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Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity .
Kevetrin hydrochloride is a potent activator of p53, induces apoptosis in TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells .
GSK2245035 is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 is used for asthma .
Rabacfosadine (GS-9219), a novel proagent of the nucleotide analogue PMEG, is designed as a cytotoxic agent that preferentially targets lymphoid cells.
GSK2245035 maleate is a highly potent and selective intranasal Toll-Like receptor 7 (TLR7) agonist with preferential Type-1 interferon (IFN)-stimulating properties. GSK2245035 maleate has pEC50s of 9.3 and 6.5 for IFNα and TFNα. GSK2245035 maleate effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood cell cultures. GSK2245035 maleate is used for asthma .
Rabacfosadine (GS-9219) succinate, a novel proagent of the nucleotide analogue PMEG, is designed as a cytotoxic agent that preferentially targets lymphoid cells .
{Boc}-Phe-Leu-Phe-Leu-Phe TFA is a formyl peptide receptor (FPR) family antagonist that preferentially inhibits activity triggered through the formyl peptide receptor .
A Aminopeptidase N (rat) (APN/CD13) is a Zn 2+ dependent membrane-bound ectopeptidase that degrades preferentially proteins and peptides with a N-terminal neutral amino acid .
{Boc}-Phe-Leu-Phe-Leu-Phe ({Boc}-FLFLF) is a formyl peptide receptor (FPR) family antagonist that preferentially inhibits activity triggered through the formyl peptide receptor .
Triacylglycerol lipase is an enzyme that preferentially hydrolyzes the outer links of triacylglycerols and acts only on the water-lipid interface. Pancreatic triacylglycerol lipase is the single most important determinant of lipid absorption .
WAY-PDA 641 is a potent and preferentialPDE-IV inhibitor, with an IC50 of 0.42 μM for canine trachealis PDE-IV. WAY-PDA 641 induces respiratory muscle relaxation and bronchodilation .
NSC 80467, a DNA damaging agent, selectively inhibits survivin. NSC 80467 preferentially inhibits DNA synthesis and results in induction of γH2AX and pKAP1, two markers of DNA damage .
G-Subtide is a G-substrate peptide localized in Purkinje cells of the cerebellum. G-Subtide has little activity distinct from background and is a preferentially phosphorylated peptide substrate of recombinant PfPKG2 protein .
113-N16B is an ionizable cationic lipid used for the generation of lipid nanoparticles (LNPs). 113-N16B delivers mRNA preferentially to pulmonary endothelial cells.
GS-829845 is a major, active metabolite of Filgotinib (HY-18300). GS-829845 is a JAK1preferential inhibitor but is approximately 10-fold less potent than the parent and with a longer half-life .
Celastrol (Standard) is the analytical standard of Celastrol. This product is intended for research and analytical applications. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration .
Corazonin is a highly conserved neuropeptide hormone of wide-spread occurrence in insects, serves a central regulator of caste identity and behavior in social insects. Corazonin is also preferentially expressed in workers and/or foragers from other social insect species .
CSK substrate is a specific substrate for C-terminal Src kinase (CSK), which binds CSK and downregulates the Src family members. CSK substrate preferentially phosphorylates certain amino acid residues that are distinct from the conserved Src C-terminal sequence .
D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis . D-Tetrahydropalmatine is a dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors . D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor .
Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes . Anabaseine is also a weak partial agonist at α4β2 nAChRs .
NAAA-IN-1 (Compound 1) is a potent and selective inhibitor of NAAA with an IC50 of 7 nM. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). NAAA-IN-1 has the potential for the research of inflammation and pain .
NAAA-IN-3 (Compound 17a) is a potent and selective inhibitor of NAAA with an IC50 of 50 nM. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). NAAA-IN-3 has the potential for the research of inflammation and pain .
BChE-IN-35 (Azo-9) is a BChE inhibitor. BChE-IN-35 has a dynamic cis/trans conformational change, where the cis isomer preferentially binds to BChE. BChE-IN-35 can be used in Alzheimer's disease (AD) research .
HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation .
PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells .
Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity . Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function .
Benzoquinoquinoxaline (BQQ) is a heterocyclic compound with an aminoalkyl side chain. Benzoquinoquinoxaline preferentially binds to DNA triplex structures, intercalates between the bases, thus, stabilising the triplex conformation. Conjugation of Benzoquinoquinoxaline to 1,10-phenanthroline specifically binds and cleaves double strand DNA at the site of formation of a triplex structure .
Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization .
