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Pristinamycin, produced by Streptomyces pristinaespiralis, is an orally active streptogramin-like antibiotic consisting of two chemically unrelated components: Pristinamycin I (PI) and Pristinamycin II (PII). Pristinamycin is highly active against many antibiotic-resistant pathogens, particularly Gram-positive bacteria, including Methicillin-resistantStaphylococcus aureus (MRSA), Vancomycin-resistantS. aureus (VRSA) and Enterococcus faecium (VREF) .
GTX-758 is an orally active, nonsteroidal, selective agonist of ERα. GTX-758 plays an important role in castration resistant prostate cancer (CRPC) research .
Cisplatin-resistant cells-IN-1 (Compound 8) has high cytotoxicity against Cisplatin (HY-17394)-resistant cells. Cisplatin-resistant cells-IN-1 reduces the metabolic activity effectively in the low nanomolar range (IC50: 0.14–1.79 μM in A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR cells) .
ZINC20451377 is a small molecule targeting hepatitis B (HBV) surface antigen (HBsAg) and can effectively inhibit wild-type hepatitis B and tenofovir (HY-13910)-resistant hepatitis B .
PPO-IN-15 (compound (R)-I-5) is a protoporphyrinogen IX oxidase (PPO) inhibitor that is effective against resistant weeds and safer in wheat and rice .
HBV-IN-22 (Compound LC5f) is an inhibitor of HBV DNA replication with IC50 values of 0.71 μM and 0.84 μM against wild-type and agent resistant HBV strains, respectively .
Lersivirine (UK-453061) is potent and selective non-nucleoside reverse transcription inhibitor (NNRTI; IC50=119 nM) with excellent efficacy against NNRTI-resistant viruses. Lersivirine exhibits potent antiretroviral activity against wild-type HIV virus and clinically relevant NNRTI-resistant strains .
MI-136 is an inhibitor of the menin-MLL protein-protein interaction (PPI), with an IC50 of 31 nM and a Kd of 23.6 nM. MI-136 shows to block AR signaling and has the potential for the study in castration-resistant tumors .
DMT-2'-F-iBu-G (5'-DMT-2'-F-ibu-dG) is a modified oligonucleotide. 2'-deoxy-2'-fluoro-modified oligonucleotides shows high nuclease resistant and retained exceptional binding affinity to the RNA targets .
Fast Red Violet LB is a dye for staining tartrate resistant acid phosphatase (TRAP). Fast Red Violet LB can be used for alkaline phosphatase (ALP) activity staining .
Fast Red Violet LB Zinc chloride is a stain that stains tartrate-resistant acid phosphatase (TRAP) and Fast Red Violet LB Zinc chloride can be used to stain alkaline phosphatase (ALP) activity .
GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway . MRSA:methicillin-resistantS. aureus; MSSA: methicillin-sensitive S. aureus
(Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule Erα biomodulator. (Rac)-ErSO-DFP againsts ERα+ breast cancer (including resistant tumors) by hyperactiving the Erα-dependent a-UPR (extracted from patent WO2022087234A1) .
EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC) .
DB07107 is a potent agent resistantT315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM .
Piperolactam A is a natural product that can be isolated from root of Piper betle. Piperolactam A exhibits promising leishmanicidal action against wild type and drug resistant strains of Leishmania donovani .
Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases .
Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases .
Rp-cAMPS triethylammonium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases .
Metyltetraprole is a promising fungicide with EC50 values of both 0.002 ppm against sensitive wild-type and G143A mutant of Zymoseptoria tritici. Metyltetraprole is effective against QoI (quinone outside inhibitor) resistant strains. Metyltetraprole inhibits the respiratory chain via complex III .
Nemadipine-A is a specific inhibitor of the EGL-19 L-type Ca 2+ channel . Nemadipine-A, a cell-permeable L-type calcium channel inhibitor, sensitizes TRAIL-resistant cancer cells to this ligand .
Dexelvucitabine (Reverset; d-d4FC), a Cytidine (HY-B0158) analog, is an orally active nucleoside reverse transcriptase inhibitor. Dexelvucitabine is a powerful agent against HIV-1-resistant viruses containing a thymidine analog and/or M184V mutation in the viral polymerase. Dexelvucitabine is a 2′-Deoxycytidine antiretroviral agent .
Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistantHIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV .
PC945, a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. PC945 is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively .
Antitubercular agent-29 (compound 6xa) is a potent agent resistant (DR) Mycobacterium tuberculosis (Mtb) inhibitor with MIC of 0.03 μg/mL against agent-susceptible (DS)-Mtb strains, MIC of 0.03-0.06 μg/mL against DR-Mtb strains, and favourable selectivity (SI>40) against Vero cells .
ACT-451840 is an orally active, potent and low-toxicity compound, showing activity against sensitive and resistant plasmodium falciparum strains. ACT-451840 targets all asexual blood stages of the parasite, has a rapid onset of action. ACT-451840 behaves in a way similar to artemisinin derivatives, with very rapid onset of action and elimination of parasite. ACT-451840 can be used for the research of malarial .
Dmt-2'fluoro-da(bz) amidite, an uniformly modified 2'-deoxy-2'-fluoro phosphorothioate oligonucleotide, is a nuclease-resistant antisense compound with high affinity and specificity for RNA targets. Dmt-2'fluoro-da(bz) amidite is also an intermediate for 5’-DMT-3’-phosphoramidite synthesis .
TP0586532 is a non-hydroxamate LpxC inhibitor (IC50=0.101 μM). TP0586532 as a compound with a low cardiovascular risk that is effective against K. pneumoniae, including resistant strains . TP0586532 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
FtsZ-IN-1 is a potent FtsZ inhibitor with quinolinium ring. FtsZ-IN-1 has stronger antibacterial activity against Gram-positive bacteria with MICs of 0.5-8 μg/mL. FtsZ-IN-1 significantly causes cell elongation of B. subtilis by enhancing FtsZ polymerization. FtsZ-IN-1 exhibits low hemolytic toxicity and low tendency to induce agent resistance. FtsZ-IN-1 has against drug-resistant bacteria activity .
Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC) .
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 inhibitory activity against HIV-1 WT and resistant strains with EC50s of 5.79 ~ 28.3 nM .
JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .
AKR1C3-IN-4 is a potent and selective aldo-keto reductase 1C3 (AKR1C3) inhibitor with an IC50 of 0.56 μM. AKR1C3-IN-4 has the potential for castrate resistant prostate cancer (CRPC) research .
JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC) .
MPD2 is a Cereblon-binding ligand-based PROTAC that degrades MPro, the main protease of SARS-CoV-2. MPD2 effectively reduced MPro protein levels in 293T cells in a time-dependent manner (DC50=296 nM). MPD2 exhibited potent antiviral activity against multiple SARS-CoV-2 strains and had enhanced potency against Nirmatrelvir (HY-138687) resistant strains. MPD2 provides a new direction for antiviral drug development against SARS-CoV-2 and other emerging coronavirus pathogens (Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker (HY-W275882)；Red: SARS-CoV-2 MPro Inhibitor MP18 (HY-158763)) .
Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains . Azvudine (hydrochloride) 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.
Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains . Azvudine 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.
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines .
Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .
JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .
JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .
Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
PTZ601 (SMP 601) is an antibiotic, which inhibits the gram-positive bacteria, including the Vancomycin (HY-B0671)-resistantEnterococcus faecium (VREF) and Methicillin (HY-121544)-resistantStaphylococcus aureus (MRSA). PTZ601 exhibits antimicrobial activity in infected mouse models .
GW695634 is an orally active prodrug of GW678248. GW695634 undergoes amidolysis in vivo to release the active ingredient GW678248, thereby inhibiting viral replication. GW678248 is a non-nucleoside reverse transcriptase inhibitor (NNRTi) with potent antiviral activity against Efavirenz (HY-10572)-resistant and Nevirapine (HY-10570)-resistantHIV and AIDS viruses .
Benzyldodecyldimethylammonium chloride dihydrate is a quaternary ammonium compound (QAC) and can be used as a biocide to target antibiotic-resistant bacteria, such as methicillin-resistant Staphylococcus aureus (MRSA), multidrug-resistant (MDR) P. aeruginosa et. al. Benzyldodecyldimethylammonium chloride dihydrate, an antimicrobial agent, bacteriostatic or bactericidal properties depending on the concentration.
Norvancomycin hydrochloride is suitable for endocarditis, osteomyelitis, pneumonia, sepsis or soft tissue infections caused by Staphylococcus aureus (including methicillin-resistant strains and multi-drug-resistant strains).
Bottromycin A2 is a natural antibiotic. Bottromycin A2 is active against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE) .
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats .
Fosfomycin (MK-0955) sodium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
Fosfomycin (MK-0955) tromethamine is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin tromethamine shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
Epoxiconazole, a fungicide, is a demethylation inhibitor of the Ergosterol biosynthesis pathway. Epoxiconazole exhibits strong inhibitory effects on both carbendazim-resistant and phenamacril-resistant isolates, and can be used for controlling many crop diseases .
Piperaquine tetraphosphate is a potent antimalaria agent. Piperaquine tetraphosphate shows inhibition for chloroquine-sensitive and the chloroquine-resistant isolates. Piperaquine tetraphosphate in combination with dihydroartemisinin has the potential for the research of chloroquine-resistant malaria .
Collinin is a anti-tubercular agent, it can be isolated from leaves of Z. schinifolium. Collinin has an excellent anti-tuberculosis effect against multidrug-resistant (MDR), extensively drug-resistant (XDR) strains .
ACT-387042 is a bacterial topoisomerase inhibitor with broad-spectrum activity against Gram-positive and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus and penicillin- and fluoroquinolone-resistant Streptococcus pneumoniae .
BE-12406B is an antitumor agent that can be found in the culture broth of a streptomycete. BE-12406B can inhibit the growth of Vincristine (HY-N0488)-resistant or Doxorubicin (HY-15142A)-resistant P388 murine leukemia cell lines as well as their parent sensitive cell line .
Defensin HNP 4 (HNP 4) is a single 11 amino acid long fragment of HNP-41-11. Defensin HNP 4 has inhibitory effect against multidrug-resistant and non-resistant strains .
TAN-1057C is a potent antibiotic which exhibits antibacterial activity against Gram-negative and Gram-positive bacteria, including Methicillin (HY-121544)-resistantStaphylococcus aureus .
Albocycline (Ingramycin) is a macrolide antibiotic, which exhibits antibacterial activities against methicillin-resistantStaphylococcus aureus (MRSA), Vancomycin (HY-B0671)-intermediate (VISA), and Vancomycin (HY-B0671)-resistantS. aureus (VRSA) strains with MICs ranging from 0.5 to 1.0 μg/mL. Albocycline exhibits no toxicity to human cells at concentration of ≤64 μg/mL .
Berbamine acetate (Compound 3a) is the derivative of Berbamine (HY-N0714). Berbamine acetate exhibits antitumor activity, inhibits growth of Imatinib (HY-15463)-resistant K562 leukemia cells, with IC50 of 6.6 μM .
Norvancomycin (hydrochloride) (Standard) is the analytical standard of Norvancomycin (hydrochloride). This product is intended for research and analytical applications. Norvancomycin hydrochloride is suitable for endocarditis, osteomyelitis, pneumonia, sepsis or soft tissue infections caused by Staphylococcus aureus (including methicillin-resistant strains and multi-drug-resistant strains).
Salvinolone is active against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). Salvinolone shows cytotoxic activity with an IC50 of 47.6 μM against the HL-60 tumor cell line for 72 h .
BE-10988 is a DNA topoisomerase inhibitor. BE-10988 inhibits the growth of Doxorubicin (HY-15142A)-resistant and vincristine-resistant P388 mouse leukemia cell lines by increasing the formation of DNA topoisomerase complexes .
(Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin[1]. Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[2][3].
Fosfomycin (calcium) (Standard) is the analytical standard of Fosfomycin (calcium). This product is intended for research and analytical applications. Fosfomycin (MK-0955) calcium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin calcium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
Antibacterial agent 68 (compound 4d) is an antibacterial agent against drug-resistantEscherichia coli. Antibacterial agent 68 has low cytotoxicity and exerts strong antibacterial activities against multidrug-resistantEscherichia coli at low concentrations as 0.007 mM .
PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib .
Lenalidomide-acetylene-Br is a PROTAC Linker taht makes up HJM-561 (HY-156698). HJM-561 is a potent, selective, and orally active EGFR PROTAC to inhiibit Osimertinib (HY-15772)-resistant EGFR triple mutations.
Cefpimizole (U-63196E) is a broad-spectrum cephalosporin antibiotic. Cefpimizole inhibits many Ampicillin (HY-B0522)-resistant bacteria, and is active against gram-negative species. Cefpimizole augments phagocytosis of macrophages and neutrophils .
Cefpimizole (U-63196E) sodium is a broad-spectrum cephalosporin antibiotic. Cefpimizole sodium inhibits many Ampicillin (HY-B0522)-resistant bacteria, and is active against gram-negative species. Cefpimizole sodium augments phagocytosis of macrophages and neutrophils .
INI-4001 is a TLR7/8 agonist, with EC50 values of 1.89 μM and 4.86 μM for TLR7/8, respectively. INI-4001 induces signaling and SEAP production through TLR7 and TLR8. INI-4001 promotes the generation of high-affinity, specific antibodies against fentanyl, preventing fentanyl from crossing the blood-brain barrier, making it an effective adjuvant for fentanyl vaccines in the opioid use disorder (OUD) population .
PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib .
Antifungal agent 73 (compound A32) is an antifungal agent for azole-resistant candidiasis. Antifungal agent 73 disrupts the fungal cell wall and cell membrane. Antifungal agent 73 shows potent in vivo antifungal activity against pathogenic fungi and fluconazole-resistant strains .
Epoxiconazole-d4 is the deuterium labeled Epoxiconazole (HY-119683). Epoxiconazole, a fungicide, is a demethylation inhibitor of the Ergosterol biosynthesis pathway. Epoxiconazole exhibits strong inhibitory effects on both carbendazim-resistant and phenamacril-resistant isolates, and can be used for controlling many crop diseases .
Epoxiconazole (Standard) is the analytical standard of Epoxiconazole. This product is intended for research and analytical applications. Epoxiconazole, a fungicide, is a demethylation inhibitor of the Ergosterol biosynthesis pathway. Epoxiconazole exhibits strong inhibitory effects on both carbendazim-resistant and phenamacril-resistant isolates, and can be used for controlling many crop diseases .
Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research .
BTdCPU is a potent heme regulated inhibitor kinase (HRI) activator that promotes eIF2α phosphorylation and induces apoptosis in Dexamethasone (HY-14648) (Dex)-resistant cancer cells. BTdCPU can be used in the study of cancers such as multiple myeloma and Dex-resistant multiple myeloma .
GSK2556286 (GSK286) is an orally active inhibitor of M. tuberculosis. GSK2556286 inhibits growth within human macrophages (IC50 = 0.07 μM). GSK2556286 is effective against both multidrug-resistant (MDR) or extensively drug-resistant (XDR) and agent-sensitive (DS) M. tuberculosis.
Streptothricin F is a bactericidal antibiotic. Streptothricin F interacts with the 30S subunit of 70S ribosome. Streptothricin F shows rapid, bactericidal activity against highly drug-resistant, carbapenem-resistantEnterobacterales (CRE) (MIC50 and MIC90: 2 and 4 μM, respectively) and Acinetobacter baumannii .
Cephalochromin is an antibiotic and an inhibitor for bacterial fatty acid synthase (FabI). Cephalochromin inhibits FabI of Staphylococcus aureus and Escherichia coli with IC50 of 1.9 and 1.8 μM. Cephalochromin inhibits gram-positive methicillin-resistantS. aureus (MRSA) and quinolone-resistantS. aureus (QRSA), with MIC of 2-8 µg/mL .
VP-4604 is a potent anti-methicillin-resistantStaphylococcus aureus (MRSA) agent. VP-4604 exhibits significant microbial growth inhibition toward Staphylococcus aureus (ATCC 43300) with MIC of 4-8 µg/mL. VP-4604 inhibits the growth of methicillin‐resistantStaphylococcus aureus with growth inhibition >95% .
VP-4556 is a potent anti-methicillin-resistantStaphylococcus aureus (MRSA) agent. VP-4556 exhibits significant microbial growth inhibition toward Staphylococcus aureus (ATCC 43300) with MIC of 8 µg/mL. VP-4556 inhibits the growth of methicillin‐resistantStaphylococcus aureus with growth inhibition >95% .
Anticancer agent 223 (Compound V-d) is an anticancer agent that triggers cell death through caspase-dependent and caspase-independent mechanisms. Anticancer agent 223 inhibits tumor spheroid formation and resensitizes cisplatin (HY-17394)-resistant A2780 cells to cisplatin (HY-17394) treatment .
DA-7867 is an antibacterial compound with activity against a wide range of bacteria, including drug-resistant bacteria. DA-7867 shows promising antibacterial activity against some clinically important pathogens, including drug-resistant bacteria. It is an amide analog of Tedizolid, reflecting the potential use of tetrazoles in the development of new antibacterial agents.
Pks13-TE inhibitor 2 (compound 32) is a 13-Thioesterase (Pks13-TE) inhibitor (IC50=1.30 μM). Pks13-TE inhibitor 2 shows good anti-tuberculosis activity against both agent-sensitive and drug-resistantMtb strains (MIC=0.0039-0.0078 μg/mL). Pks13-TE inhibitor 2 can be used in studies of multidrug-resistant TB and extensively drug-resistant TB .
Pks13-TE inhibitor 3 (compound 23) is a 13-Thioesterase (Pks13-TE) inhibitor (IC50=1.55 μM). Pks13-TE inhibitor 3 shows good anti-tuberculosis activity against both agent-sensitive and drug-resistantMtb strains (MIC=0.0625-0.25 μg/mL). Pks13-TE inhibitor 3 can be used in studies of multidrug-resistant TB and extensively drug-resistant TB .
WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50<0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine (HY-18062)-resistantP. falciparum strains) as well as T. gondii .
Ceftobiprole medocaril (BAL5788) is the parenteral proagent of Ceftobiprole (HY-112579). Ceftobiprole is a parenteral pyrrolidinone cephalosporin. Ceftobiprole is a broad-spectrum cephalosporin with high levels of in vitro activity against methicillin- (MRSA) and vancomycin-resistant staphylococci (VRSA) and penicillin-resistant streptococci. Ceftobiprole also inhibits gram-positive and gram-negative pathogens .
Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation .
Ceftobiprole medocaril (BAL5788) sodium is the parenteral proagent of Ceftobiprole (HY-112579). Ceftobiprole is a parenteral pyrrolidinone cephalosporin. Ceftobiprole is a broad-spectrum cephalosporin with high levels of in vitro activity against methicillin- (MRSA) and vancomycin-resistant staphylococci (VRSA) and penicillin-resistant streptococci. Ceftobiprole also inhibits gram-positive and gram-negative pathogens .
Antibacterial agent 83 (compound 17h) displays potent antibacterial activity against various vancomycin-resistantEnterococcus faecalis (VRE) and methicillin-resistantStaphylococcus aureus (MRSA). Antibacterial agent 83 can significantly reduce the biofilm formation of MRSA and exhibited promising selectivity. Antibacterial agent 83 is metabolically stable in human liver microsomes .
Antifungal agent 54 (compound A05) is a potent antifungal agent, against Fluconazole (HY-B0101)-resistant strains. Antifungal agent 54 is more effective than Miconazole (HY-B0454). Antifungal agent 54 inhibits Candida albicans strains with MIC values of 0.25-1 μg/mL .
Antifungal agent 55 (compound A07) is a potent antifungal agent, against Fluconazole (HY-B0101)-resistant strains. Antifungal agent 55 is more effective than Miconazole (HY-B0454). Antifungal agent 55 inhibits Candida albicans strains with MIC values of 0.25-1 μg/mL .
Antifungal agent 57 (compound A19) is a potent antifungal agent, against Fluconazole (HY-B0101)-resistant strains. Antifungal agent 57 is more effective than Miconazole (HY-B0454). Antifungal agent 57 inhibits Candida albicans strains with MIC values of 0.5-2 μg/mL .
Antifungal agent 58 (compound A21) is a potent antifungal agent, against Fluconazole (HY-B0101)-resistant strains. Antifungal agent 58 is more effective than Miconazole (HY-B0454). Antifungal agent 58 inhibits Candida albicans strains with MIC values of 0.06-8 μg/mL .
Chlorfenethol is a dehydrochlorinase inhibitor. Chlorfenethol can be used as a synergist for insecticide DDT to increase its effect on resistant strains .
Fosdevirine (GSK2248761) is is a potent, selective, non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1) replication with low nanomolar activity in vitro. Fosdevirine shows good activity against a broad range of HIV-1 strains, including efavirenz (HY-10572)-resistant clinical isolates .
Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
Telavancin (TD-6424) is a semisynthetic lipoglycopeptide vancomycin-derivative, is a novel antimicrobial agent developed by Theravance for overcoming resistant Gram-positive bacterial infections, specifically methicillin-resistantStaphylococcus aureus (MRSA). Telavancin disrupts cell membrane integrity, can be used for research of complicated skin and skin structure infections (cSSSIs) caused by Gram-positive bacteria .
Antifungal agent 56 (compound A09) is a potent antifungal agent, against Fluconazole (HY-B0101)-resistant strains. Antifungal agent 56 is more effective than Miconazole (HY-B0454). Antifungal agent 56 inhibits Candida albicans strains with MIC values of 0.03-0.25 μg/mL .
6-C-Methylquercetin-3,4'-dimethyl etheris a flavonol derivative isolated from the leaves of Bauhinia thonningii Schum. 6-C-Methylquercetin-3,4'-dimethyl ether has antibacterial activity against Gram-negative multidrug-resistant bacteria and against methicillin-resistant Staphylococcus aureus (MRSA) strains .
PL-100 is a potent HIV-1 protease inhibitor with a Ki of 36 pM and an EC50 of 16 nM. PL-100 inhibits viral replication by suppressing HIV-1 protease activity and demonstrates excellent antiviral efficacy against drug-resistant HIV strains. PL-100 can be used in research on drug-resistant HIV disease .
Loganetin is a non-toxic natural product that may be applied in the antibacterial agent development for treating multidrug-resistant Gram negative infections.
TrxR-IN-2, a potential thioredoxin reductase (TrxR) inhibitor, represents a promising candidate drug for the chemoresearch of drug-resistant hepatocellular carcinoma.
Dunnianol is a natural sesqui-neoligan with moderate antibacterial activity. Dunnianol inhibits Staphylococcus aureus and methicillin-resistantStaphylococcus aureus (MRSA).
Antibacterial agent 12, a biaryloxazolidinone analogue, is an antibacterial agent against antibiotic-susceptible and antibiotic-resistantGram-positive bacteria .
Meropenem-vaborbactam is an antibiotic against nonfermenting Gram-negative clinical isolates, including Enterobacteriaceae isolates with resistant and carbapenemase genotypes .
Nemonoxacin (TG-873870) malate is a nonfluorinated quinolone antibiotic. Nemonoxacin malate has broad-spectrum activity against Gram-positive, Gram-negative and atypical pathogens. Nemonoxacin malate can inhibit drug-resistantStreptococcus pneumoniae and (HY-121544) Methicillin-resistant Staphylococcus aureus. Nemonoxacin malate can be used for the research of community-acquired pneumonia .
BO-1 is a benzoate ester with antibacterial activity. BO-1 inhibits multidrug-resistant Staphylococcus aureus, and acts function synergistically with antibiotic, such as Ciprofloxacin (HY-B0356). BO-1 can reverse the resistance of antibiotic-resistant S. aureus strains, and decreases the level of inflammatory factors IL-6 and C-reactive protein in vivo in mice .
Piperafizine B exhibits slightly cytotoxicity in moser cells, P388 cells and Vincristine (VCR) (HY-N0488)-resistant P388 cells (IC50s is 23.8, 22.6 and 23.7 μg/mL, respectively). Piperafizine B exhibits synergistic effects with Vincristine, enhances the VCR-induced cytotoxicity and ameliorates the leukemia in mouse model .
MRT-2359 is a potent, orally active and selective GSPT1 depressant (IC50: >30 nM and <300 nM) that specifically induces apoptosis dependent on protein translation. MRT-2359 exhibits significant and preferred anti-proliferative activity in a variety of cancer cell lines, especially MYC-driven cell lines, such as non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) with high expression of N-Myc or L-Myc. MRT-2359 inhibits the growth of drug-resistant NSCLC and SCLC cells, making it suitable for cancer research .
2-Hydroxymethyl-3-hydroxyanthraquinone is an antiosteoporotic compound that inhibits osteoclastic tartrate-resistant acid phosphatase (TRAP) activity .
Kalimantacin A is a potent antibiotic. Kalimantacin A shows antibacterial activity against staphylococcus including methicillin-resistantstaphylococcus aureus (MRSA) .
Dactylocycline A is a tetracycline derivative with activity against some tetracycline-resistant microorganisms. Dactylocycline A is produced by fermentation of Dactylosporangium sp. and was found to be the most abundant glycoside in the initial fermentation. Dactylocycline A is acid-sensitive and readily hydrolyzes to the common sugar-free core substance dactylocyclinone. Although the sugar-free core has cross-resistance with tetracycline, Dactylocycline A exhibits activity against some tetracycline-resistant microorganisms .
1-Amino-2,5-anhydro-1-deoxy-D-mannitol is a potent antibacterial compound with antibacterial activity against a variety of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). The application potential of 1-Amino-2,5-anhydro-1-deoxy-D-mannitol lies in its ability to effectively combat common drug-resistant bacterial infections. 1-Amino-2,5-anhydro-1-deoxy-D-mannitol may become an emerging antibacterial agent in clinical inhibition.
Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens.
Diethofencarb is a fungicide with strong activity against Botrytis cinerea and Benzimidazole-resistant strains of Botryis spp. Diethofencarb has a role as an antifungal agrochemical .
Furalazine is an antimicrobial agent. Furalazine shows activity against drug-resistant strains of cholera bacteria. Furalazine has the potential for the research of cholera .
Antituberculosis agent-12 (compound 3408) is a narrow-spectrum antituberculosis prodrug phosphate that has the ability to inhibit drug-resistant tuberculosis infection .
Ir-CA is an antitumor agent. Ir-CA can accumulate in mitochondria and induces mitochondria dysfunction. Ir-CA induces apoptosis and autophagy. Ir-CA initiates mitophagy and cell cycle arrest to kill Cisplatin (HY-17394)-resistant A549R cells. Ir-CA can effectively inhibit metastasis by inhibiting MMP-2/MMP-9 .
Topoisomerase inhibitor 2 (18C) is a bacterial topoisomeraseinhibitor that exhibits potent broad-spectrum activity against multidrug-resistant Gram-negative bacteria .
Letermovir (AIC246) is a potent inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
DuP-721 is a broad spectrum and orally active antibacterial agent against a variety of clinically susceptible and resistant bacteria, especially M. tuberculosis .
Malacidin A is the calcium-dependent antibiotic (CDAs). Malacidin A is highly active against many antibiotic-resistant pathogens, particularly Gram-positive bacteria .
NBTIs-IN-6 is a bacterial topoisomerase inhibitor with certain antibacterial activity. Among them, the MIC90 for fluoroquinolone-resistant MRSA was 2 μg/mL .
Benalaxyl-d5 is the deuterium labeled Benalaxyl (HY-121109) . Benalaxyl is a fungicide, but A. fumigatus isolates are intrinsically resistant to Benalaxyl .
Telomycin is a calcium-dependent antibiotic, which can be produced by Streptomyces. Telomycin inhibits gram-positive bacteria, including multidrug-resistant (MDR) pathogens .
Hydroxyethyl disulfide blocks the inhibitory effect of showdomycin on methotrexate-resistant thymidylate synthase and is also protected by its substrate deoxyuridylic acid, preventing inactivation of the antibiotic .
Ceftobiprole (Ro 63-9141) is a broad-spectrum cephalosporin with high levels of in vitro activity against methicillin- (MRSA) and vancomycin-resistant staphylococci (VRSA) and penicillin-resistant streptococci with a MIC90 value of 2 μg/mL for MRSA. Ceftobiprole also inhibits gram-positive and gram-negative pathogens. Ceftobiprole can be used for the study of hospital-acquired pneumonia (excluding ventilator-associated pneumonia) and community-acquired pneumonia .
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively .
Ceftaroline fosamil hydrate is a potent cephalosporin antibiotic. Ceftaroline fosamil hydrateshows broad-spectrum activity against Gram-positive pathogens, including methicillin-resistantStaphylococcus aureus (MRSA) and multidrug-resistantStreptococcus pneumoniae, and common Gram-negative organisms. Ceftaroline fosamil hydrate has anti-infective activity, and can be used for the research of complicated skin and skin structure infections (cSSSIs) and community-acquired bacterial pneumonia (CABP) .
NecroIr1 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and Mixed Lineage Kinase (MLKL), and regulates CDK4 expression .
HSGN-94 is a potent antimicrobial agent with lipoteichoic acid (LTA) biosynthesis inhibition. HSGN-94 inhibits drug-resistant Gram-positive bacteria with MIC values of 0.25-2 μg/mL. HSGN-94 inhibits biofilm formation of MRSA and Vancomycin-resistantEnterococci. HSGN-94 also inhibits pro-inflammatory cytokines, exhibits in vivo efficacy in an MRSA murine wound infection model .
AK-HW-90 (compound 2B) is a potent panBcr-Abl inhibitor with significant inhibitory activity 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) .
Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans) .
FNDR-20123 free base is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations .
FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25/29/2/11/282 nM, respectively.) and inhibits Class III HDAC isoforms at nanomolar concentrations .
PD-1/PD-L1-IN 3, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC50s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 can be used for the research of various diseases, including cancer and infectious diseases .
PD-1/PD-L1-IN 3 TFA, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 TFA interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC50s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 TFA can be used for the research of various diseases, including cancer and infectious diseases .
SAAP 148 is an antimicrobial and antibiofilm agent, and exhibits inhibitory efficacy against antibiotic-resistant pathogens, with LC50 of 0.8-12.8 μM .
(R)-Alalevonadifloxacin mesylate is an isomer of Alalevonadifloxacin mesylate (HY-17626B). Alalevonadifloxacin mesylate is a oraly active anti-methicillin-resistantStaphylococcus aureus (MRSA) antibiotic .
Daurinoline is an alkaloid that can be isolated from the roots of Menispermum dauricum. Daurinoline may be a potential anti-tumor agent or chemosensitizer for chemo-resistant NSCLC research .
Antibacterial agent 62 is a novel redox cycling antituberculosis chemotype with potent bactericidal activity against growing and nutrient-starved phenotypically drug-resistant nongrowing bacteria.
Fabimycin is a FabI inhibitor with potent antibacterial activity against gram-negative bacteria. Fabimycin is effective against drug-resistant gram-negative Infections in vivo .
UCM53, a FtsZ inhibitor, is an antibacterial agent. UCM53 can inhibit the growth of clinical isolates of antibiotic-resistantStaphylococcus aureus and Enterococcus faecalis
Clovibactin is an antibiotic for drug-resistant bacterial pathogens without detectable resistance. Clovibactin TFA inihibits cell wall synthesis by targeting pyrophosphate of peptidoglycan precursors .
Oxacillin (sodium monohydrate) (Standard) is the analytical standard of Oxacillin (sodium monohydrate). This product is intended for research and analytical applications. Oxacillin sodium monohydrate is an antibiotic similar to Flucloxacillin used in resistant staphylococci infections study .
Sperabillin C is an antibacterial antibiotic with activity against both Gram-negative and Gram-positive bacteria, including resistant strains of Pseudomonas aeruginosa and Staphylococcus aureus .
Pretomanid-d4 is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL[1][2].
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistantE. faecium growth almost completely .
Antifungal agent 60 (compound 16) is an inhibitor of ergosterol biosynthesis with broad-spectrum antifungal activity. Antifungal agent 60 inhibits 7 human pathogenic fungal species, 2 fluconazole-resistant C. albicans isolates and 2 multi-drug resistant Candida auris isolates. Antifungal agent 60 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
Pretomanid (Standard) is the analytical standard of Pretomanid. This product is intended for research and analytical applications. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
OSC-GCDI(P) is a broad-spectrum orally active anti-influenza virus agent that exhibits significant inhibitory effects against both wild-type and Oseltamivir (HY-13317) resistant (H275Y) influenza virus strains in mouse infection models. OSC-GCDI(P) is capable of preventing not only wild-type influenza viruses but also OS-resistant variants with NA(H275Y) .
Amlodipine hydrochloride is a biologically active drug used to lower blood pressure and prevent chest pain. Amlodipine hydrochloride has shown synergistic effects with antimicrobial drugs in in vitro studies, especially against carbene peptide-resistant Acinetobacter baumannii. Amlodipine hydrochloride can be used in combination with other antibiotics to enhance the inhibitory effect against resistant bacteria. The use of amlodipine hydrochloride helps reduce the dosage requirements of the drug, reduce toxic effects, and delay the emergence of drug resistance .
Radezolid (RX-1741) is a oxazolidinone antibiotic. Radezolid is active against Staphylococcus, Chlamydia, and Legionella species, and remains active against Linezolid-resistant strains .
(3R)-7,4’-Dihydrohomoisoflavanone is a natural product with antibacterial activities against S. aureus and methicillin-resistantStaphylococcus aureus (MRSA) .
Gochnatiolide A is a dimeric sesquiterpene that can be found in Ainsliaea henryi. Gochnatiolide A exhibits antiproliferative activity against the kidney, melanoma, ovarian-resistant and glioma cell lines .
ET516 is a potent inhibitor of Androgen Receptor. ET516 significantly inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants .
SAAP 148 TFA is an antimicrobial and antibiofilm agent, and exhibits inhibitory efficacy against antibiotic-resistant pathogens, with LC50 of 0.8-12.8 μM .
Griselimycin is a compound with antituberculosis activity that exhibits good in vitro and in vivo activity against sensitive and resistant Mycobacterium tuberculosis, and its cyclohexyl derivative has high transformative potential.
Artemether (Standard) is the analytical standard of Artemether. This product is intended for research and analytical applications. Artemether is an anti-malarial compound that targets drug-resistant strains of falciparum malaria .
NecroIr2 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr2 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr2 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and mixed lineage kinase domain-like pseudokinase (MLKL), and regulates CDK4 expression .
QYL-685 is a Z-methenylcyclopropane nucleoside analog containing 2,6-diaminopurine, which has strong antiviral activity against HIV-1. QYL-685 showed activity against Zidovudine (HY-17413) resistant and Didanosine (HY-B0249) resistantHIV-1 infected clones in vitro. QYL-685 can be developed as a therapeutic drug for HIV-1 infection .
RE 11775 (m-tert-butylphenyl-N-methyl-N-(phenylthio) carbonate) is a new carbonate ester with unusually high toxicity to mosquito larvae. Laboratory and field evaluations have shown that it has potential for use in controlling sensitive and organophosphate-resistant larval and adult stages of Aedes nigromaculis (Ludlow). Preliminary studies also suggest that RE 11775 may also be useful for controlling sensitive and organophosphate-resistant Culex spccies. This new carbonate ester is relatively safe, with no adverse effects found in current testing.
PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells .
Norcyclizine is a piperazine compound that can be used for the synthesis of antimicrobial agents. 1-Benzhydrylpiperazine derivatives have been found to enhance the antibacterial activity of β-lactam antibiotics (Oxacillin, HY-B0925A) against Methicillin (HY-121544)-resistantStaphylococcus aureus (MRSA). This enhancement is likely achieved by inhibiting the allosteric site of PBP2a. Additionally, 1-Benzhydrylpiperazine can also serve as a pharmacological scaffold for the synthesis of anticancer agents .
Antibacterial agent 119 (Compound 21 g) is an antibacterial candidate against Methicillin (HY-121544)-resistantStaphylococcus aureus (MICs less than 1 μg/mL against tested strains). Antibacterial agent 119 induces ROS production. Antibacterial agent 119 also acts on the bacterial cell membrane to cause membrane breakage. Antibacterial agent 119 exhibits potent antibacterial activity with low cytotoxicity, rapid bactericidal ability, and good in vivo antibacterial activity .
Netilmicin (sulfate) (SCH-20569 (sulfate)) is an active aminoglycoside antibiotic against most Gram-negative and some Gram-positive bacteria, including certain strains resistant to gentamicin.
Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a Kd of 81 nM .
Licoricone is an flavonoid extracted from licorice, exhibits anti-helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains .
Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitory activity toward methicillin-resistant Staphylococcus aureus (MRSA) .
APF is a fluorescence probe that can selectively, and dose dependently detect certain species among ROS and that are highly resistant to autoxidation. APF can be used in enzymatic and cellular systems .
Halofantrine (SKF-102886 free base) is a highly lipophilic antimalarial active against Chloroquine-resistant strains of Plasmodium falciparum . Halofantrine blocks HERG potassium channels .
Capreomycin is a macrocyclic peptide antibiotic. Capreomycin can be used for anti-multidrug-resistant-tuberculosis research. Capreomycin can inhibit phenylalanine synthesis in in mycobacterial ribosomes translation
Pancixanthone A is a xanthone that can be isolated from Garcinia vieillardii. Pancixanthone A has antimalarial activity against chloroquino-resistant strains of Plasmodium falciparum with an IC50 of 1.6 μg/mL .
Isocudraniaxanthone A is a xanthone that can be isolated from Garcinia vieillardii. Isocudraniaxanthone A has antimalarial activity against chloroquino-resistant strains of Plasmodium falciparum with an IC50 of 2.3 μg/mL .
LCI peptide is an antimicrobial peptide with antibacterial activity. LCI peptide is active against plant pathogens, Xanthomonas and Pseudomonas, including E. coli, Gentamicin-resistant MRSA and Xoo .
Dehydrorotenone is a rotenone analog that is resistant to alkali decomposition. When treated with alkaline solution or alkaline solution containing zinc, dehydrorotenone can absorb 2 molecules of water and convert into acid solution.
Aldecalmycin is an antibiotic showing antimicrobial activities against Gram-positive bacteria including methicillin-resistantStaphylococcus aureus (MRSA) with MICs values of 6.25-25 μg/mL .
Desmethyl ferroquine (SSR97213) is the active and major metabolite of Ferroquine. Ferroquine is an antimalarial. Desmethyl ferroquine shows significant activity against Chloroquine-susceptible and resistantP. falciparum strains .
Antimicrobial agent 69 is a novel structural antimicrobial regulator and has been used to fight deadly multidrug-resistant bacterial infections, and its < b > MICs < / b > value is 2.978 μM。
TLR8 agonist 4 showed effective inhibition on wild-type and drug-resistant (lamivudine and entecavir) HBV strains. The IC50 values are 0.15 and 0.10 respectively μM.
Octenidine is a potent antibacterial agent, possessing activity against multidrug-resistant Gram-negative pathogens. Octenidine can inhibit the expression of biofilm genes and destroy the formation of biofilms .
Andrastin A meroterpenoid compound, is a farnesyltransferase inhibitor. Andrastin A inhibits the efflux of anticancer compounds from multidrug-resistant cancer cells. Andrastin A can be isolated from Penicillium species .
Antibacterial agent 230 (compound 10) is an effective Antifungal agent. The MIC value of antibacterial agent 230 against fluconazole-resistant fungi is 2.0 ~ 16.0 μg/mL .
Anti-MRSA agent 16 (Compound 4) is an inhibitor of methicillin-resistant Staphylococcus aureus (MRSA). Anti-MRSA agent 16 is effective in combination with oxacillin or meropenem in infected mice .
Antibiotic SF-2132 is a peptide antibiotic identified in Nocardiopsis sp., which exhibits inhibitory activity against β-lactam antibiotic-resistant strains, such as Pseudomonas and Escherichia .
Cefuzonam sodium is a second-generation cephalosporin antibiotic with activity against Staphylococcus aureus, which is resistant to most third-generation cephalosporins. Cefuzonam sodium is effective for preventing infection after cesarean delivery .
K13787 is an acetohydroxyacid synthase (AHAS) inhibitor with antibacterial activity. K13787 has antibacterial activity against a variety of nontuberculous mycobacteria (NTM) and clarithromycin (CLR) resistant strains .
MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line .
HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC50 values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistantC. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1 .
TXA6101 is a bacterial protein FtsZ (filamentous temperature-sensitive protein Z) inhibitor that inhibits bacterial division. TXA6101 has antimicrobial activity against MRSA isolates expressing either the G193D or G196S mutant FtsZ with the MIC value of 1 μg/mL, retains significant activity against the TXA707-resistant FtsZ mutant. TXA6101 can be used as a potential method against Gram-negative bacterial infections .
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .
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 inhibitory activity with Fluconazole. Antifungal agent 72 can be used for C. glabrata infection research .
Influenza virus-IN-8 (compound A4) is an inhibitor of influenza virus (Influenza Virus) that induces viral nucleoprotein (NP) aggregation and prevents its nuclear accumulation. Influenza virus-IN-8 has broad-spectrum anti-influenza activity and can inhibit the replication and transcription of influenza A virus. Influenza virus-IN-8 also inhibits Oseltamivir (HY-13317)-resistant H1N1/pdm09 strains .
Ru-Poma is a Ru(II)-based photosensitizer, which attenuates Cisplatin (HY-17394)-resistant tumor through photodynamic therapy (PDT). Ru-Poma photodegrades CRBN through a Pomalidomide (HY-10984) moiety. Ru-Poma induces ferroptosis, through an increase in lipid peroxide, downregulation of GPX4 and GAPDH expression. Ru-Poma exhibits cytotoxicity in A549, with IC50 of 18.46 μM and 0.37 μM in dark and upon irradiation, respectively .
Duocarmycin GA is an antibody agent conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin GA can be used against multi-agent resistant cell lines.
Duocarmycin MB is an antibody agent conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MB can be used against multi-agent resistant cell lines.
Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells .
Duocarmycin MA is an antibody agent conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MA can be used against multi-agent resistant cell lines.
EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC .
(S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells .
Artelinic acid, a derivative of Artemisinin, is an antimalarial agent for the treatment of multidrug resistant strains of Plasmodium falciparum. Artelinic acid can be administered by various routes of administration, including intravenous, intramuscular and oral routes .
Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
RLA-4842 is an iron activator containing anti-androgen. RLA-4842 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
Ortataxel (IDN 5109; BAY 59-8862) is a derivative of Paclitaxel (HY-B0015). Ortataxel exhibits activity against multiple drug-sensitive and resistant cancer cell lines .
Cyslabdan ((+)-Cyslabdan) is a novel compound with the potential to enhance the activity of imipenem against methicillin-resistant Staphylococcus aureus. Cyslabdan exerts its antibacterial effect by inhibiting the synthesis of pentapeptide cross-links .
Antifungal agent 113 (compound 9a) is a potent antifungal and antibacterial agent. Antifungal agent 113 shows good antibacterial activity against S. aureus and methicillin-resistantS. aureus .
Pyronaridine tetraphosphate is an orally active Mannich base anti-malarial agent. Pyronaridine tetraphosphate is active against P. falciparum and Echinococcus granulosus infection .
Roseoflavin, a natural pigment originally isolated from Streptomyces davawensis, is an antimetabolite analog of Riboflavin and flavin mononucleotide that has antimicrobial properties .
(-)-Heraclenol is a derivative of furocoumarin isolated from Ducrosia anethifolia. (-)-Heraclenol shows antiproliferative and cytotoxic activities on cancer cell lines .
Pyronaridine is an orally active Mannich base anti-malarial agent. Pyronaridine is active against P. falciparum and Echinococcus granulosus infection .
7-Oxo-ganoderic acid Z, a terpenoid, is a nature product that could be isolated from Resina Commiphora. 7-Oxo-ganoderic acid Z has Anti-Mycobacterium tuberculosis activity .
Pyronaridine (tetraphosphate) (Standard) is the analytical standard of Pyronaridine (tetraphosphate). This product is intended for research and analytical applications. Pyronaridine tetraphosphate is an orally active Mannich base anti-malarial agent. Pyronaridine tetraphosphate is active against P. falciparum and Echinococcus granulosus infection .
PROTAC CYP1B1 degrader-2 (compound PV2) is a von Hippel-Landau (VHL) E3 ligase-based CYP1B1 degrader with the DC50 of 1.0 nM at 24 h in A549/Taxol cells. PROTAC CYP1B1 degrader-2 inhibits growth, migration, and invasion of A549/Taxol cell(Sturcture Note:(Blue: VHL ligand (HY-112078), Black: linker (HY-W007700), Pink: CYP1B1 ligand (HY-159006) .
CYP1B1 ligand 3 (Compound A1) is a selective inhibitor for cytochrome P450 enzyme CYP1B1 with an IC50 of 11.9 nM. CYP1B1 ligand 3 can be utilized for the synthesis of PROTAC CYP1B1 degrader-2 (HY-158429) .
Arenobufagin is a natural bufadienolide from toad venom; has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells.
BRD9185 is a Dihydroorotate dehydrogenase (DHODH) inhibitor, with an EC50 of 16 nM against multidrug-resistant blood-stage parasites in vitro and is curative after just three doses in a P. berghei mouse model .
Pyrindamycin B is an antibiotic, actives against gram-positive and gram-negative bacterias, and exhibits strong therapeutic effects against both agent-sensitive and resistant cells of P388 leukemia in mice .
3,5-Difluoro-L-tyrosine is a functional, tyrosinase-resistant mimetic of tyrosine. 3,5-Difluoro-L-tyrosine can be used to analyze the substrate specificity of protein tyrosine phosphatases (PTPs) .
Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM .
Ascr#7, an ascaroside, is a hormone of nematodes. Ascr#7 is expressed during nematode development. Ascarosides can induce formation of long-lived and highly stress resistant dauer larvae .
Antitumor agent-91 is a cyclic phosphate ester derivative with anticancer and anti-proliferative activities. Antitumor agent-91 has potential application in human castration resistant prostate cancer and pancreatic cancer .
Opevesostat (MK-5684; ODM-208) is an orally active and selective CYP11A1 inhibitor. Opevesostat has the potential for the research of metastatic castration-resistant prostate cancer (mCRPC) .
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 . .
Antho-rwamide I is a neuropeptide that can be isolated from the sea anemone Anthopleura elegantissima. Antho-rwamide I is resistant to nonspecific aminopeptidases, which increases the stability of the peptide after neuronal release .
Octenidine saccharin is a potent antibacterial agent, possessing activity against multidrug-resistant Gram-negative pathogens. Octenidine saccharin can inhibit the expression of biofilm genes and destroy the formation of biofilms .
Antibacterial agent 106 (compound 8) is an orally active and potent antibacterial agent with antibiofilm activity. Antibacterial agent 106 shows potent antibacterial effect against multi-agent resistant (MDR)-Gram positive pathogens. Antibacterial agent 106 is highly effective in clearing 99.7% of the intracellular methicillin-resistant S. aureus (MRSA) harbored inside macrophages . Antibacterial agent 106 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
AG-7404 is an inhibitor of picornaviral 3C protease, with anti-poliovirus activity (EC50=0.080-0.674 μM). AG-7404 has synergy with V-073 (HY-104074) or BTA798 (HY-106254), and fully inhibits all V-073-resistant variants . AG-7404 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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 .
DS-8587 is a new fluoroquinolone with significant antibacterial activity. The MIC value of DS-8587 against clinically isolated amoxicillin-resistant Bacillus strains is superior to ciprofloxacin and levofloxacin. The antibacterial activity of DS-8587 is less affected by adeA/adeB/adeC or abeM efflux pumps, and has more advantages than ciprofloxacin. DS-8587 has a lower single-step mutation frequency than ciprofloxacin. DS-8587 may be an effective drug for inhibiting amoxicillin-resistant Bacillus infections .
GNF179 is an optimized 8,8-dimethyl imidazolopiperazine analog that exhibits antimalarial potency (IC50 of 4.8 nM against the multidrug resistant strain W2). GNF179 is orally active .
Imperialine 3-β-D-glucoside is the glycoside of Imperialine. Imperialine 3-β-D-glucoside may exhibit anti-tumor properties against multi-agent resistant tumor cells .
TCA1 is a small molecule with activity against agent-susceptible and -resistantMycobacterium tuberculosis (Mtb). TCA1 inhibits enzymes involved in cell wall and molybdenum cofactor biosynthesis, such as DprE1 and MoeW .
Scholaricine (compound 13 ) is an alkaloid isolated from the leaf and stem-bark extracts of Alstonia spatulata. Scholaricine reverse multidrug resistance in vincristine-resistant KB cells with an IC50 value of 13.35 μM .
P1 is a broad-spectrum antimicrobial peptide. P1 shows antibacterial activity against Gram-positive and Gram-negative bacteria,such as B. anthracis spores and Carbapenem-resistantA. baumannii and K. pneumoniae .
IMBI (compound 32) is an antibacterial agent that inhibits quorum sensing (QS) against drug-resistant pathogens. IMBI inhibits biofilm formation of Salmonella marcescens and restores or increases its susceptibility to antimicrobial drugs .
AC mAb-X purification resin is a special protein A resin.
Matrix: high rigidity agarose; particle size: 40~120 μm; ligand: recombinant alkali-resistant Protein A (~24KD); ADC purification resin.
Spiromesifen (BSN 2060) is a broad-spectrum
tetrachloro acid derivative acaricide. Spiromesifen reduces lipid biosynthesis via inhibition of acetyl-CoA carboxylase, and has no cross-resistance to any resistant mite or whitefly
populations .
Methyl betulonate (Betulonic acid methyl ester) is a triterpenoid. Methyl betulonate inhibits cell growth of eight tumor (including resistant) and two normal fibroblast cell lines with the IC50s >50.0 μM .
CFG920 is an orally active, nonsteroidal, reversible dual CYP17 and CYP11B2 inhibitor. CFG920 has the potential for metastatic castration-resistant prostate cancer research .
(-)-Tylophorine ((-)-(R)-Tylophorine) is a potent cytotoxic agent with activity against both drug-sensitive and multidrug-resistant cancer cell lines. (-)-Tylophorine has been explored in biomedical research for its anticancer applications .
Sutezolid (PNU-100480), an orally active oxazolidinone antimicrobial agent, acts by inhibiting bacterial protein synthesis. Sutezolid has potent activity against mycobacteria, and is used for the research of drug-resistant tuberculosis .
CWHM-1008 is a potent and orally active antimalarial agent, with EC50 values of 46 and 21 nM against agent-sensitive Plasmodium falciparum 3D7 and drug-resistant Dd2 strains, respectively .
EC1167 is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC) .
Galiellalactone is a is a small non-toxic and non-mutagenic fungal metabolite, a selective inhibitor of STAT3 signaling, with an IC50 of 250-500 nM. Galiellalactone can be used to research castration-resistant prostate cancer .
POLA1 inhibitor 1 (Compound 12) is an orally active POLA1 inhibitor. POLA1 inhibitor 1 shows antitumor activity against several tumor histotypes and Adarotene-resistant cell line .
EC1167 hydrochloride is the linker for EC1169. EC1169 is prostate-specific membrane antigen targeting-tubulysin conjugate. EC1169 hydrochloride has the potential to treat recurrent metastatic, castration-resistant prostate cancer (MCRPC) .
ASP-1 is a strong antistaphylococcal peptide with minimum inhibitory concentrations (MICs) of the purified peptide against S. aureus and methicillin-resistantS. aureus (MRSA) ranged from 2 μg/mL to 64 μg/mL .
Paenilagicin is a Gram-positive active antibiotic with a unique diphosphorylated prenyl binding mechanism that does not induce drug resistance. Paenilagicin exhibits a MIC value of 2 μg/mL against multidrug-resistant Gram-positive bacteria .
Desotamide is a cyclic hexapeptide antibiotic originally isolated from Streptomyces. It is active against S. aureus, S. pneumoniae, and methicillin-resistant S. epidermidis (MRSE; MICs=16, 12.5, and 32 μg/mL, respectively).
Antibacterial agent 220 is a potent antibacterial agent that can directly destroy bacterial cell membranes. Antibacterial agent 220 effectively combats Gram-positive and and Gram-negative pathogens, including drug-resistant strains .
Pelgifatamab (BAY-2315497) is a prostate-specific membrane antigen (PSMA) antibody. Pelgifatamab can be covalently linked to a binding moiety of 225Ac and used for metastatic castration-resistant prostate cancer (mCRPC) research .
Amdoxovir (DAPD) is an orally active nucleoside reverse transcriptase inhibitor. Amdoxovir is active against wild-type and NRTl-resistant viruses. Amdoxovir is the prodrug of dioxolane guanosine. Amdoxovir can be used for research of HIV/AIDS .
Oe-9000 is a compound with local anesthetic activity that inhibits voltage-gated Na + currents in neurons, including both TTX-resistant and TTX-sensitive currents, with effects superior to those of some other local anesthetics.
Tioxacin is an orally active bactericide agent. Tioxacin combined with aliphatic amines has activities against G(+) and G (-) bacteria, including Escherichia coliresistant to Nalidixic acid (HY-B0398) and Pseudomonas aeruginosa .
MS-073 (CP162398) is a P-glycoprotein (P-gp) inhibitor. MS-073 reverses multidrug resistance in drug-resistant cells by competitively inhibiting drug binding to P-glycoprotein .
KKL-40 is a small molecule inhibitor that targets the trans-transcription process and is effective against methicillin-sensitive and -resistant Staphylococcus aureus (S. aureus) as well as other Gram-positive pathogens including vancomycin-resistant Enterococcus faecium, Bacillus subtilis, and Streptococcus pyogenes. KKL-40 synergizes with the human antimicrobial peptide LL-37 to inhibit S. aureus, but does not synergize with other antibiotics such as daptomycin, kanamycin, or erythromycin. Trans-transcription is an extreme form of recoding, and KKL-40 inhibits trans-transcription but is nontoxic to HeLa cells .
STAT3-IN-31 (compound K2071) is a STATtic-derived STAT3 and mitotic inhibitor. STAT3-IN-31 blocks mitotic progression and affects the formation of mitotic spindles. STAT3-IN-31 also affects glioblastoma cell migration and inhibits cell proliferation in tumor spheroids. STAT3-IN-31 is also able to induce glioblastoma senescence, inhibit the growth of Temozolomide (HY-17364)-resistant cells and the secretion of the pro-inflammatory cytokine monocyte chemoattractant protein MCP-1 .
(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
Delafloxacin (RX-3341; WQ-3034; ABT492) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistantStaphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia .
5,6-Dihydroabiraterone is the metabolism of Abiraterone (HY-70013). Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, and shows antitumor activity in CRPC (castration-resistant prostate cancer) .
Epothilone F is a Microtubule/Tubulin-stabilizing agent with anti-tumor activity. Epothilone F inhibits the proliferation of breast cancer cells, non-small cell lung cancer cells, drug-resistant ovarian cancer cells .
Prostaglandin K2 (PGK2) is the 9,11-diketone formed by the oxidation of PGE2 or PGD2. Whether this compound exists biologically is uncertain; it is known to be resistant to metabolism by 15-hydroxy PGDH in vitro.
Z-Arg-Arg-βNA acetate is a sensitive dipeptide substrate of the protease Cathepsin B and resistant to proteases H and L. Z-Arg-Arg-βNA acetate can serve as an important tool for distinguishing non-Cathepsin B type proteins .
Sobuzoxane (MST-16) is an orally active topoisomerase II inhibitor. Sobuzoxane causes irreversible inhibition of cell division. Sobuzoxane can be used in the study of non-Hodgkin's lymphoma that is resistant to conventional chemotherapy or has recurred .
TNK-6123 is a potent Emivirine (HY-15353) analogue with improved activity against drug-resistant HIV mutants. TNK-6123 improves activity against Lys103Asn mutant RT .
Diethofencarb (Standard) is the analytical standard of Diethofencarb. This product is intended for research and analytical applications. Diethofencarb is a fungicide with strong activity against Botrytis cinerea and Benzimidazole-resistant strains of Botryis spp. Diethofencarb has a role as an antifungal agrochemical .
DA 1131 is an anionic Carbapenem antibiotic. DA 1131 has broad spectrum antibacterial activity for both gram-positive and gram-negative organisms. DA 1131 is resistant to degradation by various types of β-lactamases .
HI-253 is a non-nucleoside inhibitor of HIV-1 reverse transcriptase that has demonstrated greater activity than multiple anti-HIV compounds against both resistant and sensitive HIV-1 strains.
CN-CC-861 is a broad-spectrum antibiotic. CN-CC-861 shows antibiotic activities for susceptible and multidrug-resistant bacteria. CN-CC-861 shows potent bactericidal activity in vivo .
Sulbenicillin is an antibiotic that, in a study of its activity against Pseudomonas aeruginosa infection in mice, showed differences in activity against certain strains compared to other antibiotics, and activity against gentamicin-resistant strains was affected by the strain's own resistance.
Nodusmicin is a macrolide antibiotic against antibiotic-susceptible and -resistantS. aureus with MIC values of 125, 250 and 250 μg/mL for UC-76, UC-6685, and UC-6690 strains, respectively .
Adefovir dipivoxil, an adenosine analogue, is an oral proagent of the nucleoside reverse transcriptase inhibitor Adefovir. Adefovir dipivoxil inhibits both the wild type and HBV Lamivudine-resistant strains . Adefovir dipivoxil shows anti-orthopoxvirus activity.
Ceftaroline fosamil (TAK-599), a cephalosporin derivative, is an N-phosphono proagent of anti-methicillin-resistantStaphylococcus aureus (MRSA) T-91825. Ceftaroline fosamil can be used for the research of MRSA infection .
OV-1, sheep is an alpha-helical antimicrobial ovispirin peptide derived from SMAP29 peptide (sheep), which inhibits several antibiotic-resistant bacterial strains including mucoid and nonmucoid Pseudomonas aeruginosa .
RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer .
Amp1EP9 is an antimicrobial peptide. Amp1EP9 is a powerful tool for developing potent and nontoxic antimicrobial agents. Amp1EP9 has the potential for the research of multidrug-resistant bacterial infections .
VP-4509, an anti-methicillin‐resistantStaphylococcus aureus (MRSA) agent, with the MIC of 49.3 µM. VP-4509 also possesses high antibacterial activity towards gram-negative bacteria P. aeruginosa .
4,4'-Dicyanostilbene (compound 43) is a potent antimalarial agent against the Dd2 strain, with an EC50 of 27 nM. 4,4'-Dicyanostilbene exhibits in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA) .
Zolimidine, a derivate of imidazopyridine, is an orally active antiulcer agent. Zolimidine stimulates mucus secretion in intestinal mucosal cells and enhacnes intestinal wall more resistant to ulceration. Zolimidine exhibits gastroprotective effect in duodenal ulcer research .
CCCI-01 is a centrosome clustering inhibitor. CCCI-01 has selective effects on cancer. CCCI-01 can be used for the research of non-cross-resistant anti-cancer agents with blocking centrosome clustering .
Cresomycin is a bridged macrobicyclic antibiotic that can bind to the bacterial ribosome. Cresomycin exhibits efficacy against both Gram-positive and Gram-negative bacteria, including multidrug-resistant strains of Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa .
Letermovir (Standard) is the analytical standard of Letermovir. This product is intended for research and analytical applications. Letermovir (AIC246) is a potent inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.
Antibacterial agent 221 (compound 3k) is a potent inhibitor of Gram-positive Methicillin-resistantStaphylococcus aureus (MRSA). Antibacterial agent 221 shows significant cytotoxicity against human LO2 and HepG2 cells .
β-Sitosterol acetate, 95% (Sitosteryl acetate, 95%) is a sterol that can be isolated from Hechtia glomerata Zucc., which has antibacterial activity and has a MIC value of 100µg/mL against carbapenem-resistantAcinetobacter baumannii .
EC-1456 is a folate-tubulysin conjugate with significant anti-proliferative activity against FR-positive tumors, including models which were anticancer drug resistant. EC-1456 can be utilized in cancer research .
RU44790 is a monocyclic beta-lactam antibiotic that exerts potent activity against gram-negative bacteria and is highly resistant to hydrolysis by various beta-lactamases. RU44790 can be utilized in anti-bacteria research .
CGI-17341 is a 5-nitroimidazole antibacterial agent that has the activity of inhibiting sensitive and multidrug-resistant strains of Mycobacterium tuberculosis in vitro and prolonging the survival time of mice infected with Mycobacterium tuberculosis in vivo in a dose-dependent manner.
Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistantstaphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC50 value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity .
CC214-2 is an oral active and selective mTOR kinase inhibitor. CC214-2 targets to both of mTORC1 (pS6) and mTORC2 (pAktS473). CC214-2 induces autophagy, which is a potential target for host-directed therapy (HDT) in tuberculosis. CC214-2 exhibits synergistic bactericidal and sterilizing activity agasinst tuberculosis (TB), and shortens the treatment duration. CC214-2 also inhibits Rapamycin (HY-10219)-resistant signaling and the growth of glioblastomas in vitro and in vivo .
NAMPT/IDO1-IN-1 is an orally active dual inhibitor of NAMPT and IDO1 with IC50s of 57.7 nM and 233 nM, respectively. NAMPT/IDO1-IN-1 blocks NAD+ biosynthesis, inhibits proliferation and migration of Paclitaxel (HY-B0015)- and FK866 (HY-50876)-resistant NSCLC cell lines (A549/R cells). NAMPT/IDO1-IN-1 has shown antitumor effects in mice and enhanced A549/R cell sensitivity to paclitaxel .
Tubulin polymerization-IN-66 (Compound 13) inhibits colony formation and tubulin polymerization. Tubulin polymerization-IN-66 induces apoptosis. Tubulin polymerization-IN-66 inhibits cell viability of A549, A2780, SKOV3, HCC827 cells, with IC50s of 0.84, 0.38, 0.31, 0.34 nM respectively. Tubulin polymerization-IN-66 is also active against the Paclitaxel (HY-B0015)-resistant cancer cell line A2780/T and its parental cell line A2780 .
Carpachromene is a potent α-glucosidase enzyme inhibitor. Carpachromene ameliorates insulin resistance in HepG2 cells via modulating IR/IRS1/PI3k/Akt/GSK3/FoxO1 pathway .
NSC756093 is a potent inhibitor of the GBP1:PIM1 interaction. NSC756093 can potentially revert resistance to paclitaxel. NSC756093 can be used for ovarian cancer research .
CXF-009 is a selective and covalent FGFR4 inhibitor, with the IC50 of 48 nM. CXF-009 targeting Cys477 and Cys552 of FGFR4, and can be used for the study of hepatocellular carcinoma .
Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation
of PKCι in nucleus of sensitive cells but not in resistant cells.
Targocil functions as a bacteriostatic inhibitor of wall teichoic acid (WTA) biosynthesis which can inhibit the growth of methicillin-susceptible S. aureus (MSSA) and methicillin-resistantS. aureus (MRSA) with MIC90s of 2 μg/ mL for both MRSA and MSSA.
(-)-Corynoxidine is an acetylcholinesterase inhibitor with an IC50 value of 89.0 μM, isolated from the aerial parts of Corydalis speciosa .
(-)-Corynoxidine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus strains in different degrees .
Contezolid acefosamil (MRX-4) is the orally active proagent of the active antimicrobial metabolite Contezolid (MRX-I), an oxazolidinone which shows potent in vitro activity against various multidrug-resistant Gram-positive bacteria, including MRSA .
Antifungal agent 25 is a potent broad-spectrum antifungal agent. Antifungal agent 25 shows antifungal effect against Candida albicans and fluconazole-resistant strain of Candida albicans. Antifungal agent 25 stable metabolic property in vivo .
CF3–K11 is a stable antibiotic with antibacterial activity. CF3–K11 has strong antibacterial activity against Pseudomonas aeruginosa and methicillin-resistantStaphylococcus aureus (MRSA).
Clovibactin TFA is the TFA salt form of Clovibactin (HY-P10027). Clovibactin TFA is an antibiotic for drug-resistant bacterial pathogens without detectable resistance. Clovibactin TFA inihibits cell wall synthesis by targeting pyrophosphate of peptidoglycan precursors .
Spiromesifen-d9 is a deuterated labeled Spiromesifen . Spiromesifen (BSN 2060) is a broad-spectrum
tetrachloro acid derivative acaricide. Spiromesifen can interfere with lipid
biosynthesis, and has no cross-resistance to any resistant mite or whitefly
populations .
CRAMP (1-39) is an antimicrobial peptide. CRAMP (1-39) has shown potent bactericidal effects against multiple strains of Neisseria meningitidis in vitro. CRAMP (1-39) can be used to study drug-resistant bacterial infections .
L-708906 is a potent human immunodeficiency virus type 1 (HIV-1) inhibitor with an IC50 value of 12 μM. L-708906 inhibits HIV strains resistant to nonnucleoside or nucleoside reverse transcriptase inhibitors .
Villalstonine is a bisindole alkaloid with various biological activities including anticancer, antimalarial, and antiamoebic activities. Villalstonine exhibits potent antiplasmodial activity against the multidrug-resistant K1 strain of P. falciparum with an IC50 value of 0.27 μM .
Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research .
D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research .
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistantPlasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys .
S119-8 is a broad spectrum inhibitor of influenza A and B viruses, showing activity against multiple influenza B viruses and an oseltamivir-resistant influenza A virus, but does not inhibit a non-influenza virus, vesicular stomatitis nirus (VSV) .
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
GNF179 metabolite is the metabolite of GNF179, which is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.
IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models .
TCMDC-125457 is potent in inducing calcium redistribution but minimally inhibits heme crystallization. TCMDC-125457 demonstrated high efficacy when pulsed in a single-dose combination with artesunate against tightly synchronized artemisinin-resistant ring-stage parasites.
TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research .
DNA Gyrase-IN-5 (Compound 8I-w) is a potent DNA gyrase inhibitor with an IC50 of 0.10 μM. DNA Gyrase-IN-5 shows antibacterial activities against wild type and drug-resistant strains .
HIV-1 protease-IN-11 (compound 34a) is a HIV-1 protease inhibitor with an IC50 of 0.41 nM. HIV-1 protease-IN-11 also exhibits significant activity against drug-resistant variant .
Ceftolozane (CXA-101) sulfate is an antipseudomonal cephalosporin. Ceftolozane sulfate inhibits P. aeruginosa PAO1 with an MIC of 0.5 μg/mL. Ceftolozane sulfate can also inhibit β-lactam-resistantP. aeruginosa .
P-gp inhibitor 17 (compound 2g) is a P-gp inhibitor directly interacted with the transmembrane domain of P-gp. P-gp inhibitor 17 can be used for P-gp-mediated multidrug-resistant in tumor cells study .
RDEA 806 is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) that exhibits potent in vitro inhibitory activity against both wild-type HIV-1 (EC50 = 3.05 nM) and NNRTI-resistantHIV-1 .
Spiromesifen (Standard) is the analytical standard of Spiromesifen. Spiromesifen (BSN 2060) is a broad-spectrum tetrachloro acid derivative acaricide. Spiromesifen reduces lipid biosynthesis via inhibition of acetyl-CoA carboxylase, and has no cross-resistance to any resistant mite or whitefly
populations .
Fostemsavir sodium (BMS-663068 sodium) is an HIV-1 attachment inhibitor with antiviral activity against multidrug-resistant HIV-1. Co-inhibition with fostemsavir sodium also showed a trend toward reduction in markers of monocyte activation and coagulation abnormalities .
Epetraborole (GSK2251052) is a leucyl-tRNA synthetase (LeuRS) inhibitor (IC50=0.31 μM), thereby inhibiting protein synthesis. Epetraborole can be used in multidrug-resistant gram-negative pathogens infection research .
HIV-1 protease-IN-8 (compound 34b) is a potent HIV-1 protease inhibitor with an IC50 value of 0.32 nM. HIV-1 protease-IN-8 displays IC50s of 0.29 μM and 1.90 μM for wild-type HIV-1 (HIV-1NL4-3) and drug-resistant variant (HIV-1MDR), respectively. HIV-1 protease-IN-8 displays robust antiviral activity against both wild-type HIV-1 and drug-resistant variant .
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 .
Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor .
Epetraborole (GSK2251052) hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor (IC50=0.31 μM), thereby inhibiting protein synthesis. Epetraborole hydrochloride can be used in multidrug-resistant gram-negative pathogens infection research .
Upleganan (SPR206), a polymyxin analogue, and shows antibiotic activity against multidrug resistantGram-negative pathogen. The MIC values of Upleganan against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301 are both 0.125 mg/L .
Delafloxacin meglumine (ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistantStaphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia .
ALLO-2 is a potent drug-resistantSmoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM .
DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients .
Ceftaroline fosamil (inner) (TAK-599 free acid), a cephalosporin derivative, is an N-phosphono proagent of anti-methicillin-resistantStaphylococcus aureus (MRSA) T-91825. Ceftaroline fosamil (inner) can be used for the research of MRSA infection .
OYYF-175, an antimicrobial antifolate, is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 2.36 nM for Escherichia coli DHFR. OYYF-175 exhibits potent broad-spectrum antibacterial activities, especially against multi-drug resistant Gram-Negative-strains .
P-gp inhibitor 4 (Compound 8b) is a selective P-glycoprotein modulator with an EC50 of 94 nM. P-gp inhibitor 4 increases agent transport across gastro-intestinal barrier and recovers doxorubicin toxicity in multidrug resistant cancer cells .
Methicillin sodium hydrate is a narrow-spectrum β-lactam antibiotic, acts by inhibiting penicillin-binding proteins (PBPs). Methicillin sodium hydrate is active against Staphylococcus aureus and Staphylococcus epidermidis that are resistant to other penicillins. Methicillin sodium hydrate can be used for the research of skin infections, osteomyelitis, and endocarditis .
Methicillin is a narrow-spectrum β-lactam antibiotic, acts by inhibiting penicillin-binding proteins (PBPs). Methicillin is active against Staphylococcus aureus and Staphylococcus epidermidis that are resistant to other penicillins.Methicillin can be used for the research of skin infections, osteomyelitis, and endocarditis .
Zosurabalpin is a polypeptide antibiotic targeting LPS transporter (LptB2FGC complex), which can block the transport of LPS and lead to endotoxin accumulation in cells, and has shown excellent antibacterial activity against Carbapenem-resistantAcinetobacter baumanni (CRAB) .
