against clinically isolated MRSA strains. Anti-MRSA agent 13 possesses favorable biosafety, plasma tolerance stability, and a low tendency to develop resistance. Anti-MRSA agent 13 disrupts cell walls and membranes, reduces metabolic activity, causes oxidative damage, affects DNA function, and ultimately leads to MRSA death through multi-target synergies .
NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitoryactivities against hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg) .
3,4-Dicaffeoylquinic acid (Standard) is the analytical standard of 3,4-Dicaffeoylquinic acid. This product is intended for research and analytical applications. 3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidase inhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL .
Harpagoside (Standard) is the analytical standard of Harpagoside. This product is intended for research and analytical applications. Harpagoside can be obtained by Harpagophytum procumbens, which has anti-inflammatory, anti-cancer, protective activity, and efficacy. Harpagoside has an inhibitory effect on COX-1 and COX-2 active, and suppresses NO production. Harpagoside inhibits HepG2 cell lipid polysaccharide, which is a protein that is expressed horizontally and selectively, and has anti-inflammatory and latent pain effects. Harpagoside has the ability to protect the body, and has a degenerative effect on the β-oxidation (Aβ) .
Isoscopoletin (Standard) is the analytical standard of Isoscopoletin. This product is intended for research and analytical applications. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively . Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitoryactivity against HBV replication .
Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitoryactivity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
Flupirtine hydrochloride (D 9998 hydrochloride) is a selective neuropotassium channel opener with analgesic activity. Flupirtine hydrochloride is used to inhibit a variety of pain conditions, including chronic musculoskeletal pain, migraines, and neuralgia. Flupirtine hydrochloride has antidepressant and antioxidant properties and may increase the analgesic effect in combination therapy with morphine. Flupirtine hydrochloride relieves abnormally increased muscle tension and has a muscle relaxant effect. Flupirtine hydrochloride is clinically superior to other drugs, such as tramadol and pantoxan, plus its side effects are better tolerated. Flupirtine hydrochloride has a significant effect on inhibiting neural hyperexcitability and therefore exhibits inhibitory potential in various pain states .
HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitoryactivity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056) .
DBPR110 is a nonstructural protein 5A (NS5A) inhibitor with inhibitoryactivity against hepatitis C virus (HCV). DBPR110 exhibited a 50% effective concentration (EC50) of 3.9 ± 0.9 pM and a selectivity index value of over 12,800,000 by reducing HCV1b replicon reporter expression. DBPR110 also effectively reduced the activity of HCV2a replicon with an EC50 of 228.8 pM and a selectivity index value of over 173,130. DBPR110 showed synergy with interferon alpha (IFN-α), NS3 protease inhibitors, and NS5B polymerase inhibitors. The results of DBPR110 suggest that it may be an effective small molecule inhibitor against HCV NS5A .
KB 5666 is a benzoxazine derivative with lipid peroxidation inhibitoryactivity. KB 5666 showed protective effects against post-ischemic neuronal death. KB 5666 effectively protected CA1 neurons when injected 5 minutes before or immediately after ischemia. KB 5666 also showed a dose-dependent protective effect when injected within 1 hour after ischemia. KB 5666 effectively prevented the significant decrease in microtubule-associated protein 2 immunoreactivity within the dendritic field of CA1 pyramidal cells. KB 5666 prevented the decrease in [3H]PDBu binding activity in different layers of the CA1 region after ischemia. The application of KB 5666 showed the ability to improve the cellular and functional consequences of ischemia .
(S)-BMS-378806 ((S)-BMS-806) is an orally bioavailable HIV-1 inhibitor with activity against gp120-CD4 interactions. (S)-BMS-378806 exhibits micromolar inhibition of HIV-1 gp120-CD4 binding. The design and synthesis of (S)-BMS-378806 was based on a comprehensive study of protein-ligand interactions, which guided the identification and design of novel symmetrical N,N'-disubstituted aminoureas and thioureas. (S)-BMS-378806, synthesized in aqueous media using microwave irradiation, was validated for its inhibitoryactivity in HIV-1 gp120-CD4 capture ELISA .
tHGA is a compound with anti-inflammatory activity and has the activity to inhibit soybean 15-LOX. tHGA showed significant inhibitory effects in experiments on human leukocytes, with an IC50 value of 0.42 μM, which is close to the effect of commonly used standard NDGA. tHGA concentration-dependently inhibits the synthesis of 5-LOX products, especially the cysteine leukotriene LTC(4), with an IC50 value of 1.80 μM. and showed no cytotoxicity. The anti-inflammatory effects of tHGA do not appear to be through redox or metal chelation mechanisms, as the compound was negative in these bioactivity tests. tHGA works through a dual LOX/COX inhibition mechanism and has higher selectivity for 5-LOX and COX-2, with an IC50 value of 0.40 μM .
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinaseinhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitoryactivity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinaseinhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitoryactivity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
CJ-2360 is a potent and orally active ALKinhibitor with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitoryactivity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated .
3-O-β-D-Glucopyranosyl(1→2)-[a-Lrhamnopyranosyl(1→3)]-β-D-glucopyranosyl 28-O-β-D-glucuronopyranoside, a saponin, is isolated from Polaskia chichipe Backbg. 3-O-β-D-Glucopyranosyl(1→2)-[a-Lrhamnopyranosyl(1→3)]-β-D-glucopyranosyl 28-O-β-D-glucuronopyranoside shows ability to inhibit melanin biosynthesis by B16 melanoma cell with inhibitoryactivity 84.2% at 100μM[1].
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitoryactivity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
Influenza virus-IN-4 (compound 11e) is a potent influenza virus neuraminidaseinhibitor with IC50s of 3.4, 0.094, 0.79, 0.077 µM for H5N1, H5N2, H5N6, H5N8, respectively. Influenza virus-IN-4 shows NA (neuraminidase enzyme)-inhibitoryactivity. Influenza virus-IN-4 shows low cytotoxicity with an CC50 of >200 µM. Influenza virus-IN-4 shows no obvious toxicity at the dose of 1500 mg/kg in mice .
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitoryactivity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitoryactivities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD) .
ZLMT-12 (compound 35), tacrine derivatives, is a potent, orally active CDK2/9inhibitor with IC50 values of 0.002 and 0.011 μM for CDK9 and CDK2, respectively. ZLMT-12 has a weak inhibitory effect on AChE (IC50=19.023 μM) and BChE (IC50=2.768 μM). ZLMT-12 has low toxicity and antiproliferative activity. ZLMT-12 induces apoptosis and arrests the cell cycle in the S phase and G2/M phase .
SARS-CoV-2 3CLpro-IN-5 is a covalent inhibitor of 3C-like protease (3CL pro). SARS-CoV-2 3CLpro-IN-5 has inhibitoryactivity for 3CL pro with an IC50 value of 3.8 nM. SARS-CoV-2 3CLpro-IN-5 has 9.0% oral bioavailability (BA). SARS-CoV-2 3CLpro-IN-5 can be used for the research of coronavirus disease 2019 (COVID-19) .
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitoryactivity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
DAP-81 is an inhibitory agent targeting Polo-like kinases (Plks), a class of evolutionarily conserved serine/threonine kinases. DAP-81 dose-dependently increases the number of monopolar spindles in treated cells. High-resolution live-cell microscopy revealed that Plk activity is required for the assembly and maintenance of bipolar mitotic spindles. Plk inhibition destabilizes centromeric microtubules while stabilizing other spindle microtubules, leading to the formation of monopolar spindles. Further testing of compounds based on "privileged scaffolds" such as the DAP scaffold may lead to the discovery of new cell division probes and anti-microtubule agents.
CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitoryactivity. Studies have found that the inhibitoractivity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
c-Met-IN-10 (compound 26a) is a highly potent c-Met kinaseinhibitor with an IC50 value of 16 nM. c-Met-IN-10 has inhibitoryactivity against cancer cells A549, H460 and HT-29 with IC50s of 0.56 ~ 1.59 μM. c-Met-IN-10 suppresses the colony formation on HT-29 cells, induces HT-29 and A549 cells apoptosis, and inhibits A549 cells motility. c-Met-IN-10 can be used for researching anticancer .
SARS-CoV-2-IN-34 (S-20-1) is a blood brain barrier penetrable pan-coronavirus (CoV) fusioninhibitor with broad-spectrum inhibitoryactivity. SARS-CoV-2-IN-34 effectively inhibits infection by pseudotyped and authentic SARS-CoV-2, and pseudotyped variants of concern (VOCs). SARS-CoV-2-IN-34 shows high affinity to RBD in S1 and HR1 domain in S2 of SARS-CoV-2 S protein. SARS-CoV-2-IN-34 can be used for the research of infection .
1,3,5-Trihydroxy-4-prenylxanthone is a Na +/H + exchange system (Na+/H+ Exchanger (NHE)) inhibitor with a minimum inhibitory concentration of 10 μg/mL . 1,3,5-Trihydroxy-4-prenylxanthone is a phosphodiesterase type 5 (PDE5) (Phosphodiesterase (PDE)) inhibitor with an IC50 value of 3.0 μM . 1,3,5-Trihydroxy-4-prenylxanthone inhibits Lipopolysaccharide (LPS) (Lipopolysaccharides (HY-D1056))-induced NO production in RAW264.7 macrophages, and has anti-inflammatory activities .
TLR7/8/9 antagonist 2 is an orally active TLR7/8/9 antagonist. TLR7/8/9 antagonist 2 has inhibitoryactivities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50 values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis .
EGFR-IN-90 (compound 34) is an orally active EGFRinhibitor. EGFR-IN-90 shows inhibitoryactivity against EGFRL858R/T790M/C797S with an IC50 of 5.1 nM and inhibits the proliferation of the H1975-TM cell line harboring EGFRL858R/T790M/C797S with an IC50 of 0.05 μM. EGFR-IN-90 and inhibits tumor growth in the H1975-TM xenograft tumor model .
PHI-101 is an orally active FLT3 inhibitor that overcomes resistance to multiple drug-resistant mutations. PHI-101 potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitoryactivity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. PHI-101 has potential for research in relapsed or refractory acute myeloid leukemia (AML) .
Axl-IN-18 (compound 25c) is a potent and selective type II AXLinhibitor. Axl-IN-18 shows excellent AXL inhibitoryactivity (IC50=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC50=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model .
3-O-6-Deoxy-3-O-methyl-β-D-allopyranosyl-(1→4)-β-D-oleandropyranosyl-tenacigenin C can be isolated from Alocasia cucullata (Lour.) G. Don. 3-O-6-Deoxy-3-O-methyl-β-D-allopyranosyl-(1→4)-β-D-oleandropyranosyl-tenacigenin C has moderate tumor cells inhibitoryactivity against MGC-803 and HT-29 cells with IC50 values of 45.6 and 28.4 μg/mL, respectively .
Norquetiapine is an antidepressant and neuroprotective agent and is the active metabolic component of Quetiapine (HY-14544). Norquetiapine is also a partial 5-HT1A receptor agonist, and a presynaptic α2, 5-HT2C and 5-HT7 b> Receptor antagonist. Norquetiapine can also selectively inhibit norepinephrine transporter (NET), inhibit norepinephrine reuptake, and has potential inhibitory effects on bipolar depression, major depressive disorder, and generalized anxiety disorder. Norquetiapine demonstrated in vivo activity in forced swimming in mice and learned helplessness tests in rats .
AA-57 is an acidic lipophilic antibiotic isolated from the fermentation broth of Actinomycetes strain AA-57. The AA-57 strain was isolated from a soil sample collected in Koriyama City, Fukushima Prefecture, Japan. AA-57 has antibacterial properties against Gram-positive bacteria, Gram-negative bacteria, and acid-fast bacteria. AA-57 was discovered by screening actinomycete cultures for antibacterial properties. AA-57 exhibits significant antibacterial activity and has inhibitory effects against a variety of bacteria. The discovery of AA-57 provides new possibilities for antibacterial therapy.
Madecassoside (Standard) is the analytical standard of Madecassoside. This product is intended for research and analytical applications. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects.
Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibitsactivities of p38 MAPK and NF-kB , exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity[10]. Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.
L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (Ki) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RTactivity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .
PD-1/PD-L1-IN-51 (Compound III-4) is a PD-1/PD-L1inhibitor (IC50: 2.9 nM for hPD-L1). PD-1/PD-L1-IN-51 directly binds to PD-L1 to block the interaction between PD-1/PD-L1 and enhances IFN-γ release. PD-1/PD-L1-IN-51 has tumor inhibitoryactivity .
TOP1210 is a narrow-spectrum tyrosine kinase inhibitor with potent inhibitoryactivity against P38α, Src, and Syk kinases. TOP1210 effectively reduced proinflammatory cytokines released by peripheral blood monocytes, primary macrophages, HT29 cells, inflammatory cells in ulcerative colitis (UC) biopsies, and myofibroblasts isolated from inflamed colonic UC mucosa. TOP1210 showed significant anti-inflammatory effects in cell experiments and UC biopsies, superior to some selective kinase inhibitors. The multi-kinase inhibition of TOP1210 provides the possibility of obtaining a wider range of therapeutic effects, especially in the regulation of autoimmune responses .
Mequitamium iodide (LG 30435) is an antihistamine drug with antiallergic and bronchodilatory activity. Mequitamium iodide can effectively antagonize airway contraction and inflammatory responses induced by histamine and antigens. Mequitamium iodide has nanomolar affinity for the H1 and smooth muscle receptors of histamine and mequitin. Mequitamium iodide, when administered in aerosol form, significantly inhibits histamine- and antigen-induced increases in airway pressure in allergic mice. Mequitamium iodide reduces antigen-induced eosinophil accumulation in the airways. Mequitamium iodide also exhibits inhibitory effects on PAF-induced platelet aggregation and bronchoconstriction, and can be used in the study of allergic diseases such as rhinitis and asthma .
DHFR-IN-22 (Compound 8) is a DHFR (Dihydrofolate Reductase)inhibitor belonging to the class of 2,4-diaminopyrimidine compounds. DHFR-IN-22 exhibits significant inhibitoryactivity against purified DHFR enzyme and major species of nontuberculous mycobacteria (NTM), namely Mycobacterium avium and Mycobacterium abscessus. It shows an IC50 of 1.1 nM and MIC of 1.5 μg/mL against M. abscessus, and an IC50 of 6.3 nM and MIC of 0.1 μg/mL against M. avium. Additionally, it demonstrates an IC50 of 2100 nM against human DHFR. DHFR-IN-22 holds potential for studying novel strategies to combat NTM infections .
(3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid, a lanostane triterpenoids, exhibits obvious NO inhibitoryactivity on n LPS-induced BV-2 microglia cells with an IC50 of 9.55 uM. (3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid has anti-inflammatory activities .
RdRP-IN-4 (compound 11q), an aryl benzoyl hydrazide analog, is an orally active influenza A virus RNA-dependent RNA polymerase (RdRp)inhibitor by interacting with the PB1 subunit. RdRP-IN-4 exhibits potent inhibitoryactivity against the avian H5N1 flu strain with an EC50 of 18 nM in MDCK cells. RdRP-IN-4 displays excellent potency against the the H1N1 (A/PR/8/34) Flu A strain and Flu B strain (B/Lee/1940) with EC50 values of 53 nM and 20 nM, respectively. RdRP-IN-4 significantly inhibits the expression level of viral nucleoprotein (NP) in a dose-dependent manner. RdRP-IN-4 exhibits significant antiviral activity in infected mice .
R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .
H2-005 is a compound that selectively inhibits diacylglycerol acyltransferase 2 (DGAT2) and has the activity to inhibit triacylglycerol synthesis in hepatocytes and preadipocytes. H2-005 significantly reduces triacylglycerol biosynthesis in HepG2 hepatocytes and 3T3-L1 preadipocytes. H2-005 exhibits specific inhibitoryactivity in DGAT2-overexpressing HEK293 cells. H2-005 almost completely inhibits lipid droplet formation in 3T3-L1 cells when co-treated with a DGAT1 inhibitor. H2-005 will contribute to DGAT2-related lipid metabolism research and the development of drugs to inhibit metabolic diseases .
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
ML339 is a selective CXCR6 antagonist with an IC50 of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC50 of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC50 of 18 μM. ML339 has no inhibitory effect on CXCR5，CXCR4，CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research .
TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK G595RIC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control agent LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line .
PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1inhibitor, with an IC50 of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitoryactivity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase .
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
Antileishmanial agent-22 (compound 15b) is a parasite inhibitor and an antibacterial agent, with antileishmanial, antimalarial, and anti-tubercular activities. Antileishmanial agent-22 inhibits leishmanial (IC50=0.408 μM) based on antifolate mechanism. And, Antileishmanial agent-22 inhibits Folic acid and Folinic acid at 100 μM with inhibitory rates of 88% and 94%, respectively. Antileishmanial agent-22 inhibits P. berghei in vivo and in vitro, with 96.67% suppression under 48.4 μM/kg/day and 0.038 μM (IC50), respectively. Moreover, Antileishmanial agent-22 inhibits M. tuberculosis with MIC of 28.44 μM .
Almonertinib (Standard) is the analytical standard of Almonertinib. This product is intended for research and analytical applications. Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinaseinhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitoryactivity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
HDAC6-IN-49 (Compound 3) is an inhibitor for HDAC with IC50 of 0.012 and 0.735 μM for HDAC6 and HDAC1. HDAC6-IN-49 also exhibits inhibitoryactivities against MAO-B, cholinesterase (ChE), histamine receptor (H3R) and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective efficacy on SH-SY5Y cell. HDAC6-IN-49 improves cognitive function and locomotor ability in Drosophila Parkinson's disease models and in C. elegans Alzheimer's disease models .