GRP78-IN-2 (Compound FL5) is a GRP78 (Glucose Regulated Protein 78 kDa) inhibitor. GRP78-IN-2 preferentially targeting cell surface GRP78 and shows potent antiangiogenic and anticancer activities without affecting other normal cells .
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity .
Rp-8-CPT-cAMPS sodium, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS sodium preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI .
Rp-8-CPT-cAMPS, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI .
Dihydroeponemycin, an analogue of the antitumor and antiangiogenic natural product eponemycin, selectively targets the 20S proteasome. Dihydroeponemycin covalently modifies a subset of catalytic proteasomal subunits, binding preferentially to the IFN-gamma-inducible subunits LMP2 and LMP7. Dihydroeponemycin-mediated proteasome inhibition induces a spindle-like cellular morphological change and apoptosis .
ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2 .
AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP .
H-Gly-Arg-pNA hydrochloride (GR-pNA hydrochloride) is a colorimetric substrate for thrombin. H-Gly-Arg-pNA is preferentially bound by thrombin and cleaves the Gly-Arg (GR) peptide sequence, releasing p-nitroaniline (pNA) that can be detected colorimetrically at 405 nm. H-Gly-Arg-pNA hydrochloride is used as a fluorescent dye to measure thrombin activity .
Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models .
MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain .
RU 24969 is a preferential5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion .
BiP inducer X, a selective inducer of immunoglobulin heavy chain binding protein (BiP)/GRP78, is an effective ER (endoplasmic reticulum) stress inhibitor. BiP inducer X preferentially induces BiP with slight inductions of GRP94, calreticulin, and C/EBP homologous protein. BiP inducer X protects neurons from ER stress .
DAPI (dilactate) is a blue fluorescent dye that preferentially binds dsDNA and binds to minor groove AT clusters. DAPI (dilactate) is combined with dsDNA, and the fluorescence was enhanced about 20-fold. DAPI (dilactate) can be used to identify the cell cycle and specifically stains the nucleus but not the cytoplasm. DAPI (dilactate) form is more soluble in water than DAPI (dihydrochloride) form.
Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analogue. Dibutyryl-cGMP sodium preferentially activates cGMP-dependent protein kinase (PKG). Dibutyryl-cGMP sodium inhibits the release of [ 3H]-arachidonic acid from γ thrombin-stimulated human platelets. Dibutyryl-cGMP sodium induces peripheral antinociception via activation of ATP-sensitive K + channels .
RU 24969 hemisuccinate is a preferential5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 hemisuccinate could decrease fluid consumption and increase forward locomotion .
β-Endorphin, an endogenous opioid neuropeptide, is an opioid receptor agonist. β-Endorphin binds preferentially to μ-opioid receptors and is produced in certain neurons of the central and peripheral nervous system and is one of three endorphins produced in humans. β-Endorphin can be used to reduce stress and maintain homeostasis in the body and is involved in neurological pain perception regulation .
Mirogabalin (Standard) is the analytical standard of Mirogabalin. This product is intended for research and analytical applications. Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .
Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis .
Magainin 2 (Magainin II) is an?antimicrobial?peptide (AMP) isolated from the skin of the African clawed frog Xenopus laevis. Magainin 2 displays antibiotic activity against numerous gram-negative and gram-positive bacteria. Magainin 2 also is active against protozoa . Magainin 2 exerts its cytotoxicity effects by preferential interactions with anionic phospholipids abundant in bacterial membranes .
Bractoppin is a potent and selective agent-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC50: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response .
Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent INa induced by ATX-II (Nav 1.5 activator) or the SCN8A mutation N1768D with IC50 values of 141 nM and 75 nM, respectively. Relutrigine exhibits potent use-dependent block and reduces neuronal intrinsic excitability. Relutrigine has effective anticonvulsant activity .
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Ajmalicine (Standard) is the analytical standard of Ajmalicine. This product is intended for research and analytical applications. Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
(R)-AMG-193 is an isomer of AMG 193 (HY-153390). AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP .
m-PEG-OH (MW 20000) can be used as a macroinitiator to participate in the synthesis of amphiphilic block copolymers. Nanoscale micelles can be prepared by using amphiphilic block copolymers to deliver active drugs. Paclitaxel (HY-B0015), a hydrophobic anticancer agent encapsulated in micelles, has stronger activity in killing cancer cells than free Paclitaxel. And it preferentially accumulates in tumor tissue with only limited distribution in healthy organs.