Mtb-IN-5 (compound (-)17j) is an isoxazole, with anti-Mycobacterium tuberculosis (Mtb) activity. Mtb-IN-4 inhibits Mtb respiration and biofilm formation in macrophage, and enhances antibiotic isoniazid (INH) inhibition against INH-resistant Mtb mutant .
KNK423 is a specific heat shock protein (HSP) synthesis inhibitor. KNK423 improves the efficiency of Amphotericin B in inhibiting resistantAspergillus terreus by blocking HSP70. KNK423 can be used in cancer and bacterial infection research .
Anti-MRSA agent 9 (compound 39) shows antibacterial effects against clinically isolated methicillin-resistant Staphylococcus aureus (MRSA) with MIC values of 1 μg/ml. Anti-MRSA agent 9 also shows anti-MRSA efficacy in vivo .
EBP-59 is a bacterial inhibitor with antibiofilm activity against Gram-positive bacteria. EBP-59 is effective against Staphylococcus aureus and MRSA (methicillin–resistant staphylococcus aureus). EBP-59 can be used to study bacterial infections .
Antibacterial agent 226 (Compound 7f) is an antibacterial agent, that inhibits Staphylococcus aureus strains and methicillin-resistantS. aureus strain with MIC of 2 μg/mL. Antibacterial agent 226 exhibits cytotoxicity to HEK293 with IC50 of 1.9 μM .
WK88-1, a Hsp90 inhibitor, induces overall degradation of multiple oncogenic signaling molecules including EGFR, ErbB2 and ErbB3, leading to subsequent growth arrest and apoptosis in the Gefitinib-resistant H1975 cell line .
Methotrexate-γ-aspartate is a Ll210 cell dihydrofolate reductase inhibitor. Methotrexate-γ-aspartate is apparently more resistant to enzymic cleavage than is methotrexate-y-glutamate. Methotrexate-γ-aspartate can be used in antibody-targeted liposomes and is promising for research of leukemic .
Ceftazidime (GR20263), an antibiotic, has a broad spectrum activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime is also active against Enterobacteriaceae (including β-lactamase-positive strains) and is resistant to hydrolysis by most β-lactamases .
Linezolid (PNU-100766) is the first member of the class of oxazolidinone synthetic antibiotic. Linezolid acts by inhibiting the initiation of bacterial protein synthesis. Linezolid is used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics .
Besifovir Dipivoxil maleate (LB80380 maleate) is an oral proagent of LB80317. Besifovir Dipivoxil maleate (LB80380 maleate) is effective in hepatitis B virus (HBV) DNA suppression for both treatment-naive and lamivudine-resistant chronic hepatitis B (CHB) patients in preliminary studies [2]
Continentalic acid from Aralia continentalis has minimum inhibitory concentrations (MICs) of approximately 8-16 µg/mL against S. aureus, including the Methicillin (HY-121544) susceptible Staphylococcus aureus (MSSA) and Methicillin-resistantStaphylococcus aureus (MRSA) standard strains .
8-Epidiosbulbin E acetate, a furanoid, is abundant in Dioscorea bulbifera L.. 8-Epidiosbulbin E acetate exhibits broad-spectrum plasmid-curing activity against multidrug-resistant (MDR) bacteria. 8-Epidiosbulbin E acetate induces liver injury in mice .
PIP-199 is a selective inhibitor of RMI (RecQ-mediated genome instability protein) core complex/MM2 interaction, with an IC50 of 36 μM. PIP-199 can be used for the research of sensitizing resistant tumors to DNA crosslinking chemotherapeutics .
Contezolid (MRX-I), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid (MRX-I) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI) .
Laninamivir octanoate (CS-8958), a proagent of Laninamivir, is a long-acting neuraminidase (NA) inhibitor with anti-influenza virus activity. Laninamivir octanoate shows anti-influenza activity against Oseltamivir-resistant viruses, and also against the pandemic influenza viruses .
Cheilanthifoline, an alkaloid, is isolated from Corydalis calliantha. Cheilanthifoline exhibits antiplasmodial activities against Plasmodium falciparum, with IC50s of 0.90 μg/mL and 1.22 μg/mL for wild type (TM4) and multidrug resistant (K1) strains, respectively .
1-Methoxyphaseollidin, a flavonoid compound, is a lysoPAF acetyltransferase inhibitor, with an IC50 of 48 μM. 1-Methoxyphaseollidin exhibits anti-H.pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains .
Heptaplatin (SKI 2053R) is a platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant tumor cell lines. SKI-2053R is active in the research of gastric adenocarcinoma and has favorable toxicity profiles .
Anti-MRSA agent 4 (compound 7a) is a potent and selective growth inhibitor of Gram-positive Methicillin-resistantStaphylococcus aureus (MRSA), with MIC ≤ 0.26 µM. Anti-MRSA agent 4 exhibits no cytotoxic and no hemolytic activity in HEK293 cells .
Gemifloxacin, a fluoroquinolone, is a potent and orally active antipneumococcal agent. Gemifloxacin shows bactericidal activity against highly quinolone-resistant pneumococci.Gemifloxacin can be used for the research of respiratory infections, such as community-acquired pneumonia (CAP) and acute exacerbation of chronic bronchitis (AECB) .
Upifitamab is an ADC Antibody (a naked antibody of upifitamab rilsodotin), which can be used for antibody-coupled agent (ADC) synthesis. Upifitamab rilsodotin is an ADC targeting NaPi2b and is used in ovarian cancer research, particularly in platinum-resistant recurrent ovarian cancer .
Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
Laninamivir octanoate hydrate (CS-8958 hydrate), a prodrug of Laninamivir, is a long-acting neuraminidase (NA) inhibitor with anti-influenza virus activity. Laninamivir octanoate hydrate shows anti-influenza activity against Oseltamivir-resistant viruses, and also against the pandemic influenza viruses .
Kigamicin C is an anti-tumor antibiotic that selectively kills pancreatic cancer PANC-1 cells only in nutrient-poor conditions. Kigamicin C has antimicrobial activity against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) .
Netilmicin (Sch 20569) is an antibiotic. Netilmicin exhibits antibacterial activity against aminoglycoside-susceptible gram-negative strains and aminoglycoside-resistant strain, such as Escherichia coli, Pseudomonas aeruginosa, Proteus, Staphylococcus aureus, Streptococcus, Serratia, and Enterobacter, with MIC of 0.125-8 μg/mL .
(-)-Halofantrine ((-)-SKF-102886 free base; (-)-WR-171669) is an inhibitor of the malignant malaria parasite (P. falciparum) and targets multidrug-resistant P. falciparum. The pharmacokinetic parameters of (-)-Halofantrine in rats vary depending on the route of administration, distinguishing it from other isomers .
Kopsoffinol, a bisindole alkaloid, shows in vitro growth inhibitory activity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells .
VUF14862 is a robust and fatigue-resistant photoswitchable GPCR antagonist that exhibits over a 10-fold increase in H3R binding affinity upon illumination at 360 nm. VUF14862 can be utilized for spatiotemporal studies of H3R signaling .
S07-2010 is a potent pan-AKR1C (aldo-keto reductase family 1 member C) inhibitor, with IC50 values of 0.19, 0.36, 0.47, and 0.73 μM for AKR1C3, AKR1C4, AKR1C1 and AKR1C2, respectively. S07-2010 induces apoptosis in A549/DDP cells. S07-2010 strengthens the cytotoxicity of chemotherapeutic agents in drug-resistant cells. S07-2010 significantly inhibits the proliferation of drug-resistant cells .
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .
9-Oxonerolidol is a farnesane-type sesquiterpenoid with anti-pathogens activity. 9-Oxonerolidol can be isolated from Chiliadenus lopadusanus. 9-Oxonerolidol acts as a post-infectional inhibitor from plants, and inhibits Gram+ and Gram? bacteria resistant to the antibiotic .
(S)-Verapamil-d7 (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells[1][2].
ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistantALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
TP0586352 is a LpxC inhibitor that is effective against carbapenem-resistantKlebsiella pneumoniae and does not pose a cardiovascular risk. TP0586352 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
CAY10621 (SKI 5C; compound 5c) is a specific sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 3.3 μM. CAY10621 is low toxic toward cells. CAY10621 has the potential for resistant cancer tumors research .
Antibacterial agent 86 (Compound A11) is the most active and displays bacteriostatic activities against methicillin-resistant S. aureus, with MIC values as low as 0.00191 μg/mL, which is 162 and 32 times lower than that of the marketed antibiotics tiamulin and retapamulin, respectively .
Alamifovir (LY582563; MCC-478), a purine nucleotide analogue proagent, shows potent activity against wild type and lamivudine resistanthepatitis B virus (HBV). Alamifovir has high activity against HBV replication and sustained antiviral effect .
Lynronne-2 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including
MDR strains (MIC: 32-256 μg/mL for methicillin-resistant MRSA strains). Lynronne-2 is also effective against P. aeruginosa infection
Lynronne-3 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including
MDR strains (MIC: 32-128 μg/mL for methicillin-resistant MRSA strains). Lynronne-3 is also effective against P. aeruginosa infection
L-K6L9 shows antimicrobial and antibiofilm activities against P. aeruginosa from cystic fibrosis patients. L-K6L9 is stable and resistant to degradation by cystic fibrosis sputum proteases and will not induce bacterial resistance .
D-K6L9 shows antimicrobial and antibiofilm activities against P. aeruginosa from cystic fibrosis patients. D-K6L9 is stable and resistant to degradation by cystic fibrosis sputum proteases and will not induce bacterial resistance .
Jingzhaotoxin-V is a peptide that inhibits potassium currents in Xenopus laevis oocytes with an IC50 value of 604.2 nM. Jingzhaotoxin-V also inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 and 30.2 nM, respectively .
Jingzhaotoxin-34, a 35-residue polypeptide, is a neurotoxin. Jingzhaotoxin-34 inhibits tetrodotoxin-sensitive (TTX-S) sodium currents (IC50 of ~85 nM) while having no significant effects on tetrodotoxin-resistant (TTX-R) sodium currents on rat dorsal root ganglion neurons .
SF5 (2,2-Diphenylethyl isothiocyanate) is a sulforaphane analog. SF5 inhibits apoptosis by the JNK-p53-caspase pathway. SF5 can be used as a new renal protective agent for drug-resistant acute renal disease .
Fabl inhibitor 1 (Compound (S)-n31) is an orally active and potent SaFabI inhibitor (IC50 = 94.0 nM, MIC = 0.25-1 μg/mL). Fabl inhibitor 1 can be used for the research of methicillin-resistantS. aureus (MRSA) infection .
Levonadifloxacin ((S)-(-)-Nadifloxacin; WCK 771) arginine is a broad-spectrum antistaphylococcal agent. Levonadifloxacin arginine has antimicrobial activity against methicillin-susceptible Staphylococcus aureus (MSSA) and methicillin-resistant Staphylococcus aureus and reduces phagocytosis of MRSA and MSSA strains by monocytic THP-1.
Netilmicin (sulfate) (Standard) is the analytical standard of Netilmicin (sulfate). This product is intended for research and analytical applications. Netilmicin (sulfate) (SCH-20569 (sulfate)) is an active aminoglycoside antibiotic against most Gram-negative and some Gram-positive bacteria, including certain strains resistant to gentamicin.
Niranthin (Standard) is the analytical standard of Niranthin. This product is intended for research and analytical applications. Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
Epetraborole R-mandelate is a novel leucyl-tRNA synthetase (LeuRS) inhibitor (IC50=0.31 μM), thereby inhibiting protein synthesis. Epetraborole R-mandelate can be used in multidrug-resistant gram-negative pathogens infection research .
Ganaplacide (KAF156) is a first-in-class,
orally active imidazolopiperazine antimalarial agent.
Ganaplacide is active against a broad range of Plasmodium
species, including drug-resistant parasites. Ganaplacide is parasiticidal
against both asexual and sexual blood stages as well as the liver stages of the
parasite .
Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
Ceftazidime (GR20263) pentahydrate , an antibiotic, has a broad spectrum activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime pentahydrate is also active against Enterobacteriaceae (including β-lactamase-positive strains) and is resistant to hydrolysis by most β-lactamases .
Wulignan A1 is isolated from the stems of Schisandra henryi. Wulignan A1 exhibits anti-influenza virus H1N1 and H1N1-TR (a Tamiflu agent resistant virus strain) activities .
N-Acetyltyramine is a quorum-sensing inhibitor (QSI) compound produced by V. alginolyticus M3-10. N-Acetyltyramine is capable of inhibiting the QS of C. violaceum ATCC 12472. N-acetyltyramine reverses resistance in Doxorubicin-resistant leukemia P388 cells .
CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia .
Ganaplacide (KAF156) hydrochloride is a first-in-class, orally active imidazolopiperazine antimalarial agent. Ganaplacide hydrochloride is active against a broad range of Plasmodium species, including drug-resistant parasites. Ganaplacide hydrochloride is parasiticidal against both asexual and sexual blood stages as well as the liver stages of the parasite .
RO-0335 is a novel and potent diphenylether nonnucleoside reverse transcriptase inhibitor(NNRTI). RO-0335 inhibits Wt HIV-1 with an IC50 of 1.1 nM and retained activity (IC50< 100 nM) against 92% of a large number of NNRTI-resistant clinical isolates .
HIV-1 protease-IN-2 is a potent HIV-1 protease inhibitor with an IC50 of 2.53 nM. HIV-1 protease-IN-2 shows antiviral activity against DRV (Darunavir)-sensitive or DRV-resistant HIV-1 variants .
PNU-101603 is a sulfoxide metabolite of Sutezolid (HY-10392). PNU-101603 alone or combined with SQ109 (HY-14989) shows excellent activity against Mycobacterium tuberculosis (MTB), as well as against agent-susceptible and multidrug-resistant TB .
4-Hydroxyoxyphenbutazone kills both replicating and nonreplicating (NR) Mycobacterium tuberculosis (Mtb), including Mtb resistant to standard agents. 4-Hydroxyoxyphenbutazone is a potent inhibitor of cytokine production. 4-Hydroxyoxyphenbutazone is an immunosuppressive agent and has the potential for rheumatoid arthritis research .
Jingzhaotoxin-II, a 32 amino acid residues including two acidic and two basic residues, is a neurotoxin. Jingzhaotoxin-II inhibits voltage-gated sodium channels (VGSC) that significantly slows rapid inactivation of TTX-resistant (TTX-R) VGSC on cardiac myocytes with the IC50 of 0.26 μM .
Jatrophane 5 is a natural product of Jatropha carcas L. Jatrophane 5 has powerful inhibition of P-gp, higher than R(+)-verapamil (HY-14275) and Tariquidar (HY-10550) in colorectal multi-drug resistant cells (DLD1-TxR) .
Sulbactam (Standard) is the analytical standard of Sulbactam. This product is intended for research and analytical applications. Sulbactam (CP45899) is a competitive, irreversible beta-lactamase inhibitor. Sulbactam shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
Sulbactam (sodium) (Standard) is the analytical standard of Sulbactam (sodium). This product is intended for research and analytical applications. Sulbactam (CP45899) sodium is a competitive, irreversible beta-lactamase inhibitor. Sulbactam sodium shows antimicrobial activity against multidrug-resistant (MDR) acinetobacter calcoaceticus--Acinetobacter baumannii (Acb) complex .
Antibacterial agent 240 (compound 62-7c) is an antibacterial agent that can target multidrug-resistant (MDR) MRSA strains. Antibacterial agent 240 showed high biosafety and potent anti-infection activity in mouse pneumonia and mouse wound models of MRSA infection .
PAM 1392 is active orally against Plasmodium berghei in mice, P. cynofologi and P. knowlesi in monkeys and Trypanosoma cruzi in tissue cultures of mice, and hemolytic streptococci in vitro. PAM 1392 has antimalarial and antitrypanosomal activities, which is proming for rasearch of drug-resistant malaria .
Broflanilide (Standard) is the analytical standard of Broflanilide. This product is intended for research and analytical applications. Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM .
Anticancer agent 259 (Compound 3g) is a Telmisartan (HY-13955)-based cell death modulator, that interfers with the STAT5 signaling pathway, enhances the sensitivity of drug-resistant cells to Imatinib (HY-15463) with SC50 of 1.5 μM .
NVP-BVU972 is an selective and potent Met inhibitor, with an IC50 of 14 nM. NVP-BVU972 also exhibits good anti-proliferative activity against Met with drug-resistant mutations and inhibits phosphorylation. NVP-BVU972 can be used in study of cancer .
SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-na?ve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations .
SPR719 (VXc-486) is a gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple agent-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively .
FBA-IN-1 (compound 2a11) is a first-in-class, covalent and allosteric inhibitor of fructose-1,6-bisphosphate aldolase from Candida albicans (CaFBA). FBA-IN-1 inhibits the growth of Azole-resistant strains 103 with the MIC80 of 1 μg/mL .
MptpB-IN-1 (Compound 13) is a potent and orally active inhibitor of MptpB. Mycobacterium tuberculosis protein-tyrosine-phosphatase B (MptpB) is a secreted virulence factor that subverts antimicrobial activity in the host. MptpB-IN-1 reduces multidrug-resistant mycobacterium tuberculosis survival and infection burden .
Delafloxacin-d5 is deuterium labeled Delafloxacin. Delafloxacin (RX-3341; WQ-3034; ABT492) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia[1].
HIV-1 protease-IN-5 (Compound 13c) is a HIV-1 protease inhibitor with an IC50 of 1.64 nM. HIV-1 protease-IN-5 shows remarkable activity against wild-type and DRV-resistant HIV-1 variants .
Laburnetin is a kind of isoflavone antibacterial agent. Laburnetin has antibacterial activity against fungi and S. vesicarium. Laburnetin intensifies the susceptibility of Methicillin (HY-121544) resistantStaphylococcus aureus (MRSA) strains to Methicillin. Laburnetin can be used to control pests of cultivated species .
DGKζ-IN-1 (compound 9) is an inhibitor of DGKζ. DGKζ-IN-1 can be used for research in cancer related to immunocyte activation or cancer resistant to anti-PD-1 antibody/anti-PD-L1 antibody .
RG33 Peptide is a diabetes inhibitor that significantly improves glucose clearance in insulin-resistant mice. RG33 Peptide effectively solubilizes lipid vesicles and promotes cholesterol efflux in cultured macrophages. RG33 Peptide is used in research into type 2 diabetes (T2D) .
Anti-MRSA agent 8 (Compound 7g) is a DAPG derivative with strong antibacterial activity. Anti-MRSA agent 8 assertes its activity by targeting bacterial cell membranes. Anti-MRSA agent 8 can be used for the research of methicillin-resistantStaphylococcus aureus (MRSA) .
β-Yohimbine (Amsonin) is an indole alkaloid that can be isolated from Aspidosperma ulei Markgr. β-Yohimbine shows antiplasmodial activity against the Chloroquine (HY-17589A)-resistant Fc M29-Cameroon strain (IC50: > 1 μg/mL) .
CEP-8983 is a PARP-1 and PARP-2 inhibitor (IC50: 20 and 6 nM). CEP-8983 is an effective chemosensitizing agent, and can sensitize chemotherapy-resistant cell lines and subcutaneous xenografts to Temozolomide (HY-17364) and Camptothecin (HY-16560) .
Tetromycin A is a tetronic acid-based antibiotic. It reportedly has pronounced activity against Gram-positive bacteria, including methicillin-resistant S. aureus. Related tetromycin derivatives have been found to have anti-trypanosomal activity and inhibit the cysteine protease cathepsin L with Ki values in the low micromolar range.
Levonadifloxacin ((S)-(-)-Nadifloxacin; WCK 771) arginine is a broad-spectrum antistaphylococcal agent. Levonadifloxacin arginine has antimicrobial activity against methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant Staphylococcus aureus and reduces phagocytosis of MRSA and MSSA strains by monocytic THP-1 cells .
KAR425 is a potent and orally active antimalarial agent. KAR425 shows antimalarial activity against the Chloroquine-sensitive (CQS) D6, the Chloroquine-resistant (CQR) Dd2, and 7G8 strains of Plasmodium falciparum, with IC50 values of 62 nM, 55 nM, and 60 nM, respectively .
N,N-Dimethyl-idarubicin, an Idarubicin (HY-17381) derivative, is a potent histone evictor which does not induce DNA double-strand breaks. N,N-Dimethyl-idarubicin, an anthracycline, is an effective cytotoxic agent for ABCB1-overexpressing, Doxorubicin-resistant cells .
O,O-Dimethyl-cannabigerol is a natural product from Cannabis sativa. O,O-Dimethyl-cannabigerol has an antibacterial effect on drug-resistant strains of Staphylococcus aureus (MIC ranging from 1 to 2 μg/mL) . O,O-Dimethyl-cannabigerol is a nonpsychoactive constituent .
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.
Levonadifloxacin (arginine) hydrate is a broad-spectrum anti-staphylococcal agent. Levonadifloxacin (arginine) hydrate shows antibacterial activity against Methicillin (HY-121544)-susceptible Staphylococcus aureus (MSSA) and Methicillin-resistantS. aureus (MRSA) strains, with a reduction of which phagocytized in THP-1 monocytes .
Tebuquine (WR228258), a 4-aminoquinoline, is a potent antimalarial agent. Tebuquine is active against the Chloroquine (HY-17589A) sensitive HB3 strain and the Chloroquine resistant K1 strain of Plasmodium falciparum with IC50s of 0.9 nM and 20.8 nM, respectively .
NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC50 of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model .
Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistantSalmonella enterica serovar Typhimurium in macrophages .
Benzobicyclon is a 4-HPPD inhibitor and herbicide that reacts with water to form a hydrolysate of the active herbicide benzobicycline, causing bleaching and death of weeds. Benzobicyclon is effective against grass, sedge and broadleaf weeds. Benzobicyclon effectively targets sulfonylurea herbicide-resistant biotypes as well as wild-type weeds .
Contezolid acefosamil sodium (MRX-4), a new and orally active oxazolidinone, is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid acefosamil sodium (MRX-4) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI) .
Amikacin (BAY 41-6551) is a semisynthetic kanamycin analog that is active against most Gram-negative bacteria, including gentamicin- and tobramycin-resistant strains. Significant inhibitory effect. Amikacin is ototoxic and nephrotoxic. Amikacin can be used in bacteriostatic, anti-cancer and analgesic studies .
Pasotuxizumab (BAY 2010112) is a PSMA and CD3 bispecific T-cell engager (BiTE). Pasotuxizumab binds to CD3 and PSMA with KDs of 9.4 nM and 47.0 nM for human CD3 and PSMA. Pasotuxizumab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
Antibacterial agent 186 (compound 25) is a potent antibacterial agent. Antibacterial agent 186 shows antibiofilm-forming properties against clinical Staphylococcus epidermidis strains and demonstrates the capacity to eliminate existing biofilm layers. Antibacterial agent 186 has the potential for the research of multidrug-resistantStaphylococcus epidermidis .
Amikacin (Standard) is the analytical standard of Amikacin. This product is intended for research and analytical applications. Amikacin (BAY 41-6551), a semisynthetic analog of kanamycin, is very active against most gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin (BAY 41-6551) is ototoxic and nephrotoxic .
Topoisomerases/ribosomes-IN-1 (compound 30f) is an inhibitor of ribosomes and topoisomerases, and has inhibitory effects on constitutively macrolide-resistant bacteria. Topoisomerases/ribosomes-IN-1 can inhibit bacterial protein synthesis (IC50: 0.647 μM) and DNA replication (IC50: 0.218 μM) .
WCK-5153 is a Penicillin-Binding Protein 2 (PBP2) inhibitor with an IC50 of 0.14 μg/ml (for P. aeruginosa PBP2) and acts as a β-lactam enhancer against Pseudomonas aeruginosa. WCK-5153 can be used in studies of multidrug-resistant (MDR) pathogens .
BWC0977 is a potent bacterial topoisomerase inhibitor that inhibits bacterial DNA replication via inhibition of DNA gyrase and topoisomerase IV. BWC0977 exhibits a minimum inhibitory concentration (MIC90) of 0.03-2 µg/mL against MDR (Multi-Drug Resistant) Gram-negative bacteria .
CYP51-IN-21 (Compound A33) is a potent CYP51 inhibitor. CYP51-IN-21 shows excellent antifungal activities against pathogenic fungi and drug-resistant strains. CYP51-IN-21 inhibits the formation of fungal biofilm .
Albenatide (CJC 1134PC) is a modified Exendin-4 (HY-13443) analogue conjugated to human recombinant albumin (HRA) in vitro to form a long-acting DPP-4-resistantGLP-1R agonist. Albenatide covalently binds through a low-molecular chemical linker (cys-C13H19O6N3-lys) to the cysteine residue in position 34 of HRA. Albenatide increases cyclic AMP (cAMP) production in vitro. Albenatide reduces glucose excursions, food intake, gastric emptying in wild-type mice and improves glucose tolerance and reduces body weight in high-fat diet mice .
Novobiocin (Albamycin) sodium is a potent and orally active antibiotic. Novobiocin sodium also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin sodium has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin sodium shows anti-orthopoxvirus activity .
Lascufloxacin (KRP-AM1977X) is a potent and orally active fluoroquinolone antibacterial agent. Lascufloxacin potently inhibits infections caused by various pathogens, including quinolone-resistant strains. Lascufloxacin has the potential for various infectious diseases treatment, including lower respiratory tract infections .
BVDV-IN-1 is a non-nucleoside inhibitor (NNI) of bovine viral diarrhea virus (BVDV), with an EC50 of 1.8 μM. BVDV-IN-1 directly binds to a hydrophobic pocket of the BVDV RdRp. BVDV-IN-1 has antiviral activity against BVDV resistant to NNI thiosemicarbazone (TSC) .
MDP1, a Melittin-derived peptide, alters the integrity of both Gram-positive and Gram-negative bacterial membranes and kills the bacteria via membrane damages. MDP1 has a high-antibacterial activity against multidrug resistant (MDR) and reference strains of S. aureus, E. coli, and P. aeruginosa .
MDP1 acetate, a Melittin-derived peptide, alters the integrity of both Gram-positive and Gram-negative bacterial membranes and kills the bacteria via membrane damages. MDP1 acetate has a high-antibacterial activity against multidrug resistant (MDR) and reference strains of S. aureus, E. coli, and P. aeruginosa .
VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM) .
Seconeolitsine, an antibiotic, and is an inhibitor of targeting topoisomerase I (TopA). Seconeolitsine also is a new antimicrobial agent that can inhibit S. pneumoniae growth. Seconeolitsine can inhibit TopA relaxation activity with an IC50 value of 17 μM. Seconeolitsine can be used for the research of S. pneumoniae infections resistant to other antibiotics .
Levonadifloxacin ((S)-(-)-Nadifloxacin; WCK 771) is a broad-spectrum anti-staphylococcal agent. Levonadifloxacin shows antibacterial activity against Methicillin (HY-121544)-susceptible Staphylococcus aureus (MSSA) and Methicillin-resistantS. aureus (MRSA) strains, with a reduction of which phagocytized in THP-1 monocytes .
Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting antibody (DART). Lorigerlimab can block PD-1 and CTLA-4, and improves T-cell responses. Lorigerlimab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
(Rac)-Bedaquiline is the racemate of Bedaquiline. Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting both the c- and the ε-subunit. Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
Antiparasitic agent-17 (compound 5u) is an orally active antiparasitic agent. Antiparasitic agent-17 inhibits Chloroquine sensitive (Pf3D7) and Chloroquine resistant (PfK1) strain with IC50s of 0.96 μM and 1.67 μM, respectively .
MK-4965 is a nonnucleoside reverse transcriptase inhibitor (NNRTI). MK-4965 displays excellent activities against not only HIV-1 wild-type (WT) virus but also against a broad panel of NNRTI-resistant viruses and can be used for the research of HIV-1 infection .
Durlobactam sodium salt (ETX2514) is a broad-spectrum β-lactamase inhibitor with IC50s of 4, 14 and 190 nM for Class A KPC-2, Class C AmpC and Class D OXA-24, respectively. For the treatment of drug-resistant Gram-negative bacteria including Acinetobacter baumannii .
MX106-4C is a survivin inhibitor that selectively kills ABCB1-positive colorectal cancer cells. MX106-4C can exert synergistic anticancer effects with Doxorubicin or resensitize drug-resistant ABCB1 cells to Doxorubicin .
Delafloxacin (Standard) is the analytical standard of Delafloxacin. This product is intended for research and analytical applications. Delafloxacin (RX-3341; WQ-3034; ABT492) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistantStaphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia .
8-OH-cAMP (8-Hydroxy-cAMP) is a polar, membrane-impermeable cyclic adenosine monophosphate analog that is resistant to mammalian cyclic nucleotide-dependent phosphodiesterases. As a polar PKA agonist, 8-OH-cAMP is used to study the role of cAMP in the development and progression of cardiovascular and metabolic diseases .
P-gp modulator-5 (compound 25) is a modulator of P-gp and can inhibit the proliferation of multidrug resistant (MDR) tumors. P-gp modulator-5 inhibits the activity of drug efflux pumps in MDR cells, leading to a large accumulation of ROS and altered cell cycle profiles .
AST5902 mesylate is a principal metabolite of Alflutinib, exhibiting significant antineoplastic activity. AST5902 mesylate contributes to the overall pharmacological effects in the treatment of non-small cell lung cancer. AST5902 mesylate is involved in the response to activating EGFR mutations and can help overcome EGFR T790M drug-resistant mutations.
MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 is an antivirulence agent that reverses β-lactam resistance in Methicillin-resistant strains (MRSA) .
OBI-3424 (TH-3424) is a proagent that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research .
Antifungal agent 28 (compound 18) is a potent and selective antifungal agent. Antifungal agent 28 inhibits pathogenic strains of C. albicans and non-albicans species including fluconazole-resistant strains. Antifungal agent 28 inhibits Cryptococcus and Aspergillus strains. Antifungal agent 28 disrupts mature Candida biofilm .
Anti-MRSA agent 2 (compound 14) has highly inhibitory activity against Methicillin-resistantStaphylococcus 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 .
Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity .
MmpL3-IN-1 (compound 32) is a potent Mycobacterial membrane protein large 3 (MmpL3) inhibitor. MmpL3-IN-1 has anti-tuberculosis activity with the MIC<0.016 μg/mL in M. tuberculosis and can be used in studies of drug-resistant tuberculosis .
Chitin synthase inhibitor 7 (compound 9c) is a potent chitin synthase (CHS) inhibitor with an IC50 value of 0.37 mM. Chitin synthase inhibitor 7 has broad-spectrum antifungal activity against drug-resistant fungi. Chitin synthase inhibitor 7 can be used in the research of fungi infection .
Chitin synthase inhibitor 6 (compound 9b) is a potent chitin synthase (CHS) inhibitor with an IC50 value of 0.21 mM. Chitin synthase inhibitor 6 has broad-spectrum antifungal activity against drug-resistant fungi. Chitin synthase inhibitor 6 can be used in the research of fungi infection .
Mtb-IN-4 (compound 17h) is a nontoxic isoxazole, with anti-Mycobacterium tuberculosis (Mtb) activity (IC50=0.70 μM). Mtb-IN-4 inhibits Mtb respiration and biofilm formation in macrophage, and enhances antibiotic isoniazid (INH) inhibition against INH-resistant Mtb mutant .
Antitubercular agent-39 (Compound P1) is a potent antitubercular agent. Antitubercular agent-39 is active against drug-resistant strains and drug-susceptible clinical isolates. Antitubercular agent-39 inhibits Mtb strain H37Rv with a MIC less than 1 μM .
Anti-Influenza agent 5 (Compound IIB-2), chalcone-like derivative, is an influenza nuclear export inhibitor. Anti-Influenza agent 5 has inhibitory effects on oseltamivir-resistant strains. Anti-Influenza agent 5 can impede virus proliferation by blocking the export of influenza virus nucleoprotein .
Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis .
XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ .
Pyraclonil is a proporphyrinogen oxidase (PPO) inhibitor. Pyraclonil is a herbicide agent and is highly effective in controlling the susceptible (S) and multiple-herbicide-resistant (MHR) E. indica populations . Pyraclonil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Teicoplanin is a glycopeptide antibiotic indicated for use in serious infections caused by Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus and Enterococcus aureus.Teicoplanin shows antiviral activity for HIV-1, SARS-CoV1 and SARS-CoV2. Teicoplanin sodium shows anti-MRSA activity .
Allicin (diallyl thiosulfinate) is isolated from garlic including Diallyl monosulfide, Diallyl disulfide, Diallyl trisulfide, Diallyl tetrasulfide, and Methyl allyl disulphide etc. They accounts for 98% of the extract. Allicin (diallyl thiosulfinate) has highly potent antimicrobial activity, and inhibits growth of a variety of microorganisms, among them antibiotic-resistant strains .
Zotizalkib (TPX-0131) is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). Zotizalkib has strong antitumor activities .
HDAC1-IN-3 is a potent Pf HDAC1 inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistant parasite strains. HDAC1-IN-3 shows a significant in vivo killing effect against all life cycles of parasites .
Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.
Antibacterial agent 98 (compound g37) is a potent and orally active antibacterial agent. Antibacterial agent 98 inhibits the ATPase activity of Gyrase B and impairs Staphylococcus aureus (S. aureus ) DNA supercoiling. Antibacterial agent 98 shows antibacterial activity and not induce resistance development of MRSA (methicillin-resistantS. aureus) .
Colistin (Polymyxin E) is an orally active polypeptide antibiotic. Colistin has excellent activity against various Gram-negative rod-shaped bacteria, including multidrug-resistantPseudomonas aeruginosa, Acinetobacter baumannii and Klebsiella pneumoniae. Colistin is associated with nephrotoxicity. Colistin can be used for the research of infections caused by Gram-negative bacilli .
Anti-IAV agent 1 (Compound (R)-1a) is an orally active anti-influenza A virus (IAV) agent with IC50s of 0.03 and 0.06 μM against IAV H1N1 and Oseltamivir-resistant IAV H1N1 strains, respectively .
Teicoplanin sodium is a glycopeptide antibiotic indicated for use in serious infections caused by Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus and Enterococcus aureus.Teicoplanin sodium shows antiviral activity for HIV-1, SARS-CoV1 and SARS-CoV2. Teicoplanin sodium shows anti-MRSA activity .
Antibacterial agent 150 (compound 5g) is an antibacterial agent with potent antibacterial activity against both Gram-positive bacteria and Gram-negative bacteria (MIC values ranging from 1-32 μg/mL). Antibacterial agent 150 can increase survival rate of MRSA (Methicillin-resistantStaphylococcus aureus)-infected mice .
DHFR-IN-8 (compound 6r) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-8 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=15.6 ng/mL) in mouse models of systemic infection and thigh infection .
Chimaphilin is an IGF-1R inhibitor (IC50: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola .
OY-101 is an orally active, potent and specific P-glycoprotein (P-gp) inhibitor. OY-101 can sensitize drug-resistant tumors and effectively reverse tumor multidrug resistance. OY-101 is improvements in water-solubility, cytotoxicity, and reversal activity compared to Tetrandrine (HY-13764) .