Aspergillomarasmine A is a natural aminopolycarboxylic acid with potent inhibitoryactivity against class B metallo-β-lactamases (MBLs). Aspergillomarasmine A inactivates MBLs by removing a catalytic Zn2+ cofactor. Aspergillomarasmine A acts as a selective Zn2+ scavenger, promoting the dissociation of the metal cofactor, thereby indirectly inactivating NDM-1. Aspergillomarasmine A causes the loss of Zn2+ ions from the low-affinity binding site of NDM-1. The action of Aspergillomarasmine A results in the rapid degradation of Zn2+-deficient NDM-1, thereby enhancing its potency as a β-lactam enhancer. The mechanism of Aspergillomarasmine A has broad applicability among different Zn2+ chelators .
IRAK4-IN-29 is an IRAK4 inhibitor with good selectivity and low nanomolar activity. IRAK4-IN-29 can effectively block the TLR-mediated signal transduction pathway. IRAK4-IN-29 showed significant inhibitory effects in LPS- and R848-induced cytokine experiments. IRAK4-IN-29 can inhibit LPS-induced TNFα in an in vivo model, showing a similar phenotype to IRAK4 gene-deficient mice. IRAK4-IN-29 has good medicinal chemical properties, such as microsomal stability and solubility, showing potential clinical application value .
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitoryactivity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS .
PI3K-IN-28 (Compound 6c) is a potent inhibitor of PI3K. PI3K-IN-28 displays the most potent activity with lower toxic effects on MCF-10a. PI3K-IN-28 displays half-maximal inhibitory concentration (IC50, μM) values of 5.8, 2.3, and 7.9. PI3K-IN-28 is the most potent one with a selectivity index (SI) of 39 and is considered as a latent lead for further optimization of anticancer agents .
1 a /5-hydroxynitrile rubber 7 receptor antagonist (5-HT1 a k i = 8 nm, kb= 0.04 nm; 5-nitrile rubber 7K I = 451 nm, kb= 460 nm) has pde4b/pde7a inhibitoryactivity (PDE4B ic50= 80.4 μ M; Pde7a chip 50= 151.3 μ M）。 Compound 22 has a very good ability of passive penetration of biofilm and high metabolic stability in vitro. In addition, 22's pharmacological evaluation showed its pre cognitive and antidepressant properties in rat behavioral tests.
HDAC-IN-73 (compound P-503) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-73 shows IC50s values of 0.17, 0.49 µM for HDAC1 and HDAC6, respectively. Notably, HDAC-IN-73's inhibitory potency against HDAC6 is heightened, exhibiting a 9-fold greater efficacy than PsA (HY-N2150) (IC50=3.9 μM). HDAC-IN-73 shows potent antiproliferative activity, induces apoptosis, and causes cell cycle arrest at G2 / M phase. HDAC-IN-73 has the potential to be used for the research of cancer such as colon cancer .
EGFR-IN-117 (Compound 8h) exhibits inhibitoryactivity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR L858R/T790M/C797S and BaF3– C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models .
4,5-Dicaffeoylquinic acid (Standard) is the analytical standard of 4,5-Dicaffeoylquinic acid. This product is intended for research and analytical applications. 4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) is an antioxidant, can be isolated from Gynura divaricata and Laggera alata. 4,5-Dicaffeoylquinic acid reduces islet cell apoptosis and improves pancreatic function in type 2 diabetic mice, and has obvious inhibitoryactivities against yeast α-glucosidase. 4,5-Dicaffeoylquinic acid inhibits prostate cancer cells through cell cycle arrest. 4,5-Dicaffeoylquinic acid also has anti-apoptotic, anti-injury and anti-hepatitis B virus effects .
Neuroprotective agent 5 (compound 28) is a brain permeabilizing agent with anti-neuritis, anti-oxidative damage and neuroprotective effects. Neuroprotective agent 5 exhibits a potent NO inhibitory effect (EC50=0.49 μM), inhibits the release of proinflammatory factors PGE2 and TNF-α, downregulates the expression of iNOS and COX-2 proteins, and promotes the polarization of BV-2 cells from the proinflammatory M1 phenotype to the anti-inflammatory M2 phenotype. In addition, Neuroprotective agent 5 can also inhibit acetylcholinesterase (AChE) activity and Aβ42 aggregation in a dose-dependent manner. Neuroprotective agent 5 can be used for the study of Alzheimer's disease .
(5aS,6R,6aR)-MK-8666 is a selective GPR40 agonist with activity in promoting fatty acid-induced insulin secretion in pancreatic β cells and intestinal enteroendocrine cells. (5aS,6R,6aR)-MK-8666 has been studied for the inhibition of type 2 diabetes and has shown significant blood glucose lowering effects. Although (5aS,6R,6aR)-MK-8666 is considered to have potential inhibitory advantages, its development was stopped in Phase I clinical trials due to liver safety issues .
4-Methoxyphenyl isothiocyanate (4-Methylphenyl ITC) is an antioxidant, with a IC50 value of 1.25 mM for scavenging DPPH radicals. ORAC testing indicates its antioxidant capacity as 11.7 mM TE (indicating that the antioxidant efficacy of this compound is equivalent to 11.7 mmol of Trolox (HY-101445, a standard antioxidant) under the same conditions), and it extends the oxidation process by approximately 9180 seconds in the Briggs–Rauscher reaction. Additionally, 4-Methoxyphenyl isothiocyanate exhibits moderate cholinesterase inhibitoryactivity, with an inhibition rate of 30.4% against acetylcholinesterase (AChE) and 17.9% against butyrylcholinesterase (BChE). 4-Methoxyphenyl isothiocyanate holds potential for research in the fields of antioxidation and neurological disorders .
Lornoxicam (Chlortenoxicam) is an orally active oxycontin nonsteroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory, antipyretic and anticancer activities. Lornoxicam exhibits good inhibitory effects on both COX-1 and COX-2 (COX-1: IC50=0.005 μM; COX-2:IC50=0.008 μM) and inhibits the production of NO by iNOS (IC50=65 μM) and the proinflammatory cytokine IL-6 (IC50=54 μM). Lornoxicam also inhibits tumor cell proliferation and migration and induces tumor cell apoptosis. Lornoxicam can be used in the study of inflammatory pain, colorectal cancer and breast cancer .
CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitoryactivities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis .
P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 with antiplatelet activity. P2Y1/P2Y12 antagonist-1 inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. P2Y1/P2Y12 antagonist-1 exhibits potent inhibitory effects in rat thrombosis model.
Lobaric acid is a depsipeptide metabolite isolated from Stereocaulon lichen with antioxidant, antiproliferative, antiviral and enzyme inhibitoryactivities. Lobaric acid scavenges superoxide free radicals (IC50=97.9 μM) and inhibits cancer cell proliferation (EC50 of 15.2-63.9 μg/mL against leukemia, colorectal, gastric, breast, ovarian, prostate, pancreatic and lung cancer cell lines). Lobaric acid inhibits protein tyrosine phosphatase 1B (PTP1B; IC50=0.87 μM for human recombinant enzyme) and 12(S)-HETE produced by 12(S)-lipoxygenase (IC50=28.5 μM). Lobaric acid (250 μM) also reduced pathological changes in tobacco leaves infected with tobacco mosaic virus (TMV).
Dihydroberberine (Standard) is the analytical standard of Dihydroberberine. This product is intended for research and analytical applications. Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
SJ-C1044 is an orally available pan-RAFinhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibitswild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibitingkras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
(15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one shows a 5a-reductaseinhibitoryactivity with an IC50 value of 41.9 μM. (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one inhibits the growth of the ventral prostate induced by testosterone in rat. (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one is promising for research of benign prostatic hyperplasia (BPH) as well as other 5α-dihydrotestosterone (DHT)-related disorders, such as acne and male pattern baldness .
CAP-53194 is a selective Plk1 inhibitor with potential anticancer activity. CAP-53194 was identified by a high-throughput virtual screening approach using molecular docking, showing 100-fold selectivity for Plk1 over Plk2-4 and other cell cycle kinases. CAP-53194 is able to effectively exploit subtle differences between the binding sites of Plk1 and other Ser/Thr kinases, thereby enhancing their inhibitory effects. CAP-53194 meets the Lipinski compound analog criteria and passes other ADMET filters, indicating good compound compatibility. CAP-53194 belongs to a new class of potential Plk1 inhibitors suitable for subsequent compound development and testing .
CS-003 is a triple neurokinin receptor antagonist with activity in inhibiting neurokinin-related respiratory diseases. CS-003 exhibits high affinity for human neurokinin 1, 2 and 3 receptors, withKi values of 2.3 nM, 0.54 nM and 0.74 nM respectively. The Ki values of CS-003 on the guinea pig neurokinin receptor are 5.2 nM, 0.47 nM and 0.71 nM respectively, showing superior inhibitory effect. CS-003 significantly inhibits the formation of inositol phosphate involving substance P, neurokinin A and neurokinin B through competitive antagonism. CS-003 significantly inhibits citric acid-induced cough, and its effect is better than other selective neurokinin receptor antagonists .
PI3K/Akt/mTOR-IN-3 (compound 3d) is a potent PI3K/AKT/mTORinhibitor. PI3K/Akt/mTOR-IN-3 displays the inhibitoryactivity in MCF-7, HeLa and HepG2 cells, with IC50 values of 0.77, 1.23, and 4.57μM, respectively. PI3K/Akt/mTOR-IN-3 inhibits the migration of MCF-7 and HeLa cells at the concentration of 4 μM. PI3K/Akt/mTOR-IN-3 induces cell apoptosis and S phase arrest .
AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitoryactivity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD) .
2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid, a natural ursane-type triterpene, is a potent inhibitor of HIV protease (HIV Protease). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid is also an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid displays an inhibitoryactivity against nitric oxide production in Lipopolysaccharide (Lipopolysaccharides)-activated RAW 264.7 cells .
Poly (I:C):Kanamycin (1:1) sodium is an isometric complex of Poly (I:C) (HY-135748) and Kanamycin (HY-16566). Poly(I:C) sodium, a synthetic analog of double-stranded RNA, is a TLR3 and retinoic acid-inducible gene I receptor (RIG-I and b>MDA5) agonist. Poly(I:C) sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses and induce apoptosis in cancer cells . Kanamycin is an orally active antibacterial agent (Gram-negative/positive bacteria) that inhibits translocation and causes miscoding by binding to the 70S ribosomal subunit. Kanamycin shows good inhibitoryactivity against Mycobacterium tuberculosis (susceptible and drug-resistant) and Klebsiella pneumoniae, and can be used in the research of tuberculosis and pneumonia .
Epsilon-V1-2, Cys-conjugated is a biological active peptide. (This peptide is the εPKC specific inhibitor. Its inhibitoryactivity is based on εPKC translocation and MARCKS phosphorylation. This peptide interferes with εPKC interaction with the anchoring protein εRACK. This peptide contains a cysteine residue added to the C-terminus for potential S-S bond formation with a carrier protein.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
HMGB1-IN-2 (compound 15) is an inhibitor of highly conserved nuclear protein (HMGB1), showing NO inhibitory effect with IC50 value of 20.2 μM in RAW264.7 cells. HMGB1-IN-2 (30 μM) decreases the level of IL-1 β, TNF-α, caspase-1 p20, inhibits the phosphorylation of NF-κB p65, exhibits anti-apoptotic activity. HMGB1-IN-2 (15 mg/kg; ip) relives kidney injury in septic acute kidney injury mouse. HMGB1-IN-2 inhibits Huh7 cells and A549 cells with IC50s of 77.0 μM, and 82.0 μM, respectively .
EGFR-IN-97 (compound 6q) is a EGFRinhibitor. EGFR-IN-97 shows inhibitoryactivity against Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, with IC50 values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR L858R/T790M/C797S cells at the concentration of 0.8 μM .
1-Formyl-beta-carboline is an alkaloid with inhibitoryactivity against Newcastle disease virus (NDV). 1-Formyl-beta-carboline can effectively inhibit different genotypes of NDV with IC50 values within 10 μM, and its inhibition rate is more than 90% at a concentration of 20 μM. 1-Formyl-beta-carboline mainly exerts its effects by inhibiting the adsorption and entry processes in the NDV life cycle. 1-Formyl-beta-carboline has been identified as a novel HN inhibitor that can directly interact with the NDV HN protein and affect the adsorption of NDV. 1-Formyl-beta-carboline also inhibits the entry of NDV by inhibiting the PI3K/Akt signaling pathway rather than the ERK pathway .
Meridianin C is a marine natural product with anticancer activity. Meridianin C has significant inhibitory effects on four different human tongue cancer cells (YD-8, YD-10B, YD-38 and HSC-3). Meridianin C most strongly reduced the growth of YD-10B cells, the most aggressive and tumorigenic of the cell lines tested. Meridianin C also induced significant accumulation of large vesicles in YD-10B cells, validating its function through macrophagocytosis. Meridianin C reduces cellular levels of Dickkopf-related protein-3 (DKK-3), a known negative regulator of macrophagy. Meridianin C affects macrophagocytosis by downregulating DKK-3, thereby affecting cell proliferation .
Cuminaldehyde (Standard) is the analytical standard of Cuminaldehyde. This product is intended for research and analytical applications. Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC50= 0.00085 mg/mL) and α-glucosidase (IC50=0.5 mg/mL). Cuminaldehyde can modulate α-synuclein fibrils. Cuminaldehyde can induce apoptosis in colon adenocarcinoma cells by targeting topoisomerase I and II. In addition, Cuminaldehyde also exerts anti-inflammatory activity by inhibiting lipoxygenase. Cuminaldehyde has a strong inhibitory effect on the growth of Aspergillus flavus and the biosynthesis of aflatoxin B1 (AFB1). Cuminaldehyde can exert anti-injury and anti-neuropathy effects by participating in opioid receptors, L-arginine/NO/cGMP pathways and anti-inflammatory effects. Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases .
7,3',4'-Trihydroxy-3-benzyl-2H-chromene is an reversible noncompetitive neuraminidase (NA)inhibitor. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be isolated from the dried heartwood of Caesalpinia sappan L. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene has potent NAs inhibitoryactivities with IC50 values of 34.6 µM [H1N1], 39.5 µM [H3N2], and 50.5µM [H9N2], respectively. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be used for the research of influenza virus .
Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, iNOS, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
PD-L1 degrader-2 (Compound B3) is an orally active AUTAC degrader, that degrades PD-L1 through autophagy-lysosome pathway with a DC50 of 0.5 μM. PD-L1 degrader-2 exhibits inhibitoryactivity against PD-1/PD-L1 interaction with an IC50 of 22.8 nM. PD-L1 degrader-2 upregulates the expressions of Atg9b, Lamp1 and Mitf, and activates the autophagy lysosome system. PD-L1 degrader- exhibits antitumor efficacy in CT26 mouse model . (Pink: autophagy-lysosome activator (HY-159894); Black: linker (HY-W015088); Blue: PD-L1 ligand (HY-169365))
I-A09 and its derivatives, specifically 1,2,3-triazole-adamantylacetamide hybrids (5a–u), exhibit significant antitubercular activity. These hybrids were synthesized using copper-catalyzed click chemistry, combining bioactive fragments from antitubercular I-A09 and substituted adamantyl urea. The compound N-(1-adamantyl)-2-azido acetamide was reacted with various alkyl/aryl acetylenes to produce new analogues. Among them, N-(1-adamantan-1-yl)-2-(4-(phenanthren-2-yl)-1H-1,2,3-triazol-1-yl)acetamide (5t) showed the most promise with a minimum inhibitory concentration (MIC) of 3.12 μg/mL against Mycobacterium tuberculosis H37Rv, and a selectivity index greater than 15 .
SQ 31844 is a novel renin inhibitor belonging to the imidazolidinol class. This compound, which contains an imidazole ring in its active site binding group, has potent in vitro inhibition of primate renin, but not rat, pig, or dog renin. In conscious, sodium-deprived cynomolgus monkeys, both compounds produced dose-related inhibition of plasma renin activity (PRA) over a dose range of 0.001 to 1.0 μmol/kg, administered intravenously, with complete inhibition observed at the highest dose. However, a reduction in blood pressure was only observed when 10 μmol/kg was administered intravenously or by infusion. In sodium-replete monkeys, SQ 30774 inhibited the increase in arterial blood pressure and PRA following administration of exogenous monkey renin. When the compounds were administered orally at 50 μmol/kg, only SQ 31844 significantly inhibited PRA (80%). In summary, the imidazolidinol renin inhibitors have potent inhibitory effects on renin in vitro and inhibit PRA and reduce arterial blood pressure in vivo.
(R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitoryactivity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
Ferroptosis is a novel type of cell death program that is distinct from apoptosis, necroptosis and autophagy. It is dependent on iron and reactive oxygen species (ROS) and is characterized by lipid peroxidation. As a novel type of cell death, ferroptosis has distinct properties and recognizing functions involved in physical conditions or various diseases including cancers, neurodegenerative diseases, acute renal failure, etc.
MCE carefully collected a unique collection of 1,053 ferroptosis signaling pathway related compounds with ferroptosis-inducing or -inhibitoryactivity. MCE Ferroptosis Compound Library is a useful tool to study ferroptosis mechanism as well as related diseases.
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA) is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA ) TFA is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA TFA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
SHP1-IN-1 (compound 5p) is a fluorescent probe for the protein tyrosine phosphatase SHP1 containing the Src homology 2 domain. SHP1-IN-1 has SHP1 inhibitoryactivity, selectivity for Fe 3+ ions and good fluorescence properties. SHP1-IN-1 exhibits aggregation post-quenching (ACQ) effect, good interference immunity and low detection limit (5.55 μM) .
Cholesteryl n-butyrate is a cholesterol ester composed of cholesterol and butyrate, two naturally occurring substances. Cholesteryl n-butyrate can be used to synthesize solid lipid nanoparticles (SLNs) with inhibitoryactivity on the adhesion and migration of colon cancer cells, providing a delivery system for the anticancer drug butyrate .