m-PEG-OH (MW 10000) can be used as a macroinitiator to participate in the synthesis of amphiphilic block copolymers. Amphiphilic block copolymers can be used to prepare nanoscale micelles to deliver active drugs. Paclitaxel (HY-B0015), a hydrophobic anticancer agent encapsulated in micelles, has stronger activity in killing cancer cells than free Paclitaxel. And it preferentially accumulates in tumor tissue with only limited distribution in healthy organs.
m-PEG-OH (MW 1000) can be used as a macroinitiator to participate in the synthesis of amphiphilic block copolymers. Amphiphilic block copolymers can be used to prepare nanoscale micelles to deliver active drugs. Paclitaxel (HY-B0015), a hydrophobic anticancer agent encapsulated in micelles, has stronger cancer-killing activity than free Paclitaxel. And it accumulates preferentially in tumor tissues and has only limited distribution in healthy organs.
B7-33 is a single-chain relaxin mimetic. B7-33 is a selective relaxin receptor 1 (RXFP1) agonist. B7-33 binds to RXFP1 and preferentially activates thepERK pathway over cAMP in cells (with RXFP1 expression). B7-33 is an anti-fibrotic agent. B7-33 has cardioprotective effects .
GSD-11 is a potent and selective anti-austerity agent. GSD-11 inhibits the cell migration and colony formation of PANC-1 cells. GSD-11 inhibits the Akt/mTOR signaling pathway. GSD-11 has the potential for the research of pancreatic cancer[1].
DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia .
Filibuvir is an orally active, selective non-nucleoside inhibitor of the HCV nonstructural 5B protein (NS5B) RNA-dependent RNA polymerase (RdRp). Filibuvir binds noncovalently in the thumb II allosteric pocket of NS5B. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM for both isoforms, respectively . Filibuvir preferentially inhibits elongative RNA synthesis and potently decreases viral RNA accumulation .
Zaltoprofen- 13C,d3 is the 13C- and deuterium labeled Zaltoprofen. Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain[1][2][3].
ALDH1A inhibitor 673A is an ALDH1A inhibitor. ALDH1A inhibitor 673A inhibits all three ALDH1A family members (IC50: 246 nM, 230 nM, 348 nM for ALDH1A1, ALDH1A2, ALDH1A3 respectively. ALDH1A inhibitor 673A induces necroptotic cell death preferentially in CD133+ ovarian CSCs. ALDH1A inhibitor 673A also inhibits chemotherapy-resistant tumor growth .
Mirogabalin-13C2,d1 (Mixture of Diastereomers) is a C13 and deuterium labeled Mirogabalin. Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS .
CXM102 is an autophagy activator. CXM102 can induce autophagy in aged BMSCs, leading to the rejuvenation of BMSCs and preferential differentiation into osteoblasts. CXM102 promotes the nuclear translocation of transcription factor EB (TFEB) and the formation of osteoblasts. CXM102 can stimulate bone synthesis metabolism in middle-aged male mice, reduce bone marrow adipocytes, delay bone loss, lower serum inflammation levels, decrease organ fibrosis, and extend the lifespan of the mice .
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity .
JB170 is a potent and highly specific PROTAC-mediated AURORA-A (Aurora Kinase) degrader (DC50=28 nM) by linking Alisertib, to the Cereblon-binding molecule Thalidomide. JB170 preferentially binds AURORA-A (EC50=193 nM) over AURORA-B (EC50=1.4 µM). JB170-mediated S-phase arrest is caused specifically by AURORA-A depletion. JB170 has excellent ability to inhibit non-catalytic function of AURORA-A kinase .
(Z)-RG-13022 is a tyrosine kinase (TK) inhibitor, which inhibits preferentially the TK activity of the EGF receptor and inhibits EGF-stimulated growth of cultured cells. (Z)-RG-13022 exerts an IC50 of 11 μM for DNA synthesis in the HN5 cells, which is 3 times more potent than (E)-RG-13022 (IC50=38 μM). (Z)-RG-13022 can be used for research of breast cancer cells .
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation .
Propidium monoazide is a photoreactive DNA-binding dye that preferentially binds to dsDNA. Propidium monoazide (PMA) prevents DNA from dead bacteria from being amplified during the PCR. PMA-PCR enhanced both the specificity and the sensitivity of PCR . Propidium monoazide 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.