BKM1644, an acyl-tyrosine bisphosphonate amide derivative, exhibits potent anti-cancer activity. BKM1644 effectively inhibits the proliferation of metastatic, castration-resistant prostate cance (mCRPC) cells. BKM1644 sensitizes mCRPC cells to Docetaxel (HY-B0011) and retards the bone metastatic growth of prostate cance .
P-gp inhibitor 19 (Compound 6i) is a P-gp inhibitor. P-gp inhibitor 19 can inhibit the efflux of rhodamine 123 (HY-D0816) in P-gp-overexpressing leukemia cells K562/Dox and also restore the sensitivity of DOX-resistant cells .
Antibacterial agent 182 (compound 8c) is an antibacterial agent that shows antibacterial activity against various Gram-positive bacteria, particularly against Vancomycin-resistantEnterococcus faecalis (MIC ≤0.125 μg/mL). Antibacterial agent 182 inhibits biofilm formation of Staphylococcus aureus and Pseudomonas aeruginosa at sub-MIC doses .
Antifungal agent 95 (Compound CN21b) is an antifungal agent for Sclerotinia sclerotiorum and Botrytis cinerea, with EC50s of 2.11 and 0.97 μM, respectively. Antifungal agent 95 exhibits antifungal activity against resistantB. cinerea strains, with EC50s less than 10 μM .
Adefovir dipivoxil (Standard) is the analytical standard of Adefovir dipivoxil. This product is intended for research and analytical applications. Adefovir dipivoxil, an adenosine analogue, is an oral proagent of the nucleoside reverse transcriptase inhibitor Adefovir. Adefovir dipivoxil inhibits both the wild type and HBV Lamivudine-resistant strains . Adefovir dipivoxil shows anti-orthopoxvirus activity.
Biricodar dicitrate (VX 710-3) is the dicitrate salt form of Biricodar (HY-13574A). Biricodar dicitrate is an inhibitor for P-glycoprotein and multidrug resistance-associated protein 1 (MRP-1), which increases the accumulation of chemotherapy drugs within cancer cells and shows effective chemosensitizing activity in multidrug resistant cells .
Capravirine (S-1153) is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) with potent antiviral activity. Capravirine inhibits replication of HIV-1 strains that are resistant to nucleoside/nucleotide reverse transcriptase inhibitors and other NNRTIs. Capravirine is metabolized by the cytochrome P450 enzyme CYP3A4 .
Antifungal agent 115 (compound 8n) is a non-competitive chitin synthase (CHS) inhibitor with an IC50 of 93 μM. Antifungal agent 115 demonstrates good selectivity and broad-spectrum antifungal activity, exhibiting significant efficacy against drug-resistant fungi. Antifungal agent 115 can be utilized in fungi infection research .
Nidulin (Methylustin) is a depsidone isolated from a marine fungus Aspergillus unguis. Nidulin shows antifungal and antibacterial against pathogenetic strains, Pseudomonas aeruginosa, Methicillin-resistant Staphylococcus aureus and Candida albicans with inhibition zones of 9.5 mm, 9.0 mm and 9.0 mm, respectively. Nidulin exhibits potent larvicidality against brine shrimp .
V-161 is the orally active inhibitor for Na +-V-ATPase with an IC50 of 144 nM. V-161 inhibits Enterococcus hirae and Vancomycin-resistantEnterococcus faecium (VRE) under alkaline condition with MIC of 4 µg/mL and 4 µg/mL. V-161 inhibits colonization of VRE in mouse small intestine .
BD-10X (Lipase for biodiesel production) is a methanol-resistant lipase with high catalytic activity and can be used for the production of biodiesel. The reaction conditions of BD-10X are mild, which can avoid the oxidation of hydroxyl groups and the opening of double bonds, and prevent the production of by-products other than glycerol .
L-Valine (Valine) is a new nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml .
Methyl oleate is a fatty acid methyl ester (FAME) with anti-extended spectrum β-Lactamase (ESBL) potential, anticancer and antibacterial activities. Methyl oleate substantially improves the antioxidation ability but markedly impaired the antiwear capacity of zinc dialkyldithiophosphate (ZDDP). Methyl oleate is promising for research of ESBL producing multi drug resistant (MDR) pathogens .
WS-898 is a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively).
DprE1-IN-1 is a potent, orally active DprE1 inhibitor with favorable hepatocyte stability, low cytotoxicity and low hERG channel inhibition. DprE1-IN-1 displays potent activity against both agent-susceptible and clinically isolated drug-resistant Tuberculosis strains with MICs10 CFU reduction in macrophages.
HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus .
(Rac)-CCT 250863 (compound rac-21) is a selective and reversible NEK 2 inhibitor with an IC50 of 0.073 µM. (Rac)-CCT 250863 shows good effects of inducing cell cycle arrest and also can antiproliferative in cells (Pomalidomide sensitive/resistant). (Rac)-CCT 250863 induces apoptosis when combines with Pomalidomide .
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 inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
Bamlanivimab (Anti-Human SARS-CoV-2) is the first COVID-19 monoclonal antibody (mAb) to be granted Emergency Use Authorization (EUA) in November 2020 by the U.S. Food and agent Administration (FDA). However, Bamlanivimab is withdrawn in April 2021 following the rise of SARS-CoV-2 virus variants resistant to Bamlanivimab .
Permanent Orange is a synthetic pigment commonly used in the manufacture of paints and coatings. It belongs to the class of organic pigments and consists of carbon and other elements. Permanent Orange produces a bright orange color that is fade and weather resistant, making it ideal for outdoor applications. It can be mixed with other pigments to produce a range of colors and is compatible with a wide range of binders and solvents.
D-Cycloserine (Standard) is the analytical standard of D-Cycloserine. This product is intended for research and analytical applications. D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research .
Tet-20 is a biological active peptide. (Tet-20, is a synthetic cathelicidin-derived peptide. It was tested as infection-resistant coating for medical devices. When tethered on an implant surface Tet-20 exhibited broad antimicrobial activities both in vivo and in vitro. It can stop biofilm formation and appears to be non-toxic to eukaryotic cells)
Urumin has antiviral activity against the human influenza A virus. Urumin inhibits the growth of PR8 influenza virus (IC50: 3.8 μM). Urumin targets the conserved stalk of H1 hemagglutini, and is effective at neutralizing drug-resistant H1 influenza viruses. Urumin protects naive mice from lethal influenza infection .
GA32 (compound 58r) is potent androgen receptor (AR)/glucocorticoid receptor (GR) dual inhibitor with IC50 values of 0.13 μM and 0.83 μM for AR and GR, respectively. GA32 inhibits the proliferation of Enzalutamide (HY-70002) resistance castration-resistant prostate cancer both in vitro and in vivo .
Linezolid (Standard) is the analytical standard of Linezolid. This product is intended for research and analytical applications. Linezolid (PNU-100766) is the first member of the class of oxazolidinone synthetic antibiotic. Linezolid acts by inhibiting the initiation of bacterial protein synthesis. Linezolid is used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics .
Ceftazidime (Standard) is the analytical standard of Ceftazidime. This product is intended for research and analytical applications. Ceftazidime (GR20263), an antibiotic, has a broad spectrum activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime is also active against Enterobacteriaceae (including β-lactamase-positive strains) and is resistant to hydrolysis by most β-lactamases .
BING is an antimicrobial peptide that can be isolated from Japanese medaka fish. BING shows a broad-spectrum toxicity against pathogenic bacteria including drug-resistant strains. BING induces a deregulation of periplasmic peptidyl-prolyl isomerases in gram-negative bacteria, and reduces the RNA level of cpxR, which plays a crucial role in the development of antimicrobial resistance .
Fortimicin C is an antibiotic, which can be isolated from Micromonospora olivoasterospora. Fortimicin C exhibits broad-spectrum antibacterial activity, inhibits Escherichia coli, Staphylococcus aureus, Bacillus subtilis, Klebsiella pneumoniae, Salmonella typhosa and Serratia marcescens, with MICs of 0.16-0.64 μg/mL. Fortimicin C is resistant against aminoglycoside inactivating enzymes .
Hp1404 is a novel cationic antimicrobial peptide. Hp1404 has specific inhibitory activity 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 .
LXQ46 is an orally active inhibitor for protein tyrosine phosphatase 1B (PTP1B), with an IC50 of 0.190 μM. LXQ46 enhances insulin and leptin signaling pathways in insulin-resistant C2C12. LXQ46 ameliorates type 2 diabetes and increases insulin tolerance in mouse models .
Anti-MRSA agent 12 (Compound SM-5) is an antibiotic, which exhibits antibacterial activity against Staphylococcus aureus, S. epidermidis and Escherichia coli with MIC of 7.81, 7.81 and 62.5 μM. Anti-MRSA agent 12 inhibits the methicillin-resistantS. aureus (MRSA) through inhibition of biofilm formation .
Continentalic acid (Standard) is the analytical standard of Continentalic acid. This product is intended for research and analytical applications. Continentalic acid from Aralia continentalis has minimum inhibitory concentrations (MICs) of approximately 8-16 μg/mL against S. aureus, including the Methicillin (HY-121544) susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant Staphylococcus aureus (MRSA) standard strains .
9,10-trans-Dehydroepothilone D shows an antiproliferative activity against a paclitaxel-resistant cell lines overexpressing P-glycoprotein. 9,10-trans-Dehydroepothilone D also shows tubulin polymerization activity. 9,10-trans-Dehydroepothilone D is given by lactonization of Seco acid, which is promising for research of cancers .
BMS-351 (compound 18) is a potent, oral active, nonsteroidal CYP17A1 lyase inhibitor with the IC50 values of 19 nM and 4 nM aganist human CYP17A1 and cynomolgus monkeys CYP17A1,respectively. BMS-351 can be used for the study of castration-resistant prostate cancer .
Meropenem sodium is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem sodium has activity against susceptible and resistantN. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
AubipyOMe serves as a potent inhibitor of tartrate-resistant acid phosphatase (TRAP/ACP5), a metalloenzyme found in activated osteoclasts and macrophages, demonstrating IC50 values of 1.3 μM for TRAP5a and 1.8 μM for TRAP5b, while effectively inhibiting TRAP activity in extracts from murine macrophages and human lung tissue.
SMIP34 is a PELP1 inhibitor. SMIP34 binds to PELP1 with a Kd of 37.4 μM. SMIP34 inhibits cancer cell proliferation and tumor progression. SMIP34 can be used for breast cancer research, and is active against wild-type (WT), mutant (MT) ER + and therapy-resistant (TR)-ER + breast cancer .
Methicillin (sodium hydrate) (Standard) is the analytical standard of Methicillin (sodium hydrate). This product is intended for research and analytical applications. Methicillin sodium hydrate is a narrow-spectrum β-lactam antibiotic, acts by inhibiting penicillin-binding proteins (PBPs). Methicillin sodium hydrate is active against Staphylococcus aureus and Staphylococcus epidermidis that are resistant to other penicillins. Methicillin sodium hydrate can be used for the research of skin infections, osteomyelitis, and endocarditis .
Hellebrin is a bufadienolide compound extracted from plants that can inhibit tumor cell growth. Hellebrigenin shows potential in overcoming cancer cells' resistance to apoptosis stimuli and has also demonstrated anti-proliferation effects in multidrug-resistant (MDR) cancer cell models. Hellebrin can act on Na+/K+-ATPase to regulate intracellular signaling pathways .
O-Acetylsalicylhydroxamic acid is an acetylation inhibitor of prostaglandin H2 synthase that can suppress PGE2 synthesis in the body and block the cyclooxygenase activity of PGHS in vitro. O-Acetylsalicylhydroxamic acid requires the presence of the active site residue Ser-529 to act on human PGHS-1; the S529A mutant is resistant to the inactivation effects of this inhibitor .
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 inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistantN. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
MC-VC(S)-PABQ-Tubulysin M is a synthetic ADC drug-linker conjugate composed of the tubulin polymerization inhibitor Tubulysin M (an ADC Cytotoxin) (HY-N7053) and MC-VC(S)- PABQ (an ADC linker) is connected. MC-VC(S)-PABQ-Tubulysin M is effective against multidrug-resistant lymphoma cell lines and tumors .
Zabofloxacin hydrochloride (DW-224a) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin hydrochloride has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin hydrochloride is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP) .
iKIX1 is an antifungal agent and resensitizes drug-resistantC. glabrata to azole antifungals in vitro. iKIX1 inhibits the interaction between the KIX domain of the mediator subunit CgGal11A and the activation domain of CgPdr1, the IC50 and Ki values are 190.2 μM and 18 μM, respectively. iKIX1 is used for the study of multidrug resistance and C. glabrata infection .
TCS PrP Inhibitor 13, an antiprion agent, is a cellular prion protein (PrP C) inhibitor. TCS PrP Inhibitor 13, as a protease-resistant form of prion protein (PrP-res) accumulation inhibitor, shows an IC50 value of 3 nM in both ScN2a and F3 cell lines. TCS PrP Inhibitor 13 induces Schwannoma cells apoptosis .
Isepamicin (Sch 21420) is an aminoglycoside antibacterial. Isepamicin has better activity against strains producing type I 6'-acetyltransferase. Isepamicin’s antibacterial spectrum includes Enterobacteriaceae and staphylococci. Anaerobes, Neisseriaceae and streptococci are resistant. Isepamicin exhibits a strong concentration-dependent bactericidal effect, a long post-antibiotic effect (several hours) and induces adaptive resistance .
BSc5367 is a potent Nek1 inhibitor with an IC50 of 11.5 nM. NIMA-related protein kinase Nek1 is crucially involved in cell cycle regulation, DNA repair and microtubule regulation and dysfunctions of Nek1 play key roles in amyotrophic lateral sclerosis (ALS), polycystic kidney disease (PKD) and several types of radiotherapy resistant cancer .
Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
Anti-MRSA agent 3 (compound 18) has highly inhibitory activity against Methicillin-resistantStaphylococcus 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 .
BV02 is a potent 4-3-3 PPI (14-3-3 protein–protein interaction) inhibitor. BV02 shows cytotoxicity for hematopoietic cells expressing the IM (imatinib mesylate)-sensitive wild type Bcr-Abl and the IM-resistant T315I mutation. BV02 has the potential for the research of chronic myeloid leukemia .
Edatrexate (CGP 30694), as known as 10-Ethyl-10-deazaaminopterin, is Methotrexate (HY-14519) analog, exhibits antitumor activity against MTX-resistant tumors. Edatrexate is an antifolate antimetabolite, can be used for reasearch of non-small-cell lung cancer, breast cancer, non-Hodgkin's lymphoma, and cancer of the head and neck .
Carumonam (AMA-1080; Ro 17-2301) is a sulfonated monocyclic β-Lactam Antibiotic, targeting to penicillin-binding protein (PBP). Carumonam exerts highly activity against Enterobacteriaceae, Pseudomonas aeruginosa, and Haemophilus influenzae, while it weakly and even inactively inhibits Streptococcus pneumoniae and Staphylococcus aureus. Carumonam is resistant to beta-lactamase-mediated hydrolysis .
Oditrasertib (SAR443820) is an orally active and brain-penetrant receptor-interacting protein kinase 1 (RIPK1) inhibitor with an IC50 value lower than 100 nM. Oditrasertib could make nerve cells more resistant to the pathology and slow down the disease. Oditrasertib can be used for the research of neurodegenerative diseases involving inflammation or cell death .
Penicillinase (from calf stomach) is an enzyme that degrades penicillin by hydrolyzing the cyclic amide bonds in the lactam ring of penicillin, which can inactivate penicillin. Penicillinase (from calf stomach) can be isolated from penicillin resistant strains. Penicillinase (from calf stomach) has potential application as a marker for steroid hormone enzyme linked immunosorbent assay .
Xylene Fast Yellow 2G is a synthetic dye belonging to the class of azo dyes. It is commonly used in the textile industry to dye natural and synthetic fibers as well as in the paper and ink industries. Xylene Fast Yellow 2G produces a bright yellow color that is fade and wash resistant and can be applied to textiles by a variety of methods including dipping, padding and printing.
Lynronne-1 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including MDR strains (MIC: 8-32 μg/mL for methicillin-resistant MRSA strains). Lynronne-1 reduces the bacterial load in MRSA infected wound murine model. Lynronne-1 is also effective against P. aeruginosa infection .
DGKζ-IN-4 is a DGK-zeta inhibitor. DGKζ-IN-4 can be used as an active component of pharmaceutical compositions. DGKζ-IN-4 is used to treat cancers associated with immune cell activation or cancers resistant to anti-PD-1 antibody/anti-PD-11 antibody treatment .
Jingzhaotoxin-IX, a C-terminally amidated peptide composed of 35 amino acid residues, is a neurotoxin. Jingzhaotoxin-IX inhibits voltage-gated sodium channels (both tetrodotoxin-resistant and tetrodotoxin-sensitive isoforms) and Kv2.1 channel. Jingzhaotoxin-IX has no effect on delayed rectifier potassium channel Kv1.1, 1.2 and 1.3 .
AC Antibody affinity resin is AC commonly used packing. AC Antibody affinity resin has highly cross-linked agarose matrix with 85 μm of average particle size. AC Antibody affinity resin has alkali-resistant protein A derivative (E. coli) ligand. AC Antibody affinity resin can be used for antibody affinity chromatography .
Bedaquiline (Standard) is the analytical standard of Bedaquiline. This product is intended for research and analytical applications. Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
TPU-0037A is an antibiotic and a congener of lydicamycin. It inhibits the growth of Gram-positive bacteria, including methicillin-resistant S. aureus (MRSA), B. subtilis, and M. luteus (MICs=1.56-12.5 μg/mL), but not Gram-negative E. coli, P. mirabilis, P. vulgaris, or P. aeruginosa strains (MICs=>50 μg/mL).
Polymyxin B2 is a polypeptide antibiotic that has antibacterial activity, particularly against gram-negative bacteria. Polymyxin B2 kills the bacteria by binding to lipopolysaccharide molecules on the bacterial cell membrane, disrupting the integrity of the cell membrane and causing the cell contents to leak. Polymyxin B2 can be used in antibiotic development and treatment of drug-resistant strains .
Difethialone (LM-2219) is an anticoagulant rodenticide. Difethialone shows high rodenticide activity in warfarin-sensitive and resistant strains of rats and mice. Difethialone interferes with the circulation of vitamin K in the liver, preventing the synthesis of coagulation factors, resulting in the inability of the blood to coagulate properly, ultimately causing internal bleeding and death. Difethialone can be used in studies of ecological impacts .
IMTPPE is an inhibitor of the androgen receptor (AR) in C4-2 prostate cancer cells, inhibiting its transcriptional activity and protein levels. IMTPPE inhibited the proliferation of AR-positive prostate cancer cells but had no effect on AR-negative prostate cancer cells. IMTPPE also inhibited the growth of enzalutamide-resistant 22Rv1 xenograft tumors .
Nafithromycin (WCK 4873) is an orally available antibiotic that inhibits community-acquired pneumonia caused by Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, and Methicillin (HY-121544)-susceptible Staphylococcus aureus. The MIC90 of nafithromycin against macrolide-resistant and telithromycin (HY-A0062)-insensitive Streptococcus pneumoniae is 0.12 mg/liter .
LBM-415 (NVP-PDF 713) is a peptide deformylase (PDF) inhibitor that exhibits inhibitory activity 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 .
(R)-Omeprazole sodium is a gastric acid resistant compound with activity to inhibit gastric acid secretion. (R)-Omeprazole sodium is metabolized in vivo, and its metabolism is primarily affected by cytochrome P450 enzymes. The interaction between (R)-Omeprazole sodium and mannitol may affect its bioavailability in formulations. (R)-Omeprazole sodium exhibits reversible direct and metabolism-dependent inhibition of CYP2C19 .
CAMK1D-IN-1 (compound i) is a CAMK1D inhibitor that enhances CTL-induced death receptor signaling and apoptosis by impairing CAMK1D immune checkpoint function. CAMK1D-IN-1 can be used to study tumor cells that are resistant to cytotoxic T lymphocytes (CTLs) .
Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM) . Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis .
ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .
SPSB2-iNOS inhibitory cyclic peptide-2 (Compound CP2) is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 21 nM. SPSB2-iNOS inhibitory cyclic peptide-2 is reduction-resistant and oxidatively stable .
Meropenem trihydrate (SM 7338 trihydrate) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem trihydrate has activity against susceptible and resistantN. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research .
Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research .
Capreomycin sulfate is a macrocyclic peptide antibiotic that inhibits phenylalanine synthesis in mycobacterial ribosomal translation. Capreomycin sulfate has anti-amyloidogenic and pro-fibrinolytic activities, reducing amyloid-induced cytotoxicity by inhibiting the occurrence of amyloid fibrillation. Capreomycin sulfate can be used in the study of multidrug-resistant tuberculosis, type 2 diabetes, Alzheimer's disease and Parkinson's disease .
Potassium clavulanate cellulose (Potassium clavulanate:cellulose (1:1)) is a mixture of potassium clavulanate and cellulose, is a bacterial β-lactamase inhibitor. Clavulanate potassium is a form of Clavulanic acid. Clavulanate potassium fights bacteria that resistant to penicillins and other antibiotics. Potassium clavulanate with the combination of amoxicillin can be used for the research of different infections caused by bacteria, such as sinusitis, pneumonia, ear infections, bronchitis, urinary tract infections, and infections of the skin .
Terlipressin is a vasopressin analogue with potent vasoactive properties. Terlipressin is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin exerts anti-inflammatory and anti-oxidative effects. Terlipressin has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
DS86760016 is a potent leucyl-tRNA synthetase (LeuRS) inhibitor with activity against multidrug-resistant (MDR) Gram-negative bacteria, such as Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. DS86760016 inhibits LeuRS enzymes from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, with IC50s of 0.38, 0.62, and 0.16 μM, respectively .
Zabofloxacin (DW-224a Free base) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP) .
Larotaxel (XRP9881) is a taxane analogue with preclinical activity against taxane-resistant breast cancer. Larotaxel (XRP9881) exerts its cytotoxic effect by promoting tubulin assembly and stabilizing microtubules, ultimately leading to cell death by apoptosis. It presents the ability to cross the blood brain barrier and has a much lower affinity for P-glycoprotein 1 than Docetaxel .
Amikacin hydrate (BAY 41-6551 hydrate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin hydrate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin hydrate is very active against most Gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin hydrate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria .
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity . 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice .
PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistantS. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 μM, respectively .
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistantGram-negative bacterial infections treatment .
Terlipressin diacetate is a vasopressin analogue with potent vasoactive properties. Terlipressin diacetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin diacetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin diacetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity .
SPR206 acetate is a polymyxin analog with antibiotic activity against Gram-negative pathogens, including multidrug-resistant (MDR) variants. SPR206 acetate has an anti-bacterial infection effect by interacting with the bacterium’s outer membrane. The MIC values of SPR206 acetate against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301 are both 0.125 mg/L .
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .
Nitrocefin is a highly activated, chromogenic cephalosporin derivative. Nitrocefin is a chromogenic β-lactamase substrate. Nitrocefin undergoes a distinctive color change from yellow to red as the amide bond in the β-lactam ring is hydrolyzed by β-lactamase. Nitrocefin is used in competitive inhibition studies in developmental work on β-lactamase-resistant antibiotics .
Bedaquiline impurity 2-d6 is deuterium labeled Bedaquiline. Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit[1]. Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis[2].
HBV-IN-23 (Compound 5k) is an inhibitor of HBV DNA replication with an IC50 of 0.58 μM. HBV-IN-23 inhibits HBV DNA replication in both agent sensitive and resistant HBV strains. HBV-IN-23 shows anti-hepatocellular carcinoma cell (HCC) activities. HBV-IN-23 induces HepG2 cells apoptosis .
Rucaparib (AG014699) acetate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib acetate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib acetate has the potential for castration-resistant prostate cancer (CRPC) research .
Rucaparib (AG014699) hydrochloride is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib hydrochloride is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib hydrochloride has the potential for castration-resistant prostate cancer (CRPC) research .
ANT3310 sodium is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC50 values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). ANT3310 sodium potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). ANT3310 sodium can be used in the research of bacterial infection .
TP0480066 is a selective topoisomerase II inhibitor 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 inhibitory activity to N. gonorrhoeae, can be used in study of gonorrhea .
AKR1C3-IN-9 is a selective inhibitor of Aldo-keto Reductase 1C3 (AKR1C3) with an IC50 value of 8.92 nM. AKR1C3-IN-9 significantly reverses the Doxorubicin (HY-15142A) (DOX) resistance in a resistant breast cancer cell line .
Mtb-IN-2 (compound 10c) is an antimicrobial agent against Mycobacterium tuberculosis (Mtb), without cytotoxicity. Mtb-IN-2 significantly decreases colony-forming units (CFU) in spleen of murine tuberculosis models, and distinguishes both drug-sensitive and drug-resistant Mtb H37Rv strains. Mtb-IN-2 affects methionine metabolism but not folate pathway directly.
(Rac)-Bedaquiline-d6 is the deuterium labeled Bedaquiline (HY-14881) . Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
DYB-03 is an oral active HIF-1α/EZH2 inhibitor. DYB-03 inhibits migration, invasion, and angiogenesis of lung cancer cells and HUVECs in vitro and in vivo. DYB-03 induces apoptosis in 2-ME2 - and GSK126 -resistant of A549 and H460 cells .
6β-Prostaglandin I1 (6β-PGI1) is an analog of prostaglandin I2 (PGI2) that is resistant to hydrolysis in aqueous solutions. 6β-Prostaglandin I1 can reduce gastric acid secretion with an ID50 (dose causing 50% inhibition) of approximately 3.0 μg/kg/min (intravenous injection) .
PNU-100766-d8 is deuterated labeled Linezolid (HY-10394). Linezolid (PNU-100766) is the first member of the class of oxazolidinone synthetic antibiotic. Linezolid acts by inhibiting the initiation of bacterial protein synthesis. Linezolid is used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics .
Telavancin hydrochloride is the hydrochloride form of Telavancin (HY-112959). Telavancin hydrochloride is a semisynthetic derivative of vancomycin, and exhibits antibacterial efficacy through inhibition of cell wall synthesis and disruption of cell membrane barrier function. Telavancin hydrochloride is efficient against antibiotic resistantS. aureus strains MRSA, VISA, and hVISA. Telavancin hydrochloride attenuates gram positive bacteria induced complicated skin and skin structure infections (cSSSI) .
Ceftazidime (pentahydrate) (Standard) is the analytical standard of Ceftazidime (pentahydrate). This product is intended for research and analytical applications. Ceftazidime (GR20263) pentahydrate , an antibiotic, has a broad spectrum activity against Gram-positive and Gram-negative aerobic bacteria. Ceftazidime pentahydrate is also active against Enterobacteriaceae (including β-lactamase-positive strains) and is resistant to hydrolysis by most β-lactamases .
Antibacterial agent 227 (Compd 29) is a SerRS (Seryl-tRNA synthetase) inhibitor. Antibacterial agent 227 has a significant inhibitory effect on the growth of planktonic and biofilm culture of Staphylococcus aureus 25923 with MIC (minimum inhibitory concentration) value of 32 µg/ml. Antibacterial agent 227 can be proposed as effective antiseptic toward multidrug-resistant biofilm-forming S. aureus isolates .
Benzobicyclon (Standard) is the analytical standard of Benzobicyclon. This product is intended for research and analytical applications. Benzobicyclon is a 4-HPPD inhibitor and herbicide that reacts with water to form a hydrolysate of the active herbicide benzobicycline, causing bleaching and death of weeds. Benzobicyclon is effective against grass, sedge and broadleaf weeds. Benzobicyclon effectively targets sulfonylurea herbicide-resistant biotypes as well as wild-type weeds .
A-39355 is a compound that can overcome multidrug resistance and has the activity of reversing multidrug resistance. A-39355 can enhance the cytotoxicity of antitumor compounds in multidrug-resistant cells, increase the accumulation of compounds in cells, inhibit the efflux of compounds, and compared with calcium antagonists, it has no serious hypotensive effect. Its activity may be unrelated to the ability to block calcium transport.
A-30312 is a compound that can overcome multidrug resistance and has the activity of reversing multidrug resistance. A-30312 can enhance the cytotoxicity of antitumor compounds in multidrug-resistant cells, increase the accumulation of compounds in cells, inhibit the efflux of compounds, and compared with calcium antagonists, it has no serious hypotensive effect. Its activity may be unrelated to the ability to block calcium transport.
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 .
Ianthelliformisamine C ditrifluoroacetate is an antibiotic enhancer with activity against resistant Gram-negative bacteria. Ianthelliformisamine C ditrifluoroacetate has been shown to improve the efficacy of doxycycline against Pseudomonas aeruginosa. Ianthelliformisamine C ditrifluoroacetate was prepared using peptide coupling, resulting in high chemical yields of 27 to 91%. Ianthelliformisamine C ditrifluoroacetate exhibits its mechanism of action by inducing ATP efflux and causing membrane depolarization in bacterial cells.
Polymyxin B2 Sulfate is a polypeptide antibiotic that has antibacterial activity, particularly against gram-negative bacteria. Polymyxin B2 Sulfate kills the bacteria by binding to lipopolysaccharide molecules on the bacterial cell membrane, disrupting the integrity of the cell membrane and causing the cell contents to leak. Polymyxin B2 Sulfate can be used in antibiotic development and treatment of drug-resistant strains .
Artocarpesin is a flavonoid compound. Artocarpesin has inhibitory effects on methicillin-resistantStaphylococcus aureus (MRSA). Artocarpesin inhibits the production of NO, PGE2 and ROS by inhibiting COX-2 and iNOS expression, and plays an anti-inflammatory role. In addition, Artocarpesin inhibits platelet aggregation by inhibiting cyclic nucleotides and MAPKs, which can be used in the study of cardiovascular diseases .
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-resistantStaphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .
Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistantleishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities .
Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistantleishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities .
Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research .
SPR741 acetate (NAB741 acetate) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 acetate increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 acetate inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 acetate .
SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 .
Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent .
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM . Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM .
Antibacterial agent 102 (compound 32) possesses potent in vitro and in vivo antibacterial activity, with MICs < 0.5 μg/mL in Staphylococcus aureus (S. aureus). Antibacterial agent 102 also moderately inhibits CYP3A4 with an IC50 value of 6.148 μM. Antibacterial agent 102 can reduce Methicillin-resistantStaphylococcus aureus (MRSA) load in thigh infected mice .
Rucaparib (AG014699) camsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib camsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib camsylate has the potential for castration-resistant prostate cancer (CRPC) research .
Rucaparib (AG014699) tartrate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib tartrate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib tartrate has the potential for castration-resistant prostate cancer (CRPC) research .
Wychimicin A is a spirotetronate polyketide, can be isolated from the rare actinomycete Actinocrispum wychmicini strain MI503-AF4. Wychimicin A shows strong antibacterial activity against methicillin-resistantStaphylococcus. aureus (IC50=0.125-0.5 μg/mL) and Enterococcus. faecalis/faecium (IC50=0.125-0.25 μg/mL) .
Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer .
(E/Z)-4,4'-Dicyanostilbene is the isomer of 4,4'-Dicyanostilbene (HY-W112166A), and can be used as an experimental control. 4,4'-Dicyanostilbene (compound 43) is a potent antimalarial agent against the Dd2 strain, with an EC50 of 27 nM. 4,4'-Dicyanostilbene exhibits in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA) .
Jingzhaotoxin-V, a 29-residue polypeptide, is derived from the venom of the spider Chilobrachys jingzhao. Jingzhaotoxin-V inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 nM and 30.2 nM, respectively. Jingzhaotoxin-V also inhibits Kv4.2 potassium currents expressed in Xenpus Laevis oocytes (IC50 of 604.2 nM) .
ATP Synthesis-IN-1 (Compound 4), quinoline derivative, is a potent inhibitor of PA ATP synthesis activity. ATP Synthesis-IN-1 has PA ATP synthesis inhibition with IC50 value of 11.1μg/mL. ATP Synthesis-IN-1 also has antibacterial activity. ATP Synthesis-IN-1 can be used for the research of drug-resistant PA infection .
YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7 WT and Cdk7 as, although Cdk7 as is relatively resistant to this compound as well .
AC Antibody purification resin 2 is based on spherical, highly cross-linked agarose beads with a narrow size distribution and high mechanical stability. Used for the separation and purification of complex antibodies such as monoclonal antibody, double antibody, multi-antibody and Fc fusion protein .
Substrate: highly crosslinked agarose microspheres; Particle size: 65μm; Ligand: alkali-resistant recombinant Protein A; ADC purified resin.
LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections .
Tasquinimod-d3 (ABR-215050-d3) is the deuterium labeled Tasquinimod (HY-10528). Tasquinimod is an oral antiangiogenic agent, which plays an important role in castration-resistant prostate cancer. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor .
Nitrocefin (Standard) is the analytical standard of Nitrocefin. This product is intended for research and analytical applications. Nitrocefin is a chromogenic β-lactamase substrate that undergoes a distinctive color change from yellow to red as the amide bond in the β-lactam ring is hydrolyzed by β-lactamase. Nitrocefin is used in competitive inhibition studies in developmental work on β-lactamase-resistant antibiotics .
Loxapine (succinate) (Standard) is the analytical standard of Loxapine (succinate). This product is intended for research and analytical applications. Loxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistantSalmonella enterica serovar Typhimurium in macrophages .
TPU-0037C is a metabolite of the marine actinomycete S. platensis that is structurally similar to Lydicamycin (HY-125414). It is active against Gram-positive bacteria (MICs=0.39-3.13 μg/mL), including methicillin-resistant S. aureus strains (MIC=3.13 μg/mL), but is ineffective against Gram-negative bacteria (MICs=>50 μg/mL).
BMS-737 (compound 33) is a non-steroidal, reversible small molecule inhibitor. BMS-737 exhibits 11-fold selectivity for CYP17 lyase over CYP17 hydroxylase. BMS-737 is designed to inhibit castration-resistant prostate cancer (CRPC) and significantly reduces testosterone levels without significant effects on orrodermal hormone and glucocorticoid levels .
JWJ-01-306 is a molecular glue that targets the C2H2 zinc finger transcription factor ZBTB11. JWJ-01-306 degrades ZBTB11, reduces the oxidative phosphorylation (OXPHOS) and tricarboxylic acid (TCA) cycle, and inhibits the proliferation of KAS-resistant PDAC cells. JWJ-01-306 exhibits good pharmacokinetic characteristics in mouse model .
Novobiocin (Standard) is the analytical standard of Novobiocin. This product is intended for research and analytical applications. Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity [4] .
Novobiocin (sodium) (Standard) is the analytical standard of Novobiocin (sodium). This product is intended for research and analytical applications. Novobiocin (Albamycin) sodium is a potent and orally active antibiotic. Novobiocin sodium also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin sodium has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin sodium shows anti-orthopoxvirus activity .
Pheanthine (Compound 2) is an antiplasmodial agent, that inhibits chloroquine-resistantPlasmodium falciparum K-1 (IC50 is 0.8 μM) and chloroquine-sensitive P. falciparum strain NF54 A19A (IC50 of 0.03 μM). Pheanthine exhibits low cytotoxicity in human lung fibrosblast (MRC-5, IC50 is 11.2 μM) and macrophages (PMM, IC50 is 8 μM) .