Human serum albumin (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, NF-κB, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) (HSA) is the most abundant protein in plasma and is a major determinant of plasma oncotic pressure. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) exhibits antioxidant, anticoagulant, anti-inflammatory, anti-platelet aggregation activities as well as colloid osmotic action. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) can block the inhibitory effect of GML on human T cells, providing protective function for T cells. Human serum albumin (Cell culture grade, Endotoxin<0.125 EU/mg) is also associated with cardiovascular diseases and can partially prevent the LPS (HY-D1056) induced oxidative stress, as well as the upregulation of NF-κB, iNOS, and peroxynitrite (ONOO −) in the vascular wall, contributing to the reduction of blood pressure .
Pisiferic acid is an antibacterial agent with inhibitoryactivity against Gram-negative/positive bacteria such as P. vulgaris, S. aureus and B. subtilis. Pisiferic acid can be used to study bacterial infections .
Trospectomycin dihydrochloride is a spectinomycin analogue with anti-Chlamydia trachomatis activity. Trospectomycin dihydrochloride can be used as an effective inhibitory option to help fight related infections. Trospectomycin dihydrochloride has shown significant potential for clinical application.
Betamethasone 17-Propionate is a compound used to study its effects on endotoxin-induced uveitis in rats. It has the activity of inhibiting the infiltration of cells into the aqueous humor in endotoxin-induced uveitis by eye drops and systemic administration at a certain dose. However, its inhibitory effect is relatively weak compared with some other compounds. At the same time, the dose for systemic administration is 1mg/kg. In addition, Betamethasone 17-Propionate has a weaker inhibitory effect on the release of IL-8 from rat peritoneal exudate cells in an in vitro interleukin-8 (IL-8) release assay than betamethasone. Moreover, the simultaneous addition of betamethasone dipropionate and betamethasone 17-Propionate reduces the inhibitory effect of betamethasone on cell infiltration and IL-1β gene expression.
4-Methylumbelliferyl β-D-mannopyranoside is a substrate that exhibits β-mannosidase activity. 4-Methylumbelliferyl β-D-mannopyranoside can be used to study β-mannosidase deficiency. The reactivity of 4-Methylumbelliferyl β-D-mannopyranoside shows different inhibitory effects on various substrates.
Isothiazole-5-carboxylic acid (8-Isoquinoline-methaneaminedihydrochloride) is an organic compound with antibacterial, anticancer and anti-inflammatory properties. Isothiazole-5-carboxylic acid can be used to develop novel compounds to combat various diseases. Isothiazole-5-carboxylic acid exhibits a wide range of potential pharmacological activities and helps improve existing inhibitory schemes.
5'-Ethylcarboxamido-2',3'-isopropylidene adenosine is an adenosine receptor agonist that promotes the activity of A2B adenosine receptors. 5'-Ethylcarboxamido-2',3'-isopropylidene adenosine can be used to study the role of adenosine in physiological processes. 5'-Ethylcarboxamido-2',3'-isopropylidene adenosine is used as a potential inhibitory target in compound development.
Phenyl(9H-purin-6-yl)amine is an antibacterial compound with the activity of inhibiting bacterial growth. The application of phenyl(9H-purin-6-yl)amine can be used to develop new antibacterial compounds. Phenyl(9H-purin-6-yl)amine has shown potential inhibitory effects in medical research.
Fusion Inhibitory Peptide (Z-D-Phe-Phe-Gly-OH, FIP, Virus Replication Inhibitory Peptide) is a potent inhibitor of the virus replication, by inhibiting the membrane fusing activity of a viral glycoprotein .
Bradykinin potentiator B (Bradykinin potentiating peptide B) is venom of Agkistrodon halys blomhoffi. Bradykinin potentiator B is a potent ACEinhibitor. Bradykinin potentiator inhibits the activity of bradykinin inhibitory peptidase .
Gastric Inhibitory Polypeptide (1-30), porcine lacks the C-terminal 12 amino acid residues of natural gastric inhibitory polypeptide (GIP), exhibits biologic activity by potentiating the release of insulin and somatostatin .
Polyphemusin II-Derived Peptide (T140), a CXCR4inhibitor, shows high inhibitoryactivity against HIV-1 entry and the inhibitory effect on the binding of an anti-CXCR4 monoclonal antibody (12G5) to CXCR4 .
Diplacol ia a natural compound from from Mimulus clevelandi and shows potent inhibitoryactivities against lipopolysaccharide (LPS)-induced nitric oxide production .
Plipastatin A1 is a lipopeptide with enzyme inhibitory and immunosuppressive activities. Plipastatin A1 is found in Bacillus cereus and inhibits phospholipase A2 (PLA2), PLC, and PLD .
TANDEM (Des-N-tetramethyltriostin A) is a synthetic antibiotic drug that has the activity of inhibiting the growth of tumor cells. TANDEM can be used in combination with chemotherapy to enhance the inhibitory effect. TANDEM has shown significant inhibitory effects on a variety of cancer cell lines in in vitro experiments. The structure of TANDEM allows it to effectively target tumor cells during the inhibition process. TANDEM's mechanism of action involves interfering with cell proliferation and survival pathways .
BMAP-27 is an antimicrobial peptide capable of disrupting the membrane integrity of microorganisms. Due to its membrane permeability, MAP-27 has inhibitoryactivity against both bacteria and cancer cells .
Low molecular weight protamine is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitoryactivity. Low molecular weight protamine can inhibit tumor growth and is used in cancer research .
Fmoc-D-Thi-OH (Fmoc-D-2-Thienylalanine) is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize AS-Z-P with thrombin inhibitoryactivity .
Fmoc-5-Ava-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize fatty acid-based dimeric peptides with PSD-95 inhibitoryactivity .
ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity .
Fmoc-Phe(4-tBu)-OH is an amino acid derivative with an Fmoc protecting group, which can be used to synthesize rOicPaPhe(p-Me)-NH(2) with platelet aggregation activation inhibitoryactivity .
BRC4wt (BRC4 repeat motif) is part of the BRACA2 tumor suppressor protein, which exhibits inhibitoryactivity against interaction of the BRACA2 protein with RAD51, and is involved in the repair of DNA damage .
CRAMP-18 (mouse) is an antibiotic peptide without hemolytic activity. CRAMP-18 (mouse) has good inhibitoryactivity against Gram-negative bacteria, such as S. typhimurium and P. aeruginosa. CRAMP-18 (mouse) has the potential to study antifungal, antibacterial and antitumor .
Macropin (MAC-1 peptide) is an antimicrobial peptide found in the venom of the solitary bee Macropis fulvipes. Macropin has antibacterial activity against both Gram-positive and Gram-negative bacteria, and also exhibits inhibitoryactivity against fungi and moderate hemolytic activity against human erythrocytes. Macropin can be used in research on anti-infective therapy .
Epitalon is an anti-aging agent and a telomerase activator. Epitalon has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon can be used for cancer, old age and Retinitis Pigmentosa .
Dodecapeptide AR71 is an inhibitor of melanoma inhibitoryactivity (MIA). Dodecapeptide AR71 can reduce cell migration, reduce metastasis formation, and increase immune response. Dodecapeptide AR71 can be used in research on the treatment of malignant melanoma .
KWWCRW is a Holliday linker inhibitory peptide with anticancer activity. KWWCRW inhibits homologous recombination repair (HDR) during DNA repair by binding to the reactive Holliday linker intermediate and preventing its degradation, and inhibits site-specific recombination by bacteriophage in vitro .
Hp1404 is a novel cationic antimicrobial peptide. Hp1404 has specific inhibitoryactivity against Gram-positive bacteria, including Staphylococcus aureus (MRSA) resistant to Laburnetin (HY-N7382). Hp1404 has antimicrobial activity, low toxicity, and is not prone to drug resistance, and can be used in the research of antimicrobial agents .
Cyclo(-Met-Pro) is a cyclic dipeptide consisting of the amino acids methionine and proline. Cyclo(-Met-Pro) exhibits weak inhibitoryactivity against the influenza A virus (H3N2) (5 mM, 2.1% inhibition), while cis-cyclo(Leu-Pro) and cis-cyclo(Phe-Pro) shows significant antiviral activity .
Epitalon TFA is an anti-aging agent and a telomerase activator. Epitalon TFA has an inhibitory effect of the on the development of spontaneous tumors in mice, has geroprotective actions and intranasal administration increases neuronal activity. Epitalon TFA can be used for cancer, old age and Retinitis Pigmentosa .
NoxaBH3 is a cysteine-based cross-linked peptide with increased cell permeability and higher inhibitoryactivity against Mcl-1. NoxaBH3 binds to the endogenous CXCR4 ligand to produce ubiquitin-Noxabh3 conjugate. NoxaBH3 is then delivered to cancer cells .
[D-pGlu1,D-Phe2,D-NaI3,6]-Gn-RH is a gonadotropin-releasing hormone (Gn-RH) agonist that has a dose-dependent inhibitoryactivity on progesterone secretion from cultured human granulosa cells.
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA) is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
Suc-Ala-Glu-Pro-Phe-pNA (Suc-AEPF-pNA ) TFA is a chromogenic substrate for the peptidylprolyl isomerase Pin1. Suc-Ala-Glu-Pro-Phe-pNA TFA can be used to evaluate the inhibitory effect of the target compound on Pin1, and catalytic activity of Pin1, etc .
Boc-β-Ala-ol (3-(Boc-amino)-1-propanol) is an alanine derivative with a Boc protecting group at the N-terminus, which can be used to synthesize bioactive peptide mimics, such as Nα-Benzoyl-α-azaornithine phenyl ester, which has trypsin inhibitoryactivity .
Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin Bactivity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis .
SGP8 (IAVPGEVA) is an octapeptide produced by hydrolysis of soybean 11S globulin, which has the effects of regulating lipid metabolism, inflammation and fibrosis. SGP8 (IAVPGEVA) exhibits inhibitoryactivity against DPP4 and inhibits the JNK-c-Jun signaling pathway, and has the ability to inhibit non-alcoholic steatohepatitis (NASH) .
U-85548E is an HIV protease inhibitor with nanomolar affinity for HIV-1 aspartic protease. By studying its structure-activity relationship, a potent nanomolar inhibitor with inhibitory effects on both HIV-1 and HIV-2 proteases was designed, and its binding mode was studied by X-ray crystallography and molecular modeling.
Lys-[Des-Arg9]Bradykinin, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin has low inhibitoryactivity on B2 receptors .
Lys-[Des-Arg9]Bradykinin TFA, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin TFA has low inhibitoryactivity on B2 receptors .
Retro-indolicidin is a biological active peptide. (Reverse peptide of indolicidin (Rev4) is a 13-amino acid residue peptide based on the sequence of indolicidin. Indolicidin, a member of the cathelicidin protein family, is a 13-amino acid residue cationic, antimicrobial peptide-amide isolated from the cytoplasmic granules of bovine neutrophils. The synthetic peptide Rev4 has been shown to possess strong antimicrobial as well as protease inhibitoryactivities in vitro.)
[Nle20] H4 peptide (16−23) is a peptide with strong inhibitoryactivity against histone methyltransferase SETD8 (Kd=0.14 μM), which inhibitsSETD8's methylation of histone H4 by competing with SETD8's substrate binding site. [Nle20] H4 peptide (16−23) can be used as a lead compound for anticancer therapy .
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitoryactivity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
Defensin HNP-3 human is a cytotoxic antibiotic peptide known as "defensin". Defensin HNP-3 human has inhibitoryactivity against Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Defensin HNP-3 human is initially synthesized as the 94 amino acids preproHNP(1-94), which is hydrolyzed to proHNP(20-94) and converted to mature HNP(65-94) after the removal of anion precursors .
Angiotensin 1-7 (Ang-(1-7)) is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 inhibits purified canine ACEactivity (IC50=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .
Angiotensin 1-7 (Ang-(1-7)) acetate is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 acetate inhibits purified canine ACEactivity (IC50=0.65 μM). Angiotensin 1-7 acetate acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 acetate blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium .
RW3 is a small cationic hexapeptide with amphiphilic properties. RW3 targets the plasma membrane of bacteria and works by inhibiting cell respiration and cell wall synthesis. RW3 shows high biological activity against gram-positive bacteria and does not show significant cytotoxic or hemolytic effects in previous studies. RW3 quickly kills 97% of the initial colony forming units (CFU) within 10 minutes at twice the minimum inhibitory concentration (MIC). RW3 can be used in antimicrobial and antifungal studies .
[D-Ser14]-Humanin is a bioactive peptide in which the Ser14 residue of Humanin (HY-P1928) is changed from L-form to D-form. [D-Ser14]-Humanin has potent inhibitoryactivity against the fibrillation of amyloid-β. Humanin (HY-P1928) inhibits the aging-related death of various cells caused by amyloid fibrils and oxidative stress, and [D-Ser14]-Humanin has better cell protection activity than Humanin (HY-P1928). [D-Ser14]-Humanin can be used in the study of Alzheimer's disease .
SARS-CoV-2-IN-34 (S-20-1) is a blood brain barrier penetrable pan-coronavirus (CoV) fusioninhibitor with broad-spectrum inhibitoryactivity. SARS-CoV-2-IN-34 effectively inhibits infection by pseudotyped and authentic SARS-CoV-2, and pseudotyped variants of concern (VOCs). SARS-CoV-2-IN-34 shows high affinity to RBD in S1 and HR1 domain in S2 of SARS-CoV-2 S protein. SARS-CoV-2-IN-34 can be used for the research of infection .
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
Epsilon-V1-2, Cys-conjugated is a biological active peptide. (This peptide is the εPKC specific inhibitor. Its inhibitoryactivity is based on εPKC translocation and MARCKS phosphorylation. This peptide interferes with εPKC interaction with the anchoring protein εRACK. This peptide contains a cysteine residue added to the C-terminus for potential S-S bond formation with a carrier protein.Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
Cyanidin-3-O-galactoside chloride (Ideain chloride) is a component from extract peel of hawthorn fruit (EPHF) with the value of 179.4 mg/g. EPHF exhibits strong AChEinhibitoryactivity .
Schiarisanrin A (Kadsulignan J) is a lignan with inhibitoryactivity on NO production. Schiarisanrin A inhibits NO production in BV-2 cells with an IC50 of 9.6 μM .
Withanoside V (Standard) is the analytical standard of Withanoside V. This product is intended for research and analytical applications. Withanoside V, a withanolide glycoside, exhibits inhibitoryactivity for tachyphylaxis to Clonidine in isolated guinea-pig ileum .
Kadsulignan H (compound 13) is a lignan with inhibitoryactivity on NO production. Kadsulignan H inhibits NO production in BV-2 cells with an IC50 of 14.1 μM .
Methyl 4-O-caffeoylquinate is an extract naturally
derived from the leaf ofIlex paraguariensis. Methyl
4-O-caffeoylquinate has human neutrophilic elastase (HNE) inhibitoryactivity
.
Cyanidin-3-O-galactoside (chloride) (Standard) is the analytical standard of Cyanidin-3-O-galactoside (chloride). This product is intended for research and analytical applications. Cyanidin-3-O-galactoside chloride (Ideain chloride) is a component from extract peel of hawthorn fruit (EPHF) with the value of 179.4 mg/g. EPHF exhibits strong AChE inhibitoryactivity .
Danshenol B is a diterpenoid. Danshenol B has strong aldose reductase (AR) inhibitoryactivity with IC50 value of 0.042μM. Danshenol B can be used for the research of diabetic related complication resulted by metabolic abnormality, such as cataracts, retinopathy, neuropathy, and nephropathy .
Licoagrochalcone C, a flavonoid, reveals efficacious inhibitoryactivity on NF-κB transcription. Licoagrochalcone C shows significant inhibitoryactivity on LPS (HY-D1056)-induced NO production .
Artanin is a coumarin, has biological activities related to Alzheimer’s disease. Artanin exerts function including AChEinhibitory and AChE- and self-induced amyloid beta (Aβ) aggregation inhibitoryactivities, with IC50s of 51 μM, 98 μM, and 124 μM, respectively .
Calceolarioside B is a natural product isolated from Akebia quinata leaves. Calceolarioside B exhibits significant inhibitoryactivity against rat lens aldose reductase (RLAR) with an IC50 of 23.99 μM. Calceolarioside B displays inhibitory effect on DPPH radical scavenging activity with an IC50 of 94.60 μM .
Licopyranocoumarin is an isoflavonoid that shows CYP3A4inhibitoryactivity with an IC50 of 32 μM. Licopyranocoumarin has potent neuroprotective activities .
Cryptosporiopsin A, a polyketide with antifungal activity, exhibits motility inhibitory and lytic activities against zoospores of the grapevine downy mildew pathogen Plasmopara viticola .
Phenazoviridin is a free radical scavenger. Phenazoviridin shows strong inhibitoryactivity against lipid peroxidation in rat brain homogenate and exhibits antihypoxic activity in mice .
Streptovitacin A is a compound with antibacterial and antiproliferative activities isolated from microorganisms, which has inhibitory effects on a variety of bacteria and tumor cells.
Saptomycin D is an antibiotic with antitumor activity isolated from the Streptomyces sp. HP530 strain. Saptomycin D exhibits potent inhibitory effects against Gram-positive bacteria, while demonstrating weaker inhibitoryactivities against certain Gram-negative bacteria and yeasts. Saptomycin D also displays remarkable antitumor properties. Saptomycin D is applicable in research within the field of oncology .
Methylpiperic acid is a piperine alkaloid with significant MAO inhibitoryactivity (IC503.6 μM). Methylpiperic acid is less effective against MAO-B (IC 501.6 μM) than MAO-A (IC5027.1 μM) has a bidirectional inhibitory effect. Methylphenidate is used to treat mental disorders .
Apterin is a natural compound with anti-inflammatory activity. Apterin shows significantly inhibitoryactivity on NO production in RAW264.7 cells with an IC50 value of 41.8 μM .