EAD1 TFA is an aluminum-activated malate transporter with activity in regulating corn ear development. EAD1 TFA is preferentially expressed in the xylem of immature ears and localized across the plasma membrane. The EAD1 TFA transports malic acid in the apical part of developing inflorescences, and its deletion results in reduced malic acid content in this part. The overexpression of EAD1 TFA was significantly positively correlated with ear length and the number of kernels per row. EAD1 TFA serves as a potential genetic resource to help improve grain yield in maize .
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor 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 inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins .
YM-244769 dihydrochloride is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 dihydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 dihydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 dihydrochloride can also increase urine volume and urinary excretion of electrolytes in mice .
YM-244769 is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 can also increase urine volume and urinary excretion of electrolytes in mice .
YM-244769 hydrochloride is a potent, selective and orally active Na +/Ca 2+ exchanger (NCX) inhibitor. YM-244769 hydrochloride preferentially inhibits NCX3 and suppresses the unidirectional outward NCX current (Ca 2+ entry mode), with IC50s of 18 nM and 50 nM, respectively. YM-244769 hydrochloride efficiently protects against hypoxia/reoxygenation-induced SH-SY5Y neuronal cell damage. YM-244769 hydrochloride can also increase urine volume and urinary excretion of electrolytes in mice .
Urocortin III (human) is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) selectively binds to type 2 CRF receptors with Ki values of 13.5, 21.7, and >100 nM for mCRF2β, rCRF2α, and hCRF1, respectively. Urocortin III (human) mediates somatostatin-dependent negative feedback control of Insulin (human) (HY-P0035) secretion .
Steffimycin B is an anthracycline bacterial metabolite originally isolated from Streptomyces. It binds to DNA, preferentially intercalating at sites containing cytosine and guanine.2 Steffimycin B is cytotoxic to MCF-7, KB, NCI-H187, and Vero cells (IC50s=3.5, 6.75, 3.28, and 10.5 μM, respectively). It is active against M. tuberculosis (MIC=5.2 nM), B. cereus (MIC=1.56 μg/mL), and P. falciparum (IC50=2.19 μM).
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM .
Ro 09-1428 is a broad-spectrum parenteral cephalosporin. Ro 09-1428 has potent antibacterial activities against Pseudomonas aeruginosa and Acinetobacter caloaceticus, with MIC90s of 0.39 and 6.25 μg/mL, respectively, better than Ceftazidime (HY-B0593). Additionally, Ro 09-1428 shows high activity against Escherichia coli, Kkbsielia pneumoniae, Proteus mirabilis, P. aeruginosa, staphylococci, and more. Ro 09-1428 preferentially attacks PBP 3 for target in E. coli and P. aeruginosa, which is promising for research of septicemias and serious P. aeruginosa infections .
Stachybotramide is a natural fungal metabolite with the property of modulating the activity of cholesteryl ester transfer protein (CETP). Stachybotramide stimulates the transfer of cholesteryl esters (CE) from high-density lipoprotein (HDL) to very-low-density lipoprotein (VLDL) and low-density lipoprotein (LDL), increasing the transfer efficiency by 1.3- to 1.5-fold. Stachybotramide slightly reduced the transfer of cholesteryl esters from LDL and VLDL to HDL at 0.5 mM. The effect of Stachybotramide on the transfer of triglycerides (TG) from HDL was not significant. By these results, Stachybotramide was shown to preferentially stimulate the CETP-mediated transfer of cholesteryl esters from HDL to VLDL and LDL .
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
cis-Lomibuvir (cis-VX-222) is the cis-isomer of Lomibuvir. Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis . cis-Lomibuvir is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects .
NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties .
DAPI (dilactate) is a blue fluorescent dye that preferentially binds dsDNA and binds to minor groove AT clusters. DAPI (dilactate) is combined with dsDNA, and the fluorescence was enhanced about 20-fold. DAPI (dilactate) can be used to identify the cell cycle and specifically stains the nucleus but not the cytoplasm. DAPI (dilactate) form is more soluble in water than DAPI (dihydrochloride) form.
Propidium monoazide is a photoreactive DNA-binding dye that preferentially binds to dsDNA. Propidium monoazide (PMA) prevents DNA from dead bacteria from being amplified during the PCR. PMA-PCR enhanced both the specificity and the sensitivity of PCR . Propidium monoazide 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.
Lyso BD-1, preferentially colocalized in lysosomes and lipid droplets, displays excellent photocytotoxicity (5.57 μM) on triple negative breast cancer cells under white light. Lyso BD-1 displays emission band at 560nm .