A-803467 is a potent and selective tetrodotoxin-resistantNav1.8 sodium channel blocker (IC50=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter .
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively .
Riviciclib shows antitumor activity on cisplatin-resistant cells .
c[Arg-Arg-Arg-Arg-Nal-Nal-Nal] (Compound 9C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 25 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively .
Antimalarial agent 11 (compound 1), a spirocyclic chromane, is a potent antimalarial agent. Antimalarial agent 11 exhibits excellent potency with an EC50 of 350 nM against the Chloroquine-resistant Dd2 strain. Antimalarial agent 11 has EC50s of 1.48 µM and 1.81 µM against D6 and ARC08-022 strains, respectively .
HIV-1 inhibitor-13 (compound 16c) is a orally active and potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI), with IC50 of 0.14 μM (HIV-1 RT). HIV-1 inhibitor-13 shows activity against a panel of HIV-1resistant strains, with EC50 values of 2.85-18.0 nM .
Antitubercular agent-28 (compound 2) is a potent antitubercular agent with an IC50 value of 1.5 µM, an MIC value of 4.5 µM, an IC90 value of 2.5 µM. Antitubercular agent-28 shows antimycobacterial activity for resistant isolates of Mycobacterium tuberculosis H37Rv. Antitubercular agent-28 shows effective intracellular antimycobacterial activity and low cytotoxicity .
Antitubercular agent-27 (compound 1) is a potent antitubercular agent with an IC50 value of 3.2 µM, an MIC value of 7.8 µM, an IC90 value of 7.0 µM. Antitubercular agent-27 shows antimycobacterial activity for resistant isolates of Mycobacterium tuberculosis H37Rv. Antitubercular agent-27 shows effective intracellular antimycobacterial activity and low cytotoxicity .
Wychimicin C is a spirotetronate polyketide, can be isolated from the rare actinomycete Actinocrispum wychmicini strain MI503-AF4. Wychimicin C shows strong antibacterial activity against methicillin-resistantStaphylococcus. aureus (IC50=0.125-0.5 μg/mL) and Enterococcus. faecalis/faecium (IC50=0.125-0.25 μg/mL) .
Akt3 degrader 1 (compound 12l) is a selective Akt3 degrader that overcomes Osimertinib (HY-15772)-induced resistance in H1975OR NSCLC cells. Akt3 degrader 1 also has anti-proliferative activity and significantly inhibits tumour growth in mice. Akt3 degrader 1 can be used in the study of drug-resistant non-small cell lung cancer .
DVR-01 is a HBV inhibitor with EC50 values of 1.7 and 1.6 μM in AML12HBV10 and HepDES19 cells, respectively. DVR-01 shows antiviral activity against drug-resistant HBV mutants with EC50s of 2.403-3.273 μM. DVR-01 can be used for the research of HBV infection and related diseases .
Benzquinamide (P2647) is an antiemetic which can bind to the α2A, α2B, and α2Cadrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells .
DprE1-IN-5 (Compound 10) is a DprE1 inhibitor. DprE1-IN-5 has anti-TB activity against Mtb H37Rv strain (MIC: 4 μM). DprE1-IN-5 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-5 has high microsomal stability .
YXG-158 (Compound 23-h) is an orally active AR degrader and CYP17A1 inhibitor. YXG-158 has AR degradation activity with DC50 value of 1.28 μM. YXG-158 can inhibit CYP17A1 with IC50 value of 100 nM. XG-158 can be used for the research of enzalutamide-resistant prostate cancer .
PK-10 is a synergistic antibacterial agent of Fluconazole (HY-B0101) and has strong antifungal activity against a variety of Fluconazole-resistant Candida albicans strains. PK-10 combined with Fluconazole can inhibit hyphae formation and induce the accumulation of reactive oxygen species. It further causes damage to mitochondrial membrane potential, reduces intracellular ATP content, and leads to mitochondrial dysfunction .
HIV-1 protease-IN-13 (compound 18d) is a potent HIV-1 protease inhibitor with an IC50 value of 0.54 nM. HIV-1 protease-IN-13 also shows potent activity against HIV-1DRVRS (DRV-resistant mutation) and HIV-1NL4_3 variant (wild type) .
KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice .
Tubulysin B is a highly cytotoxic peptide and potent microtubule destabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties .Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis .
SGR-1505 is an orally active MALT1 allosteric inhibitor. SGR-1505 inhibits MALT1 enzymatic activity and shows anti-proliferative activity in BTK inhibitor (BTKi)-sensitive and BTKi-resistant activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines. SGR-1505 can be used for research of B-cell lymphomas .
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 .
Vedroprevir (GS-9451) is an inhibitor for HCV NS3/4A protease with an IC50 of 3.2 nM. Vedroprevir is also an inhibitor for breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM. Vedroprevir inhibits P-gp, MRP1 and MRP2 with IC50 of 34, 14.9 and 12 μM, respectively. Vedroprevir exhibits good pharmacokinetic characteristics in rats and dogs .
Chevalone B was isolated from the ethyl acetate extract of the marine sponge-associated fungus Aspergillus similanensis. The structure of Chevalone B was confirmed by 1D and 2D NMR spectroscopy. Chevalone B showed antimicrobial activity against Gram-positive and Gram-negative bacteria, Candida albicans, and multidrug-resistant strains from the environment. Studies on Chevalone B have shown its potential value in antimicrobial applications.
Pyraclonil (Standard) is the analytical standard of Pyraclonil. This product is intended for research and analytical applications. Pyraclonil is a proporphyrinogen oxidase (PPO) inhibitor. Pyraclonil is a herbicide agent and is highly effective in controlling the susceptible (S) and multiple-herbicide-resistant (MHR) E. indica populations . Pyraclonil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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 inhibitory activity against both wild-type and mutated target enzymes.
Amikacin disulfate (BAY 41-6551 dissulfate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin disulfate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin disulfate is very active against most Gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin disulfate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria .
Meropenem-d6 is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL)[1][2].
The Tubulysin family of secondary metabolites was originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. These compounds are potent microtubule destabilizers and anti-microtubule toxins (anti-microtubule toxins), with effective IC50 concentrations against multidrug-resistant cancer cell lines. In the picomole range. Tubulysins are ideal candidates for incorporation into small active molecule conjugate (SMDC) delivery systems and are commonly used in ADC synthesis as ADC cytotoxins (ADC Cytotoxin) .
Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively .
Riviciclib hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells .
Amikacin sulfate (BAY 41-6551 sulfate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin sulfate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin sulfate is very active against most Gram-negative bacteria including gentamicin- and tobramycin-resistant strains. Amikacin sulfate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria .
Sulfadoxine-d3 is a deuterium labeled Sulfadoxine (HY-B0439). Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine (HY-18062), for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections[1][2][3][4].
EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 TFA increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 TFA inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 TFA .
Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC) .
Faropenem is a potent and orally active beta-lactam antibiotic. Faropenem demonstrates broad-spectrum in vitro antimicrobial activity against many gram-positive and -negative aerobes and anaerobes. Faropenem is resistant to hydrolysis by nearly all beta-lactamases, including extended-spectrum beta-lactamases and AmpC beta-lactamases. Faropenem is developed as an oral proagent, faropenem medoxomil, for the research of respiratory tract infections .
XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma .
MsbA-IN-6 is a potent inhibitor of MsbA. MsbA-IN-6 is an antibiotic. Gram-negative ATP-binding cassette (ABC) transporter MsbA, an essential inner membrane protein, transports lipopolysaccharide from the inner leaflet to the periplasmic face of the inner membrane. MsbA-IN-6 kills Escherichia coli through inhibition of its ATPase and transport activity, with no loss of activity against clinical multidrug-resistant strains .
c[Arg-Arg-Arg-Arg-Dip-Dip-Dip] (Compound 8C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 12.5 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively .
CFM-4 is a potent small molecular antagonist of CARP-1/APC-2 binding. CFM-4 prevents CARP-1 binding with APC-2, causes G2M cell cycle arrest, and induces apoptosis with an IC50 range of 10-15 μM. CFM-4 also suppresses growth of drug-resistant human breast cancer cells .
Pentamidine (MP-601205) dimesylate is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dimesylate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dimesylate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dimesylate has the potential for Gambian trypanosomiasis, antimony-resistantleishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities .
Chitin synthase inhibitor 12 is a chitin synthase inhibitor. Chitin synthase inhibitor 12 shows excellent inhibitory activity 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 synthase inhibitor. Chitin synthase inhibitor 10 shows excellent chitin synthase inhibitory activity 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) .
PSI-353661 (GS-558093) is a purine nucleotide NS5B polymerase inhibitor against HCV infection. PSI-353661 shows EC90s of 8 nM and 11 nM for wild type and S282T resistant replicons of HCV. PSI-353661 can produce high concentrations of the active triphosphate in primary human hepatocytes .
MC-1-F2 is a FOXC2 inhibitor that reduces epithelial-mesenchymal transition (EMT) markers in breast cancer cells, suppresses cancer stem cell (CSC) properties and reduces invasiveness in castration-resistant prostate cancer (CRPC) cells. There is a synergistic effect between MC-1-F2 and Docetaxel, which has the potential to be used in combination to study CRPC .
DprE1-IN-7 (Compound 64) is a DprE1 inhibitor. DprE1-IN-7 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-7 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-7 has high microsomal stability and medium clearance .
DprE1-IN-6 (Compound 56) is a DprE1 inhibitor. DprE1-IN-6 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-6 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-6 has high microsomal stability and medium clearance .
AC3-I, myristoylated is a biological active peptide. (This is a myristoylated form of Autocamtide-3-Derived Inhibitory Peptide (AC3-I), a highly specific inhibitor of Calmodulin-Dependent Protein Kinase ll (CaMKII) that is resistant to proteolysis. AC3-I is derived from Autocamtide-3, a substrate for CaMKII, with the Thr-9 phosphorylation site substituted with Ala.)
KSK-104 has potent antibacterial activity against Mycobacterium tuberculosis (MIC=0.78 μM). The role of KSK-104 is mainly involved in the synthesis and recovery pathways of pyridoxal 5'-phosphate (PLP), PLP-dependent enzymes and oxidative stress networks. KSK-104, as a candidate molecule for novel anti-tuberculosis drugs, can be used to develop research against drug-resistant mycobacterium tuberculosis .
Ficellomycin is a nitrogen-containing bicyclic antibiotic with strong activity against Gram-positive bacteria, including multidrug-resistant strains of Staphylococcus aureus. Ficellomycin works by inducing the formation of defective 34S DNA fragments, which interfere with the semi-conservative DNA replication process. These fragments lack the ability to integrate into larger DNA segments and eventually form a complete bacterial chromosome. Ficellomycin can be used in research for various bacterial diseases .
BQ7876 is a probe targeting prostate-specific membrane antigen (PSMA) that contains a DOTA chelator. BQ7876, after being radiolabeled with radionuclide (177Lu), functions in both radionuclide imaging and tumor cell destruction by specifically binding to PSMA. BQ7876 shows potential for research in the field of metastatic castration-resistant prostate cancer (mCRPC) . BQ7876 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
PTP1B-IN-25 (Compound 19) is a PTP1B inhibitor with remarkable antiviral, antibacterial, and antidiabetic activities. PTP1B-IN-25 has IC50 values of 0.37 μM, 8.6 μM, 3.7 μM, and 29 μM against PTP1B, HIV, α-Glucosidase, and methicillin-resistantStaphylococcus aureus (MRSA) respectively .
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 resistantStaphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well .
Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistantleishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities .
Docusate Sodium (Dioctyl sulfosuccinate sodium salt) is one of the main components in stool softeners. Docusate Sodium is a sulfated surfactant and may inactivate viral pathogens by disrupting viral envelopes and/or denaturing/disassociating proteins. Docusate Sodium is effective in vitro against wild type and drug-resistant strains of HSV type 1 and 2. Docusate Sodium is an obesogen. Docusate Sodium with developmental exposure leads to increased adult adiposity, inflammation, metabolic disorder and dyslipidemia in offspring fed a standard diet in mice .
Virginiamycin S1 is a cyclic hexadepsipeptide antibiotic, inhibits bacterial protein synthesis at the level of aminoacyl-tRNA binding and peptide bond formation. Virginiamycin S1 belongs to the type B compounds in the streptogramin family and is produced by Streptomyces virginiae, shows a strong bactericidal activity against a wide range of Gram-positive bacteria. Virginiamycin S1 together with virginiamycin M1 is more effective in treat multidrug-resistant bacterial infections [1][2].
Vinaxanthone (SM-345431) is a potent and selective semaphorin3A, phospholipase C (PLC) and FabI inhibitor, with IC50s of 0.1-0.2 μM and 0.9 mM for semaphorin3A and FabI. Vinaxanthone inhibits the substrate (t-o-NAC thioester) and the cofactor (NADPH) with Kis of 3.1 μM and 1.0 μM, respectively. Vinaxanthone can be used to handle infections caused by multidrug-resistant pathogens .
UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli.
WX-081, an anti-tuberculosis agent, displays excellent anti-mycobacterial activity against M. tuberculosis H37Rv and low cytotoxicity. WX-081 exhibits potent activity with MIC50s of 0.083 and 0.11 μg/mL for agent susceptible tuberculosis (DS-TB) and multidrug resistant tuberculosis (MDR-TB) strains. WX-081 also inhibits hERG channel with the IC50 of 1.89 μM.
P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells .
Zifanocycline (KBP-7072) TFA is an orally active, semi-synthetic aminomethylcycline antibiotic that inhibits the normal function of bacterial ribosomes. Zifanocycline TFA has broad spectrum in vitro antimicrobial activity against Gram-positive and Gram-negative bacteria, including many multidrug-resistant pathogens. Zifanocycline TFA is indicated for the study of acute bacterial skin and skin structure infections, community-acquired bacterial pneumonia, and complicated intra-abdominal infections .
Tipranavir-d7 is deuterated labeled Tipranavir (HY-15148). Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
Antibiofilm agent-7 (Compound 9) exhibits potent antibiofilm activity with IC50 of 60, 133.32, and 19.67 µg/mL against S. aureus, E. coli, and methicillin-resistant S. aureus (MRSA), respectively. Antibiofilm agent-7 has antibacterial activity for S. aureus, E. coli, C. albicans, and MRSA, with MIC values of 4.88, 78.13, 9.77 and 39.06 µg/mL, respectively .
Tipranavir (Standard) is the analytical standard of Tipranavir. This product is intended for research and analytical applications. Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
Phomoxanthone A is a xanthone dimer, which can be isolated from Phomopsis. Phomoxanthone A exhibits antimalarial and antitubercular activities against Plasmodium falciparum (K1, multidrug-resistant strain, IC50 is 0.11 µg/mL) and Mycobacterium tuberculosis (H37Ra strain, MIC is 0.50 µg/mL). Phomoxanthone A exhibits cytotoxicity in cells KB, BC-1 and Vero, IC50 is 0.99, 0.51 and 1.4 µg/mL, respectively .
Saquayamycin D is an antibiotic, which can be isolated from Streptomyces nodosus culture broth. Saquayamycin D exhibits antibacterial activity against various gram-positive bacteria with MIC of 12.5-50 μg/mL. Saquayamycin D inhibits the proliferation of Doxorubicin (HY-15142)-sensitive P388/S and Doxorubicin-resistant P388/ADR with IC50 of 0.15 and 0.15 μg/mL .
PARP1/2-IN-3 (Compound 29) is an orally active inhibitor for PARP 1 and PARP 2 with IC50 of 0.2235 nM and <0.001 nM. PARP1/2-IN-3 inhibits the proliferation of Capan-1 wildtype, AZD2281 or BMN673 resistant cells with IC50 of 1.82-9.98 nM. PARP1/2-IN-3 exhibits antitumor efficacy in mice .
8-Deazahomofolic acid is an inhibitor of thymidylate synthase (TS) and other folate-related enzymes. 8-Deazahomofolic acid shows inhibitory activity 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 .
Bcl-2-IN-22 (compound 1) is a gold(I) NHC complex with anticancer activity. Bcl-2-IN-22 induces apoptosis via the mitochondrial pathway with an IC50 value of 0.014 μM. In addition, Bcl-2-IN-22 targets BCL-2 family members and exhibits pro-apoptosis and resensitization properties in multidrug-resistant leukemia cells that overexpress BCL?2 .
Difethialone (Standard) is the analytical standard of Difethialone. This product is intended for research and analytical applications. Difethialone (LM-2219) is an anticoagulant rodenticide. Difethialone shows high rodenticide activity in warfarin-sensitive and resistant strains of rats and mice. Difethialone interferes with the circulation of vitamin K in the liver, preventing the synthesis of coagulation factors, resulting in the inability of the blood to coagulate properly, ultimately causing internal bleeding and death. Difethialone can be used in studies of ecological impacts .
Meropenem (Standard) is the analytical standard of Meropenem. This product is intended for research and analytical applications. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Permanent Orange (Standard) is the analytical standard of Permanent Orange. This product is intended for research and analytical applications. Permanent Orange is a synthetic pigment commonly used in the manufacture of paints and coatings. It belongs to the class of organic pigments and consists of carbon and other elements. Permanent Orange produces a bright orange color that is fade and weather resistant, making it ideal for outdoor applications. It can be mixed with other pigments to produce a range of colors and is compatible with a wide range of binders and solvents.
BC-7013 is a novel semi-synthetic pleuromutilin derivative. BC-7013 has excellent activity against Gram-positive pathogenic bacteria. BC-7013 exhibits potent antibacterial properties against both Staphylococcus, Streptococcus and penicillin-resistantStreptococcus pneumoniae. BC-7013 has activity against Gram-positive pathogenic bacteria, BC-7013 is useful in the research of acute bacterial skin and skin structure infection (ABSSSI) .
Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively . Grazoprevir inhibits SARS-CoV-2 3CL pro activity .
Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively . Grazoprevir potassium salt inhibits SARS-CoV-2 3CL pro activity .
Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively . Grazoprevir sodium salt inhibits SARS-CoV-2 3CL pro activity .
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 resistantStaphylococcus aureus. Eltrombopag Olamine can induce apoptosis in hepatocellular carcinomab (HCC) as well .
Pentamidine-d4 (dihydrochloride) is the deuterium labeled Pentamidine dihydrochloride. Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].
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 inhibitory activity against HBV replication .
Tubulysin D is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin D can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin D displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin D inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin E is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin E can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin E displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin E inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin C is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin C can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin C displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin C inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin F is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin F can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin F displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin F inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin G is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin G can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin G displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin G inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin H is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin H can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin H displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin H inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin I is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin I can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin I displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin I inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin M is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin M can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin M displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin M inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 . (Z)-Ligustilide is orally active, it inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .
Cephradine (Cefradine) monohydrate is a broad-spectrum and orally active cephalosporin. Cephradine monohydrate is active against both grampositive and gram-negative pathogens and effective in eradicating most penicillinase-producing organisms known to be resistant to penicillin G, penicillin V, and ampicillin. Cephradine monohydrate has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine monohydrate blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
Taletrectinib (DS-6051b) is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants .
PSMα3 is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 penetrates and modulates human monocyte-derived DCs by altering the TLR2- or TLR4-induced maturation, inhibiting pro- and anti-inflammatory cytokine production and reducing antigen uptake. PSMα3 is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA) .
Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively . Grazoprevir hydrate inhibits SARS-CoV-2 3CL pro activity .
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 .
Zifanocycline (KBP-7072) is a semisynthetic third-generation aminomethylcycline antibiotic that inhibits the normal function of the bacterial ribosome. Zifanocycline exhibits a broad spectrum of in vitro antibacterial activity against Gram-positive and Gram-negative bacteria, including many multidrug-resistant pathogens. Zifanocycline is available in both oral and injectable formulations. Zifanocycline can be used for the research of acute bacterial skin and skin structure infections, community-acquired bacterial pneumonia, and complicated intra-abdominal infections .
Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory 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 .
Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC50 values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkA G595R, TrkA G667C, TrkA G667S, TrkA F589L and TrkC G623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis .
Antituberculosis agent-2 (Compound 8d) is an antituberculosis agent against agent-sensitive and multidrug-resistant tuberculosis. Antituberculosis agent-2 shows anti-tuberculosis activity with MIC values of 0.454, 1.757 and 1.644 μg/mL against M. tuberculosis H37Rv, 13946 and 14862, respectively. Antituberculosis agent-2 displays favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability .
Antifungal agent 30 (compound A18) is a potent antifungal agent. Antifungal agent 30 shows excellent antifungal activity against Candida albicans (CPCC400616) and Aspergillus fumigatus, with MIC of 0.03 and 0.5 μg/mL, respectively. Antifungal agent 30 also shows excellent antifungal activity against fluconazole-resistant strains. The potent antifungal activity of Antifungal agent 30 mainly causes by hydrogen and coordination bond interaction with the CYP51 .
C16-K-cBB1 is a potent and selective antimicrobial agent for MRSA (Methicillin resistantStaphylococcus aureus), with a MIC of 1 µg/mL. C16-K-cBB1 has very good selectivity, as it has weak hemolytic activity. C16-K-cBB1 is able to kill MRSA cells in a matter of 120 min at a concentration of 12.5 μg/mL .
Antibacterial agent 144 (compound 8e) is an antibacterial agent，with better effect against multi-resistantStaphylococcus aureus than Chloromycin and Amoxicillin (HY-B0467A). Antibacterial agent 144 destroys the cytoplasmic membrane of bacteria，and inhibits the biofilms formation. Antibacterial agent 144 binds to HSA (Kd=13.2 μM)，and exerts bactericidal efficacy. Antibacterial agent 144 also binds with DNA to for supramolecular complex to obstruct DNA replications .
HIV-1 inhibitor-57 (Compound 12g) is a HIV inhibitor. HIV-1 inhibitor-57 is active against wild-type and five prevalent NNRTI-resistant HIV-1 strains with EC50 values ranging from 0.024 to 0.0010 μM. HIV-1 inhibitor-57 forms additional interactions with residues around the binding site in HIV-1 RT .
Cysteine protease inhibitor-3 (Compound 15) is a Cysteine protease inhibitor. Cysteine protease inhibitor-3 inhibits Pf3D7, PfW2, PfFP2 and PfFP3 with IC50s of 0.74 μM, 1.05 μM, 3.5 μM, and 4.9 μM, respectively. Cysteine protease inhibitor-3 has anti-plasmodial efficacy against both drug-sensitive and drug-resistant parasites .
Antileishmanial agent-21 (compound 4e) is an antileishmanial agent that targets the Leishmania pteridine reductase 1 (Lm-PTR1). Antileishmanial agent-21 has an anti-folate mechanism, and folic acid and leucovorin can reverse the anti-leishmanial activity of Antileishmanial agent-21. Antileishmanial agent-21 inhibits the Chloroquine (HY-17589A)-resistant strain of Plasmodium falciparum (RKL9) with an IC50 of 0.0198-0.096 μM .
K11 is an antimicrobial peptide. K11 is active against MDR/XDR K. pneumoniae isolates (MIC: 8-512 μg/mL), and inhibits bacterial biofilm formation. K11 can act synergistically with antibiotics (Chloramphenicol (HY-B0239), Meropenem (HY-13678), Rifampicin (HY-B0272), etc.) against drug-resistantK. pneumoniae. K11 has high thermal and wide pH stability .
Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
Meropenem-d6-1 (SM 7338-d6-1) is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
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 .
CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC50: 75 nM). CYP1B1-IN-7 also reverses resistance (IC50: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011) .
Meropenem (trihydrate) (Standard) is the analytical standard of Meropenem (trihydrate). This product is intended for research and analytical applications. Meropenem trihydrate (SM 7338 trihydrate) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem trihydrate has activity against susceptible and resistantN. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Pentamidine (Standard) is the analytical standard of Pentamidine. This product is intended for research and analytical applications. Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistantleishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities .
Omiganan pentahydrochloride is a cationic peptide compound with a broad antibacterial profile. Omiganan pentahydrochloride is capable of inhibiting a variety of bacteria, including yeast, and is active against both gram-positive and gram-negative bacteria. Omiganan pentahydrochloride is able to interact with the bacterial cell membrane, causing the destruction of the cell membrane and the death of the bacteria. Omiganan pentahydrochloride can be used for the study of antimicrobial activity against pathogens commonly associated with catheter-associated infections, including strains with drug-resistant phenotypes .
Anacardic acid diene is a polyunsaturated form of anacardic acid (HY-N2020) that has been found in cashew nut shell liquid. It has antibacterial activity against methicillin resistant S. aureus (MRSA) and S. mutans (MICs=12.5 and 6.25 μg/mL, respectively). Anacardic acid diene has schistosomicidal activity against adult S. mansoni worms when used at a concentration of 100 μM. It also inhibits soybean lipoxygenase-1 in a time-dependent manner.
IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species and has diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties. It is cytotoxic to L5178Y murine leukemia cells (IC50=0.54 ng/ml).1 IKD-8344 inhibits growth of the mycelial form of C. albicans (MIC=6.25 μg/mL) and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia.
Enopeptin A, originally isolated from a culture broth of Streptomyces sp. RK-1051, is a depsipeptide antibiotic that contains two unusual amino acids (N-methylalanine and 4-methylproline) and features a pentaenone side chain. It is effective against Gram-positive bacteria, including methicillin-resistant S. aureus (MIC=25 μg/mL), and Gram-negative bacteria, including mutant forms of E. coli and P. aeruginosa (MICs=200 μg/mL); however, it is not inhibitory to fungi.
Lolamicin is a Gram-negative specific antibiotic. Lolamicin is active against more than 130 multidrug-resistant clinical isolates, has shown efficacy in multiple mouse models of acute pneumonia and sepsis infection, and protects the gut microbiome of mice against secondary infection with Clostridium difficile. The selective killing of pathogenic gram-negative bacteria by Lolamicin is a result of the low sequence homology of pathogenic bacteria and symbiotic bacteria. Lolamicin can be used in the study of infection caused by Gram-negative pathogens .
Valanimycin is an antibiotic, which inhibits Escherichia coli (BE1121) through interaction with DNA. Valanimycin exhibits cytotoxicity to mouse leukemia L1210, P388/S (doxorubicin (HY-15142A)-sensitive), and P388/ADR (doxorubicin-resistant), with IC50 of 0.79, 2.65, and 1.44 μg/mL, respectively. Valanimycin exhibits antitumor efficacy against ehrlich ascites tumors or L1210 in mice .
SGC8158 is an inhibitor of PRMT7 and can be used to study the cellular function of PRMT7. SGC8158 decreases monomethylarginine levels of Hsp70 (the best characterized PRMT7 substrate). SGC8158 induces growth inhibition in various cancer cells (IC50: 2-9 μM), as well as multidrug-resistant (MDR) cancer cells. SGC8158 also enhances Doxorubicin (HY-15142A) induced DNA damage and Its cytotoxicity .
Pantinin-2 is a cysteine-free toxic peptide found in the emperor scorpion (paninus imperator). Pantinin-2 has high activity against Gram-positive bacteria but weak activity against Gram-negative bacteria. Pantinin-2 also exhibits activity against Candida tropicalis and has relatively mild hemolytic activity against human erythrocytes. Pantinin-2 can be used in the development of antimicrobial drugs for drug-resistant pathogens .
Antibacterial agent 231 (derivative 8) is an antimicrobial agent against multidrug-resistant Helicobacter pylori (H. pylori) with a minimum inhibitory concentration of 0.25–0.5 μg/mL. Antibacterial agent 231 directly targets the protein transposase subunit SecA and the outer membrane protein assembly factor BamD to inhibit the trafficking and assembly of bacterial outer membrane proteins (OMPs). Antibacterial agent 231 can be used to study the effects of antibiotic treatment on intestinal microbial balance .
Capreomycin (sulfate) (Standard) is the analytical standard of Capreomycin (sulfate). This product is intended for research and analytical applications. Capreomycin sulfate is a macrocyclic peptide antibiotic that inhibits phenylalanine synthesis in mycobacterial ribosomal translation. Capreomycin sulfate has anti-amyloidogenic and pro-fibrinolytic activities, reducing amyloid-induced cytotoxicity by inhibiting the occurrence of amyloid fibrillation. Capreomycin sulfate can be used in the study of multidrug-resistant tuberculosis, type 2 diabetes, Alzheimer's disease and Parkinson's disease .
LLC1 is an amiloride (HY-B0285) derivative with cytotoxicity against breast cancer cells, particularly those resistant to treatment. The IC50 values of LLC1 for MCF7, MCF7 MX-100, MCF7 TS, MCF7 TR-1, and MCF7 TR-5 are 13, 12, 25, 26, and 19 mM, respectively. LLC1 shows potential for research in the field of cancer therapy .
Acorafloxacin hydrochloride (JNJ-Q2 hydrochloride) is a broad-spectrum fluoroquinolone anti-bacterial drug being developed for the treatment of acute bacterial skin and skin-structure infections and community-acquired pneumonia .
Acorafloxacin hydrochloride (Avarofloxacin ) is an aminoethylidenylpiperidine fluoroquinolone that demonstrates antibacterial effect against numerous Gram-positive bacteria with a mean 0.12 mg/L MIC90 value .
Acorafloxacin hydrochloride (JNJ-Q2) has potential for treatment of methicillin-resistant Staphylococcus aureus (MRSA) infections .
L-Valine (Standard) is the analytical standard of L-Valine. This product is intended for research and analytical applications. L-Valine (Valine) is a new nonlinear semiorganic material. L-Valine standrd causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine standrd inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
(R)-Omeprazole (sodium) (Standard) is the analytical standard of (R)-Omeprazole (sodium). This product is intended for research and analytical applications. (R)-Omeprazole sodium is a gastric acid resistant compound with activity to inhibit gastric acid secretion. (R)-Omeprazole sodium is metabolized in vivo, and its metabolism is primarily affected by cytochrome P450 enzymes. The interaction between (R)-Omeprazole sodium and mannitol may affect its bioavailability in formulations. (R)-Omeprazole sodium exhibits reversible direct and metabolism-dependent inhibition of CYP2C19 .
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 inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
Inarigivir soproxil (SB9200) is an agonist of innate immunity and shows potent antiviral activity against resistantHCV variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems. Inarigivir soproxil, an orally bioavailable proagent of SB 9000, has broad-spectrum antiviral activity against RNA viruses including HCV, norovirus, respiratory syncytial virus and influenza and HBV .
Avarofloxacin (JNJ-Q2) is a broad-spectrum fluoroquinolone antibacterial agent being developed for the treatment of acute bacterial skin and skin-structure infections and community-acquired pneumonia with oral activity. Avarofloxacin (JNJ-Q2) is an aminoethylidenylpiperidine fluoroquinolone that demonstrates antibacterial effect against numerous Gram-positive bacteria with a mean 0.12 mg/L MIC90 value. Avarofloxacin (JNJ-Q2) has potential for treatment of methicillin-resistant Staphylococcus aureus (MRSA) infections .
4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity . 4'-Ethynyl-2'-deoxyadenosine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
(S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
7-O-Methylaloeresin A is 5-methylchromone glycoside isolated from Commiphora socotrana (Burseraceae). 7-O-Methylaloeresin A exhibits good activity against multiple agent resistant Staphylococcus aureus (NCTC 11994) and Salmonella typhimurium (ATCC 1255) with MIC values of 0.72 and 0.18 mM, respectively. 7-O-Methylaloeresin A has antioxidant activities, gives IC50 values of 0.026 mM and 0.021 mM for DPPH and 2-deoxyribose degradation assay, respectively.
AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF) .
FIT-039 is a selective, ATP-competitive and orally active CDK9 inhibitor with an IC50 of 5.8 μM for CKD9/cyclin T1. FIT-039 does not inhibit other CDKs and other kinases. FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistantHSVs and other DNA viruses.
PSMα3 TFA is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 TFA penetrates and modulates human monocyte-derived DCs by altering the TLR2- or TLR4-induced maturation, inhibiting pro- and anti-inflammatory cytokine production and reducing antigen uptake. PSMα3 TFA is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA) .
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
DprE1-IN-4 is a potent and orally active noncovalent DprE1 inhibitor with an IC50 of 0.90 μg/mL. DprE1-IN-4 exhibits potent in vitro activity against M. tuberculosis H37Rv and drug-resistant tuberculosis strain with MIC values of 0.12 μg/mL and 0.24 μg/mL, respectively. DprE1-IN-4 displays acceptable pharmacokinetic property and shows significant bactericidal activity in an acute mouse model of tuberculosis.
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistantStaphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells .
HDAC-IN-39 (compound 16c) is a potent HDAC inhibitor, with IC50 values of 1.07 μM (HDAC1), 1.47 μM (HDAC2), and 2.27 μM (HDAC3), respectively. HDAC-IN-39 also significantly inhibits microtubule polymerization. HDAC-IN-39 induces cell cycle arrest at the G2/M phase. HDAC-IN-39 displays promising anticancer activity against resistant cancer cells .
Antimicrobial agent-2 (compound V-a) is a broad-spectrum antimicrobial agent, possessing inhibitory activity against various Gram-positive and -negative bacteria. Antimicrobial agent-2 has excellent inhibitory effect on Methicillin-resistantStaphylococcus 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 .
Rubone, a chalcone analog, is a modulator of miR-34a. Rubone upregulates miR-34a expression in a p53 dependent manner, downregulates the downstream target Bcl-2 and Cyclin D1 expression, and suppresses hepatocellular carcinoma (HCC) growth in vivo. Rubone enhances the anticancer effect of Paclitaxel (PTX; HY-B0015) in PTX-resistant prostate cancer cell lines by reversing the expression of miR-34a downstream targets .
S 1360 is a potent and selective inhibitor of HIV-1 integrase. S 1360 inhibits the catalytic activity of purified integrase (
IC50: 20 nM). The EC50, and CC50 of S 1360
in MTT assay (MT-4 cells infected with HIV-1 IIIB) are 200 nM and 12 μM, respectively. S 1360 has antiviral activity against both X4 tropic and R5 tropic strains, as well as NRTI, NNRTI and PI drug-resistant variants .
VPC-3033 is an androgen receptor antagonist. VPC-3033 has a strong androgen DHT replacement potency (IC50: 0.625-2.5 μM), can effectively inhibit androgen receptor transcriptional activity (IC50=0.3 μM), and has a strong androgen receptor degradation ability. In addition, VPC-3033 exhibits significant anti-androgen receptor activity against prostate cancer cells resistant to Enzalutamide (HY-70002) .
5-Fluoroorotic acid (monohydrate) (5-Fluorouracil-6-carboxylic acid Mono(hydrate); 5-FOA) is used to detect URA3 gene expression in yeast molecular genetic constructs. Yeast with an active URA3 gene (which encodes orotidine-5'-monophosphate decarboxylase) convert 5-FOA to fluorodeoxyuridine, which is toxic to cells. Resistant yeast strains carrying mutations in the URA3 gene will grow in the presence of 5-FOA if uracil is added to the culture medium.
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 .
HP211206 is a SARS-CoV-2 main protease (M pro) PROTAC degrader. HP211206 effectively degrades SARS-CoV-2 M pro and its drug-resistant mutants. HP211206 has an IC50 of 181.9 nM and a DC50 of 621 nM for M pro. HP211206 has antiviral activity. (Pink: H117 (HY-170599); Black: linker (HY-B0236); Blue: E3 ligase ligand (HY-41547)) .