Arcapillin is a flavonoid that can be isolated from Artemisia capillaris Thunb. Arcapillin has antispasmodic activity. Arcapillin also has moderate PTP1Binhibitoryactivity .
Aculene D, a fungal metabolite, shows quorum sensing (QS) inhibitoryactivity against Chromobacterium violaceum CV026, and could significantly reduce violacein production in N-hexanoyl-l-homoserine lactone (C6-HSL) induced C. violaceum CV026 cultures at sub-inhibitory concentrations .
Camellianin B, a flavonoid compound, is a Camellianin A metabolite. Camellianin B has antioxidant and angiotensin converting enzyme (ACE)inhibitoryactivities .
Rubinaphthin A is a naphthohydroquinone that can be found in the roots of Rubia yunnanensis. Rubinaphthin A exhibits inhibitoryactivity against tobacco mosaic virus (TMV) .
Lyciumin A, a cyclic octapeptide, exhibits inhibitoryactivity on proteases, renin and angiotensin-converting enzyme. Lyciumin A can be used for the research of hypertension .
Tinospinoside C is a bioactive?clerodane diterpene glycoside compound. Tinospinoside C shows inhibitoryactivities of NO production with an IC50 value of 218 μM .
(+)-Epieudesmin is an antineoplastic agent. (+)-Epieudesmin has marginal cancer cell line inhibitoryactivities. (+)-Epieudesmin inhibits the growth of Gram-negative pathogen .
Hellicoside is a natural product that can be obtained from plantain. Hellicoside has inhibitoryactivity against cAMP phosphodiesterase and 5-lipoxygenase .
Calceolarioside B (Standard) is the analytical standard of Calceolarioside B. This product is intended for research and analytical applications. Calceolarioside B is a natural product isolated from Akebia quinata leaves. Calceolarioside B exhibits significant inhibitoryactivity against rat lens aldose reductase (RLAR) with an IC50 of 23.99 μM. Calceolarioside B displays inhibitory effect on DPPH radical scavenging activity with an IC50 of 94.60 μM .
Sinulatumolin E (compound 6), a terpenoid, displays significant TNF-αinhibitoryactivity with an IC50 of 3.6 μM. Sinulatumolin E (compound 6) exhibits anti-inflammatory activity .
Enocyanin is an anthocyanin extracted from grapes. Enocyanin shows inhibitory effect on the leucine aminopeptidase, acid phosphatase, γ-glutamyl transpeptidase and esterase activity .
Osmanthuside B can be isolated from Pseuderanthemum carruthersii (Seem.) Guill. var. atropurpureum (Bull.) Fosb and has weak acetylcholinesterase inhibitoryactivity .
Psychotridine is a natural alkaloid isolated from Psychotria colorata, reveals an analgesic activity in nervous system and an inhibitory efficacy towards platelet aggregation .
Massarigenin C is a compound that can be isolated from Massarina tunicata. Massarigenin C has inhibitoryactivity against Bacillus subtilis (ATCC 6051) .
Decarestrictine D exhibits inhibitoryactivity against cholesterol levels. Decarestrictine D is utilized as receptor for glycosylation reactions to synthesize novel hybrid antibiotics .
Leucosceptoside A is a phenylethanoid glycoside with anti-hyperglycemic and anti-hypertensive activities. Leucosceptoside A shows inhibitoryactivity against α-glucosidase and PKCα (IC50 of 19.0 μM) .
Limochromin is a pigment produced by Streptomyces limosus that strongly inhibits the reverse transcriptase of avian myeloid leukemia virus (AMV). The inhibitoryactivity of limochromin is not affected by changes in the concentration of template-primer, substrate or carrier protein, but its inhibitory effect is significantly reduced when the concentration of AMV reverse transcriptase increases. Limochromin can be used to develop antiviral treatments .
(+)-Medioresinol Di-O-β-D-glucopyranoside is a lignan glucoside with strong inhibitoryactivity of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterase .
Scirpusin B (compound 5) is a dimeric antioxidant isolated from Scirpus maritimus L.. Scirpusin B exhibits antitumor, antifungal, insecticidal, and plant growth inhibitoryactivities.
Trifolirhizin is a pterocarpan flavonoid isolated from the roots of Sophora flavescens. Trifolirhizin possesses potent tyrosinaseinhibitoryactivity with an IC50 of 506 μM . Trifolirhizin exhibits potential anti-inflammatory and anticancer activities .
Rabelomycin is antibiotic, which exhibits antimicrobial activity against gram positive bacteria. Rabelomycin exhibits inhibitoryactivity against inducible nitric oxide synthase (iNOS) with an IC50 of 63.9 μM .
Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitoryactivities.
Ofloxacin (Hoe-280) is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase. Ofloxacin shows inhibitoryactivity against vaccinia virus (VV).
Terphenyllin is a naturally abundant p-terphenyl metabolite isolated from the coral derived fungus Aspergillus candidus, has significant α-glucosidaseinhibitoryactivity .
Minimolide F is a sesquiterpene lactone. Minimolide F has inhibitoryactivity against human nasopharyngeal cancer cells. Minimolide F can be used for the research of cancer .
Luotonin A is an antiviral and antiphytopathogenic fungus agent. Luotonin A has good antiviral activity against tobacco mosaic virus (TMV). Luotonin A also has certain inhibitoryactivity on topoisomerase I and topoisomerase II. Luotonin A shows antitumor activity .
Kushenol B is an isoprenoid flavonoid isolated from S. flavescens, has antimicrobial, anti-inflammatory and antioxidant activities . Kushenol B has inhibitoryactivity against cAMP phosphodiesterase (PDE), with an IC50 of 31 µM .
Strictamine (compound 2) is an alkaloid with antiviral activity. Strictamine has significant inhibitoryactivity against herpes simplex virus (HSV) and adenovirus (ADV), with EC50 values ??of 0.36 μg/mL and 0.28 μg/mL, respectively .
1-Docosanol (Behenyl alcohol) is a saturated fatty alcohol with reported inhibitoryactivity against lipid-enveloped viruses, including herpes simplex virus (HSV) .
Escin IB is a saponin isolated from skin and the endosperm of seeds of horse chestnut (Aesculus hippocastanum). Escin IB shows inhibitory effect on pancreatic lipaseactivity .
N-Caffeoyl O-methyltyramine is a class of alkaloid isolated from Cuscuta reflexa with strong inhibitoryactivity against α-glucosidase (IC50 of 103.58 μM) .
Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitoryactivity toward methicillin-resistant Staphylococcus aureus (MRSA) .
Lonicerin is an anti-algE (alginate secretion protein) flavonoid with inhibitoryactivity for P. aeruginosa. Lonicerin prevents inflammation and apoptosis in LPS-induced acute lung injury .
Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities .
Neochlorogenic acid methyl ester (5-O-Caffeoylquinic acid methyl ester) is an HBVinhibitor. Neochlorogenic acid methyl ester can be isolated from L. japonica flower buds with potent HBV inhibitoryactivity .
6',7'-Epoxybergamottin is a metabolism of Penicillium digitatum. 6',7'-Epoxybergamottin can be used in study the cytochrome P450 3A4inhibitoryactivity .
Thiolopyrrolone A (compound 1) exhibits antibacterial activities against BCG, M. tuberculosis and S. aureus with minimum inhibitory concentrations (MIC) of 10, 10 and 100 μg/mL, respectively .
15-epi-Danshenol A is a diterpenoid with an immune-modulating activity. 15-epi-Danshenol A shows inhibitory effect on B lymphoblasts cells in a concentration-dependent manner .
Antimycin A2 is the component of the antibiotic antimycin A. Antimycin A is an antibiotic, that exhibits inhibitoryactivity against fungi and some insects through inhibition of respiration and cytochrome b reoxidation .
Brevianamide F (Cyclo(L-Pro-L-Trp)) is a mycotoxin isolated from Colletotrichum gloeosporioides, with antibacterial activity. Brevianamide F shows potent PI3Kαinhibitoryactivity with an IC50 of 4.8 μM .
5-Hydroxyoxindole is a structural analog of uric acid. 5-Hydroxyoxindole has DPPH radical scavenging activities and lipid peroxidation-inhibitoryactivities. 5-Hydroxyoxindole can be used for the research of oxidative stress-mediated disorders .
Talaromycesone A is an oxaphenalenone dimer compound. Talaromycesone A exhibits potent antibacterial activities with an IC50 of 3.70 μM, against human pathogenic Staphylococcus strains. Talaromycesone A displays potent acetylcholinesterase inhibitoryactivities with an IC50 of 7.49 μM .
(R)-tert-OMe-byakangelicin is a kind of furanocoumarin, which has inhibitoryactivity to liver drug metabolizing enzyme (DME) activity. (R)-tert-OMe-byakangelicin can be isolated from immature fruits of Angelica sinensis .
Lucidadiol is a natural compound isolated from Ganoderma lucidum. Lucidadiol exhibits acetylcholinesterase-inhibitory activity, with IC50 values of 31 μM. Lucidadiol shows antiviralactivity against influenza virus type A and HSV type 1 .
Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinaseactivity. Taxifolin exhibits significant inhibitoryactivity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Quercetin 3-O-(6''-O-galloyl)-β-D-glucoside (Tellimoside) is a flavonol glycoside with strong inhibitoryactivity against the growth of Microcystis aeruginosa .
Herpotrichone A shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.41 μM.
Dalbergioidin, a well-known anthocyanin, ameliorates doxorubicin-induced renal fibrosis by suppressing the TGF-β signal pathway. Dalbergioidin exhibits tyrosinase inhibitoryactivity with an IC50 of 20 mM .
Persiconin is a tyrosinase Inhibitor. Persiconin can be isolated from Prunus persica. Persiconin has tyrosinase inhibitoryactivity of 46% at 500 μM. Persiconin can be used in whitening research .
Drechslerine A has neuraminidaseinhibitoryactivity (IC50: 0.79 μM). Drechslerine A is a terpene that can be isolated from endophytic Cochliobolus. Drechslerine A can be used for research of Influenza Virus .
Crocapeptin C is a cyclic depsipeptide that can be extrated from Melittangium boletus. Crocapeptin C exhibits potent inhibitoryactivity against chymotrypsin with an IC50 value of 0.5 µM .
Hyalodendrin ((+)-Hyalodendrin) is a fungal growth inhibitor with inhibitoryactivity against wood decay fungi. Hyalodendrin has low phytotoxicity, with an acute toxicity (LD50) of 75 mg/kg in mice .
Methylsticin (Standard) is the analytical standard of Methylsticin. This product is intended for research and analytical applications. Methylsticin is a kavalactone isolated from the Piper methysticum . Methylsticin exhibit osteoclast formation inhibitoryactivity .
Militarine (Standard) is the analytical standard of Militarine. This product is intended for research and analytical applications. Militarine, a glycosidic compound isolated from Bletilla striata, exhibits plant growth-inhibitoryactivity .
Stemoninine is a lycoris alkaloid that can be used as an antitussive. Stemoninine has significant inhibitoryactivity against human acetylcholinesterase (AChE) (IC50=5.52 μM) .
Flavanone (Standard) is the analytical standard of Flavanone. This product is intended for research and analytical applications. Flavanone is a naturally occurring flavone. Flavanone has inhibitoryactivity for human estrogen synthetase (aromatase) .
Antibiotic SF-2132 is a peptide antibiotic identified in Nocardiopsis sp., which exhibits inhibitoryactivity against β-lactam antibiotic-resistant strains, such as Pseudomonas and Escherichia .
Lagunamycin is a 5-lipoxygenase inhibitor isolated from the culture medium of Streptomyces sp. AA0310. Lagunamycin has a significant inhibitoryactivity against rat 5-lipoxygenase with an IC50 value of 6.08 μM. Lagunamycin can effectively inhibit 5-lipoxygenase without causing lipid peroxidation, indicating that it has an effective inhibitory effect without causing side effects.
Pectolinarigenin (Standard) is the analytical standard of Pectolinarigenin. This product is intended for research and analytical applications. Pectolinarigenin is a dual inhibitor of COX-2/5-LOX. Anti-inflammatory activity . Pectolinarigenin has potent inhibitoryactivities on melanogenesis .
Nocardicin A is a beta-lactam antibiotic with selective antibacterial activity. Nocardicin A has moderate antibacterial activity against a broad spectrum of Gram-negative bacteria including Proteus and Pseudomonas; it has no inhibitory effect on Staphylococcus, Mycobacterium, fungi, and yeast .
Enrofloxacin monohydrochloride (BAY Vp 2674 monohydrochloride) is an effective antibiotic with an MIC90 of 0.312 μg/mL for Mycoplasma bovis. Enrofloxacin monohydrochloride shows inhibitoryactivity against vaccinia virus (VV).
Herpotrichone B shows potent anti-neuroinflammatory activity in lipopolysaccharide (LPS)-induced BV-2 microglial cells with the half maximal inhibitory concentration (IC50) value of 0.11 μM.
Phaeosphaone D is a thiodiketopiperazine alkaloid compound isolated from Phaeosphaeria fuckelii, an endophytic fungus. Phaeosphaone D displays mushroom tyrosinase inhibitoryactivity with an IC50 value of 33.2 μM .
Sorbifolin, a flavone glucoside, can be isolated from the Pterogyne nitens. Sorbifolin has myeloperoxidase inhibitory and radical scavenging activities. Sorbifolin is also a MPOinhibitor with an IC50 value of 19.2 nM .
Acetyl-binankadsurin A (compound 5) is a lignan isolated from Kadsura longipedunculata. Acetyl-binankadsurin A has low inhibitoryactivity against HIV-1 protease, with IC50 >100 μg/mL .
Aloveroside A is a triglucosylnaphthalene derivative isolated from ethanolic extract of aloe vera. Aloveroside A has weak bACE inhibitoryactivity (inhibition rate at a dose of 100 μg/mL is approximately 18.68%) .
Kagimminols A is a cembrene-type diterpenoids and can be isolated from an Okeania sp. marine cyanobacterium. Kagimminols A shows selective growth-inhibitoryactivity against the causative agent of human African trypanosomiasis .
Saframycin S is an antibiotic with a racemomycin group that exhibits inhibitoryactivity against Ehrlich ascites tumors. The LD50 of Saframycin S in ddY mice is 3.2 mg/kg (i.p.) .
(±)-Taxifolin ((±)-Dihydroquercetin) is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinaseactivity. Taxifolin exhibits significant inhibitoryactivity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
8-Methylsulfinyloctyl isothiocyanate, an isothiocyanate, has antimicrobial activity and remarkable inhibitoryactivity against plant growth . 8-Methylsulfinyloctyl isothiocyanate impair COX-2 mediated inflammatory responses in LPS stimulated raw macrophages .
(-)-Taxifolin is the less active enantiomer of Taxifolin. Taxifolin exhibits important anti-tyrosinaseactivity. Taxifolin exhibits significant inhibitoryactivity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Mulberroside F is one of the main bioactive constituents in mulberry (Morus alba L.) . Mulberroside F shows inhibitory effects on tyrosinaseactivity and on the melanin formation. Mulberroside F also exhibits superoxide scavenging activity that is involved in the protection against auto-oxidation .
Ilexoside O is a triterpene saponin isolated from the roots of Ilex pubescens. Ilexoside O exhibits weak xanthine oxidase (XOD)inhibitoryactivity (IC50=53.05 μM) .
3-Methylcarbazole is an carbazole alkaloid compound with anticancer effects. 3-Methylcarbazole shows growth inhibitoryactivity (IC50 of 25 μg/mL) on human fibrosarcoma HT-1080 cells .
Curcolonol is a furan type sesquiterpene. Curcolonol can be isolated from several medical herbs. Curcolonol has inhibitoryactivity for LIM kinase 1. Curcolonol can be used for the research of breast cancer .
Kanshone B (Compound 5) is isolated from the
natural Nardostachys chinensis. Kanshone B shows inhibitoryactivity against LPS-induced NO production (IC50=11.5 μM)
.
Chloramultilide B is a lindenane dimer that can be isolated from Chloranthus serratus. Chloramultilide B has inhibitoryactivities against Candida albicans and C.parapsilosis with a MIC value of 0.068 μM .
Araloside A (Standard) is the analytical standard of Araloside A. This product is intended for research and analytical applications. Araloside A (Chikusetsusaponin IV) is a component of Panax japonicus, with low-renin-inhibitoryactivity, with an IC50 of 77.4 μM .
DL-Homocysteine thiolactone (hydrochloride) (Standard) is the analytical standard of DL-Homocysteine thiolactone (hydrochloride). This product is intended for research and analytical applications. DL-Homocysteine thiolactone hydrochloride is a cyclic amino acid derivative that exhibits root-growth inhibitoryactivity.
Sandosaponin A (Soyasaponin Bd) is a saponin with inhibitoryactivity against human recombinant aldehyde reductase (hAKR1B1). Sandosaponin A can inhibit the reduction of l-idose and 4-hydroxynonenal to varying degrees. The presence of Sandosaponin A reveals the challenges posed by the masking effect of conventional aldehyde reductase inhibitors in mixtures when exploring differential aldehyde reductase inhibitors. The inhibitory mechanism of Sandosaponin A may be related to its mode of action on different substrates .
Evodol is a natural product isolated from the dried and nearly ripe fruits of Euodia rutaecarpa. Evodol shows inhibitoryactivity against NO production . Evodol possesses larvicidal activity against the Asian tiger mosquitoes with a LC50 value of 32.43 μg/ml .
Norchelerythrine is an alkaloid isolated from the roots of Zanthoxylum capense with antibacterialactivity against gram-positive and gram-negative bacteria. Norchelerythrine exhibits inhibitoryactivity against Staphylococcus aureus, Pseudomonas aeruginosa, and Enterococcus faecalis and Escherichia coli with MIC values >50 µg/mL .
Cassiaside C (Toralactone 9-O-β-D-gentiobioside) is a naphthopyrone isolated from the seed of Cassia tora and has inhibitoryactivity on advanced glycation end products (AGE) formation in vitro .