H-Gly-Arg-pNA hydrochloride (GR-pNA hydrochloride) is a colorimetric substrate for thrombin. H-Gly-Arg-pNA is preferentially bound by thrombin and cleaves the Gly-Arg (GR) peptide sequence, releasing p-nitroaniline (pNA) that can be detected colorimetrically at 405 nm. H-Gly-Arg-pNA hydrochloride is used as a fluorescent dye to measure thrombin activity .
113-N16B is an ionizable cationic lipid used for the generation of lipid nanoparticles (LNPs). 113-N16B delivers mRNA preferentially to pulmonary endothelial cells.
m-PEG-OH (MW 10000) can be used as a macroinitiator to participate in the synthesis of amphiphilic block copolymers. Amphiphilic block copolymers can be used to prepare nanoscale micelles to deliver active drugs. Paclitaxel (HY-B0015), a hydrophobic anticancer agent encapsulated in micelles, has stronger activity in killing cancer cells than free Paclitaxel. And it preferentially accumulates in tumor tissue with only limited distribution in healthy organs.
m-PEG-OH (MW 1000) can be used as a macroinitiator to participate in the synthesis of amphiphilic block copolymers. Amphiphilic block copolymers can be used to prepare nanoscale micelles to deliver active drugs. Paclitaxel (HY-B0015), a hydrophobic anticancer agent encapsulated in micelles, has stronger cancer-killing activity than free Paclitaxel. And it accumulates preferentially in tumor tissues and has only limited distribution in healthy organs.
m-PEG-OH (MW 20000) can be used as a macroinitiator to participate in the synthesis of amphiphilic block copolymers. Nanoscale micelles can be prepared by using amphiphilic block copolymers to deliver active drugs. Paclitaxel (HY-B0015), a hydrophobic anticancer agent encapsulated in micelles, has stronger activity in killing cancer cells than free Paclitaxel. And it preferentially accumulates in tumor tissue with only limited distribution in healthy organs.
{Boc}-Phe-Leu-Phe-Leu-Phe ({Boc}-FLFLF) is a formyl peptide receptor (FPR) family antagonist that preferentially inhibits activity triggered through the formyl peptide receptor .
Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
Magainin 2 (Magainin II) is an?antimicrobial?peptide (AMP) isolated from the skin of the African clawed frog Xenopus laevis. Magainin 2 displays antibiotic activity against numerous gram-negative and gram-positive bacteria. Magainin 2 also is active against protozoa . Magainin 2 exerts its cytotoxicity effects by preferential interactions with anionic phospholipids abundant in bacterial membranes .
RGD-targeted Proapoptotic Peptide is a peptide. The C-terminal RGD-4C peptide (ACDCRGDCFC) binds preferentially to integrins at sites of tumor angiogenesis.
{Boc}-Phe-Leu-Phe-Leu-Phe TFA is a formyl peptide receptor (FPR) family antagonist that preferentially inhibits activity triggered through the formyl peptide receptor .
G-Subtide is a G-substrate peptide localized in Purkinje cells of the cerebellum. G-Subtide has little activity distinct from background and is a preferentially phosphorylated peptide substrate of recombinant PfPKG2 protein .
Corazonin is a highly conserved neuropeptide hormone of wide-spread occurrence in insects, serves a central regulator of caste identity and behavior in social insects. Corazonin is also preferentially expressed in workers and/or foragers from other social insect species .
CSK substrate is a specific substrate for C-terminal Src kinase (CSK), which binds CSK and downregulates the Src family members. CSK substrate preferentially phosphorylates certain amino acid residues that are distinct from the conserved Src C-terminal sequence .
Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
β-Endorphin, an endogenous opioid neuropeptide, is an opioid receptor agonist. β-Endorphin binds preferentially to μ-opioid receptors and is produced in certain neurons of the central and peripheral nervous system and is one of three endorphins produced in humans. β-Endorphin can be used to reduce stress and maintain homeostasis in the body and is involved in neurological pain perception regulation .
Muscle homing peptide M12 can preferentially bind to surface protein of muscle cells. Muscle homing peptide M12 mediates enhanced cellular uptake of nanoparticles (NPs) in myoblasts in vitro. Muscle homing peptide M12 is covalently conjugated to PLGA-PEG NPs via the N-terminal α-amino groups of peptides using the N-hydroxysuccinimide ester reaction .
B7-33 is a single-chain relaxin mimetic. B7-33 is a selective relaxin receptor 1 (RXFP1) agonist. B7-33 binds to RXFP1 and preferentially activates thepERK pathway over cAMP in cells (with RXFP1 expression). B7-33 is an anti-fibrotic agent. B7-33 has cardioprotective effects .