Tubulin polymerization-IN-73 (Compound 37) is an inhibitor for microtubule polymerization with an IC50 of 1.8 μM. Tubulin polymerization-IN-73 arrests the cell cycle at G2/M phase, induces apoptosis in A549 cell, inhibits the proliferation of A549 WT and A549/T resistant cell with IC50 of 0.023 μM and 0.057 μM. Tubulin polymerization-IN-73 exhibits antitumor efficacy in mouse model .
Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants .
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice .
Manumycin A is a polyketide antibiotic and an inhibitor of thioredoxin reductase 1 (TrxR-1). Manumycin A can inhibit the growth of breast cancer cells and exert its anti-tumor activity through LC3. Manumycin A can downregulate the release of pro-inflammatory cytokines in human monocytes stimulated by TNF α, and has potential anti-inflammatory activity. Manumycin A can inhibit the Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration resistant prostate cancer cells to suppress exosome biogenesis and secretion .
Albiglutide fragment (GLP-1 (7-36) analog) TFA is an active fragment of Albiglutide (7-36) and a glucagon-like peptide-1 (GLP-1) analog (a long-acting GLP-1 receptor agonist). Albiglutide is produced by the fusion of DPP-4 resistant GLP-1 dimer with the human albumin gene. Moreover, Albiglutide fragment TFA significantly reduces glycosylated hemoglobin (A1C) and is used in type 2 diabetes (T2D) studies .
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
Bifenthrin is a synthetic pyrethroid insecticide. Bifenthrin prolongs the opening time of Nav1.8 sodium channels, leading to membrane depolarization and conductance block in the insect nervous system, thereby disrupting neural function. Bifenthrin was effective in inhibiting A. gambiae (LD50=0.15 ng/mg) and C. quinquefasciatus (LD50=0.16 ng/mg). Bifenthrin has good lethality against susceptible and resistant mosquitoes and is very effective in inhibiting blood sucking and can be developed as a mosquito-removal netting material .
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
Albiglutide fragment (GLP-1 (7-36) analog) is an active fragment of Albiglutide (7-36) and a glucagon-like peptide-1 (GLP-1) analog (a long-acting GLP-1 receptor agonist). Albiglutide is produced by the fusion of DPP-4 resistant GLP-1 dimer with the human albumin gene. Moreover, Albiglutide fragment significantly reduces glycosylated hemoglobin (A1C) and is used in type 2 diabetes (T2D) studies .
Antimycobacterial agent-6 (compound 25) is a potent inhibitor of Mycobacterium tuberculosis (Mtb)，targeting to both wild-type and fluoroquinolone-resistant Mtb strains. Antimycobacterial agent-6 inhibits Mtb DprE1-C387S mutant with MIC90s of 0.9 μM (H37Rv)，0.9 μM (MoxR)，0.5 μM (DprE1-P116S)，respectively .
SMAP-18 is a biological active peptide. (SMAP-18 is a 18-amino acid residue peptide amide which is a truncated form of SMAP-29. Sheep myeloid antimicrobial peptide-29 (SMAP-29) displays extremely high antimicrobial activity against Pseudomonas strains, other Gram-negative bacteria, and multidrug-resistant pathogens. SMAP-18 displays much higher cell selectivity as compared to parental SMAP-29 because of its decreased hemolytic activity and retained antimicrobial activity.)
hCA/Wnt/β-catenin-IN-1 (Compd 15) is an inhibitor of hCA (Ki: 33.6, 24.1, 6.8 nM for hCA II, hCA IX, hCA XII). hCA/Wnt/β-catenin-IN-1 reduces P-gp activity. hCA/Wnt/β-catenin-IN-1 also inhibits Wnt/β-catenin signaling pathway. hCA/Wnt/β-catenin-IN-1 inhibits cancer cell viability, including the NCI/ADR-RES DOX-resistant cell line .
EPI-001 (Standard) is the analytical standard of EPI-001. This product is intended for research and analytical applications. EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
PSMA binder-2 is a ligand for PSMA and can be used to synthesize Ac-PSMA-trillium. Ac-PSMA-trillium is a suitable PSMA-targeting compound with improved PSMA binding properties and pharmacokinetic properties. PSMA ligands have different biological applications after being modified with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
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 inhibitory activity 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 resistantStaphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well .
Nornidulin is a depsidone originally isolated from A. nidulans that has antibacterial activity against M. tuberculosis and M. ranoe as well as antifungal activity against T. tonsurans and M. audouini. It also inhibits the growth of methicillin-resistant S. aureus (MRSA; MIC=2 μg/mL).2 Nornidulin has cytotoxic activity in MOLT-3 cells (IC50=35.7 μM) but not HuCCA-1, HepG2, or A549 cells (IC50s=>116.4 μM).
PSMA-trillium is a PSMA targeting compound, consisting of a PSMA targeting molecule (PSMA binder), a Macropa chelating molecule, and a group that regulates pharmacokinetics (PK modifier). PSMA-trillium is a non-radioactive form of Actinium-225-PSMA-Trillium (BAY 3563254) with improved PSMA targeting and pharmacokinetic properties. PSMA-trillium can bind Ac through the Macropa chelating molecule, or the radioactive isotope 225Actinium. Actinium-225-PSMA-Trillium is a potent inhibitor of metastatic castration-resistant prostate cancer (mCRPC) .
Docusate (Sodium) (Standard) is the analytical standard of Docusate (Sodium). This product is intended for research and analytical applications. Docusate Sodium (Dioctyl sulfosuccinate sodium salt) is one of the main components in stool softeners. Docusate Sodium is a sulfated surfactant and may inactivate viral pathogens by disrupting viral envelopes and/or denaturing/disassociating proteins. Docusate Sodium is effective in vitro against wild type and drug-resistant strains of HSV type 1 and 2. Docusate Sodium is an obesogen. Docusate Sodium with developmental exposure leads to increased adult adiposity, inflammation, metabolic disorder and dyslipidemia in offspring fed a standard diet in mice .
Amikacin (disulfate) (Standard) is the analytical standard of Amikacin (disulfate). This product is intended for research and analytical applications. Amikacin disulfate (BAY 41-6551 dissulfate) is an aminoglycoside antibiotic and a semisynthetic analog of kanamycin. Amikacin disulfate is bactericidal, acting directly on the 30S and 50S bacerial ribosomal subunits to inhibit protein synthesis. Amikacin disulfate is very active against most Gram-negative bacteria including gentamicin-and tobramycin-resistant strains. Amikacin disulfate also inhibits the infections caused by susceptible Nocardia and nontuberculous mycobacteria .
Pentamidine (isethionate) (Standard) is the analytical standard of Pentamidine (isethionate). This product is intended for research and analytical applications. Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities .
FtsZ-IN-10 is a bacterial division inhibitor that interferes with the normal assembly of FtsZ. FtsZ-IN-10 specifically binds to Bacillus subtilis FtsZ monomers, thereby affecting their polymerization behavior. FtsZ-IN-10 may also activate nucleotide-free archaeal FtsZ to form ordered polymers. FtsZ-IN-10 can hinder the localization of FtsZ in the Z ring and inhibit bacterial cell division. Chlorinated analogs of FtsZ-IN-10 show the ability to inhibit the growth of antibiotic-resistant clinical isolates such as Staphylococcus aureus and Enterococci .
Cephradine (monohydrate) (Standard) is the analytical standard of Cephradine (monohydrate). This product is intended for research and analytical applications. Cephradine (Cefradine) monohydrate is a broad-spectrum and orally active cephalosporin. Cephradine monohydrate is active against both grampositive and gram-negative pathogens and effective in eradicating most penicillinase-producing organisms known to be resistant to penicillin G, penicillin V, and ampicillin. Cephradine monohydrate has been used in the research of genitourinary, gastrointestinal and respiratory tract infections, and in infections of the skin and soft tissues. Cephradine monohydrate blocks solar-ultraviolet induced skin inflammation through direct inhibition of TOPK .
Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum .
Methotrexate metabolite (DAMPA) is an active metabolite of Methotrexate. Methotrexate is a Folic acid (HY-16637) antagonist, widely used as an immunosuppressant. Methotrexate metabolite is an antimalarial agent that inhibits parasite growth under physiological folic acid conditions, with IC50 values of 446 nM and 812 nM against folic acid-sensitive strains and highly resistant strains, respectively. Methotrexate metabolite exhibits pharmacokinetic characteristics of rapid clearance and extensive metabolism, with a mean clearance rate of 1.9 l/kg/h and a mean terminal half-life of 51 minutes. Methotrexate metabolite is promising for research in the field of inflammation .
4-Methylesculetin is an orally active coumarin derivative, with potent anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase activity. 4-Methylesculetin protects bone resorption by reducing the elevated levels of bone-joint exoglycosidases, cathepsin-D and tartrate resistant acid phosphatases. 4-Methylesculetin ameliorats the upregulated non-enzymatic inflammatory markers like TNF-α, IL-1β, IL-6, COX-2 and PGE2, which is promising for research of inflammatory diseases .
Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins .
Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF. Deoxyshikonin inhibited colorectal cancer (CRC) through the PI3K/Akt/mTOR pathway. Deoxyshikonin has proangiogenesis effect and antitumor activity. Deoxyshikonin is an antibacterial agent against methicillin-resistantS. aureus (MRSA) and S. pneumonia (MIC=17 μg/mL) .
Teduglutide TFA is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide TFA can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide TFA can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis .
4(1H)-Quinolinone, 1-methyl-2-(5Z)-5-undecen-1-yl- (compound 2) is a quinolone alkaloid that can be isolated from Cnidium. 4(1H)-Quinolinone, 1-methyl-2-(5Z)-5-undecen-1-yl- has methicillin-resistant Staphylococcus aureus (MRSA) activity, with MIC values of 32 μg/mL (ATCC 33591) and 16 μM/mL (ATCC 25923), respectively .
SA09-Cu is a noncompetitive and potent NDM-1 inhibitor with an IC50 of 9.6 nM. SA09-Cu can convert NDM-1 into an inactive state by oxidizing the Zn(II)-thiolate site of the enzyme and avoids to be reduced by intracellular thiols of bacteria. SA09-Cu exhibits excellent inhibition against a series of clinical NDM-1-producing carbapenem-resistant Enterobacteriaceae (CRE) in restoring the Meropenem (HY-13678) effect, and slows down the development of carbapenem resistance .
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.
CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target (CYP51/PD-L1) inhibitor, with IC50 values of 0.17 and 0.021 μM, respectively. CYP51/PD-L1-IN-4 exhibits excellent antifungal and antidrug-resistant fungal activity in vitro. CYP51/PD-L1-IN-4 can be used for fungal infections research .
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 resistantStaphylococcus aureus. Eltrombopag Olamine can induce apoptosis in hepatocellular carcinomab (HCC) as well .
Protorubradirin is an antibiotic that can be isolated from Streptomyces achromogenes var. rubradirin together with Rubradirin. Protorubradirin has inhibitory activity 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 .
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 .
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 inhibitory activity against HBV replication .
COX-1/2-IN-9 (Compound 3n) is a potent and selective inhibitor of COX-1/2, with IC50 values of 0.031 µM and 0.01 µM, respectively. COX-1/2-IN-9 possesses both antibacterial and anti-inflammatory activities, effectively inhibiting MRSA 1478 (MIC=50 μg/mL) and multidrug-resistantS. lentus (MIC=50 μg/mL). COX-1/2-IN-9 holds significant potential to alleviate MRSA-induced pneumonia in immunocompromised states .
HDAC-IN-76 (compound 6i) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-76 IC50 values of 30 nM and 98 nM for Pf3D7 (chloroquine (HY-17589A) drug-susceptible strain) and PfDd2 (chloroquine (HY-17589A) drug-resistant strain), has a highly potent antimalarial activity against asexual blood-stage Plasmodium, respectively, and exhibits selective inhibition against parasites, with IC50 values of 7 nM and 9 nM for human HDAC1 and HDAC6, respectively, while inhibiting PfHDAC1 .
Virginiamycin S1 (Standard) is the analytical standard of Virginiamycin S1. This product is intended for research and analytical applications. Virginiamycin S1 is a cyclic hexadepsipeptide antibiotic, inhibits bacterial protein synthesis at the level of aminoacyl-tRNA binding and peptide bond formation. Virginiamycin S1 belongs to the type B compounds in the streptogramin family and is produced by Streptomyces virginiae, shows a strong bactericidal activity against a wide range of Gram-positive bacteria. Virginiamycin S1 together with virginiamycin M1 is more effective in treat multidrug-resistant bacterial infections .
KSK120 is a potent inhibitor of drug-resistant infections with specific activity against Chlamydia trachomatis (C. trachomatis). KSK120 inhibits the developmental cycle of C. trachomatis, thereby reducing the infectivity of progeny bacteria. KSK120 targets the glucose-6-phosphate (G-6P) metabolic pathway of C. trachomatis, showing its potential application in antimicrobial inhibition. The mechanism of KSK120 may involve inhibition of the transcriptional machinery, which provides new ideas for the development of specific drugs against C. trachomatis infection .
Melicopine is an alkaloid found in Z. simulans with antimalarial and anticancer activities. It exhibits inhibitory activity against chloroquine-sensitive 3D7 and chloroquine-resistant Dd2 strains of P. falciparum, with IC50 values of 29.7 and 33.7 µg/mL, respectively. Melicopine is cytotoxic to prostate cancer cells PC-3M and LNCaP (IC50 values of 47.9 and 37.8 µg/mL), but has no effect on non-cancerous HEK293 cells (IC50 greater than 100 µg/mL). Melicopine holds promise for research in anticancer and anti-infection fields .
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM).
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells .
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 .
WNY0824 (PLK1/BRD4-IN-1) is an orally active dual inhibitor of PLK1 and BET protein families, with IC50 values of 22, 402.5, 150.7, 103.9, and 311.9 nmol/L for PLK1, BRD2, BRD3, BRD4, and BRDT, respectively. WNY0824 induces cell cycle arrest and apoptosis by inhibiting AR- and MYC-mediated transcriptional processes. In addition, WNY0824 also inhibits tumor growth in Enzalutamide (HY-70002) resistant CRPC xenograft tumor models .
Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC50 values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis .
HVH-2930 is an inhibitor for heat shock protein 90 (HSP90). HVH-2930 inhibits cell viability of BT474 (Trastuzumab (HY-P9907) sensitive) and JIMT-1 (Trastuzumab (HY-P9907) resistant), with IC50 of 6.86 μM and 4.42 μM, through downregulation of HSP90 clients HER2, p-HER2, AKT, p-AKT, cyclin D1 and survivin. HVH-2930 exhibits antitumor efficacy in mouse models. HVH-2930 exhibits good pharmacokinetic characteristics in mice .
Sp-8-Br-PET-cGMPS is a membrane-permeable PKG agonist and a membrane-permeable inhibitor of retinal-type cGMP-gated ion channels, as well as an activator of cGMP-dependent protein kinases I α and I β. Sp-8-Br-PET-cGMPS is resistant to mammalian cyclic nucleotide-dependent phosphodiesterases, has no metabolic side effects, and is more lipophilic and permeable than Sp-8-pCPT-cGMPS. Sp-8-Br-PET-cGMPS can be used to study the role of cGMP signaling pathways in the nervous system .
6-(12-Tridecene-1-yl)-2,4-Dihydroxy benzoic acid (Compound 2) exhibits antibacterial activity against methicillin-resistantStaphylococcus aureus (MRSA) and Vancomycin enterococci (VRE). 6-(12-Tridecene-1-yl)-2,4-Dihydroxy benzoic acid interfers with the integrity and function of the bacterial cell membrane, and affects metabolism in MRSA. 6-(12-Tridecene-1-yl)-2,4-Dihydroxy benzoic acid exhibits anti-inflammatory and anti-infective efficacy, and promotes angiogenesis in mice .
CHMFL-48 is an orally active BCR-ABL kinase inhibitor targeting both wild-type (wt) and various imatinib-resistant mutants. The IC50 values for CHMFL-48 against ABL wild-type and ABL T315I mutant are 1 nM and 0.8 nM, respectively. CHMFL-48 exerts its effects by blocking the autophosphorylation of BCR-ABL wild-type and mutant forms, which impacts downstream signaling mediators such as STAT5 and CRKL, leading to cell cycle arrest and induction of apoptosis. CHMFL-48 holds potential for research into chronic myeloid leukemia (CML) .
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) .
BMS-986169 is an inhibitor of the glutamate N-methyl-D-aspartate 2B receptor (GluN2B). BMS-986169 has a high binding affinity for the allosteric regulatory site of the GluN2B subunit, with a Ki value of 4.03-6.3 nM. BMS-986169 can inhibit the function of GluN2B receptors in Xenopus oocytes, with an IC50 value of 24.1 nM. BMS-986169 can also inhibit the activity of the hERG channel, with an IC50 value of 28.4 μM. BMS-986169 can be used in research on treatment-resistant depression .
Bifenthrin (Standard) is the analytical standard of Bifenthrin. This product is intended for research and analytical applications. Bifenthrin is a synthetic pyrethroid insecticide. Bifenthrin prolongs the opening time of Nav1.8 sodium channels, leading to membrane depolarization and conductance block in the insect nervous system, thereby disrupting neural function. Bifenthrin was effective in inhibiting A. gambiae (LD50=0.15 ng/mg) and C. quinquefasciatus (LD50=0.16 ng/mg). Bifenthrin has good lethality against susceptible and resistant mosquitoes and is very effective in inhibiting blood sucking and can be developed as a mosquito-removal netting material .
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 .
NDI-Lyso is a lysosome-targeted anticancer agent that induces the formation of rigid long fibers in cancer cell lysosomes through an enzyme-instructed self-assembly (EISA) mechanism catalyzed by cathepsin B. This process triggers lysosomal swelling, membrane permeabilization (LMP), and membrane disruption, ultimately leading to cancer cell apoptosis via a non-classical caspase-independent pathway. NDI-Lyso exhibits significant selective anticancer activity in various cancer cell lines and drug-resistant cancer cells (IC50 ~10 μM) while showing low toxicity to normal cells (IC50 > 60 μM) .
D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells .
Antiproliferative agent-23 is a microtubule-destabilizing agent (MDA) and efficiently disturbes the tubulin-microtubule system. Antiproliferative agent-23 induces apoptosis via a mitochondrion-dependent pathway by downregulating the Bcl-2 protein, upregulating Bax and Cyt c proteins, and activating the caspase cascade. Antiproliferative agent-23 initiates reactive oxygen species (ROS)-mediated endoplasmic reticulum stress in A549/CDDP cells (cisplatin resistant cancer cell line) via the PERK/ATF4/CHOP signaling pathway. Antiproliferative agent-23 has anti-tumor activity .
DHFR-IN-9 (compound 8A) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-9 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=0.25 μg/mL) and has anti-infective effects in mouse models of systemic infection and thigh infection caused by it (dose: 2.5 mg /kg, 5 mg/kg; ip). DHFR-IN-9 has stronger anticancer activity than paclitaxel (Y-B0015) in a mouse model of breast cancer (dose: 2.5 mg/kg; ip; once every 3 days) .
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 inhibitory activity 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) .
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 RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistantRT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .
TRK-IN-30 (Compound C11) is the inhibitor for tropomyosin receptor kinase (TRK) that inhibits TRKA, TRKB and TRKC and drug resistant mutant TRKA G595R with an IC50 of 1.8, 0.98, 3.8, and 54 nM, respectively. TRK-IN-30 inhibits the activation of the downstream PI3K/AKT and MEK/ERK signaling pathways. TRK-IN-30 inhibits the colony formation and cell migration of Km-12, arrests the cell cycle at G0/G1 phase, and induces apoptosis in Km-12 .
Ivaltinostat (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat induces apoptosis and has anti-tumour effects .
Anti-inflammatory agent 84 (Compound 4D) is a derivative of Coumarin (HY-N0709) with antimicrobial and anti-inflammatory activities. Anti-inflammatory agent 84 inhibits E. coli, Candida albicans, Staphylococcus aureus and methicillin-resistantS. aureus (MRSA), with MIC of 312, 156, 19 and 316 μg/mL, respectively. Anti-inflammatory agent 84 inhibits biofilm formation of S. aureus, E. coli and MRSA, with IC50 of 185, 321 and 99 μM, respectively. Anti-inflammatory agent 84 inhibits nitric oxide production in Lipopolysaccharide (HY-D1056)-stimulated RAW264.7 macrophage cell .
Diacetylcercosporin is a perylenequinone produced by Cercospora and Septoria that has diverse biological activities. Diacetylcercosporin inhibits the growth of P. falciparum strains that are sensitive and resistant to chloroquine (IC50s=2.75 and 1.94 μM for D6 and W2 clones, respectively) and L. donovani parasites (IC50=3.1 μM) in vitro. Diacetylcercosporin exhibits cytotoxicity against SK-MEL, KB, BT549, and SKOV3 human cancer cell lines (IC50s=4.8-8.7 μM). Diacetylcercosporin is also a phytotoxin that inhibits the growth of lettuce and bentgrass at a concentration of 1.62 mM.
Isosulfazecin (iSZ) is a novel β-lactam antibiotic produced by Pseudomonas acidophilus sp., synthesized in a nutrient solution supplemented with glycerol and sodium thiosulfate under aerobic conditions in parallel with bacterial growth. It is purified by chromatography and crystallization from aqueous methanol. Physicochemical analysis determined its molecular formula to be C12H20N4O9S, showing a structure with a β-lactam ring, methoxyl and sulfonate groups. Acid hydrolysis yields L-alanine and D-glutamic acid. iSZ is a diastereomer of sulfadiazine and exhibits moderate activity against both gram-positive and gram-negative bacteria, but potent activity against bacteria resistant to β-lactam antibiotics .
9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections .
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated?MTOR?mutants and the growth of rapamycin-resistant cancer cells.?BC-LI-0186 is a promising agent for lung cancer research .
Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat formic inhibits deacetylation of histone H3 and tubulin. Ivaltinostat formic induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat formic enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat formic induces apoptosis and has anti-tumour effects .
C6 Ceramide (C6-Cer) is a short-chain, cell-permeable ceramide pathway activator with anticancer activity. C6 Ceramide-mediated miR-29b expression participates in the progression of multiple myeloma through suppressing the proliferation, migration and angiogenesis of endothelial cells by targeting Akt signal pathway. C6 Ceramide exhibits multiple anti-cancer properties including cell cycle arrest, Apoptosis, inhibition of tumor growth and enhances the effects of chemotherapy in drug-resistant cancer cells. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
HIV-1 inhibitor-58 (Compound 10c) is a broad-spectrum antiviral agent. HIV-1 inhibitor-58 is a non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-58 inhibits WT strain IIIB, NNRTI-resistant strains (such as K103N and E138K) in MT-4 cells, with EC50 less than 50 nM. HIV-1 inhibitor-58 also inhibits CYP2C9 and CYP2C19 (IC50: 2.06 μM, 1.91 μM). HIV-1 inhibitor-58 can be used for HIV infection reserch .
MAO A/HSP90-IN-2 (compound 4-C) is a dual inhibitor of HSP90and MAO A with the IC50 values of 0.016 and 4.58 μM, respectively. MAO A/HSP90-IN-2 increases HSP70 expression and reduces HER2 and phospho-Akt expression, and decreases IFN-γ induced PD-L1 expression in GL26 cells. MAO A/HSP90-IN-2 inhibits the growth of Temozolomide (HY-17364) -sensitive and -resistant GBM cells, colon cancer, leukemia, non-small cell lung and other cancers, and has potential to inhibit tumor immune escape [1].
PSMA binder-1 is a ligand for PSMA and can be used to synthesize Ac-PSMA-trillium. Ac-PSMA-trillium is a suitable PSMA-targeting compound with improved PSMA binding properties and pharmacokinetic properties. PSMA ligands have different biological applications after being modified with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or it can be labeled with 225Ac (to obtain Actinium-225-PSMA-Trillium (BAY 3563254)), which has a radioactive killing effect; it can be used as a Macropa chelator for targeted radionuclide therapy (TRT) , has a strong inhibitory effect on metastatic castration-resistant prostate cancer (mCRPC) .
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
SPSB2-iNOS inhibitory cyclic peptide-1 TFA is the TFA salt form of SPSB2-iNOS inhibitory cyclic peptide-1(HY-P10383). SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
Rp-8-bromo-PET-Cyclic GMPS (Rp-8-bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.
Citreamicin alpha (LL-E 19085-alpha) is an antibiotic whose in vitro antimicrobial activity against 429 clinical isolates of Gram-positive cocci has been tested by the agar dilution method. These microorganisms included 313 strains of Staphylococci and 116 strains of Streptococci. The in vitro activity of Citreamicin alpha was compared with that of ampicillin, amoxicillin, ceftriaxone, erythromycin, and vancomycin. For Staphylococci, the MIC values of Citreamicin alpha ranged from 0.12-4.0 μg/ml, and for Streptococcus pyogenes of the genus Streptococcus, it was 0.03-0.12 μg/ml. However, enterococci were relatively resistant, requiring 2.0 μg/ml of the agent to inhibit 64% of the 62 tested strains. The in vitro activity of this antibiotic was much better than that of ampicillin, amoxicillin, ceftriaxone, and erythromycin, but comparable or slightly inferior to that of vancomycin.
BP13944 is a potential small molecule inhibitor discovered by high-throughput screening. It can effectively inhibit the expression of dengue virus (DENV) replicons with an EC50 value of 1.03±0.09 μM. BP13944 can inhibit the replication or viral RNA synthesis of all four serotypes of DENV, but is ineffective against Japanese encephalitis virus. BP13944 may target the DENV NS3 protease, and the E66G amino acid substitution in the NS3 protease region will cause the virus to become resistant to BP13944. BP13944 has no obvious cytotoxicity. As there is currently no effective dengue vaccine and treatment, BP13944, as an effective small molecule inhibitor, may become a potential agent for the treatment of dengue in the future.
Maleic Acid (Standard) is the analytical standard of Maleic Acid. This product is intended for research and analytical applications. Maleic Acid is a Glutamate Decarboxylase (GAD) inhibitor of E. coli and L. monocytogenes.
IC50 & Target: GAD .
In Vitro: The MICs of WT 10403S for the acids (e.g., Maleic Acid) are 34 mM, 25 mM, 31 mM and 30 mM which correspond to pH values prior to growth of 4.84, 5.14, 5.32 and 5.02 respectively. Of all compounds tested, Maleic Acid is the least inhibitory despite acting at a lower pH (4.84). The most acid resistant (10403S) and the weakest (EGD-e) strain are challenged with 8.6 mM and 4.3 mM of each organic acid at pH 3 and 3.3 respectively. On both strains, Maleic Acid is the most bactericidal .
Evo312 is a dose-dependent inhibitor of protein kinase CβⅠ (PKCβⅠ) (IC50 is 117.34 nM). Evo312 induces PANC-GR (acquired gemcitabine-resistant PC cells) cell cycle arrest and apoptosis by inhibiting PKCβ1 protein expression. Evo312 has antiproliferative effects in pancreatic cancer cells PANC-1 and PANC-GR cells with IC50 of 0.08 μM and 0.07 μM, and in human normal pancreatic ductal epithelial cells HPDE6-c7 with IC50 of 2.95 μM. Evo312 exhibits antitumor activity in a PANC-GR cell transplantation mouse model .
YJ1206 is an orally active, selective CDK12/CDK13 PROTAC degrader with an IC50 of 12.55 nM for in VCaP cells. YJ1206 increases DNA damage, induces apoptosis, and promotes tumor regression in orthotopic WA74 patient-derived xenograft (PDX) mice models of resistant prostate cancer. YJ1206 suppresses tumor growth in vivo in conjunction with AKT pathway inhibitors. YJ1206 is composed of the CDK12/CDK13 degradation agent (HY-168658), a linker (HY-W004328), and a VHL E3 ubiquitin ligase (HY-W453548). (Pink: Navitoclax; Blue: VHL ligand; Black: linker) .
D-Mannitol (Standard) is the analytical standard of D-Mannitol. This product is intended for research and analytical applications. D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat 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 inhibitory activity against Mycobacterium tuberculosis (susceptible and drug-resistant) and Klebsiella pneumoniae, and can be used in the research of tuberculosis and pneumonia .
Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
9-Aminoacridine-13C6 is the 13C-labeled 9-Aminoacridine(HY-B1422). 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistantK. pneumoniae infections .
9-Aminoacridine (Standard) is the analytical standard of 9-Aminoacridine. This product is intended for research and analytical applications. 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections .
Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities. It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s=3.94, 0.6, 2.21, 4.55, and 2.21 μg/mL, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50=5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestrin (0.1 μg/mL) induces apoptosis in HL-60 cells. It induces heart, thymus, and liver tissue necrosis in mice when administered at doses ranging from 18 to 30 mg/kg.
USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .
Apalcillin (PC-904) in combination with Ro 48-1220, a penam sulfone β-lactamase inhibitor, demonstrated broad-spectrum activity against gram-negative aerobic and anaerobic bacteria, excluding Klebsiella oxytoca. It exhibited potent activity against β-lactamase-producing Moraxella catarrhalis, Haemophilus influenzae, and Neisseria gonorrhoeae, with effective MICs (11 μg/mL). The combination also inhibited Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Acinetobacter species at low MICs (0.25 to 4 μg/mL). However, its efficacy against oxacillin-resistant staphylococci and certain gram-positive organisms was limited. Apalcillin/Ro 48-1220 showed comparable efficacy to piperacillin/tazobactam against some extended-spectrum β-lactamase-producing Escherichia coli but was less effective against SHV-type β-lactamases .
CL-385319 is an N-substituted piperidine compound with inhibitory activity 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 .
Neospiramycin I is a macrolide antibiotic and a derivative of Spiramycin I (HY-N7141). Neospiramycin I is effective against the macrolide-sensitive KB210 strain of S. aureus, but ineffective against the macrolide-resistant KB224 strain, with minimum inhibitory concentrations (MIC) of 3.12 and greater than 100 µg/mL, respectively; it is also effective against B. cereus, B. subtilis, M. luteus, E. coli, and K. pneumoniae, with respective MIC values of 1.56, 3.12, 3.12, 0.2, 50, and 12.5 µg/mL. Neospiramycin I binds to the ribosomes of E. coli, with an inhibitory concentration 50 (IC50) of 1.2 µM. It protects mice from death in a type III S. pneumoniae infection model, with an effective dose 50 (ED50) of 399.8 mg/kg .
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM .
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
Lys(CO-C3-p-I-Ph)-O-tBu is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules. Lys(CO-C3-p-I-Ph)-O-tBu can increase the residence time of PSMA ligand in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-O-tBu also reduces salivary gland absorption, possibly extending the half-life of the active compound. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .
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 inhibitory activity against COX isomerases, further emphasizing its specificity as a prostate cancer inhibitory compound .
Lys(CO-C3-p-I-Ph)-OMe is a pharmacokinetic modifier (PK modifier) that can improve the PK properties of PSMA ligand molecules (such as Ac-PSMA-trillium). Lys(CO-C3-p-I-Ph)-OMe can increase the residence time of Ac-PSMA-trillium in plasma by increasing its binding capacity to albumin. Lys(CO-C3-p-I-Ph)-OMe also reduces salivary gland absorption of Ac-PSMA-trillium, potentially extending its half-life. Ac-PSMA-trillium is a suitable PSMA-targeting compound that has different biological applications after modification with different radioactive isotopes. If labeled with 111In, it can be used as DOTA chelating agent and imaging agent. Or labeled with 225Ac as a Macropa chelator for targeted radionuclide therapy (TRT) in the study of metastatic castration-resistant prostate cancer (mCRPC) .
Milbemycin A4 oxime (5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime) is a derivative of Milbemycin A4 (HY-126906) and a component of Milbemycin oxime (HY-B0778), both of which have insecticidal and nematicidal activities. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae in naturally infected dogs with D. immitis and inhibits the growth of clinical isolates of Candida glabrata (MIC80=16-32 μg/mL). Milbemycin A4 oxime (2.5 μg/mL) blocks the efflux of Fluconazole (HY-B0101) from clinical isolates of Candida glabrata. Milbemycin A4 oxime enhances doxorubicin-induced cell growth inhibition and increases the intracellular accumulation of doxorubicin and P-glycoprotein substrate Rhodamine 123 (HY-D0816) in doxorubicin-resistant but not sensitive MCF-7 breast cancer cells in a concentration-dependent manner.
Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC50s of 0.49 nM (ABL), 0.78 nM (ABL T315I), 9.5 nM (ABL E255K), 2.0 nM (ABL F317I), 7.4 nM (ABL G250E), 1.0 nM (ABL H396P), 2.8 nM (ABL M351T), 12 nM (ABL Q252H), and 4.1 nM (ABL Y253F), respectively . Vamotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
Bicyclol (SY801) is an orally active derivative of the traditional Chinese medicine Schisandra chinensis, which has antiviral, anti-inflammatory, immunomodulatory, antioxidant, anti-steatosis, anti-fibrotic and anti-tumor activities. Bicyclol regulates the expression of heat shock proteins and plays an anti-apoptosis role in hepatocytes. Bicyclol reduces the activation of NF-κB and the levels of inflammatory factors in hepatocytes infected with hepatitis C virus (HCV) by inhibiting the activation of the ROS-MAPK-NF-κB pathway, and prevents ferroptosis in acute liver injury. Bicyclol can change the expression of Mdr-1, GSH/GST and Bcl-2, increase the intracellular concentration of anticancer drugs, and sensitize drug-resistant cells to anticancer drugs. Bicyclol inhibits the proliferation of human malignant hepatoma cells by regulating the PI3K/AKT pathway and the Ras/Raf/MEK/ERK pathway. Bicyclol can be used in the study of chronic hepatitis, acute liver injury, nonalcoholic fatty liver disease, liver fibrosis and hepatocellular carcinoma .
HIV-1 inhibitor-30 (compound 10i) is a potent HIV-1 inhibitor with an EC50 value of 40 nM and an IC50 value of 80 nM for HIV-1 RT DNA polymerase. HIV-1 inhibitor-30 has highly antiretroviral activity against seven non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant HIV-1 strains (RT-K103N; RT-Y181C; RT-K103N,Y181C; RT-L100I,K103N; RT-Y188L; RT-K103N,G190A; RT-K103N,V108I) with IC50s of 0.04~1.42 μM. HIV-1 inhibitor-30 can be used for researching AIDS .
(6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol is an antibacterial compound. (6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol can be isolated from the roots of Atractylodes japonica. (6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol has anti-methicillin-resistantStaphylococcus aureus (MRSA) activity with MIC values of 4-32 μg/mL. (6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol can be used for the research of bacterial infection . (6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
TST1N-224 is a potent response regulator VraRC inhibitor. TST1N-224 can disrupt VraRC-DNA complex formation (IC50=60.2 μM). TST1N-224 exhibits interference with VraRC binding to its cognate DNA through a fast-on-fast-off binding mechanism (KD=23.4 μM). TST1N-224 predominantly interacts with the α9- and α10-helixes of the DNA-binding domain of VraR. TST1N-224 inhibits the growths of S. aureus (SA; MIC>126 μM), Methicillin-resistantS. aureus (MRSA; MIC>126 μM), and Vancomycin-intermediate S. aureus (VISA; MIC=63 μM). TST1N-224, an antimicrobial agent, evidently enhances the susceptibility of VISA to both Vancomycin (HY-B0671) and Methicillin (HY-B0974) .