Ganoderenic acid K is a natural product, that can be isolated from fruiting bodies of Ganoderma lucidum. Ganoderenic acid K shows strong inhibitoryactivity against HMG-CoA reductase (HMGCR) with IC50 of 16.5 μM .
Acantrifoside E (Compound 8) is a nature compound. Acantrifoside E can be isolated from the 90% ethanol extract of Salacia cochinchinensis. Acantrifoside E has none α-glucosidase inhibitoryactivity .
N-cis-Feruloyl tyramine (cis-N-(4-Hydroxyphenethyl) ferulamide) is a natural phenolic compound, exhibits modest inhibitoryactivity on LPS-activated NO production in RAW 264.7 cells .
Dehydroperilloxin is a natural compound isolated from the dichloromethane extract of the stems of Perilla frutescens var. acuta. Dehydroperilloxin possesses inhibitoryactivity against cyclooxygenase-1, with the IC50 value of 30.4 μM .
Kagimminol B, a cembrene-type diterpenoid, can be isolated from an Okeania sp. marine cyanobacterium. Kagimminol B shows selective growth-inhibitoryactivity against the causative agent of human African trypanosomiasis .
Tetrahydrobostrycin is a secondary metabolite from Aspergillus sp., which exhibits a weak inhibitoryactivity against Staphylococcus aureus and Escherichia coli (100 mg/disc with the inhibition zones of 15 and 9.2 mm in diameter) .
Hippeastrine hydrobromide is an active alkaloid that exhibits a good dose-dependent inhibitory effect on topoisomerase I (Top I) with an IC50 of 7.25?μg/mL. Hippeastrine hydrobromide exhibits antiproliferative and anticancer activities .
S-(+)-Marmesin (Standard) is the analytical standard of S-(+)-Marmesin. This product is intended for research and analytical applications. S-(+)-Marmesin is a natural coumarin, exhibiting COX-2/5-LOX dual inhibitoryactivity.
Rawsonol is a brominated diphenylmethane derivative obtained from the green alga Avrainuika rawsoni. Rawsonol exhibits inhibitoryactivity against 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, with activities related to cholesterol biosynthesis inhibition or other metabolic pathways involving HMG-CoA reductase activity .
Kaempferol 3-O-gentiobioside is a flavonoid isolated from C. alata leaves with antidiabetic activity. Kaempferol 3-O-gentiobioside possesses activity against α-glucosidase and displays carbohydrate enzyme inhibitory effect with an IC50 of 50.0 µM .
Hamaudol is a chromone isolated from Saposhnikovia divaricata. Hamaudol shows significant inhibitoryactivity on cyclooxygenase (COX)-1 and COX-2activities with IC50 values of 0.30, 0.57 mM, respectively, and has potent analgesia and anti-inflammary effects .
Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitoryactivity on β-secretion (BACE) (IC50=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release.
Phenethyl ferulate is a major constituent ofQianghuo, shows inhibitoryactivity against cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) with IC50 values of 4.35 μM and 5.75 μM, respectively .
Tetrahydroamentoflavone (Amentoflavanone) is a potent xanthine oxidase (XO)inhibitor. Tetrahydroamentoflavone has inhibitoryactivity for XO with IC50 and Ki values of 92 nM and 0.982 μM, respectively. Tetrahydroamentoflavone can be used for the research of inflammatory disorders and gout .
Clausine E, is a alkaloid which can be isolated from Clausena excavata, is a inhibitor of fat mass and obesity-associated protein (FTO) demethylase. Clausine E shows inhibitoryactivities against proliferation of synoviocytes and cancer cells.
Mortatarin G (compound 3) is a prenylated flavonoid, that can be isolated from mulberry leaves. Mortatarin G exhibits good α-glucosidaseinhibitoryactivity, with an IC50 of 20.4±1.4 μM .
6β-Hydroxyipolamiide can be isolated from the methanolic extract of S. jamaicensis leaves. 6β-Hydroxyipolamiide has α-glucosidaseinhibitoryactivity with an IC50 of 539.17 μg/mL .
HPSE1-IN-1 (compound 16) is a selective inhibitor of Heparanase-1 (HPSE1) with moderate inhibitoryactivity against exo-β-d-glucuronidase (GUSβ) and glucocerebrosidase (GBA) .
Simocyclinone D8 is an anthracycline antibiotic with antibacterial and antitumor activity against Gram-positive bacteria. Simocyclinone D8 inhibitsDNA gyrase and thus has an inhibitory effect on a variety of tumor cell lines .
5-Feruloylquinic acid (Standard) is the analytical standard of 5-Feruloylquinic acid. This product is intended for research and analytical applications. 5-Feruloylquinic acid (5-FQA) possesses antioxidative effects and tyrosinase inhibitoryactivities .
Protorubradirin is an antibiotic that can be isolated from Streptomyces achromogenes var. rubradirin together with Rubradirin. Protorubradirin has inhibitoryactivity against HIV reverse transcriptase. In vitro studies have shown that Protorubradirin also inhibits Staphylococcus aureus strains and Streptococci. In infected mice, subcutaneous injection of Protorubradirin showed in vivo inhibitory efficacy against antibiotic-resistant Staphylococcus aureus strains. However, oral administration may result in a significant reduction in the activity of Protorubradirin, possibly due to faster cleavage of its C-nitroso sugar in the acidic gastric environment compared to Rubradirin .
Purpurogallin is a naturally phenol extracted from the plants of Quercus spp, has potent xanthine oxidase (XO)inhibitoryactivity with an IC50 of 0.2 µM. Purpurogallin has antioxidant and anti-inflammatory effects .
Velutin is an aglycone extracted from Flammulina velutipes, with inhibitoryactivity against melanin biosynthesis. Velutin reduces osteoclast differentiation and down-regulates HIF-1α through the NF-κB pathway .
Triptoquinone B ((+)-Triptoquinone B), a sesquiterpene alkaloid, is an interleukin-1inhibitor. Triptoquinone B shows potent inhibitoryactivities against interleukin 1α and β releases for human peripheral mononuclear cells .
Chaetosemin J, an antifungal metabolite, exhibits inhibitoryactivity against plant pathogenic fungi Botrytis cinerea, Alternaria solani, Magnaporthe oryzae, and Gibberella saubinettii, with MIC values ranging from 12.5-25 μM .
Cryptomeridiol is a platelet-activating factor (PAF) receptor binding inhibitor. Cryptomeridiol has melanogenesis inhibitoryactivity in the α-MSH (HY-P0252)-stimulated B16 melanoma cells .
Aloeresin G is a chromone glycoside that can be isolated from Aloe. Aloeresin G has a weak inhibitory effect on TNFα-induced NF-κB transcriptional activity, with an IC 50 value of 40.02 μM .
Hyperelamine A (compound 5) is a polycyclic polyprenylated acylphloroglucinols (PPAPs). Hyperelamine A exhibits inhibitoryactivity against LPS-activated NO production in BV-2 cells via TLR-4/NF κB signaling .
Talaroderxine D (compound 4) has biofilm inhibitory effect. Talaroderxine D shows antimicrobial activities against Bacillus subtilis and Staphylococcus aureus with MIC values of 2.1 and 8.3 μg/mL .
Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase .
Glyurallin B is a flavonoid, that can be isolated from licorice (Glycyrrhiza inflata and Glycyrrhiza uralensis). Glyurallin B shows ABTS + radical scavenging activity and the inhibitoryactivity on lipid peroxidation, with EC50 values of 11.9 ± 0.58 μM and 15.3 ± 1.26 μM, respectivley .
Trifolirhizin (Standard) is the analytical standard of Trifolirhizin. This product is intended for research and analytical applications. Trifolirhizin is a pterocarpan flavonoid isolated from the roots of Sophora flavescens. Trifolirhizin possesses potent tyrosinase inhibitoryactivity with an IC50 of 506 μM . Trifolirhizin exhibits potential anti-inflammatory and anticancer activities .
Lentinellic acid is an antimicrobial and cytotoxic diterpenoid with biological activity. Lentinellic acid exerts its antimicrobial activity by inhibiting the growth of microorganisms. Lentinellic acid also shows inhibitory effects on tumor cells and has potential anticancer properties. The structure of lentinellic acid was determined by spectroscopic methods and single crystal X-ray analysis .
Prunin is a potent inhibitor of human enterovirus A71 (HEVA71). Prunin shows strong inhibitoryactivity against protein tyrosine phosphatase 1B (PTP1B), with an IC50 of 5.5 μM .
15a-Hydroxy-3,11,23-trioxo-lanost-8,20-dien-26-oic acid, a Lanostane triterpenoid, possesses NO production inhibitoryactivities of LPS-induced microglia .
19-O-Acetylchaetoglobosin A, a cytochalasan alkaloid, is a fungal metabolite originally isolated from C. globosum that has actin polymerization inhibitory and cytotoxic activities. 19-O-Acetylchaetoglobosin A is cytotoxic to HeLa cervical cancer cells .
Isodonal is a N-pentane diterpene compound with potential cytotoxic, antitumor, inhibitory oxidative phosphorylation and antiingestion activities. Isodonal can be isolated from the leaves of Isodon wikstroemioides and is used in the study of gastrointestinal diseases, anti-tumor and anti-inflammatory .
Chamigrenol is a Na +/K +-ATPaseinhibitor with an IC50 value of 15.9 μg/mL. Chamigrenol shows strong inhibitoryactivities against Gram-positive and Gram-negative bacteria except Escherichia coli, with MIC values of 50 µg/mL .
7-O-Methylaloesinol is a chromone derivative. 7-O-Methylaloesinol shows significant inhibitory effects against TNFα-induced NF-κB transcriptional activity with an IC50 value of 29.07 μM .
3,3′-Bisdemethylpinoresinol, lignin, is a nature product and has MMP-1 inhibitoryactivity in UVA-irradiated human dermal fibroblasts. 3,3′-Bisdemethylpinoresinol can be isolated from the seeds of Morinda citrifolia .
Taxiphyllin (2R-Taxiphyllin) is a plant cyanogenic glycoside, which exhibits inhibitoryactivity for tyrosinase . Taxiphyllin exhibits cytotoxicity in BRL-3A cellls with an IC50 of 18.75 μm and antimicrobial activities against Staphylococcus aureus with an EC50 of 0.96 μM .
Taxifolin (Standard) is the analytical standard of Taxifolin. This product is intended for research and analytical applications. Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitoryactivity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Methyl gallate (Standard) is the analytical standard of Methyl gallate. This product is intended for research and analytical applications. Methyl gallate is a plant phenolic with antioxidant, anticancer, and anti-inflammatory activities. Methyl gallate also shows bacterial inhibition activity. Methyl gallate also has anti-HIV-1 and HIV-1 enzyme inhibitoryactivities.
5,7-Diacetoxy-8-methoxyflavone is a natural product that could come from scutellaria genus plants. 5,7-Diacetoxy-8-methoxyflavone has inhibitoryactivity for cAMP phosphodiesterase .
Protosappanin A dimethyl acetal is a homoisoflavonoid. Protosappanin A dimethyl acetal can be isolated from Caesalpinia sappan. Protosappanin A dimethyl acetal is also a competive inhibitor with significant xanthine oxidaseinhibitoryactivity (IC50=50.7 μM) .
Vibralactone D (Compound 1) is a metabolite isolated and cultured from natural basidiomycetes Boreostereum vibrans. Vibralactone D shows weak inhibitoryactivity against isoenzymes of 11b-hydroxysteroid dehydrogenase (HSD) (IC50 85.7 μM).
Detoxin D1 is a compound with antihistamine activity and a new type of H1 antagonist. In the suppression of seasonal allergic rhinitis, a daily dose of 10-30 mg has an equivalent and highly effective inhibitory effect compared with placebo and has good safety.
Bruceine D is a Notchinhibitor with anti-cancer activity and induces apoptosis in several human cancer cells. Bruceine D is an effective botanical insect antifeedant with outstanding systemic properties, causing potent pest growth inhibitoryactivity . Bruceine D has strong anthelminticactivity against D. intermedius with an EC50 value of 0.57 mg/L .
Tribuloside is a flavonoid that can be isolated from Tribulus terrestris L . Tribuloside exhibits anti-mycobacterialactivity against the non-pathogenic Mycobacterium species with a minimum inhibitory concentration (MIC) of 5.0 mg/mL. Tribuloside has 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity .
Solidagonic acid inhibitsHSET motor activity by promoting the conversion from abnormal monopolar to bipolar spindles. Solidagonic acid suppresses fission yeast cell death and enables reversion of the mitotic spindles from a monopolar to bipolar morphology. Solidagonic acid showed the growth inhibitoryactivity on the seedlings of Lactuca sativa L. and Lolium multiflorum Lam .
Oligomycin E is a antitumor antibiotic that can be isolated from Streptomyces. Oligomycin E has significant antifungal activity, showing minimal inhibitory concentrations (MICs) values between 2 and 75μg/mL. Oligomycin E has strong antitumor activity against HeLa cells, with an IC50 of 0.014 μg/mL .
Gypenoside XLVI is one of the major dammarane-type triterpenoid saponins from Gynostamma pentaphallum . Gypenoside XLVI has a tetracyclic triterpene structure and possess potent non-small cell lung carcinoma A549 cell inhibitoryactivity .
Oroxylin A-7-O-glucuronide (Oroxyloside; Oroxylin A-7-O-β-D-glucuronide) is a flavonoid glucuronide isolated from the dried root of Scutellaria baicalensis, with prolyl oligopeptidase (POP)inhibitoryactivity .
Benzomalvin A is a potent antagonist of neurokinin receptor isolated from Penicillium sp. Benzomalvin A shows inhibitoryactivity against substance P with Ki values of 12, 42 and 43 μM at the guinea pig, rat and human neurokinin NK1 receptors, respectively .
STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitoryactivity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3 .
AS-2077715 is an antifungal agent that shows inhibitoryactivity against the Trichophyton species. AS-2077715 can be obtained from the fermentation broth of Capnodium sp. 339855. AS-2077715 can be used to study fungal infections .
Ofloxacin (Standard) is the analytical standard of Ofloxacin. This product is intended for research and analytical applications. Ofloxacin (Hoe-280) is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase. Ofloxacin shows inhibitoryactivity against vaccinia virus (VV).
Prudomestin (Standard) is the analytical standard of Prudomestin. This product is intended for research and analytical applications. Prudomestin, isolated from the heartwood of Prunus domestica, shows potent xanthine oxidase (XO) inhibitoryactivity (IC50≈6?μM) .
Kayaflavone is an amentoflavone type biflavonoid. Kayaflavone has an inhibitoryactivity against amyloid-β42 cytotoxicity in PC-12 cells with an EC50 value of 5.29 μΜ. Kayaflavone is promising for research of Alzheimer’s disease .
FR 106969 (A26771E) is a platelet activating factor antagonist with anti-inflammatory activity. FR 106969 can be used to alleviate inflammatory responses. FR 106969 has shown potential inhibitory effects on inflammation-related diseases in studies .
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitoryactivity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population .
3-O-Methylellagic acid is a nature product that can be isolated from Myrciaria cauliflora, with anti-inflammatory activity. 3-O-Methylellagic acid shows an inhibitory effect on glucose transport assay. 3-O-Methylellagic acid has antibacterial activity, with a MIC of 32 μg/mL for Staph. Aureus ATCC 25923 .
6-Benzoylheteratisine is an Aconitum alkaloid with potential neuroprotective activity. 6-Benzoylheteratisine can antagonize tetrodotoxin, inhibit the increase of [Na +]i, [Ca 2+]i and glutamate release, and block sodium channels. 6-Benzoylheteratisine has an inhibitory effect on the neuronal activity underlying epileptiform burst discharge .
(±)-ε-Viniferin is a racemate of ε-Viniferin (HY-N3841). (±)-ε-Viniferin exhibits P450inhibitory antioxidants, as well as hepato-protective and antimicrobial activities. (±)-ε-Viniferin has antibacterial and antibiofilm activity against Gram-positive bacteria Streptococcus pneumoniae with a MIC of 20 μM .
Epibetulinic acid exhibits potent inhibitory effects on NO and prostaglandin E2 (PGE2) production in mouse macrophages (RAW 264.7) stimulated with bacterial endotoxin with IC50s of 0.7 and 0.6 μM, respectively. Anti-inflammatory activity .
Debromohymenialdisine (10Z-Debromohymenialdisine) is a pyrrole alkaloid. Debromohymenialdisine has moderate inhibitoryactivity with an IC50 value of 881 nM in the initial Raf/MEK-1/MAPK signaling cascade assay. Debromohymenialdisine can be used for the research of proliferation and differentiation .
Limonianin (Atalantoflavone) is a flavone, that can be isolated from Erythrina sigmoidea and the root bark of Citrus limonia. Limonianin presents inhibitory effect against P. gingivalis. Limonianin shows cytotoxic activity against multidrug-resistant (MDR) cancer cell lines .
Mollicellin I (compound 1) is a depsidone. The growth inhibitoryactivity of Mollicellin I on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines is not significant, with GI50s >10 μg/mL .
α-Glucosidase-IN-37 (Compound 11) moderately inhibits LPS-induced NO production with an IC50 value of 23.7 μM in macrophages. α-Glucosidase-IN-37 has weak inhibitoryactivity against α-Glucosidase .
Lantic acid is a triterpenoid compound possessing antimicrobial activity. Lantic acid exhibits inhibitory effects on a broad range of both Gram-positive and Gram-negative bacteria, with particular potency against Escherichia coli and Bacillus subtilis. Lantic acid is utilized in the research and development of antimicrobial agents .
Lonicerin (Standard) is the analytical standard of Lonicerin. This product is intended for research and analytical applications. Lonicerin is an anti-algE (alginate secretion protein) flavonoid with inhibitoryactivity for P. aeruginosa. Lonicerin prevents inflammation and apoptosis in LPS-induced acute lung injury .