Huwentoxin-IV is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV has analgesic effects on animal models of inflammatory and neuropathic pain .
Huwentoxin-IV TFA is a potent and selective sodium channel blocker, inhibits neuronal Nav1.7, Nav1.2, Nav1.3 and Nav1.4 with IC50s of 26, 150, 338 and 400 nM, respectively. Huwentoxin-IV TFA preferentially blocks peripheral nerve subtype Nav1.7 by binding neurotoxin receptor site 4. Huwentoxin-IV TFA has analgesic effects on animal models of inflammatory and neuropathic pain .
Urocortin III (human) is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III (human) preferentially binds and activates CRF-R2 and has a discrete central nervous system and peripheral distribution. Urocortin III (human) selectively binds to type 2 CRF receptors with Ki values of 13.5, 21.7, and >100 nM for mCRF2β, rCRF2α, and hCRF1, respectively. Urocortin III (human) mediates somatostatin-dependent negative feedback control of Insulin (human) (HY-P0035) secretion .
Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration .
D-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis . D-Tetrahydropalmatine is a dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors . D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor .
Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .
Magainin 2 (Magainin II) is an?antimicrobial?peptide (AMP) isolated from the skin of the African clawed frog Xenopus laevis. Magainin 2 displays antibiotic activity against numerous gram-negative and gram-positive bacteria. Magainin 2 also is active against protozoa . Magainin 2 exerts its cytotoxicity effects by preferential interactions with anionic phospholipids abundant in bacterial membranes .
Celastrol (Standard) is the analytical standard of Celastrol. This product is intended for research and analytical applications. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
Cimicifugoside, a triterpenoid isolated from Cimicifuga simplex, is a novel specific nucleoside transport inhibitor that displays synergistic potentiation of methotrexate cytotoxicity . Cimicifugoside shows immunosuppressive activity, which is preferentially directed toward B-cell function with larger doses being required for suppression of T-cell function .
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity .
Ajmalicine (Standard) is the analytical standard of Ajmalicine. This product is intended for research and analytical applications. Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
Stachybotramide is a natural fungal metabolite with the property of modulating the activity of cholesteryl ester transfer protein (CETP). Stachybotramide stimulates the transfer of cholesteryl esters (CE) from high-density lipoprotein (HDL) to very-low-density lipoprotein (VLDL) and low-density lipoprotein (LDL), increasing the transfer efficiency by 1.3- to 1.5-fold. Stachybotramide slightly reduced the transfer of cholesteryl esters from LDL and VLDL to HDL at 0.5 mM. The effect of Stachybotramide on the transfer of triglycerides (TG) from HDL was not significant. By these results, Stachybotramide was shown to preferentially stimulate the CETP-mediated transfer of cholesteryl esters from HDL to VLDL and LDL .
APEG1 Isoform 3 potentially regulates the growth and differentiation of arterial smooth muscle cells. APEG1 Protein, Human (His) is the recombinant human-derived APEG1 protein, expressed by E. coli , with C-His labeled tag. The total length of APEG1 Protein, Human (His) is 113 a.a., with molecular weight of ~15 kDa.
PRAME is located in the CRL2 E3 ubiquitin-protein ligase complex and directs ubiquitination and degradation, specifically targeting the truncated MSRB1/SEPX1 selenoprotein.It is recruited to active promoter regions and is involved in chromatin regulation.Melanoma antigen preferentially/PRAME, Human (His) is the recombinant human-derived Melanoma antigen preferentially/PRAME, expressed by E.coli , with N-6*His labeled tag.
Zaltoprofen- 13C,d3 is the 13C- and deuterium labeled Zaltoprofen. Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain[1][2][3].
Mirogabalin-13C2,d1 (Mixture of Diastereomers) is a C13 and deuterium labeled Mirogabalin. Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS .
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes . Talsaclidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Propidium monoazide is a photoreactive DNA-binding dye that preferentially binds to dsDNA. Propidium monoazide (PMA) prevents DNA from dead bacteria from being amplified during the PCR. PMA-PCR enhanced both the specificity and the sensitivity of PCR . Propidium monoazide 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.
HZ166 is a GABAA receptor subtype-selective benzodiazepine site agonist with preferential activity at α2- and α3-GABAA receptors. HZ166 shows anti-hyperalgesic effects . HZ166 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
113-N16B is an ionizable cationic lipid used for the generation of lipid nanoparticles (LNPs). 113-N16B delivers mRNA preferentially to pulmonary endothelial cells.
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