PH11 is a novel focal adhesion kinase (FAK) inhibitor that rapidly induces apoptosis in TRAIL-resistant PANC-1 cells when combined with TRAIL, but has no effect on normal human fibroblasts. The study found that PH11 downregulates c-FLIP through inhibition of FAK and phosphatidylinositol-3-kinase (PI3K)/AKT pathways, thereby restoring the TRAIL apoptotic pathway, suggesting that this combination therapy may provide an attractive therapeutic strategy for the safe and effective treatment of pancreatic cancer. PH11 selectively inhibits c-FLIP expression by modulating upstream signaling pathways and may represent an innovative therapeutic strategy. Although further work is needed to fully elucidate the mechanism of PH11-induced TRAIL sensitization, we believe that our results will provide a new approach to target c-FLIP without the risk of interfering with caspase-8 processing, which could potentially lead to TRAIL resistance. This study also suggests a role for the FAK/AKT signaling pathway in regulating c-FLIP expression in TRAIL-induced apoptosis, and this understanding will provide important clues to control the resistance mechanism to optimize the potential of TRAIL-based pancreatic cancer treatment.
5,6-Epoxyeicosatrienoic acid-d11 (5,6-EET-d11) is deuterium labeled 5,6-Epoxyeicosatrienoic acid. 5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5,6-Epoxyeicosatrienoic acid is provided as a mixture of the free acid and lactone .
Resistance refers to the decrease in the effectiveness of drugs in treating diseases or symptoms. Due to the increasing global antibiotic resistance, it may threaten our ability to treat common infectious diseases. Drug resistance is also the main cause of chemotherapy failure in malignant tumors. In approximately 50% of cases, drug resistance exists even before chemotherapy begins. There are many mechanisms of anticancer drug resistance, including increased protein expression that leads to drug removal, mutations in drug binding sites, recovery of tumor protein production, and pre-existing genetic heterogeneity in tumor cell populations. In addition, the issue of drug resistance seems to have affected the development of new anticancer drugs. Drug resistance may be caused by various conditions, such as mutations, epigenetic modifications, and upregulation of drug efflux protein expression. Overcoming multidrug resistance in cancer treatment is becoming increasingly important.
MCE designs a unique collection of 459 anti-drug-resistant compounds. It is a good tool to be used for research on cancer and other diseases.
Tuberculosis (TB), usually caused by bacteria (Mycobacterium tuberculosis), is an infectious disease that mainly affects the lungs. According to the statistics of the World Health Organization (WHO), 10 million people suffer from tuberculosis every year, and 1.5 million people die of tuberculosis every year, which makes tuberculosis the number one killer of infectious diseases.
Tuberculosis can be cured through the standard 6-month course of treatment of four kinds of antibiotics. Common drugs include rifampicin and isoniazid. In some cases, TB bacteria do not respond to standard drugs, that is, patients with drug-resistant tuberculosis. The treatment of drug-resistant tuberculosis takes longer and is more complex. In the face of the resurgence of tuberculosis in the world and the rapid emergence of multi drug resistant tuberculosis, it is very important to develop new anti-tuberculosis drugs or new clinical treatment schemes for existing anti mycobacterium drugs.
MCE supplies a unique collection of 115 compounds with clear anti-tuberculosis activity. MCE Anti-tuberculosis Compound Library is a useful tool for anti-tuberculosis related research and anti-tuberculosis drug development
Antibacterial agents are a group of materials that fight against pathogenic bacteria. Thus, by killing or reducing the metabolic activity of bacteria, their pathogenic effect in the biological environments will be minimized. The most widely used antibacterial agents exert their effects on bacterial cell wall synthesis, protein synthesis, DNA replication and metabolic pathways. However, resistance to antimicrobial agents has become a major source of morbidity and mortality worldwide. The main mechanisms of resistance are limiting uptake of a drug, modification of a drug target, inactivation of a drug, and active efflux of a drug. Therefore, it is an urgent need to develop new drugs targeted at resistant organisms.
MCE offers a unique collection of 1,514 compounds with validated antibacterial activities. MCE antibacterial compound library is an effective tool for drug repurposing screening, combination screening and biological investigation.
Chinese herbal therapy is an important part of Traditional Chinese Medicine (TCM). It has been used for centuries in China, where herbs are considered fundamental therapy for many acute and chronic conditions. Many studies indicated TCM exerted an overall regulatory effect via multi-component and multi-target network. Active components from Traditional Chinese Medicine possess many medicinal properties such as antioxidant, anti-cancer, and anti-bacterial effects, which makes it an important source of new drugs. Nearly 200 modern medicines have been developed either directly or indirectly from the plants used as medicines in China. For example, artemisinin, used in multidrug resistant malaria, was first isolated from the Chinese herb Artemisia annua L. Today, scientists continue to identify compounds in Chinese herbal remedies that may be useful in the development of new therapeutic agents applicable in Western medicine.
MCE designs a unique collection of 2,915 active compounds of Chinese Herbal Medicines. MCE Traditional Chinese Medicine Active Compound Library is a useful tool for discovery new drugs from TCM.
9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections .
Fast Red Violet LB is a dye for staining tartrate resistant acid phosphatase (TRAP). Fast Red Violet LB can be used for alkaline phosphatase (ALP) activity staining .
Permanent Orange is a synthetic pigment commonly used in the manufacture of paints and coatings. It belongs to the class of organic pigments and consists of carbon and other elements. Permanent Orange produces a bright orange color that is fade and weather resistant, making it ideal for outdoor applications. It can be mixed with other pigments to produce a range of colors and is compatible with a wide range of binders and solvents.
Xylene Fast Yellow 2G is a synthetic dye belonging to the class of azo dyes. It is commonly used in the textile industry to dye natural and synthetic fibers as well as in the paper and ink industries. Xylene Fast Yellow 2G produces a bright yellow color that is fade and wash resistant and can be applied to textiles by a variety of methods including dipping, padding and printing.
Permanent Orange (Standard) is the analytical standard of Permanent Orange. This product is intended for research and analytical applications. Permanent Orange is a synthetic pigment commonly used in the manufacture of paints and coatings. It belongs to the class of organic pigments and consists of carbon and other elements. Permanent Orange produces a bright orange color that is fade and weather resistant, making it ideal for outdoor applications. It can be mixed with other pigments to produce a range of colors and is compatible with a wide range of binders and solvents.
Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
9-Aminoacridine (Standard) is the analytical standard of 9-Aminoacridine. This product is intended for research and analytical applications. 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistant K. pneumoniae infections .
Dmt-2'fluoro-da(bz) amidite, an uniformly modified 2'-deoxy-2'-fluoro phosphorothioate oligonucleotide, is a nuclease-resistant antisense compound with high affinity and specificity for RNA targets. Dmt-2'fluoro-da(bz) amidite is also an intermediate for 5’-DMT-3’-phosphoramidite synthesis .
1-Amino-2,5-anhydro-1-deoxy-D-mannitol is a potent antibacterial compound with antibacterial activity against a variety of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). The application potential of 1-Amino-2,5-anhydro-1-deoxy-D-mannitol lies in its ability to effectively combat common drug-resistant bacterial infections. 1-Amino-2,5-anhydro-1-deoxy-D-mannitol may become an emerging antibacterial agent in clinical inhibition.
β-Sitosterol acetate, 95% (Sitosteryl acetate, 95%) is a sterol that can be isolated from Hechtia glomerata Zucc., which has antibacterial activity and has a MIC value of 100µg/mL against carbapenem-resistantAcinetobacter baumannii .
Meropenem sodium is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem sodium has activity against susceptible and resistantN. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans) .
PD-1/PD-L1-IN 3 TFA, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 TFA interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC50s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 TFA can be used for the research of various diseases, including cancer and infectious diseases .
Defensin HNP 4 (HNP 4) is a single 11 amino acid long fragment of HNP-41-11. Defensin HNP 4 has inhibitory effect against multidrug-resistant and non-resistant strains .
Telomycin is a calcium-dependent antibiotic, which can be produced by Streptomyces. Telomycin inhibits gram-positive bacteria, including multidrug-resistant (MDR) pathogens .
SAAP 148 is an antimicrobial and antibiofilm agent, and exhibits inhibitory efficacy against antibiotic-resistant pathogens, with LC50 of 0.8-12.8 μM .
Clovibactin is an antibiotic for drug-resistant bacterial pathogens without detectable resistance. Clovibactin TFA inihibits cell wall synthesis by targeting pyrophosphate of peptidoglycan precursors .
SAAP 148 TFA is an antimicrobial and antibiofilm agent, and exhibits inhibitory efficacy against antibiotic-resistant pathogens, with LC50 of 0.8-12.8 μM .
Griselimycin is a compound with antituberculosis activity that exhibits good in vitro and in vivo activity against sensitive and resistant Mycobacterium tuberculosis, and its cyclohexyl derivative has high transformative potential.
Capreomycin is a macrocyclic peptide antibiotic. Capreomycin can be used for anti-multidrug-resistant-tuberculosis research. Capreomycin can inhibit phenylalanine synthesis in in mycobacterial ribosomes translation
LCI peptide is an antimicrobial peptide with antibacterial activity. LCI peptide is active against plant pathogens, Xanthomonas and Pseudomonas, including E. coli, Gentamicin-resistant MRSA and Xoo .
Antho-rwamide I is a neuropeptide that can be isolated from the sea anemone Anthopleura elegantissima. Antho-rwamide I is resistant to nonspecific aminopeptidases, which increases the stability of the peptide after neuronal release .
P1 is a broad-spectrum antimicrobial peptide. P1 shows antibacterial activity against Gram-positive and Gram-negative bacteria,such as B. anthracis spores and Carbapenem-resistantA. baumannii and K. pneumoniae .
ASP-1 is a strong antistaphylococcal peptide with minimum inhibitory concentrations (MICs) of the purified peptide against S. aureus and methicillin-resistantS. aureus (MRSA) ranged from 2 μg/mL to 64 μg/mL .
Paenilagicin is a Gram-positive active antibiotic with a unique diphosphorylated prenyl binding mechanism that does not induce drug resistance. Paenilagicin exhibits a MIC value of 2 μg/mL against multidrug-resistant Gram-positive bacteria .
Desotamide is a cyclic hexapeptide antibiotic originally isolated from Streptomyces. It is active against S. aureus, S. pneumoniae, and methicillin-resistant S. epidermidis (MRSE; MICs=16, 12.5, and 32 μg/mL, respectively).
Z-Arg-Arg-βNA acetate is a sensitive dipeptide substrate of the protease Cathepsin B and resistant to proteases H and L. Z-Arg-Arg-βNA acetate can serve as an important tool for distinguishing non-Cathepsin B type proteins .
KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .
OV-1, sheep is an alpha-helical antimicrobial ovispirin peptide derived from SMAP29 peptide (sheep), which inhibits several antibiotic-resistant bacterial strains including mucoid and nonmucoid Pseudomonas aeruginosa .
Amp1EP9 is an antimicrobial peptide. Amp1EP9 is a powerful tool for developing potent and nontoxic antimicrobial agents. Amp1EP9 has the potential for the research of multidrug-resistant bacterial infections .
EC-1456 is a folate-tubulysin conjugate with significant anti-proliferative activity against FR-positive tumors, including models which were anticancer drug resistant. EC-1456 can be utilized in cancer research .
PL-3994 is a natriuretic peptide receptor-A (NPR-A) agonist that is resistant to neutral endopeptidase and acts as a bronchodilator. PL-3994 produces concentration-dependent relaxation of pre-contracted guinea-pig trachea with an IC50 value of 42.7 nM .
Clovibactin TFA is the TFA salt form of Clovibactin (HY-P10027). Clovibactin TFA is an antibiotic for drug-resistant bacterial pathogens without detectable resistance. Clovibactin TFA inihibits cell wall synthesis by targeting pyrophosphate of peptidoglycan precursors .
CRAMP (1-39) is an antimicrobial peptide. CRAMP (1-39) has shown potent bactericidal effects against multiple strains of Neisseria meningitidis in vitro. CRAMP (1-39) can be used to study drug-resistant bacterial infections .
Lynronne-2 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including
MDR strains (MIC: 32-256 μg/mL for methicillin-resistant MRSA strains). Lynronne-2 is also effective against P. aeruginosa infection
Lynronne-3 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including
MDR strains (MIC: 32-128 μg/mL for methicillin-resistant MRSA strains). Lynronne-3 is also effective against P. aeruginosa infection
L-K6L9 shows antimicrobial and antibiofilm activities against P. aeruginosa from cystic fibrosis patients. L-K6L9 is stable and resistant to degradation by cystic fibrosis sputum proteases and will not induce bacterial resistance .
D-K6L9 shows antimicrobial and antibiofilm activities against P. aeruginosa from cystic fibrosis patients. D-K6L9 is stable and resistant to degradation by cystic fibrosis sputum proteases and will not induce bacterial resistance .
Jingzhaotoxin-V is a peptide that inhibits potassium currents in Xenopus laevis oocytes with an IC50 value of 604.2 nM. Jingzhaotoxin-V also inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 and 30.2 nM, respectively .
Jingzhaotoxin-34, a 35-residue polypeptide, is a neurotoxin. Jingzhaotoxin-34 inhibits tetrodotoxin-sensitive (TTX-S) sodium currents (IC50 of ~85 nM) while having no significant effects on tetrodotoxin-resistant (TTX-R) sodium currents on rat dorsal root ganglion neurons .
Jingzhaotoxin-II, a 32 amino acid residues including two acidic and two basic residues, is a neurotoxin. Jingzhaotoxin-II inhibits voltage-gated sodium channels (VGSC) that significantly slows rapid inactivation of TTX-resistant (TTX-R) VGSC on cardiac myocytes with the IC50 of 0.26 μM .
RG33 Peptide is a diabetes inhibitor that significantly improves glucose clearance in insulin-resistant mice. RG33 Peptide effectively solubilizes lipid vesicles and promotes cholesterol efflux in cultured macrophages. RG33 Peptide is used in research into type 2 diabetes (T2D) .
MDP1, a Melittin-derived peptide, alters the integrity of both Gram-positive and Gram-negative bacterial membranes and kills the bacteria via membrane damages. MDP1 has a high-antibacterial activity against multidrug resistant (MDR) and reference strains of S. aureus, E. coli, and P. aeruginosa .
MDP1 acetate, a Melittin-derived peptide, alters the integrity of both Gram-positive and Gram-negative bacterial membranes and kills the bacteria via membrane damages. MDP1 acetate has a high-antibacterial activity against multidrug resistant (MDR) and reference strains of S. aureus, E. coli, and P. aeruginosa .
Fmoc-D-homoArg(Et)2-OH (hydrochloride) is a Fmoc-protected derivative of D-Homoarginine (HArg) that renders peptides and proteins resistant to proteolysis by trypsin. Fmoc-D-homoArg(Et)2-OH (hydrochloride) can be used as a cleavable ADC linker to synthesize antibody-drug conjugates (ADCs) .
KLA seq acetate is a cell membrane-penetrating α-helical amphipathic model peptide. KLA seq acetate conjugates peptide nucleic acids (PNAs) for delivery to mammalian cells. KLA seq acetate covalently links targeted mRNA and fluorescein to form a delivery system that has low re-export and is less resistant to serum effects .
Tet-20 is a biological active peptide. (Tet-20, is a synthetic cathelicidin-derived peptide. It was tested as infection-resistant coating for medical devices. When tethered on an implant surface Tet-20 exhibited broad antimicrobial activities both in vivo and in vitro. It can stop biofilm formation and appears to be non-toxic to eukaryotic cells)
Urumin has antiviral activity against the human influenza A virus. Urumin inhibits the growth of PR8 influenza virus (IC50: 3.8 μM). Urumin targets the conserved stalk of H1 hemagglutini, and is effective at neutralizing drug-resistant H1 influenza viruses. Urumin protects naive mice from lethal influenza infection .
BING is an antimicrobial peptide that can be isolated from Japanese medaka fish. BING shows a broad-spectrum toxicity against pathogenic bacteria including drug-resistant strains. BING induces a deregulation of periplasmic peptidyl-prolyl isomerases in gram-negative bacteria, and reduces the RNA level of cpxR, which plays a crucial role in the development of antimicrobial resistance .
Hp1404 is a novel cationic antimicrobial peptide. Hp1404 has specific inhibitory activity 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 .
Lynronne-1 is an antimicrobial peptide. Lynronne-1 is active against Gram-positive bacterials, including MDR strains (MIC: 8-32 μg/mL for methicillin-resistant MRSA strains). Lynronne-1 reduces the bacterial load in MRSA infected wound murine model. Lynronne-1 is also effective against P. aeruginosa infection .
Jingzhaotoxin-IX, a C-terminally amidated peptide composed of 35 amino acid residues, is a neurotoxin. Jingzhaotoxin-IX inhibits voltage-gated sodium channels (both tetrodotoxin-resistant and tetrodotoxin-sensitive isoforms) and Kv2.1 channel. Jingzhaotoxin-IX has no effect on delayed rectifier potassium channel Kv1.1, 1.2 and 1.3 .
Polymyxin B2 is a polypeptide antibiotic that has antibacterial activity, particularly against gram-negative bacteria. Polymyxin B2 kills the bacteria by binding to lipopolysaccharide molecules on the bacterial cell membrane, disrupting the integrity of the cell membrane and causing the cell contents to leak. Polymyxin B2 can be used in antibiotic development and treatment of drug-resistant strains .
SKF 106760 is a potent platelet fibrin receptor (glycoprotein IIb/IIIa) antagonist with significant antiplatelet and antithrombotic activities. SKF 106760 inhibits platelet aggregation in dogs in vitro and prevents thrombus formation in stenotic carotid arteries. SKF 106760 has also shown elimination effects against aspirin-resistant thrombi that develop in the setting of high-grade stenosis .
SPSB2-iNOS inhibitory cyclic peptide-2 (Compound CP2) is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 21 nM. SPSB2-iNOS inhibitory cyclic peptide-2 is reduction-resistant and oxidatively stable .
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistantGram-negative bacterial infections treatment .
Terlipressin diacetate is a vasopressin analogue with potent vasoactive properties. Terlipressin diacetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin diacetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin diacetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research .
SPR741 acetate (NAB741 acetate) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 acetate increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 acetate inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 acetate .
SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 .
Jingzhaotoxin-V, a 29-residue polypeptide, is derived from the venom of the spider Chilobrachys jingzhao. Jingzhaotoxin-V inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC50 values of 27.6 nM and 30.2 nM, respectively. Jingzhaotoxin-V also inhibits Kv4.2 potassium currents expressed in Xenpus Laevis oocytes (IC50 of 604.2 nM) .
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
c[Arg-Arg-Arg-Arg-Nal-Nal-Nal] (Compound 9C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 25 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively .
SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 TFA increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 TFA inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 TFA .
Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively .
c[Arg-Arg-Arg-Arg-Dip-Dip-Dip] (Compound 8C) shows broad-spectrum activity against drug-resistant Gram-positive and Gram-negative bacteria, with MICs of 3.1, 3,1, 12.5, and 12.5 μg/mL for MRSA (ATCC BAA-1556), S. aureus (ATCC 29213), P. aeruginosa (ATCC 27883), and E. coli (ATCC 25922), respectively .
AC3-I, myristoylated is a biological active peptide. (This is a myristoylated form of Autocamtide-3-Derived Inhibitory Peptide (AC3-I), a highly specific inhibitor of Calmodulin-Dependent Protein Kinase ll (CaMKII) that is resistant to proteolysis. AC3-I is derived from Autocamtide-3, a substrate for CaMKII, with the Thr-9 phosphorylation site substituted with Ala.)
BQ7876 is a probe targeting prostate-specific membrane antigen (PSMA) that contains a DOTA chelator. BQ7876, after being radiolabeled with radionuclide (177Lu), functions in both radionuclide imaging and tumor cell destruction by specifically binding to PSMA. BQ7876 shows potential for research in the field of metastatic castration-resistant prostate cancer (mCRPC) . BQ7876 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
PSMα3 is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 penetrates and modulates human monocyte-derived DCs by altering the TLR2- or TLR4-induced maturation, inhibiting pro- and anti-inflammatory cytokine production and reducing antigen uptake. PSMα3 is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA) .
K11 is an antimicrobial peptide. K11 is active against MDR/XDR K. pneumoniae isolates (MIC: 8-512 μg/mL), and inhibits bacterial biofilm formation. K11 can act synergistically with antibiotics (Chloramphenicol (HY-B0239), Meropenem (HY-13678), Rifampicin (HY-B0272), etc.) against drug-resistantK. pneumoniae. K11 has high thermal and wide pH stability .
Omiganan pentahydrochloride is a cationic peptide compound with a broad antibacterial profile. Omiganan pentahydrochloride is capable of inhibiting a variety of bacteria, including yeast, and is active against both gram-positive and gram-negative bacteria. Omiganan pentahydrochloride is able to interact with the bacterial cell membrane, causing the destruction of the cell membrane and the death of the bacteria. Omiganan pentahydrochloride can be used for the study of antimicrobial activity against pathogens commonly associated with catheter-associated infections, including strains with drug-resistant phenotypes .
Pantinin-2 is a cysteine-free toxic peptide found in the emperor scorpion (paninus imperator). Pantinin-2 has high activity against Gram-positive bacteria but weak activity against Gram-negative bacteria. Pantinin-2 also exhibits activity against Candida tropicalis and has relatively mild hemolytic activity against human erythrocytes. Pantinin-2 can be used in the development of antimicrobial drugs for drug-resistant pathogens .
SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
PSMα3 TFA is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 TFA penetrates and modulates human monocyte-derived DCs by altering the TLR2- or TLR4-induced maturation, inhibiting pro- and anti-inflammatory cytokine production and reducing antigen uptake. PSMα3 TFA is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA) .
Albiglutide fragment (GLP-1 (7-36) analog) TFA is an active fragment of Albiglutide (7-36) and a glucagon-like peptide-1 (GLP-1) analog (a long-acting GLP-1 receptor agonist). Albiglutide is produced by the fusion of DPP-4 resistant GLP-1 dimer with the human albumin gene. Moreover, Albiglutide fragment TFA significantly reduces glycosylated hemoglobin (A1C) and is used in type 2 diabetes (T2D) studies .
Albiglutide fragment (GLP-1 (7-36) analog) is an active fragment of Albiglutide (7-36) and a glucagon-like peptide-1 (GLP-1) analog (a long-acting GLP-1 receptor agonist). Albiglutide is produced by the fusion of DPP-4 resistant GLP-1 dimer with the human albumin gene. Moreover, Albiglutide fragment significantly reduces glycosylated hemoglobin (A1C) and is used in type 2 diabetes (T2D) studies .
SMAP-18 is a biological active peptide. (SMAP-18 is a 18-amino acid residue peptide amide which is a truncated form of SMAP-29. Sheep myeloid antimicrobial peptide-29 (SMAP-29) displays extremely high antimicrobial activity against Pseudomonas strains, other Gram-negative bacteria, and multidrug-resistant pathogens. SMAP-18 displays much higher cell selectivity as compared to parental SMAP-29 because of its decreased hemolytic activity and retained antimicrobial activity.)
R892 is a selective and efficient bradyKinin B1 receptor antagonist with significant antagonistic activity. The pA2 values of R892 in human and rabbit B1 receptors are 8.8 and 8.6 respectively, indicating its strong anti-activity at these receptors. R892 exhibits selectivity with ID50 values of 2.8 nM and >600 nM for B1 and B2 receptors, respectively, and has no endogenous agonist activity. R892 is resistant to aminopeptidase and kininase II (ACE) degradation and exhibits metabolic stability .
Teduglutide TFA is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide TFA can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide TFA can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis .
SPSB2-iNOS inhibitory cyclic peptide-2 TFA is the TFA salt form of SPSB2-iNOS inhibitory cyclic peptide-2 (HY-P10384). SPSB2-iNOS inhibitory cyclic peptide-2 TFA is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 21 nM. SPSB2-iNOS inhibitory cyclic peptide-2 TFA is reduction-resistant and oxidatively stable .
NDI-Lyso is a lysosome-targeted anticancer agent that induces the formation of rigid long fibers in cancer cell lysosomes through an enzyme-instructed self-assembly (EISA) mechanism catalyzed by cathepsin B. This process triggers lysosomal swelling, membrane permeabilization (LMP), and membrane disruption, ultimately leading to cancer cell apoptosis via a non-classical caspase-independent pathway. NDI-Lyso exhibits significant selective anticancer activity in various cancer cell lines and drug-resistant cancer cells (IC50 ~10 μM) while showing low toxicity to normal cells (IC50 > 60 μM) .
SPSB2-iNOS inhibitory cyclic peptide-1 TFA is the TFA salt form of SPSB2-iNOS inhibitory cyclic peptide-1(HY-P10383). SPSB2-iNOS inhibitory cyclic peptide-1 is an inhibitor for the interaction of SPRY domain and SOCS-box protein 2 (SPSB2) and iNOS, through binding SPSB2 on iNOS site with KD of 4.4 nM. SPSB2-iNOS inhibitory cyclic peptide-1 is resistant to the proteases pepsin, trypsin and α-chymotrypsin. SPSB2-iNOS inhibitory cyclic peptide-1 is stable in human plasma and in oxidative environment .
Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
Pelgifatamab (BAY-2315497) is a prostate-specific membrane antigen (PSMA) antibody. Pelgifatamab can be covalently linked to a binding moiety of 225Ac and used for metastatic castration-resistant prostate cancer (mCRPC) research .
Upifitamab is an ADC Antibody (a naked antibody of upifitamab rilsodotin), which can be used for antibody-coupled agent (ADC) synthesis. Upifitamab rilsodotin is an ADC targeting NaPi2b and is used in ovarian cancer research, particularly in platinum-resistant recurrent ovarian cancer .
Rilotumumab (AMG 102) is an anti-HGF (anti-hepatocyte growth factor) monoclonal antibody, inhibits HGF/MET-driven signaling. Rilotumumab shows anti-tumor activity, and can be used in castration-resistant prostate cancer (CRPC) and solid tumor research .
Pasotuxizumab (BAY 2010112) is a PSMA and CD3 bispecific T-cell engager (BiTE). Pasotuxizumab binds to CD3 and PSMA with KDs of 9.4 nM and 47.0 nM for human CD3 and PSMA. Pasotuxizumab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
Bamlanivimab (Anti-Human SARS-CoV-2) is the first COVID-19 monoclonal antibody (mAb) to be granted Emergency Use Authorization (EUA) in November 2020 by the U.S. Food and agent Administration (FDA). However, Bamlanivimab is withdrawn in April 2021 following the rise of SARS-CoV-2 virus variants resistant to Bamlanivimab .
Lorigerlimab (MGD019) is a bispecific IgG4 dual-affinity re-targeting antibody (DART). Lorigerlimab can block PD-1 and CTLA-4, and improves T-cell responses. Lorigerlimab can be used for research of metastatic castration-resistant prostate cancer (mCRPC) .
Pristinamycin, produced by Streptomyces pristinaespiralis, is an orally active streptogramin-like antibiotic consisting of two chemically unrelated components: Pristinamycin I (PI) and Pristinamycin II (PII). Pristinamycin is highly active against many antibiotic-resistant pathogens, particularly Gram-positive bacteria, including Methicillin-resistantStaphylococcus aureus (MRSA), Vancomycin-resistantS. aureus (VRSA) and Enterococcus faecium (VREF) .
Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent androgen receptor (AR) inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
Fosfomycin (MK-0955) sodium is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis. Fosfomycin sodium shows both in vivo and in vitro activity against a wide range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria .
Piperolactam A is a natural product that can be isolated from root of Piper betle. Piperolactam A exhibits promising leishmanicidal action against wild type and drug resistant strains of Leishmania donovani .
Lupeol (Standard) is the analytical standard of Lupeol. This product is intended for research and analytical applications. Lupeol (Clerodol; Monogynol B; Fagarasterol) is an active pentacyclic?triterpenoid, has anti-oxidant, anti-mutagenic, anti-tumor and anti-inflammatory activity. Lupeol is a potent?androgen receptor (AR)?inhibitor and can be used for cancer research, especially prostate cancer of androgen-dependent phenotype (ADPC) and castration resistant phenotype (CRPC) .
Bottromycin A2 is a natural antibiotic. Bottromycin A2 is active against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE) .
Collinin is a anti-tubercular agent, it can be isolated from leaves of Z. schinifolium. Collinin has an excellent anti-tuberculosis effect against multidrug-resistant (MDR), extensively drug-resistant (XDR) strains .
BE-12406B is an antitumor agent that can be found in the culture broth of a streptomycete. BE-12406B can inhibit the growth of Vincristine (HY-N0488)-resistant or Doxorubicin (HY-15142A)-resistant P388 murine leukemia cell lines as well as their parent sensitive cell line .
Albocycline (Ingramycin) is a macrolide antibiotic, which exhibits antibacterial activities against methicillin-resistantStaphylococcus aureus (MRSA), Vancomycin (HY-B0671)-intermediate (VISA), and Vancomycin (HY-B0671)-resistantS. aureus (VRSA) strains with MICs ranging from 0.5 to 1.0 μg/mL. Albocycline exhibits no toxicity to human cells at concentration of ≤64 μg/mL .
Salvinolone is active against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE). Salvinolone shows cytotoxic activity with an IC50 of 47.6 μM against the HL-60 tumor cell line for 72 h .
BE-10988 is a DNA topoisomerase inhibitor. BE-10988 inhibits the growth of Doxorubicin (HY-15142A)-resistant and vincristine-resistant P388 mouse leukemia cell lines by increasing the formation of DNA topoisomerase complexes .
Streptothricin F is a bactericidal antibiotic. Streptothricin F interacts with the 30S subunit of 70S ribosome. Streptothricin F shows rapid, bactericidal activity against highly drug-resistant, carbapenem-resistantEnterobacterales (CRE) (MIC50 and MIC90: 2 and 4 μM, respectively) and Acinetobacter baumannii .
Cephalochromin is an antibiotic and an inhibitor for bacterial fatty acid synthase (FabI). Cephalochromin inhibits FabI of Staphylococcus aureus and Escherichia coli with IC50 of 1.9 and 1.8 μM. Cephalochromin inhibits gram-positive methicillin-resistantS. aureus (MRSA) and quinolone-resistantS. aureus (QRSA), with MIC of 2-8 µg/mL .
6-C-Methylquercetin-3,4'-dimethyl etheris a flavonol derivative isolated from the leaves of Bauhinia thonningii Schum. 6-C-Methylquercetin-3,4'-dimethyl ether has antibacterial activity against Gram-negative multidrug-resistant bacteria and against methicillin-resistant Staphylococcus aureus (MRSA) strains .
Loganetin is a non-toxic natural product that may be applied in the antibacterial agent development for treating multidrug-resistant Gram negative infections.
Dunnianol is a natural sesqui-neoligan with moderate antibacterial activity. Dunnianol inhibits Staphylococcus aureus and methicillin-resistantStaphylococcus aureus (MRSA).
Piperafizine B exhibits slightly cytotoxicity in moser cells, P388 cells and Vincristine (VCR) (HY-N0488)-resistant P388 cells (IC50s is 23.8, 22.6 and 23.7 μg/mL, respectively). Piperafizine B exhibits synergistic effects with Vincristine, enhances the VCR-induced cytotoxicity and ameliorates the leukemia in mouse model .
2-Hydroxymethyl-3-hydroxyanthraquinone is an antiosteoporotic compound that inhibits osteoclastic tartrate-resistant acid phosphatase (TRAP) activity .
Kalimantacin A is a potent antibiotic. Kalimantacin A shows antibacterial activity against staphylococcus including methicillin-resistantstaphylococcus aureus (MRSA) .
Dactylocycline A is a tetracycline derivative with activity against some tetracycline-resistant microorganisms. Dactylocycline A is produced by fermentation of Dactylosporangium sp. and was found to be the most abundant glycoside in the initial fermentation. Dactylocycline A is acid-sensitive and readily hydrolyzes to the common sugar-free core substance dactylocyclinone. Although the sugar-free core has cross-resistance with tetracycline, Dactylocycline A exhibits activity against some tetracycline-resistant microorganisms .
Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer that effectively suppresses castration resistant prostate cancer cell proliferation and invasion.
Malacidin A is the calcium-dependent antibiotic (CDAs). Malacidin A is highly active against many antibiotic-resistant pathogens, particularly Gram-positive bacteria .
Daurinoline is an alkaloid that can be isolated from the roots of Menispermum dauricum. Daurinoline may be a potential anti-tumor agent or chemosensitizer for chemo-resistant NSCLC research .
Sperabillin C is an antibacterial antibiotic with activity against both Gram-negative and Gram-positive bacteria, including resistant strains of Pseudomonas aeruginosa and Staphylococcus aureus .
(3R)-7,4’-Dihydrohomoisoflavanone is a natural product with antibacterial activities against S. aureus and methicillin-resistantStaphylococcus aureus (MRSA) .
Gochnatiolide A is a dimeric sesquiterpene that can be found in Ainsliaea henryi. Gochnatiolide A exhibits antiproliferative activity against the kidney, melanoma, ovarian-resistant and glioma cell lines .
Artemether (Standard) is the analytical standard of Artemether. This product is intended for research and analytical applications. Artemether is an anti-malarial compound that targets drug-resistant strains of falciparum malaria .
Licoricone is an flavonoid extracted from licorice, exhibits anti-helicobacter pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains .
Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitory activity toward methicillin-resistant Staphylococcus aureus (MRSA) .
Pancixanthone A is a xanthone that can be isolated from Garcinia vieillardii. Pancixanthone A has antimalarial activity against chloroquino-resistant strains of Plasmodium falciparum with an IC50 of 1.6 μg/mL .
Isocudraniaxanthone A is a xanthone that can be isolated from Garcinia vieillardii. Isocudraniaxanthone A has antimalarial activity against chloroquino-resistant strains of Plasmodium falciparum with an IC50 of 2.3 μg/mL .
Dehydrorotenone is a rotenone analog that is resistant to alkali decomposition. When treated with alkaline solution or alkaline solution containing zinc, dehydrorotenone can absorb 2 molecules of water and convert into acid solution.
Aldecalmycin is an antibiotic showing antimicrobial activities against Gram-positive bacteria including methicillin-resistantStaphylococcus aureus (MRSA) with MICs values of 6.25-25 μg/mL .
Andrastin A meroterpenoid compound, is a farnesyltransferase inhibitor. Andrastin A inhibits the efflux of anticancer compounds from multidrug-resistant cancer cells. Andrastin A can be isolated from Penicillium species .
Antibiotic SF-2132 is a peptide antibiotic identified in Nocardiopsis sp., which exhibits inhibitory activity against β-lactam antibiotic-resistant strains, such as Pseudomonas and Escherichia .
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .
Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells .
Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
Cyslabdan ((+)-Cyslabdan) is a novel compound with the potential to enhance the activity of imipenem against methicillin-resistant Staphylococcus aureus. Cyslabdan exerts its antibacterial effect by inhibiting the synthesis of pentapeptide cross-links .