N-Methylcalycinine is a nature product with AChE inhibitoryactivity. N-Methylcalycinine can be isolated from the roots of Stephania epigaea. N-Methylcalycinine can be used for the research of asthma, cancer, dysentery, fever, hyperglycemia, intestinal complaints, inflammation, sleep disturbances, tuberculosis and so on .
Eupenicisirenin C (compound 1) is a sirenin derivative. Eupenicisirenin C has strong NF-κBinhibitoryactivities. Eupenicisirenin C suppresses effects on cGAS-STING pathway. Eupenicisirenin C inhibits RANKL-induced osteoclast differentiation in bone marrow macrophage cells .
Tachioside inhibits nitric oxide production in lipopolysaccharide (HY-D1056)-stimulated RAW 264.7 cells with IC50 value of 12.14 μM. Tachioside has anti-obesity, antioxidant and α-glucosidaseinhibitoryactivities .
Kopsoffinol, a bisindole alkaloid, shows in vitro growth inhibitoryactivity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells .
Isoscoparin-7-O-glucoside is a flavonoid compound found in barley leaves. The total phenolic content (TPC) of isoscoparin-7-O-glucoside is positively correlated with COX-2 inhibitoryactivity, indicating anti-inflammatory activity. Isoscoparin-7-O-glucoside can be used in the study of inflammation .
Cephalandole B is an indigo alkaloid that has the activity of inhibiting IL-17A gene expression. Cephalandole B significantly inhibited the activity of IL-17A luciferase reporter gene in Jukat cells, and this inhibitory effect was dose-dependent. Cephalandole B may have important application prospects in inflammation-related research .
11-oxo-mogroside V is a natural sweetener that exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2-, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes . Medicagenic acid (Castanogenin) has low enzyme inhibitoryactivities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE .
Plantanone B is a moderate antioxidant-agent with an IC50 of 169.8±5.2 μM. Plantanone B shows significant ovine COX-1 and moderate COX-2 inhibitoryactivities. Plantanone B has the potential for inflammation-related diseases research .
11-O-β-D-glucopyranosyl thamnosmonin, a coumarin glucosides, can be isolated from the roots of Angelica apaensis. 11-O-β-D-glucopyranosyl thamnosmonin has weak inhibitoryactivity on the aggregation of rabbit platelets induced by PAF, AA, and ADP .
Escin IB (Standard) is the analytical standard of Escin IB. This product is intended for research and analytical applications. Escin IB is a saponin isolated from skin and the endosperm of seeds of horse chestnut (Aesculus hippocastanum). Escin IB shows inhibitory effect on pancreatic lipase activity .
DPP-IV-IN-5 is isolated from the fruits of Lycium barbarum. DPP-IV-IN-5 exerts moderate agonistic activities for peroxisome proliferator-activated receptor (PPARγ) with EC50 values of 10.09 - 44.26 μM and also presents inhibitoryactivity on dipeptidyl peptidase-4 (DPPIV) with an IC50 value of 47.13 μM .
Grape seed extract is a natural product, with anti-inflammatory and anti-proliferative effects. Grape seed extract shows inhibitoryactivity on the fat-metabolizing enzymes pancreatic lipase and lipoprotein lipase. Grape seed extract induces apoptotic in human colorectal cancer cells .
4-Nitrophenyl-N-acetyl-β-D-galactosaminide has inhibitoryactivity against GlcNAc and GalNAc with Kis of 1.15 mM and 0.51 mM, respectively. 4-Nitrophenyl-N-acetyl-β-D-galactosaminide is extracted from Trichomonas foetus (T. foetus)
Angelol G, a coumarin, can be isolated from Campylotropis hirtella. Angelol G shows inhibitoryactivity for prostate specific antigen (PSA)IC50 value of 152.1μM. Angelol G can be used for the research of benign prostate hyperplasia (BPH) .
Artocarpin is an isoprenoid-substituted flavonoid, that can be isolated from the wood of Artocarpus heterophyllus. Artocarpin inhibits melanin biosynthesis in B16 melanoma cells without inhibiting tyrosinase. The presence of the isoprenoid-substituted moiety enhanced the inhibitoryactivity on melanin production in B16 melanoma cells .
Kapurimycin A1 is an anbitiotic that can be isolated from Streptomyces. Kapurimycin A1 has a significant inhibitory effect on Gram-positive bacteria, exhibits cytotoxicity to cultured mammalian cells, and shows strong antitumor activity against the mouse leukemia P388 cell line .
Meleagrin is a roquefortine C-derived alkaloid produced by fungi of the genus Penicillium and has antimicrobial and anti-proliferative activities. Meleagrin is a class of FabIinhibitor. Meleagrin is a lead c-Metinhibitory entity useful for the control of c-Met-dependent metastatic and invasive breast malignancies .
NADH-IN-1 has NADH:ubiquinone oxidoreductaseinhibitoryactivity with an IC50 value of 27 μM. NADH-IN-1 can effectively stimulate glucose uptake in vitro. NADH-IN-1 is readily metabolised by the liver. NADH-IN-1 can be used for researching diabetes .
1-Docosanol (Standard) is the analytical standard of 1-Docosanol. This product is intended for research and analytical applications. 1-Docosanol (Behenyl alcohol) is a saturated fatty alcohol with reported inhibitoryactivity against lipid-enveloped viruses, including herpes simplex virus (HSV) .
Propioxatin B is a tricyclic sesquiterpenoid compound isolated from the root of vetiver grass. It has anti-tuberculosis activity and inhibitory effects on a variety of drug-resistant mutants of Mycobacterium tuberculosis. In computer simulation docking studies, it showed binding affinity with bacterial DNA gyrase and has a certain safety in vivo.
ent-Toddalolactone is a natural compound with anti-inflammatory and anticancer activities. Ent-Toddalolactone has shown inhibitory effects on phosphodiesterase-4 (PDE4) in vitro and is a potential drug target for inhibiting asthma and chronic obstructive pulmonary disease. The activity of ent-Toddalolactone is related to its unique chemical structure, and some of its derivatives showed IC50 values below 10 μM in inhibition experiments, showing high biological activity .
2-Hydroxycinnamic acid is a phenolic acid with antimicrobial and antioxidant properties. 2-Hydroxycinnamic acid has antimicrobial activity against Staphylococcus aureus and is not susceptible to drug resistance. 2-Hydroxycinnamic acid shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC50 of 0.3 mM. In addition, 2-Hydroxycinnamic acid has neuroprotective and antitumor activity .
6-Prenylquercetin-3-Me ether is a natural product that can be extracted from G. uralensis leaves.
6-Prenylquercetin-3-Me ether has radical scavenging activity toward DPPH. 6-Prenylquercetin-3-Me ether also has inhibitoryactivity against α-glucosidase .
3-Hydroxybakuchiol can be isolated from Otholobium mexicanum J. W. Grimes. 3-Hydroxybakuchiol is an electron transport chain (ETC)inhibitor. 3-Hydroxybakuchiol has antitumor activity, and induces tumor cell apoptosis. 3-Hydroxybakuchiol also has moderate inhibitoryactivity against α-glucosidase (IC50: 345 μM) .
Cirsimarin (Standard) is the analytical standard of Cirsimarin. This product is intended for research and analytical applications. Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase .
Guanfu base A hydrochloride is an antiarrhythmic alkaloid with the ability to inhibit CYP2D6 enzyme activity. Guanfu base A hydrochloride can be used to inhibit arrhythmia-related diseases. Guanfu base A hydrochloride exhibits inhibitory effects on CYP2D6 in different species of organisms, including humans, monkeys, and dogs. The biological activity of Guanfu base A hydrochloride makes it have potential clinical application value .
Apiin, a major constituent of Apium graveolens leaves with anti-inflammatory properties. Apiin shows significant inhibitoryactivity on nitrite (NO) production (IC50 = 0.08 mg/mL) in-vitro and iNOS expression (IC50 = 0.049 mg/ mL) in LPS-activated J774.A1 cells .
Pogostone is isolated from patchouli oil with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml . Pogostone induces cell apoptosis and autophagy .
Cymarin, a cardiac glycoside, potently inhibits the Palytoxin (PTX)-induced K + release (IC50=0.42 μM). Cymarin reveals an antitumor activity against breast cancer and pancreatic cancer. Cymarin exhibits antifeedant and growth inhibitory effects as crop protectant .
cis-Ferulic acid 4-O-β-D-glucopyranoside (compound 7) is a phenolic glycosid, which can be isolated from Nitraria sibirica.. cis-Ferulic acid 4-O-β-D-glucopyranoside exhibits antioxidant activity and potent inhibitory effect on Phosphatase PTP1B .
Hedycoronen A has inhibitoryactivity on the IL-6, IL-12 p40, and TNF-α production in LPS-Stimulated BMDCs, with IC50s of 9.1 μM, 5.6 μM, and 46.0 μM. Hedycoronen A can be isolated from Hedychium coronarium .
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
Alisol F is a triterpene isolated from Alisma orinentale, has immunosuppressive and anti-virus functions. Alisol F exhibits inhibitoryactivity in vitro on hepatitis B virus (HBV) surface antigen (HBsAg) secretion of the HepG2.2.15 cell line with an IC50 of 0.6 μM .
Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses the potential anti-tumor bioactivity, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitoryactivity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM .
Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 17.38 μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products .
Ebelactone A is a mycolic acid β-lactone, which exhibits inhibitoryactivity for esterase, lipase, fMet aminopeptidase (fMet AP) and PNBase, with IC50s of 56, 3, 8 and 7.5 μM, respectively . Ebelactone A inhibitscutinase, exhibits plants protective potency against Erysiphe graminis .
SHP2-IN-29 (Compound 3) is a potent SHP2inhibitor with an IC50 value of 0.18 μM. SHP2-IN-29 also has inhibitoryactivity against PTP1B and TCPTP, with IC50 values of 4.27 and 4.74 μM, respectively.
Scirpusin A is a naturally occurring compound extracted from the legume plant Caragana rosea Turcz, exhibiting anti-HIVactivity. Scirpusin A demonstrates significant inhibitory effects against HIV-1 (EC50=7 μg/mL). Scirpusin A is utilized in research towards the development of anti-HIV therapeutics .
N-Caffeoyl O-methyltyramine (Standard) is the analytical standard of N-Caffeoyl O-methyltyramine. This product is intended for research and analytical applications. N-Caffeoyl O-methyltyramine is a class of alkaloid isolated from Cuscuta reflexa with strong inhibitoryactivity against α-glucosidase (IC50 of 103.58 μM) .
Aloenin (Standard) is the analytical standard of Aloenin. This product is intended for research and analytical applications. Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitoryactivity on β-secretion (BACE) (IC50=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release .
5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl (compound 8) can be isolated from Dendrobium infundibulum (D. infundibulum). 5,4'-Dihydroxy-3,4,3'-trimethoxybibenzyl has no inhibitoryactivity against α-glucosidase and pancreatic lipase .
Polyphyllin G is isolated from the rhizomes of Paris yunnanensis, with antimicrobial and anticancer activity. Polyphyllin G prevents the growth of both Gram-positive and Gram-negative bacteria with minimum inhibitory concentrations (MICs) .
Polyphyllin G induces apoptosis dependent on the activations of caspase-8, -3, and -9, induces autophagy .
4-Allylcatechol (4-Allylpyrocatechol) is a xylan isolated from the root of Piper taiwanense. 4-Allylcatechol has a strong inhibitoryactivity against collagen-induced platelet aggregation (IC50=5.3 μM). In addition, 4-Allylcatechol has anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv (MIC=27.6 μg/mL) .
Ilicicolin C exhibits antibacterial activity against Pseudomonas syringae with IC50 of 28.5 µg/mL. Ilicicolin C exhibits weak inhibitoryactivities against acetylcholinesterase (AChE) and β-glucuronidase with IC50 of 30-43 µg/mL. Ilicicolin C exhibits weak cytoxicity in human lung fibroblasts with IC50 of 64-120 µg/mL. Ilicicolin C affects seed germination and root tip growth of lettuce .
Milbemycin oxime is an orally active macrolide with broad-spectrum antiparasitic activity. Milbemycin oxime is a mixture of oximes consisting of oxime derivatives corresponding to milbemycin A4 and A3. Milbemycin oxime binds to glutamate-gated chloride channels and has inhibitory potency against intestinal nematodes and lung/heart worms .
CS-722 Free base is a synthesized centrally acting muscle relaxant, and has a muscle relaxant activity and depressant effectson the spinal reflex . CS-722 Free base inhibits spontaneous inhibitory postsynaptic currents and excitatory postsynaptic currents in hippocampal cultures probably by an inhibition of both sodium and calcium currents .
ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol and can be isolated from Vitis vinifera, displays a potent inhibitory for all the CYPactivities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity .
Validamycin A, a fungicidal, is an agricultural antibiotic. Validamycin A is originally isolated from Streptomyces hygroscopicus var. limoneus. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL . Validamycin A shows potent inhibitoryactivity against trehalase of Rhizoctonia solani, with an IC50 of 72 μM . Validamycin A is a reversible tyrosinaseinhibitor, with a Ki of 5.893 mM .
Harringtonolide is a potent RACK1inhibitor (IC50=39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction between FAK and RACK1. Harringtonolide has plant growth inhibitory, antiviral, anti-inflammatory, and antiproliferation activities .
Magnoloside B is an α-glucosidaseinhibitor (IC50=0.69 mM), which can be obtained from Magnolia officinalis stem bark. Magnoloside B shows moderate inhibitoryactivity against MGC-803 and HepG2 cells. Magnoloside B has the potential to study cancer and diabetes .
Alternaphenol B2 is a selective IDH1inhibitor from the coral-derived fungus Parengyodontium album SCSIO SX7W11. Alternaphenol B2 shows inhibitoryactivity against isocitrate dehydrogenase mutant R132H (IDH1m), with IC50 values of 41.9 μM .
Sartorypyrone A (20-O-Acetylsartorypyrone D) is a monocyclic terpenoid isolated from the soil fungus Neosartorya fischeri. Sartorypyrone A exhibits in vitro growth inhibitoryactivity against MCF-7, NCI-H460, and A375-C5 cell lines, and has potential anticancer properties.
20(R)-Ginsenoside Rg2 (Standard) is the analytical standard of 20(R)-Ginsenoside Rg2. This product is intended for research and analytical applications. 20(R)-Ginsenoside Rg2 shows inhibitory effects on lung cancer NCI-H1650 cells. Anti-cancer activities .
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
PC-766B is a macrolide antibiotic. PC-766B is active against Gram-positive bacteria, and some fungi and yeasts, but inactive against Gram-negative bacteria. PC-766B shows antitumor activity against murine tumor cells. PC-766B has weak inhibitoryactivity against Na +, K +-ATPase .
Kaempferol 3-O-gentiobioside (Standard) is the analytical standard of Kaempferol 3-O-gentiobioside. This product is intended for research and analytical applications. Kaempferol 3-O-gentiobioside is a flavonoid isolated from C. alata leaves with antidiabetic activity. Kaempferol 3-O-gentiobioside possesses activity against α-glucosidase and displays carbohydrate enzyme inhibitory effect with an IC50 of 50.0 μM .
Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
Pterostilbene is a stilbenoid isolated from blueberries and Pterocarpus marsupium . Shows anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic and anti-obesity properties . Pterostilbene blocks ROS production , also exhibits inhibitoryactivity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide .
Lyoniside is a lignan glycoside with antioxidant, allelopathic and antifungal activities, which can be isolated from the rhizomes and stems of bilberry (Vaccinium myrtillus L.). Lyoniside exhibits radical scavenging properties with an IC50 value of 23 μg/mL in DPPH assay. Lyoniside inhibits the mycelial growth of Fusarium oxysporum and Mucor hiemalis at 50 μg/mL with inhibitory rates of 78% and 80%, respectively .
Protoapigenone is an antineoplastic agent isolated from ferns. Protoapigenone has significant inhibitoryactivity against Hep G2, Hep 3B, MCF-7, A549 and MDAMB-231, with IC50s values of 1.60, 0.23, 0.78, 3.88 and 0.27 μg/mL respectively .
Majoranaquinone exhibits a high antibacterial effect against 4 Staphylococcus, 1 Moraxella, and 1 Enterococcus strains. Majoranaquinone shows substantial efflux pump inhibitoryactivity in Escherichia coliATCC 25922 strain. Majoranaquinone is found to be an effective biofilm formation inhibitor on E.coli, ATCC 25922 and E. coli K-12 AG100 bacteria .
Altromycin F is an anthraquinone-derived antibiotic produced by the actinomycete AB 1246E-26 isolated from a South African bush soil. Altromycin F has antibacterial activity against Gram-positive bacteria, particularly Streptococcus and Staphylococcus, with a microbial inhibitory concentration (MIC) ranging from 0.2-3.12 μg/mL .
Talaroterphenyl A (compound 1) is a p-terphenyl derivative present in the mangrove sediment-derived fungus Talaromyces sp. SCSIO 41412, which exhibits phosphodiesterase 4 (PDE4) inhibitoryactivity (IC50=1.2 μM). Talaroterphenyl A also exhibits anti-inflammatory and anti-fibrotic activities, significantly reducing the mRNA levels of pro-inflammatory cytokines IL-6, TNF-α, and IL-1β .
Kanamycin (Kanamycin A) sulfate is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin sulfate shows good inhibitoryactivity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
Medicagenic acid (Standard) is the analytical standard of Medicagenic acid. This product is intended for research and analytical applications. Medicagenic acid (Castanogenin) is isolated from the roots of Herniaria glabra, exhibits potent fungistatic effects against several plant pathogens and human dermatophytes . Medicagenic acid (Castanogenin) has low enzyme inhibitoryactivities, the target enzymes are xanthine oxidase, collagenase, elastase, tyrosinase, ChE .