(-)-Heraclenol is a derivative of furocoumarin isolated from Ducrosia anethifolia. (-)-Heraclenol shows antiproliferative and cytotoxic activities on cancer cell lines .
7-Oxo-ganoderic acid Z, a terpenoid, is a nature product that could be isolated from Resina Commiphora. 7-Oxo-ganoderic acid Z has Anti-Mycobacterium tuberculosis activity .
Arenobufagin is a natural bufadienolide from toad venom; has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells.
Ascr#7, an ascaroside, is a hormone of nematodes. Ascr#7 is expressed during nematode development. Ascarosides can induce formation of long-lived and highly stress resistant dauer larvae .
Imperialine 3-β-D-glucoside is the glycoside of Imperialine. Imperialine 3-β-D-glucoside may exhibit anti-tumor properties against multi-agent resistant tumor cells .
Scholaricine (compound 13 ) is an alkaloid isolated from the leaf and stem-bark extracts of Alstonia spatulata. Scholaricine reverse multidrug resistance in vincristine-resistant KB cells with an IC50 value of 13.35 μM .
(-)-Tylophorine ((-)-(R)-Tylophorine) is a potent cytotoxic agent with activity against both drug-sensitive and multidrug-resistant cancer cell lines. (-)-Tylophorine has been explored in biomedical research for its anticancer applications .
Nodusmicin is a macrolide antibiotic against antibiotic-susceptible and -resistantS. aureus with MIC values of 125, 250 and 250 μg/mL for UC-76, UC-6685, and UC-6690 strains, respectively .
Adefovir dipivoxil, an adenosine analogue, is an oral proagent of the nucleoside reverse transcriptase inhibitor Adefovir. Adefovir dipivoxil inhibits both the wild type and HBV Lamivudine-resistant strains . Adefovir dipivoxil shows anti-orthopoxvirus activity.
Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistantstaphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC50 value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity .
Carpachromene is a potent α-glucosidase enzyme inhibitor. Carpachromene ameliorates insulin resistance in HepG2 cells via modulating IR/IRS1/PI3k/Akt/GSK3/FoxO1 pathway .
(-)-Corynoxidine is an acetylcholinesterase inhibitor with an IC50 value of 89.0 μM, isolated from the aerial parts of Corydalis speciosa .
(-)-Corynoxidine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus strains in different degrees .
Villalstonine is a bisindole alkaloid with various biological activities including anticancer, antimalarial, and antiamoebic activities. Villalstonine exhibits potent antiplasmodial activity against the multidrug-resistant K1 strain of P. falciparum with an IC50 value of 0.27 μM .
D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research .
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistantPlasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys .
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 .
Continentalic acid from Aralia continentalis has minimum inhibitory concentrations (MICs) of approximately 8-16 µg/mL against S. aureus, including the Methicillin (HY-121544) susceptible Staphylococcus aureus (MSSA) and Methicillin-resistantStaphylococcus aureus (MRSA) standard strains .
8-Epidiosbulbin E acetate, a furanoid, is abundant in Dioscorea bulbifera L.. 8-Epidiosbulbin E acetate exhibits broad-spectrum plasmid-curing activity against multidrug-resistant (MDR) bacteria. 8-Epidiosbulbin E acetate induces liver injury in mice .
Cheilanthifoline, an alkaloid, is isolated from Corydalis calliantha. Cheilanthifoline exhibits antiplasmodial activities against Plasmodium falciparum, with IC50s of 0.90 μg/mL and 1.22 μg/mL for wild type (TM4) and multidrug resistant (K1) strains, respectively .
1-Methoxyphaseollidin, a flavonoid compound, is a lysoPAF acetyltransferase inhibitor, with an IC50 of 48 μM. 1-Methoxyphaseollidin exhibits anti-H.pylori activity against the CLAR and AMOX-resistant strain as well as four CLAR (AMOX)-sensitive strains .
Kigamicin C is an anti-tumor antibiotic that selectively kills pancreatic cancer PANC-1 cells only in nutrient-poor conditions. Kigamicin C has antimicrobial activity against Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA) .
Kopsoffinol, a bisindole alkaloid, shows in vitro growth inhibitory activity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells .
9-Oxonerolidol is a farnesane-type sesquiterpenoid with anti-pathogens activity. 9-Oxonerolidol can be isolated from Chiliadenus lopadusanus. 9-Oxonerolidol acts as a post-infectional inhibitor from plants, and inhibits Gram+ and Gram? bacteria resistant to the antibiotic .
Niranthin (Standard) is the analytical standard of Niranthin. This product is intended for research and analytical applications. Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
Wulignan A1 is isolated from the stems of Schisandra henryi. Wulignan A1 exhibits anti-influenza virus H1N1 and H1N1-TR (a Tamiflu agent resistant virus strain) activities .
Jatrophane 5 is a natural product of Jatropha carcas L. Jatrophane 5 has powerful inhibition of P-gp, higher than R(+)-verapamil (HY-14275) and Tariquidar (HY-10550) in colorectal multi-drug resistant cells (DLD1-TxR) .
Laburnetin is a kind of isoflavone antibacterial agent. Laburnetin has antibacterial activity against fungi and S. vesicarium. Laburnetin intensifies the susceptibility of Methicillin (HY-121544) resistantStaphylococcus aureus (MRSA) strains to Methicillin. Laburnetin can be used to control pests of cultivated species .
β-Yohimbine (Amsonin) is an indole alkaloid that can be isolated from Aspidosperma ulei Markgr. β-Yohimbine shows antiplasmodial activity against the Chloroquine (HY-17589A)-resistant Fc M29-Cameroon strain (IC50: > 1 μg/mL) .
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.
Novobiocin (Albamycin) sodium is a potent and orally active antibiotic. Novobiocin sodium also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin sodium has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin sodium shows anti-orthopoxvirus activity .
Seconeolitsine, an antibiotic, and is an inhibitor of targeting topoisomerase I (TopA). Seconeolitsine also is a new antimicrobial agent that can inhibit S. pneumoniae growth. Seconeolitsine can inhibit TopA relaxation activity with an IC50 value of 17 μM. Seconeolitsine can be used for the research of S. pneumoniae infections resistant to other antibiotics .
Teicoplanin is a glycopeptide antibiotic indicated for use in serious infections caused by Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus and Enterococcus aureus.Teicoplanin shows antiviral activity for HIV-1, SARS-CoV1 and SARS-CoV2. Teicoplanin sodium shows anti-MRSA activity .
Allicin (diallyl thiosulfinate) is isolated from garlic including Diallyl monosulfide, Diallyl disulfide, Diallyl trisulfide, Diallyl tetrasulfide, and Methyl allyl disulphide etc. They accounts for 98% of the extract. Allicin (diallyl thiosulfinate) has highly potent antimicrobial activity, and inhibits growth of a variety of microorganisms, among them antibiotic-resistant strains .
Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.
Colistin (Polymyxin E) is an orally active polypeptide antibiotic. Colistin has excellent activity against various Gram-negative rod-shaped bacteria, including multidrug-resistantPseudomonas aeruginosa, Acinetobacter baumannii and Klebsiella pneumoniae. Colistin is associated with nephrotoxicity. Colistin can be used for the research of infections caused by Gram-negative bacilli .
Teicoplanin sodium is a glycopeptide antibiotic indicated for use in serious infections caused by Gram-positive bacteria, including Methicillin-resistant Staphylococcus aureus and Enterococcus aureus.Teicoplanin sodium shows antiviral activity for HIV-1, SARS-CoV1 and SARS-CoV2. Teicoplanin sodium shows anti-MRSA activity .
Chimaphilin is an IGF-1R inhibitor (IC50: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola .
Adefovir dipivoxil (Standard) is the analytical standard of Adefovir dipivoxil. This product is intended for research and analytical applications. Adefovir dipivoxil, an adenosine analogue, is an oral proagent of the nucleoside reverse transcriptase inhibitor Adefovir. Adefovir dipivoxil inhibits both the wild type and HBV Lamivudine-resistant strains . Adefovir dipivoxil shows anti-orthopoxvirus activity.
Nidulin (Methylustin) is a depsidone isolated from a marine fungus Aspergillus unguis. Nidulin shows antifungal and antibacterial against pathogenetic strains, Pseudomonas aeruginosa, Methicillin-resistant Staphylococcus aureus and Candida albicans with inhibition zones of 9.5 mm, 9.0 mm and 9.0 mm, respectively. Nidulin exhibits potent larvicidality against brine shrimp .
L-Valine (Valine) is a new nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
Methyl oleate is a fatty acid methyl ester (FAME) with anti-extended spectrum β-Lactamase (ESBL) potential, anticancer and antibacterial activities. Methyl oleate substantially improves the antioxidation ability but markedly impaired the antiwear capacity of zinc dialkyldithiophosphate (ZDDP). Methyl oleate is promising for research of ESBL producing multi drug resistant (MDR) pathogens .
D-Cycloserine (Standard) is the analytical standard of D-Cycloserine. This product is intended for research and analytical applications. D-Cycloserine is an antibiotic which targets sequential bacterial cell wall peptidoglycan biosynthesis enzymes. D-Cycloserine is a partial NMDA agonist that can improve cognitive functions. D-Cycloserine can be used for multidrug-resistant tuberculosis research .
Fortimicin C is an antibiotic, which can be isolated from Micromonospora olivoasterospora. Fortimicin C exhibits broad-spectrum antibacterial activity, inhibits Escherichia coli, Staphylococcus aureus, Bacillus subtilis, Klebsiella pneumoniae, Salmonella typhosa and Serratia marcescens, with MICs of 0.16-0.64 μg/mL. Fortimicin C is resistant against aminoglycoside inactivating enzymes .
Continentalic acid (Standard) is the analytical standard of Continentalic acid. This product is intended for research and analytical applications. Continentalic acid from Aralia continentalis has minimum inhibitory concentrations (MICs) of approximately 8-16 μg/mL against S. aureus, including the Methicillin (HY-121544) susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant Staphylococcus aureus (MRSA) standard strains .
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 inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistantN. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
Capreomycin sulfate is a macrocyclic peptide antibiotic that inhibits phenylalanine synthesis in mycobacterial ribosomal translation. Capreomycin sulfate has anti-amyloidogenic and pro-fibrinolytic activities, reducing amyloid-induced cytotoxicity by inhibiting the occurrence of amyloid fibrillation. Capreomycin sulfate can be used in the study of multidrug-resistant tuberculosis, type 2 diabetes, Alzheimer's disease and Parkinson's disease .
Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity . 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice .
Polymyxin B1 is a potent antimicrobial lipopeptide first derived from Bacilus polymyxa. Polymyxin B1 is the major component in Polymyxin B (HY-A0248). Polymyxin B1 can induce lysis of bacterial cells through interaction with their membranes. Polymyxin B1 has the potential for multidrug-resistantGram-negative bacterial infections treatment .
Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity .
Artocarpesin is a flavonoid compound. Artocarpesin has inhibitory effects on methicillin-resistantStaphylococcus aureus (MRSA). Artocarpesin inhibits the production of NO, PGE2 and ROS by inhibiting COX-2 and iNOS expression, and plays an anti-inflammatory role. In addition, Artocarpesin inhibits platelet aggregation by inhibiting cyclic nucleotides and MAPKs, which can be used in the study of cardiovascular diseases .
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-resistantStaphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH .
Tectol, isolated from Lippia sidoides, exhibits significant activity against human leukemia cell lines HL60 and CEM . Tectol is a farnesyltransferase (FTase) inhibitor with IC50s of 2.09 and 1.73 μM for human and T. brucei FTase, respectively. Tectol inhibits drug-resistant strain of P. falciparum (FcB1) with an IC50 of 3.44 μM .
Wychimicin A is a spirotetronate polyketide, can be isolated from the rare actinomycete Actinocrispum wychmicini strain MI503-AF4. Wychimicin A shows strong antibacterial activity against methicillin-resistantStaphylococcus. aureus (IC50=0.125-0.5 μg/mL) and Enterococcus. faecalis/faecium (IC50=0.125-0.25 μg/mL) .
Novobiocin (sodium) (Standard) is the analytical standard of Novobiocin (sodium). This product is intended for research and analytical applications. Novobiocin (Albamycin) sodium is a potent and orally active antibiotic. Novobiocin sodium also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin sodium has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin sodium shows anti-orthopoxvirus activity .
Pheanthine (Compound 2) is an antiplasmodial agent, that inhibits chloroquine-resistantPlasmodium falciparum K-1 (IC50 is 0.8 μM) and chloroquine-sensitive P. falciparum strain NF54 A19A (IC50 of 0.03 μM). Pheanthine exhibits low cytotoxicity in human lung fibrosblast (MRC-5, IC50 is 11.2 μM) and macrophages (PMM, IC50 is 8 μM) .
Wychimicin C is a spirotetronate polyketide, can be isolated from the rare actinomycete Actinocrispum wychmicini strain MI503-AF4. Wychimicin C shows strong antibacterial activity against methicillin-resistantStaphylococcus. aureus (IC50=0.125-0.5 μg/mL) and Enterococcus. faecalis/faecium (IC50=0.125-0.25 μg/mL) .
Tubulysin B is a highly cytotoxic peptide and potent microtubule destabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties .Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis .
Chevalone B was isolated from the ethyl acetate extract of the marine sponge-associated fungus Aspergillus similanensis. The structure of Chevalone B was confirmed by 1D and 2D NMR spectroscopy. Chevalone B showed antimicrobial activity against Gram-positive and Gram-negative bacteria, Candida albicans, and multidrug-resistant strains from the environment. Studies on Chevalone B have shown its potential value in antimicrobial applications.
Ficellomycin is a nitrogen-containing bicyclic antibiotic with strong activity against Gram-positive bacteria, including multidrug-resistant strains of Staphylococcus aureus. Ficellomycin works by inducing the formation of defective 34S DNA fragments, which interfere with the semi-conservative DNA replication process. These fragments lack the ability to integrate into larger DNA segments and eventually form a complete bacterial chromosome. Ficellomycin can be used in research for various bacterial diseases .
Virginiamycin S1 is a cyclic hexadepsipeptide antibiotic, inhibits bacterial protein synthesis at the level of aminoacyl-tRNA binding and peptide bond formation. Virginiamycin S1 belongs to the type B compounds in the streptogramin family and is produced by Streptomyces virginiae, shows a strong bactericidal activity against a wide range of Gram-positive bacteria. Virginiamycin S1 together with virginiamycin M1 is more effective in treat multidrug-resistant bacterial infections [1][2].
Vinaxanthone (SM-345431) is a potent and selective semaphorin3A, phospholipase C (PLC) and FabI inhibitor, with IC50s of 0.1-0.2 μM and 0.9 mM for semaphorin3A and FabI. Vinaxanthone inhibits the substrate (t-o-NAC thioester) and the cofactor (NADPH) with Kis of 3.1 μM and 1.0 μM, respectively. Vinaxanthone can be used to handle infections caused by multidrug-resistant pathogens .
Phomoxanthone A is a xanthone dimer, which can be isolated from Phomopsis. Phomoxanthone A exhibits antimalarial and antitubercular activities against Plasmodium falciparum (K1, multidrug-resistant strain, IC50 is 0.11 µg/mL) and Mycobacterium tuberculosis (H37Ra strain, MIC is 0.50 µg/mL). Phomoxanthone A exhibits cytotoxicity in cells KB, BC-1 and Vero, IC50 is 0.99, 0.51 and 1.4 µg/mL, respectively .
Meropenem (Standard) is the analytical standard of Meropenem. This product is intended for research and analytical applications. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
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 inhibitory activity against HBV replication .
Tubulysin D is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin D can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin D displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin D inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin E is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin E can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin E displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin E inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin C is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin C can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin C displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin C inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin F is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin F can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin F displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin F inhibits microtubule/Tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin G is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin G can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin G displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin G inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin H is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin H can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin H displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin H inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin I is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin I can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin I displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin I inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
Tubulysin M is a highly cytotoxic anti-microtubule toxin (anti-microtubule toxins) that is synthesized as an ADC cytotoxin (ADC Cytotoxin). Tubulysin M can be isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin M displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the low nanomolar range. Tubulysin M inhibits microtubule/tubulin polymerization and leads to cell cycle arrest and apoptosis .
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 . (Z)-Ligustilide is orally active, it inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .
PSMα3 is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 penetrates and modulates human monocyte-derived DCs by altering the TLR2- or TLR4-induced maturation, inhibiting pro- and anti-inflammatory cytokine production and reducing antigen uptake. PSMα3 is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA) .
Valanimycin is an antibiotic, which inhibits Escherichia coli (BE1121) through interaction with DNA. Valanimycin exhibits cytotoxicity to mouse leukemia L1210, P388/S (doxorubicin (HY-15142A)-sensitive), and P388/ADR (doxorubicin-resistant), with IC50 of 0.79, 2.65, and 1.44 μg/mL, respectively. Valanimycin exhibits antitumor efficacy against ehrlich ascites tumors or L1210 in mice .
Capreomycin (sulfate) (Standard) is the analytical standard of Capreomycin (sulfate). This product is intended for research and analytical applications. Capreomycin sulfate is a macrocyclic peptide antibiotic that inhibits phenylalanine synthesis in mycobacterial ribosomal translation. Capreomycin sulfate has anti-amyloidogenic and pro-fibrinolytic activities, reducing amyloid-induced cytotoxicity by inhibiting the occurrence of amyloid fibrillation. Capreomycin sulfate can be used in the study of multidrug-resistant tuberculosis, type 2 diabetes, Alzheimer's disease and Parkinson's disease .
L-Valine (Standard) is the analytical standard of L-Valine. This product is intended for research and analytical applications. L-Valine (Valine) is a new nonlinear semiorganic material. L-Valine standrd causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine standrd inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
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 inhibitory activity to both M. tuberculosis (sensitive and drug-resistant ) and K. pneumonia, which can be used in studies of tuberculosis and pneumonia .
7-O-Methylaloeresin A is 5-methylchromone glycoside isolated from Commiphora socotrana (Burseraceae). 7-O-Methylaloeresin A exhibits good activity against multiple agent resistant Staphylococcus aureus (NCTC 11994) and Salmonella typhimurium (ATCC 1255) with MIC values of 0.72 and 0.18 mM, respectively. 7-O-Methylaloeresin A has antioxidant activities, gives IC50 values of 0.026 mM and 0.021 mM for DPPH and 2-deoxyribose degradation assay, respectively.
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistantStaphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
Rubone, a chalcone analog, is a modulator of miR-34a. Rubone upregulates miR-34a expression in a p53 dependent manner, downregulates the downstream target Bcl-2 and Cyclin D1 expression, and suppresses hepatocellular carcinoma (HCC) growth in vivo. Rubone enhances the anticancer effect of Paclitaxel (PTX; HY-B0015) in PTX-resistant prostate cancer cell lines by reversing the expression of miR-34a downstream targets .
Manumycin A is a polyketide antibiotic and an inhibitor of thioredoxin reductase 1 (TrxR-1). Manumycin A can inhibit the growth of breast cancer cells and exert its anti-tumor activity through LC3. Manumycin A can downregulate the release of pro-inflammatory cytokines in human monocytes stimulated by TNF α, and has potential anti-inflammatory activity. Manumycin A can inhibit the Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration resistant prostate cancer cells to suppress exosome biogenesis and secretion .
4-Methylesculetin is an orally active coumarin derivative, with potent anti-oxidant and anti-inflammatory activities. 4-Methylesculetin inhibits myeloperoxidase activity. 4-Methylesculetin protects bone resorption by reducing the elevated levels of bone-joint exoglycosidases, cathepsin-D and tartrate resistant acid phosphatases. 4-Methylesculetin ameliorats the upregulated non-enzymatic inflammatory markers like TNF-α, IL-1β, IL-6, COX-2 and PGE2, which is promising for research of inflammatory diseases .
Deoxyshikonin increases the expression of VEGF-C and VEGF-A mRNA in HMVEC-dLy, promotes HIF-1α and HIF-1β subunit interaction and binds to specific DNA sequences targeted by HIF. Deoxyshikonin inhibited colorectal cancer (CRC) through the PI3K/Akt/mTOR pathway. Deoxyshikonin has proangiogenesis effect and antitumor activity. Deoxyshikonin is an antibacterial agent against methicillin-resistantS. aureus (MRSA) and S. pneumonia (MIC=17 μg/mL) .
4(1H)-Quinolinone, 1-methyl-2-(5Z)-5-undecen-1-yl- (compound 2) is a quinolone alkaloid that can be isolated from Cnidium. 4(1H)-Quinolinone, 1-methyl-2-(5Z)-5-undecen-1-yl- has methicillin-resistant Staphylococcus aureus (MRSA) activity, with MIC values of 32 μg/mL (ATCC 33591) and 16 μM/mL (ATCC 25923), respectively .
Protorubradirin is an antibiotic that can be isolated from Streptomyces achromogenes var. rubradirin together with Rubradirin. Protorubradirin has inhibitory activity 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 .
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 inhibitory activity against HBV replication .
Virginiamycin S1 (Standard) is the analytical standard of Virginiamycin S1. This product is intended for research and analytical applications. Virginiamycin S1 is a cyclic hexadepsipeptide antibiotic, inhibits bacterial protein synthesis at the level of aminoacyl-tRNA binding and peptide bond formation. Virginiamycin S1 belongs to the type B compounds in the streptogramin family and is produced by Streptomyces virginiae, shows a strong bactericidal activity against a wide range of Gram-positive bacteria. Virginiamycin S1 together with virginiamycin M1 is more effective in treat multidrug-resistant bacterial infections .
Melicopine is an alkaloid found in Z. simulans with antimalarial and anticancer activities. It exhibits inhibitory activity against chloroquine-sensitive 3D7 and chloroquine-resistant Dd2 strains of P. falciparum, with IC50 values of 29.7 and 33.7 µg/mL, respectively. Melicopine is cytotoxic to prostate cancer cells PC-3M and LNCaP (IC50 values of 47.9 and 37.8 µg/mL), but has no effect on non-cancerous HEK293 cells (IC50 greater than 100 µg/mL). Melicopine holds promise for research in anticancer and anti-infection fields .
6-(12-Tridecene-1-yl)-2,4-Dihydroxy benzoic acid (Compound 2) exhibits antibacterial activity against methicillin-resistantStaphylococcus aureus (MRSA) and Vancomycin enterococci (VRE). 6-(12-Tridecene-1-yl)-2,4-Dihydroxy benzoic acid interfers with the integrity and function of the bacterial cell membrane, and affects metabolism in MRSA. 6-(12-Tridecene-1-yl)-2,4-Dihydroxy benzoic acid exhibits anti-inflammatory and anti-infective efficacy, and promotes angiogenesis in mice .
D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells .
Isosulfazecin (iSZ) is a novel β-lactam antibiotic produced by Pseudomonas acidophilus sp., synthesized in a nutrient solution supplemented with glycerol and sodium thiosulfate under aerobic conditions in parallel with bacterial growth. It is purified by chromatography and crystallization from aqueous methanol. Physicochemical analysis determined its molecular formula to be C12H20N4O9S, showing a structure with a β-lactam ring, methoxyl and sulfonate groups. Acid hydrolysis yields L-alanine and D-glutamic acid. iSZ is a diastereomer of sulfadiazine and exhibits moderate activity against both gram-positive and gram-negative bacteria, but potent activity against bacteria resistant to β-lactam antibiotics .
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
Citreamicin alpha (LL-E 19085-alpha) is an antibiotic whose in vitro antimicrobial activity against 429 clinical isolates of Gram-positive cocci has been tested by the agar dilution method. These microorganisms included 313 strains of Staphylococci and 116 strains of Streptococci. The in vitro activity of Citreamicin alpha was compared with that of ampicillin, amoxicillin, ceftriaxone, erythromycin, and vancomycin. For Staphylococci, the MIC values of Citreamicin alpha ranged from 0.12-4.0 μg/ml, and for Streptococcus pyogenes of the genus Streptococcus, it was 0.03-0.12 μg/ml. However, enterococci were relatively resistant, requiring 2.0 μg/ml of the agent to inhibit 64% of the 62 tested strains. The in vitro activity of this antibiotic was much better than that of ampicillin, amoxicillin, ceftriaxone, and erythromycin, but comparable or slightly inferior to that of vancomycin.
Maleic Acid (Standard) is the analytical standard of Maleic Acid. This product is intended for research and analytical applications. Maleic Acid is a Glutamate Decarboxylase (GAD) inhibitor of E. coli and L. monocytogenes.
IC50 & Target: GAD .
In Vitro: The MICs of WT 10403S for the acids (e.g., Maleic Acid) are 34 mM, 25 mM, 31 mM and 30 mM which correspond to pH values prior to growth of 4.84, 5.14, 5.32 and 5.02 respectively. Of all compounds tested, Maleic Acid is the least inhibitory despite acting at a lower pH (4.84). The most acid resistant (10403S) and the weakest (EGD-e) strain are challenged with 8.6 mM and 4.3 mM of each organic acid at pH 3 and 3.3 respectively. On both strains, Maleic Acid is the most bactericidal .
D-Mannitol (Standard) is the analytical standard of D-Mannitol. This product is intended for research and analytical applications. D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells .
(6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol is an antibacterial compound. (6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol can be isolated from the roots of Atractylodes japonica. (6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol has anti-methicillin-resistantStaphylococcus aureus (MRSA) activity with MIC values of 4-32 μg/mL. (6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol can be used for the research of bacterial infection . (6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
The ACP5 protein may have a crucial role in bone resorption, particularly in the enzymatic activities involved in breaking down bone tissue. ACP5 is linked to the osteoclastic trap, which has higher affinity for nucleotide tri- and diphosphates. Understanding ACP5's mechanisms in bone resorption and its interactions with nucleotide substrates could offer insights into its role in maintaining bone health. ACP5 Protein, Mouse (HEK293, His) is the recombinant mouse-derived ACP5 protein, expressed by HEK293 , with C-His labeled tag. The total length of ACP5 Protein, Mouse (HEK293, His) is 305 a.a., with molecular weight of ~35.8-38 kDa.
The ACP5 protein actively dephosphorylates osteopontin and bone sialoprotein. Its upregulated expression in pathological conditions like Gaucher and Hodgkin diseases, hairy cell, B-cell, and T-cell leukemias suggests a potential association with these diseases. This underscores ACP5's relevance in diverse pathological states, indicating its role in modulating pathways related to bone health and hematopoietic system disorders. ACP5 Protein, Human (HEK293, His) is the recombinant human-derived ACP5 protein, expressed by HEK293 , with C-His labeled tag. The total length of ACP5 Protein, Human (HEK293, His) is 299 a.a., with molecular weight of ~35 kDa.
ATP synthase alpha chain; ATP synthase alpha chain; mitochondrial; ATP synthase subunit alpha; ATP synthase subunit alpha mitochondrial; ATP synthase; H+ transporting; mitochondrial F1 complex; alpha subunit 1; cardiac muscle; ATP synthase; H+ transporting; mitochondrial F1 complex; alpha subunit; 1; ATP synthase; H+ transporting; mitochondrial F1 complex; alpha subunit; isoform 1; cardiac muscle; ATP synthase; H+ transporting; mitochondrial F1 complex; alpha subunit; isoform 2; non-cardiac muscle-like 2; ATP sythase F1 ATPase; alpha subunit; ATP5A; Atp5a1; ATP5AL2; ATPA_HUMAN; ATPM; Epididymis secretory sperm binding protein Li 123m; hATP1; HEL-S-123m; MC5DN4; mitochondrial; Mitochondrial ATP synthetase; Mitochondrial ATP synthetase oligomycin resistant; Modifier of Min 2; Modifier of Min 2 mouse homolog; Modifier of Min 2; mouse; homolog of; MOM2; OMR; ORM; OTTHUMP00000163475
ATP5F1A is an important component of mitochondrial ATP synthase (complex V) that coordinates ATP production from ADP by utilizing the transmembrane proton gradient. As part of the F-type ATPase, the α and β subunits of ATP5F1A form the catalytic core to achieve ATP hydrolysis. ATP5F1A Protein, Human (His-SUMO) is the recombinant human-derived ATP5F1A protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag. The total length of ATP5F1A Protein, Human (His-SUMO) is 510 a.a., with molecular weight of ~71.2 kDa.
Pretomanid-d4 is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL[1][2].
Delafloxacin-d5 is deuterium labeled Delafloxacin. Delafloxacin (RX-3341; WQ-3034; ABT492) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and Klebsiella pneumonia[1].
(Rac)-Fosfomycin (benzylamine)- 13C3 is the 13C labeled Fosfomycin[1]. Fosfomycin (MK-0955) is a broad-spectrum antibiotic. Fosfomycin can cross blood-brain barrier penetrating, and irreversibly inhibits an early stage in cell wall synthesis. Fosfomycin shows anti-bacteria activity for a range of bacteria, including multidrug-resistant (MDR), extensively drug-resistant (XDR), and pan-drug-resistant (PDR) bacteria[2][3].
Epoxiconazole-d4 is the deuterium labeled Epoxiconazole (HY-119683). Epoxiconazole, a fungicide, is a demethylation inhibitor of the Ergosterol biosynthesis pathway. Epoxiconazole exhibits strong inhibitory effects on both carbendazim-resistant and phenamacril-resistant isolates, and can be used for controlling many crop diseases .
Benalaxyl-d5 is the deuterium labeled Benalaxyl (HY-121109) . Benalaxyl is a fungicide, but A. fumigatus isolates are intrinsically resistant to Benalaxyl .
Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
Spiromesifen-d9 is a deuterated labeled Spiromesifen . Spiromesifen (BSN 2060) is a broad-spectrum
tetrachloro acid derivative acaricide. Spiromesifen can interfere with lipid
biosynthesis, and has no cross-resistance to any resistant mite or whitefly
populations .
(S)-Verapamil-d7 (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells[1][2].
Bedaquiline impurity 2-d6 is deuterium labeled Bedaquiline. Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit[1]. Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis[2].
(Rac)-Bedaquiline-d6 is the deuterium labeled Bedaquiline (HY-14881) . Bedaquiline (TMC207) is a diarylquinoline agent and inhibits Mycobacterium tuberculosis (Mtb) F1FO-ATP synthase through targeting of both the c- and the ε-subunit . Bedaquiline has uncoupler activity. Bedaquiline is used for the multi-agent resistant tuberculosis .
PNU-100766-d8 is deuterated labeled Linezolid (HY-10394). Linezolid (PNU-100766) is the first member of the class of oxazolidinone synthetic antibiotic. Linezolid acts by inhibiting the initiation of bacterial protein synthesis. Linezolid is used for the treatment of serious infections caused by Gram-positive bacteria that are resistant to several other antibiotics .
Tasquinimod-d3 (ABR-215050-d3) is the deuterium labeled Tasquinimod (HY-10528). Tasquinimod is an oral antiangiogenic agent, which plays an important role in castration-resistant prostate cancer. Tasquinimod binds to the regulatory Zn 2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor .
Meropenem-d6 is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL)[1][2].
Sulfadoxine-d3 is a deuterium labeled Sulfadoxine (HY-B0439). Sulfadoxine is a sulfonamide that is used, usually in combination with Pyrimethamine (HY-18062), for multidrug-resistant Plasmodium falciparum and P. vivax inhibition. Unlike PYR, Sulfadoxine has no impact on HIV replication or MT-2 cell cycle progression. But also Sulfadoxine exhibits suppression on respiratory, and urinary tract infections[1][2][3][4].
Tipranavir-d7 is deuterated labeled Tipranavir (HY-15148). Tipranavir (PNU-140690) inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-protease inhibitor (PI)-resistant HIV-1 isolates with IC50s of 66-410 nM . Tipranavir inhibits SARS-CoV-2 3CL pro activity .
Pentamidine-d4 (dihydrochloride) is the deuterium labeled Pentamidine dihydrochloride. Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities[1][2][3][4].
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 .
Meropenem-d6-1 (SM 7338-d6-1) is the deuterium labeled Meropenem. Meropenem (SM 7338) is a carbapenem antibiotic with broad-spectrum antibacterial activity. Meropenem has activity against susceptible and resistant N. gonorrhoeae (MIC value of 0.02-0.06 mg/mL), H. influenzae (MIC value of 0.03-0.12 mg/mL), and H. ducreyi (MIC value of 0.015-0.12 mg/mL) .
9-Aminoacridine-13C6 is the 13C-labeled 9-Aminoacridine(HY-B1422). 9-Aminoacridine, a fluorescent probe, acts as an indicator of pH for quantitative determination of transmembrane pH gradients (inside acidic). 9-Aminoacridine is an antimicrobial. 9-Aminoacridine exerts its antimicrobial activity by interacting with specific bacterial DNA and disrupting the proton motive force in K. pneumoniae. 9-Aminoacridine is a HIV-1 inhibitor and inhibits HIV LTR transcription highly dependent on the presence and location of the amino moiety. 9-Aminoacridine inhibits virus replication in HIV-1 infected cell lines. 9-Aminoacridine is used as a Rifampin (RIF; HY-B0272) adjuvant for the multidrug-resistantK. pneumoniae infections .
5,6-Epoxyeicosatrienoic acid-d11 (5,6-EET-d11) is deuterium labeled 5,6-Epoxyeicosatrienoic acid. 5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM. (±)5,6-Epoxyeicosatrienoic acid is provided as a mixture of the free acid and lactone .
Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains . Azvudine (hydrochloride) 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.
Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains . Azvudine 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.
AG-7404 is an inhibitor of picornaviral 3C protease, with anti-poliovirus activity (EC50=0.080-0.674 μM). AG-7404 has synergy with V-073 (HY-104074) or BTA798 (HY-106254), and fully inhibits all V-073-resistant variants . AG-7404 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Pyraclonil is a proporphyrinogen oxidase (PPO) inhibitor. Pyraclonil is a herbicide agent and is highly effective in controlling the susceptible (S) and multiple-herbicide-resistant (MHR) E. indica populations . Pyraclonil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
CN-CC-861 is a broad-spectrum antibiotic. CN-CC-861 shows antibiotic activities for susceptible and multidrug-resistant bacteria. CN-CC-861 shows potent bactericidal activity in vivo .
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, is an antiretroviral agent which is potent against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity . 4'-Ethynyl-2'-deoxyadenosine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
DMT-2'-F-iBu-G (5'-DMT-2'-F-ibu-dG) is a modified oligonucleotide. 2'-deoxy-2'-fluoro-modified oligonucleotides shows high nuclease resistant and retained exceptional binding affinity to the RNA targets .
Dmt-2'fluoro-da(bz) amidite, an uniformly modified 2'-deoxy-2'-fluoro phosphorothioate oligonucleotide, is a nuclease-resistant antisense compound with high affinity and specificity for RNA targets. Dmt-2'fluoro-da(bz) amidite is also an intermediate for 5’-DMT-3’-phosphoramidite synthesis .
Azvudine (RO-0622) hydrochloride is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine hydrochloride exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine hydrochloride inhibits NRTI-resistant viral strains . Azvudine (hydrochloride) 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.
Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC50s ranging from 0.03 to 6.92 nM) and HIV-2 (EC50s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains . Azvudine 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.
L-Valine (Valine) is a new nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
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