(E/Z)-Aureusidin is a flavonoid compound with antioxidant activity. (E/Z)-Aureusidin can inhibit the production of reactive oxygen species and reduce cell damage. (E/Z)-Aureusidin has anti-inflammatory effects and can reduce the expression of inflammatory factors. (E/Z)-Aureusidin has inhibitory effects on a variety of bacteria, indicating its potential antimicrobial properties .
2-Hydroxycinnamic acid (Standard) is the analytical standard of 2-Hydroxycinnamic acid. This product is intended for research and analytical applications. 2-Hydroxycinnamic acid is a phenolic acid with antimicrobial and antioxidant properties. 2-Hydroxycinnamic acid has antimicrobial activity against Staphylococcus aureus and is not susceptible to drug resistance. 2-Hydroxycinnamic acid shows inhibitory effects on infection of HIV/SARS-CoV S pseudovirus with an IC50 of 0.3 mM. In addition, 2-Hydroxycinnamic acid has neuroprotective and antitumor activity .
Ganoderic acid SZ is a natural product with 3-hydroxy-3-methylglutaryl-CoA reductase inhibitoryactivity. Ganoderic acid SZ shows stronger activity than the positive control atorvastatin in inhibiting HMG-CoA reductase. Ganoderic acid SZ exhibits significant inhibition of yeast-derived α-glucosidase with IC50 values achieved at very low concentrations. Ganoderic acid SZ also exhibits cytotoxicity against K562 cells with IC?? values in the range of 10-20 μM .
Pseudouridimycin (PUM) is an antibiotic that selectively inhibits bacterial RNA polymerase (RNAP), with an IC50 of about 0.1 μM and a minimum inhibitory concentration (MIC) of 4 - 6 μg/mL. Pseudouridimycin is a C-nucleoside analogue that's effective against both Gram-negative and Gram-positive bacteria. Pseudouridimycin inhibits bacterial growth in vitro and shows activity in a mouse model of purulent streptococcal peritonitis .
Moracin P is a 2-arylbenzofuran isolated from the Mori Cortex Radicis. Moracin P exhibits potent in vitro inhibitoryactivity against hypoxia-inducible factor (HIF-1). Moracin P reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin P has neuroprotective and anti-inflammatory effects .
Moracin O is a 2-arylbenzofuran isolated from the Morus alba Linn. . Moracin O exhibits potent in vitro inhibitoryactivity against hypoxia-inducible factor (HIF-1). Moracin O reduces oxygen-glucose deprivation (OGD)-induced reactive oxygen species (ROS) production. Moracin O has neuroprotective and anti-inflammatory effects .
1-Methyl-2-nonyl-4(1H)-quinolone, a quinolone alkaloid, is a potent and selective MAO-B (monoamine oxidase) inhibitor. 1-Methyl-2-nonyl-4(1H)-quinolone exhibites inhibitoryactivity on leukotriene biosynthesis, with an IC50 of 12.1 μM .
N6-Benzyladenosine is an adenosine receptor agonist, has a cytoactive activity. N6-Benzyladenosine arrests cell cycle at G0/G1 phase and induces cell apoptosis. N6-Benzyladenosine also exerts inhibitory effect on T. gondii adenosine kinase and glioma - .
2-Hydroxy-3-methylanthraquinone (compound 1) is a natural compound isolated from a water extract of Hedyotis diffusa WILLD. 2-Hydroxy-3-methylanthraquinone shows inhibitoryactivity against protein tyrosine kinases v-src and pp60src, and induces growth arrest and apoptosis in the HepG2 cancer cells .
δ-Viniferin is a resveratrol dehydrodimer, an isomer of ε-Viniferin (HY-N3841) . ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol, displays a potent inhibitory for all the CYPactivities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity.
Tricetin 3',4',5'-trimethyl ether (5,7-Dihydroxy-3',4',5'-trimethoxyflavone) is a flavone glucoside, that can be isolated the flowers of Chrysanthemum sinensea. Tricetin 3',4',5'-trimethyl ether displays xanthine oxidase competitive-type inhibitoryactivity, with an IC50 of 0.51 μM and a Ki of 0.37 μM .
Halociline, a derivative of alkaloids, that can be isolated from the marine fungus Penicillium griseofulvum.
Halociline targets MAPK1, MMP-9, and PIK3CA in gastric cancer cells, potentially mediated by diverse pathways including cancer, lipid metabolism, atherosclerosis, and EGFR tyrosine kinase inhibitor resistance. Halociline possesses antimicrobial, antioxidant and biofilm inhibitoryactivities .
Apiin (Standard) is the analytical standard of Apiin. This product is intended for research and analytical applications. Apiin, a major constituent of Apium graveolens leaves with anti-inflammatory properties. Apiin shows significant inhibitoryactivity on nitrite (NO) production (IC50 = 0.08 mg/mL) in-vitro and iNOS expression (IC50 = 0.049 mg/ mL) in LPS-activated J774.A1 cells .
Pogostone (Standard) is the analytical standard of Pogostone. This product is intended for research and analytical applications. Pogostone is isolated from patchouli oil?with anti-bacterial and anti-cancer activities.?Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 μg/ml .?Pogostone induces cell apoptosis and autophagy .
(Rac)-Ganoderic acid C2 is the racemate of Ganoderic acid C2 (HY-N1517). Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses anti-tumor, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitoryactivity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM[ .
Sophoflavescenol is a prenylated flavonol, which shows great inhibitoryactivity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
2′-Hydroxygenistein is a natural product that can be isolated from Crotalaria pallida and C. assamica. 2′-Hydroxygenistein shows anti-inflammatory activity. 2′-Hydroxygenistein shows significant concentration-dependent inhibitory effects on the release of β-glucuronidase and lysozyme from rat neutrophils, with IC50 values of 5.9 ± 1.4 and 9.7 ± 3.5 μM, respectively .
Waldiomycin is an antibiotic that can be isolated from Streptomyces sp. MK844-mF10 that has inhibitory effects on low GC-content Gram-positive bacteria. Waldiomycin inhibits the activity of WalK kinase by targeting its ATP-binding domain, thereby blocking the WalK/WalR signal transduction system, which plays a role in cell growth and division .
Silydianin (Standard) is the analytical standard of Silydianin. This product is intended for research and analytical applications. Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 17.38?μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products .
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta .
Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models , has selective inhibitoryactivity towards cyclooxygenase-2 (COX-2) .
Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways .
Zingibroside R1 is dammaranae-type triterpenoid saponin, isolated from rhizomes, taproots, and lateral roots of Panax japonicas C. A. Meyer, shows excellent anti-tumor effects as well as anti-angiogenic activity .
Zingibroside R1 possesses some anti-HIV-1activity.
Zingibroside R1 has inhibitory effects on the 2-deoxy-D-glucose (2-DG) uptake by EAT cells (IC50=91.3 μM) .
Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro .
Validamycin A (Standard) is the analytical standard of Validamycin A. This product is intended for research and analytical applications. Validamycin A, a fungicidal, is an agricultural antibiotic. Validamycin A is originally isolated from Streptomyces hygroscopicus var. limoneus. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL . Validamycin A shows potent inhibitoryactivity against trehalase of Rhizoctonia solani, with an IC50 of 72 μM . Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM .
Evoxine (Haplophytin B) is a compound that selectively inhibits CO2-induced immunosuppression and has activity in inhibiting the expression of interleukin-6 and chemokine CCL2 in human THP-1 macrophages. Evoxine shows antimicrobial activity against a wide range of bacteria, especially performing well in minimum inhibitory concentration (MIC) tests against Escherichia coli, Bacillus subtilis, and Staphylococcus aureus. Evoxine extracts may find application in crude drug preparations in West Africa, provided that their in vivo toxicity results are negative .
11(α)-Methoxysaikosaponin F is a triterpenoid saponin isolated from Bupleurum marginatum Wall.ex DC(ZYCH) which is a promising therapeutic for liver fibrosis. 11(α)-Methoxysaikosaponin F has an IC50 of 387.7 nM with viability of hepatic stellate cells-T6 (HSCs-T6). Triterpenoid saponins have numerous targets, important network positions, and strong inhibitoryactivity .
(4Z)-Lachnophyllum lactone is a enyne derivative. (4Z)-Lachnophyllum lactone shows growth inhibitoryactivity against Lemna paucicostata (IC50=104 μM), which is a problematic and invasive weed . (4Z)-Lachnophyllum lactone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
3-Acetyl-11-keto-ursolic acid (Compound 18) is a triterpenoid compound derived from Eriobotrya japonicaleaves. 3-Acetyl-11-keto-ursolic acid has 11B-hydroxysteroid dehydrogenase 1 (11b-HSD1) inhibitoryactivity. 3-Acetyl-11-keto-ursolic acid can be used for anti-diabetes research .
Mollicellin H is a secondary metabolite of the fungus C. brasiliense and has a wide range of biological activities, including immunomodulation, cytotoxicity and anti-tumor effects. The growth inhibitory effects (GI50s) of Mollicellin H on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines are 5.1 μg/mL, 6.5 μg/mL and 2.5 μg/mL respectively .
Milbemycin oxime (Standard) is the analytical standard of Milbemycin oxime. This product is intended for research and analytical applications. Milbemycin oxime is an orally active macrolide with broad-spectrum antiparasitic activity. Milbemycin oxime is a mixture of oximes consisting of oxime derivatives corresponding to milbemycin A4 and A3. Milbemycin oxime binds to glutamate-gated chloride channels and has inhibitory potency against intestinal nematodes and lung/heart worms .
Pterostilbene (Standard) is the analytical standard of Pterostilbene. This product is intended for research and analytical applications. Pterostilbene is a stilbenoid isolated from blueberries and Pterocarpus marsupium . Shows anti-oxidant, anti-inflammatory, anti-carcinogenic, anti-diabetic and anti-obesity properties . Pterostilbene blocks ROS production , also exhibits inhibitoryactivity against various free radicals such as DPPH, ABTS, hydroxyl, superoxide and hydrogen peroxide .
11-oxo-mogroside V (Standard) is the analytical standard of 11-oxo-mogroside V. This product is intended for research and analytical applications. 11-oxo-mogroside V is a natural sweetener that exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2-, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
Oroxylin A-7-O-glucuronide (Standard) is the analytical standard of Oroxylin A-7-O-glucuronide. This product is intended for research and analytical applications. Oroxylin A-7-O-glucuronide (Oroxyloside; Oroxylin A-7-O-β-D-glucuronide) is a flavonoid glucuronide isolated from the dried root of Scutellaria baicalensis, with prolyl oligopeptidase (POP) inhibitoryactivity .
Ganoderic acid C2 (Standard) is the analytical standard of Ganoderic acid C2. This product is intended for research and analytical applications. Ganoderic acid C2 is a bioactive triterpenoid in Ganoderma lucidum. Ganoderic acid C2 possesses the potential anti-tumor bioactivity, antihistamine, anti-aging and cytotoxic effects. Ganoderic acid C2 exhibits high inhibitoryactivity against the rat lens aldose reductase (RLAR) with an IC50 of 3.8 µM .
3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidaseinhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL .
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitoryactivity against mushroom tyrosinase with an IC50 of 53.6 μM .
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM . Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL . Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM .
5,7,3' -tri-O-Methyl (-)-epicatechin (Compound 13) is a phospholipase Cγ1 (PLCγ1) inhibitor. 5,7,3' -tri-o-methyl (-)-epicatechin has a methylene dioxy benzene ring and can express inhibitoryactivity against PLCγ1. 5,7,3' -tri-O-Methyl (-)-epicatechin can be used in the study of chemotherapy and chemopexic agents for cancer .
Angeloylbinankadsurin A (compound 7) is an anti-rheumatoid arthritis (RA) agent that can be isolated from EtOAc and CH2Cl2 extracts of Black Tiger Beard. Angeloylbinankadsurin A exhibits inhibitoryactivity on RA-FLS cells (IC50=11.70 μM). Angeloylbinankadsurin A is slightly toxic to human cancer cell lines (Hela and BGC-823) (IC50=19.9 μM, 21.93 μM) .
ε-Viniferin (Standard) is the analytical standard of ε-Viniferin. This product is intended for research and analytical applications. ε-Viniferin (epsilon-Viniferin), the dimer of Resveratrol and can be isolated from Vitis vinifera, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative capacity .
3β-Acetoxy-hop-22(29)-ene (compound 1) is a potent anti-inflammatory agent. 3β-Acetoxy-hop-22(29)-ene shows high inhibitoryactivity of yeast α-glucosidase, with an IC50 of 5.74 μM. 3β-Acetoxy-hop-22(29)-ene inhibitsMPO (myeloperoxidase) activity in a dose-dependent manner in mouse ear edema model induced by 12-O-tetradecanoylphorbol acetate (TPA), with an IC50 of 0.23 μmol/ear .
Norartocarpetin is a tyrosinaseinhibitor. Norartocarpetin has strong tyrosinase inhibitoryactivity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
(±)-Aiphanol is a newly discovered stilbenolignan analog. (±)-Aiphanol exhibits significant anti-inflammatory activity, acting through inhibition of COX-1 and COX-2. The inhibitory effect on COX-1 (IC50 = 1.9 μM) is particularly strong, while the effect on COX-2 (IC50= 9.9 μM) is relatively weak .(±)-Aiphanol effectively inhibitsVEGFR2 (IC50=0.92 µM). (±)-Aiphanol blocks angiogenesis and promotes apoptosis through inhibition of VEGFR2 and COX2 activity. (±)-Aiphanol is orally active .
Esculentoside A (Standard) is the analytical standard of Esculentoside A. This product is intended for research and analytical applications. Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta .
Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models , has selective inhibitoryactivity towards cyclooxygenase-2 (COX-2) .
Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways .
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specificinhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitoryactivity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively . Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitoryactivity against HBV replication .
Tropolone is a seven-membered non-benzenoid aromatic compound, which is the precursor of many Azulene derivatives. Tropolone is a potent mushroom tyrosinaseinhibitor with an IC50 value of 0.4 μM. Its inhibitory effect can be achieved by dialysis or excess CU 2+ Reversa. Tropolone exhibits broad anti-viral and anti-fungal activity and is synergistic upon co-treatment with nucleos(t)ide analog drugs. Tropolone is a promising candidate for research in osteosarcoma .
(24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid is a potent PTP1Binhibitor, with an IC50 of 0.4 μM. (24E)-3,4-Secocucurbita-4,24-diene-3,26,29-trioic acid exhibits potent PTP1Binhibitoryactivity without cytotoxicity .
Ginsenoside Rb3 (Standard) is the analytical standard of Ginsenoside Rb3. This product is intended for research and analytical applications. Ginsenoside Rb3 is extracted from steamed Panax ginseng C. A. Meyer. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
Neodidymelliosides A (compound 1)It is a secondary metabolite of fungi and has a significant inhibitory effect on Staphylococcus aureus and Candida albicans biofilms. Neodidymelliosides AIt also has anti-cancer activity and can inhibit KB3.1 (cervix),PC-3 (prostate),MCF-7(breast),SKOV-3 (ovary),A431 (skin )and A549 (lung )Cell viability of cell lines .
Methyl 5-hydroxy-1H-indole-3-carboxylate is a marine natural product with isocitrate lyase inhibitoryactivity. Methyl 5-hydroxy-1H-indole-3-carboxylate is found in Hyrtios erectus. Methyl 5-hydroxy-1H-indole-3-carboxylate can be used to study its interaction with specific biological targets .
Kanamycin (sulfate) (Standard) is the analytical standard of Kanamycin (sulfate). This product is intended for research and analytical applications. Kanamycin (Kanamycin A) sulfate is an orally active antibacterial (gram-negative/positive bacteria) agent, inhibits translocation and causes misencoding by binding to the 70 S ribosomal subunit. Kanamycin sulfate shows good inhibitoryactivity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
Angiotensin 1-7 (Ang-(1-7)) is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 inhibits purified canine ACEactivity (IC50=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 μM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 μM) . Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis . Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo .
Angiotensin 1-7 (Ang-(1-7)) acetate is an endogenous heptapeptide from the renin-angiotensin system (RAS) with a cardioprotective role due to its anti-inflammatory and anti-fibrotic activities in cardiac cells. Angiotensin 1-7 acetate inhibits purified canine ACEactivity (IC50=0.65 μM). Angiotensin 1-7 acetate acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 acetate blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium .
Harpagoside can be obtained by Harpagophytum procumbens, which has anti-inflammatory, anti-cancer, protective activity, and efficacy. Harpagoside has an inhibitory effect on COX-1 and COX-2 active, and suppresses NO production. Harpagoside inhibits HepG2 cell lipid polysaccharide, which is a protein that is expressed horizontally and selectively, and has anti-inflammatory and latent pain effects. Harpagoside has the ability to protect the body, and has a degenerative effect on the β-oxidation (Aβ) .
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects . Mulberroside A shows inhibitoryactivity against mushroom tyrosinase with an IC50 of 53.6 μM .
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterialactivity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains .
8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide (compound 3), a sesquiterpene, has anti-LIMK1activity. 8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide has inhibitory property on cell motility .
Lucidone, an anti-inflammatory agent that can be isolated from the fruit of Lindera erythrocarpa Makino. Lucidone inhibits LPS-induced NO and PGE2 production in RAW 264.7 mouse macrophages. Lucidone also decreases TNF-α secretion, iNOS and COX-2 expression. Lucidone prevents NF-κB translocation and inhibitsJNK and p38MAPK signals. Lucidone also has inhibitoryactivity against Dengue virus (DENV) (EC50=25 μM) .
Bavachalcone (Standard) is the analytical standard of Bavachalcone. This product is intended for research and analytical applications. Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro .
Arcopilin A (compound Arcopilin A(1))is an antibacterial agent. Arcopilin A has weak inhibitory effects on fungal pathogens and Gram-positive bacteria, with IC50 values of 8.9 μg/mL and 14 μg/mL for cells KB-3-1 and L929, but it can effectively destroy preformed biofilms of Staphylococcus aureus. Arcopilin A can enhance the activities of gentamicin (GM; HY-K1050) and vancomycin (Vac; HY-B0671) by 115 and 31 times, respectively .
Racemomycin B (229-B; Streptothricin D), the main component from Streptomyces lavendulae OP-2, is a streptothricin antibiotic containing three β-lysine groups. RM-B exhibits antimicrobial activity against plant pathogenic microorganisms and effectively inhibits the growth of Brassica rapa L. roots at 50 ppm. RM-B showed a minimum inhibitory concentration (MIC) of 0.4 μg/ml against Pseudomonas syringae pv. tabaci IFO-3508 and a MIC range of 0.1-2.0 μg/ml against six strains of Fusarium oxysporum, showing stronger antimicrobial activity than RM-A and RM-C. The biological activity of racemomycin compounds increases with the increase in the number of β-lysine groups.
Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects.
Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibitsactivities of p38 MAPK and NF-kB [5][6], exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity . Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.
(±)-Catechin (rel-Cianidanol) This is a green tea polyester. Catechin possesses anti-cancer activity, which has led to its demise. (±)-Catechin 具有两种forms (+)-Catechin and its reflection body (-)-Catechin. (+)-Catechin inhibitory environment-1 (COX-1) IC50 为 1.4 μM. (-)-Catechin has the effect of promoting hBM-MSC adipose cell differentiation, increasing adipose tissue, and PPARγ horizontal. (±)-Catechin has anti-diabetic, anti-hypertrophic, anti-diabetic, anti-cardiovascular, anti-infective, and liver-protecting effects.
4-Hydroxycanthin-6-one is a novel quinoline alkaloid isolated from the stem bark of the tree Ailanthus altissima. Five other known compounds were also found in the study. The structures of the new compounds were determined by interpretation of physical and spectroscopic data, and their absolute configurations were determined by electronic circular dichroism spectroscopy and quantum chemical calculations. These compounds showed significant inhibitoryactivity against lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, showing potential anti-inflammatory properties .
Curcumin (Standard) is the analytical standard of Curcumin. This product is intended for research and analytical applications. Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
Mulberroside A (Standard) is the analytical standard of Mulberroside A. This product is intended for research and analytical applications. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitoryactivity against mushroom tyrosinase with an IC50 of 53.6 μM .
4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) is an antioxidant, can be isolated from Gynura divaricata and Laggera alata. 4,5-Dicaffeoylquinic acid reduces islet cell apoptosis and improves pancreatic function in type 2 diabetic mice, and has obvious inhibitoryactivities against yeast α-glucosidase. 4,5-Dicaffeoylquinic acid inhibits prostate cancer cells through cell cycle arrest. 4,5-Dicaffeoylquinic acid also has anti-apoptotic, anti-injury and anti-hepatitis B virus effects .
3,4-Dicaffeoylquinic acid (Standard) is the analytical standard of 3,4-Dicaffeoylquinic acid. This product is intended for research and analytical applications. 3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidase inhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL .
Harpagoside (Standard) is the analytical standard of Harpagoside. This product is intended for research and analytical applications. Harpagoside can be obtained by Harpagophytum procumbens, which has anti-inflammatory, anti-cancer, protective activity, and efficacy. Harpagoside has an inhibitory effect on COX-1 and COX-2 active, and suppresses NO production. Harpagoside inhibits HepG2 cell lipid polysaccharide, which is a protein that is expressed horizontally and selectively, and has anti-inflammatory and latent pain effects. Harpagoside has the ability to protect the body, and has a degenerative effect on the β-oxidation (Aβ) .
Isoscopoletin (Standard) is the analytical standard of Isoscopoletin. This product is intended for research and analytical applications. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively . Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitoryactivity against HBV replication .
Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitoryactivity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
3-O-β-D-Glucopyranosyl(1→2)-[a-Lrhamnopyranosyl(1→3)]-β-D-glucopyranosyl 28-O-β-D-glucuronopyranoside, a saponin, is isolated from Polaskia chichipe Backbg. 3-O-β-D-Glucopyranosyl(1→2)-[a-Lrhamnopyranosyl(1→3)]-β-D-glucopyranosyl 28-O-β-D-glucuronopyranoside shows ability to inhibit melanin biosynthesis by B16 melanoma cell with inhibitoryactivity 84.2% at 100μM[1].
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitoryactivity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
1,3,5-Trihydroxy-4-prenylxanthone is a Na +/H + exchange system (Na+/H+ Exchanger (NHE)) inhibitor with a minimum inhibitory concentration of 10 μg/mL . 1,3,5-Trihydroxy-4-prenylxanthone is a phosphodiesterase type 5 (PDE5) (Phosphodiesterase (PDE)) inhibitor with an IC50 value of 3.0 μM . 1,3,5-Trihydroxy-4-prenylxanthone inhibits Lipopolysaccharide (LPS) (Lipopolysaccharides (HY-D1056))-induced NO production in RAW264.7 macrophages, and has anti-inflammatory activities .
3-O-6-Deoxy-3-O-methyl-β-D-allopyranosyl-(1→4)-β-D-oleandropyranosyl-tenacigenin C can be isolated from Alocasia cucullata (Lour.) G. Don. 3-O-6-Deoxy-3-O-methyl-β-D-allopyranosyl-(1→4)-β-D-oleandropyranosyl-tenacigenin C has moderate tumor cells inhibitoryactivity against MGC-803 and HT-29 cells with IC50 values of 45.6 and 28.4 μg/mL, respectively .
AA-57 is an acidic lipophilic antibiotic isolated from the fermentation broth of Actinomycetes strain AA-57. The AA-57 strain was isolated from a soil sample collected in Koriyama City, Fukushima Prefecture, Japan. AA-57 has antibacterial properties against Gram-positive bacteria, Gram-negative bacteria, and acid-fast bacteria. AA-57 was discovered by screening actinomycete cultures for antibacterial properties. AA-57 exhibits significant antibacterial activity and has inhibitory effects against a variety of bacteria. The discovery of AA-57 provides new possibilities for antibacterial therapy.
Madecassoside (Standard) is the analytical standard of Madecassoside. This product is intended for research and analytical applications. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects.
Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibitsactivities of p38 MAPK and NF-kB , exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity[10]. Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.
(3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid, a lanostane triterpenoids, exhibits obvious NO inhibitoryactivity on n LPS-induced BV-2 microglia cells with an IC50 of 9.55 uM. (3β,7β,12β,20Z)-3,7,12-Trihydroxy-11,15,23-trioxo-lanost-8,20-dien-26-oic acid has anti-inflammatory activities .
Aspergillomarasmine A is a natural aminopolycarboxylic acid with potent inhibitoryactivity against class B metallo-β-lactamases (MBLs). Aspergillomarasmine A inactivates MBLs by removing a catalytic Zn2+ cofactor. Aspergillomarasmine A acts as a selective Zn2+ scavenger, promoting the dissociation of the metal cofactor, thereby indirectly inactivating NDM-1. Aspergillomarasmine A causes the loss of Zn2+ ions from the low-affinity binding site of NDM-1. The action of Aspergillomarasmine A results in the rapid degradation of Zn2+-deficient NDM-1, thereby enhancing its potency as a β-lactam enhancer. The mechanism of Aspergillomarasmine A has broad applicability among different Zn2+ chelators .
4,5-Dicaffeoylquinic acid (Standard) is the analytical standard of 4,5-Dicaffeoylquinic acid. This product is intended for research and analytical applications. 4,5-Dicaffeoylquinic acid (Isochlorogenic acid C) is an antioxidant, can be isolated from Gynura divaricata and Laggera alata. 4,5-Dicaffeoylquinic acid reduces islet cell apoptosis and improves pancreatic function in type 2 diabetic mice, and has obvious inhibitoryactivities against yeast α-glucosidase. 4,5-Dicaffeoylquinic acid inhibits prostate cancer cells through cell cycle arrest. 4,5-Dicaffeoylquinic acid also has anti-apoptotic, anti-injury and anti-hepatitis B virus effects .
Lornoxicam (Chlortenoxicam) is an orally active oxycontin nonsteroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory, antipyretic and anticancer activities. Lornoxicam exhibits good inhibitory effects on both COX-1 and COX-2 (COX-1: IC50=0.005 μM; COX-2:IC50=0.008 μM) and inhibits the production of NO by iNOS (IC50=65 μM) and the proinflammatory cytokine IL-6 (IC50=54 μM). Lornoxicam also inhibits tumor cell proliferation and migration and induces tumor cell apoptosis. Lornoxicam can be used in the study of inflammatory pain, colorectal cancer and breast cancer .
Dihydroberberine (Standard) is the analytical standard of Dihydroberberine. This product is intended for research and analytical applications. Dihydroberberine is a naturally occurring isoquinoline alkaloid with anti-inflammatory, anti-atherosclerotic, hypolipidemic and anti-tumor activities. Dihydroberberine inhibits the human ether-related gene (hERG) channel and significantly reduces the expression of heat shock protein 90 (Hsp90) and its interaction with hERG. Dihydroberberine also blocks the TLR4/MyD88/NF-κB signaling pathway to reduce pro-inflammatory cytokines and immunoglobulins, and has inhibitory effects on DSS (HY-116282C)-induced experimental colitis. Dihydroberberine also increases the sensitivity of lung cancer to sunitinib (HY-10255A), with synergistic efficacy .
(15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one shows a 5a-reductaseinhibitoryactivity with an IC50 value of 41.9 μM. (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one inhibits the growth of the ventral prostate induced by testosterone in rat. (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one is promising for research of benign prostatic hyperplasia (BPH) as well as other 5α-dihydrotestosterone (DHT)-related disorders, such as acne and male pattern baldness .
2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid, a natural ursane-type triterpene, is a potent inhibitor of HIV protease (HIV Protease). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid is also an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid displays an inhibitoryactivity against nitric oxide production in Lipopolysaccharide (Lipopolysaccharides)-activated RAW 264.7 cells .
1-Formyl-beta-carboline is an alkaloid with inhibitoryactivity against Newcastle disease virus (NDV). 1-Formyl-beta-carboline can effectively inhibit different genotypes of NDV with IC50 values within 10 μM, and its inhibition rate is more than 90% at a concentration of 20 μM. 1-Formyl-beta-carboline mainly exerts its effects by inhibiting the adsorption and entry processes in the NDV life cycle. 1-Formyl-beta-carboline has been identified as a novel HN inhibitor that can directly interact with the NDV HN protein and affect the adsorption of NDV. 1-Formyl-beta-carboline also inhibits the entry of NDV by inhibiting the PI3K/Akt signaling pathway rather than the ERK pathway .
Meridianin C is a marine natural product with anticancer activity. Meridianin C has significant inhibitory effects on four different human tongue cancer cells (YD-8, YD-10B, YD-38 and HSC-3). Meridianin C most strongly reduced the growth of YD-10B cells, the most aggressive and tumorigenic of the cell lines tested. Meridianin C also induced significant accumulation of large vesicles in YD-10B cells, validating its function through macrophagocytosis. Meridianin C reduces cellular levels of Dickkopf-related protein-3 (DKK-3), a known negative regulator of macrophagy. Meridianin C affects macrophagocytosis by downregulating DKK-3, thereby affecting cell proliferation .
Cuminaldehyde (Standard) is the analytical standard of Cuminaldehyde. This product is intended for research and analytical applications. Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC50= 0.00085 mg/mL) and α-glucosidase (IC50=0.5 mg/mL). Cuminaldehyde can modulate α-synuclein fibrils. Cuminaldehyde can induce apoptosis in colon adenocarcinoma cells by targeting topoisomerase I and II. In addition, Cuminaldehyde also exerts anti-inflammatory activity by inhibiting lipoxygenase. Cuminaldehyde has a strong inhibitory effect on the growth of Aspergillus flavus and the biosynthesis of aflatoxin B1 (AFB1). Cuminaldehyde can exert anti-injury and anti-neuropathy effects by participating in opioid receptors, L-arginine/NO/cGMP pathways and anti-inflammatory effects. Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases .
7,3',4'-Trihydroxy-3-benzyl-2H-chromene is an reversible noncompetitive neuraminidase (NA)inhibitor. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be isolated from the dried heartwood of Caesalpinia sappan L. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene has potent NAs inhibitoryactivities with IC50 values of 34.6 µM [H1N1], 39.5 µM [H3N2], and 50.5µM [H9N2], respectively. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be used for the research of influenza virus .
MIA proteins exhibit significant growth inhibitory effects on melanoma cells in vitro, extending their effects to various neuroectodermal tumors such as gliomas. In addition to playing an inhibitory role in cell growth, MIA proteins are also involved in molecular interactions, interacting with FASLG and TMIGD2. MIA Protein, Human (His) is the recombinant human-derived MIA protein, expressed by E. coli , with C-6*His labeled tag. The total length of MIA Protein, Human (His) is 107 a.a., with molecular weight of ~14.0 kDa.
MIA proteins exhibit significant growth inhibitory effects on melanoma cells in vitro, extending their effects to various neuroectodermal tumors such as gliomas. In addition to playing an inhibitory role in cell growth, MIA proteins are also involved in molecular interactions, interacting with FASLG and TMIGD2. MIA Protein, Human (N-His) is the recombinant human-derived MIA protein, expressed by E. coli , with N-6*His labeled tag. The total length of MIA Protein, Human (N-His) is 107 a.a., with molecular weight of ~14.0 kDa.
Otoraplin/OTOR Protein, Human (CHO) is a protein encoded by OTOR gene, is homologous to the protein encoded by CDRAP/MIA, and may acts in cartilage development and maintenance.
(±)-Taxifolin-13C3 ((±)-Dihydroquercetin-13C3) is a derivative of (±)-Taxifolin, labeled with 13C3. (±)-Taxifolin is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitoryactivity against collagenase with an IC50 value of 193.3 μM . Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity .
Eltrombopag- 13C4 (SB-497115- 13C4) is 13 sup>C-labeled Z-Eltrombopag. Z-Eltrombopag is an orally active thrombopoietin-receptor non-peptide agonist with platelet-stimulating activity for the study of chronic immune thrombocytopenia. Eltrombopag also has strong inhibitory effects on multidrug-resistant Staphylococcus aureus (Staphylococcus aureus) and can induce apoptosis (apoptosis) in liver cancer cells .
4-Ethyloctanoic acid- 13C2 is 13C labeled Cuminaldehyde (HY-Y0790). Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity .
PD-L1-IN-4 (Compound X18) is an orally active PD-L1inhibitor that exhibits remarkable inhibitoryactivity against the PD-1/PD-L1 interaction (IC50 = 1.3 nM) and enhances PD-L1 inhibitory effect on T cells (EC50 = 152.8 nM). PD-L1-IN-4 can be used for the research of cancer .
NDV-IN-1 is an antiviral agent with high neuraminidaseinhibitoryactivity. NDV-IN-1 exhibits in vitro inhibitoryactivity against Newcastle disease virus (NDV). NDV-IN-1 significantly inhibits NDV infection of Vero cells by preventing the release of virus particles from infected cells . Neuraminidase-IN-12 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
COX-2-IN-46 (compound 5m) is an anti-inflammatory agent with potent analgesic activity. COX-2-IN-46 exhibits a significant inhibitory effect on COX-2 (IC50=87.74 nM) .
COX-1-IN-2 (compound 5h) is an anti-inflammatory agent with potent analgesic activity. COX-1-IN-2 exhibits a significant inhibitory effect on COX-1 (IC50=38.76 nM) .
7ETMC is a cytochrome P450 inhibitor with selective inhibition of human cytochrome P450s 1A1 and 1A2. 7ETMC has inhibitory effects on P450s 1A1 and 1A2 with IC?? values of 0.46μM and 0.50μM, respectively, within the first six minutes, and has no inhibitoryactivity against P450s 2A6 and 2B1. Except for 7-ethynyl-3-methyl-4-phenylcoumarin, the remaining inhibitors show mechanism-based inhibition of P450s 1A1 and 1A2.
iNOS/COX-2-IN-3 (compound 7d) is a dual inhibitor of iNOS and COX-2, with potential anti-inflammatory activity against LPS (HY-D1056)-induced RAW 264.7 cells (IC50=3.48 μM). iNOS/COX-2-IN-3 has good plasma stability, oral activity and gastric safety, and its inhibitoryactivity on iNOS and COX-2 expression is 5.43-fold and 2.37-fold that of Indomethacin (HY-14397), respectively .
5-Phenyl-1-pentyne (Pent-4-ynylbenzene) is a compound with antibacterial and antitumor activity, which can effectively inhibit the growth of certain cancer cells. 5-Phenyl-1-pentyne is often used as a reaction intermediate in organic synthesis to promote a variety of chemical reactions. 5-Phenyl-1-pentyne is also used in the synthesis of new compounds to improve the bioavailability and inhibitory effect of the compounds.
TOP1210 is a narrow-spectrum tyrosine kinase inhibitor with potent inhibitoryactivity against P38α, Src, and Syk kinases. TOP1210 effectively reduced proinflammatory cytokines released by peripheral blood monocytes, primary macrophages, HT29 cells, inflammatory cells in ulcerative colitis (UC) biopsies, and myofibroblasts isolated from inflamed colonic UC mucosa. TOP1210 showed significant anti-inflammatory effects in cell experiments and UC biopsies, superior to some selective kinase inhibitors. The multi-kinase inhibition of TOP1210 provides the possibility of obtaining a wider range of therapeutic effects, especially in the regulation of autoimmune responses .
L-Adenosine is a metabolically stable enantiomeric analog and also is a potential probe. L-Adenosine has weakly inhibitoryadenosine deaminase (ADA)activity with an Ki value of 385 μM. L-Adenosine can be used for the research of adenosine uptake and accumulation .
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