NI-57 is an inhibitor of bromodomain and plant homeodomain finger-containing (BRPF) famlily of proteins, with IC50s of 3.1, 46 and 140 nM for BRPF1, BRPF2 (BRD1) and BRPF3, respectively. 了解更多
Duocarmycin MA is an antibody drug conjugates (ADCs) toxin. Duocarmycin is a DNA alkylating agent that binds in the minor groove. Duocarmycin MA can be used against multi-drug resistant cell lines. 了解更多
GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM. 了解更多
SB-772077B dihydrochloride is an aminofurazan-based Rho kinase (ROCK) inhibitor with IC50s of 5.6 nM and 6 nM toward ROCK1 and ROCK2, respevtively. 了解更多
MB-07811 (VK-2809) is an orally active HepDirect prodrug of MB07344, a liver-targeted thyroid hormone receptor-β agonist. MB-07811 has cholesterol and triglycerides lowering activity. 了解更多
ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively. 了解更多
Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. 了解更多
ELX-02 sulfate (NB-124 sulfate) is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). ELX-02 sulfate is being developed as a therapy for genetic diseases caused by nonsense mutations. 了解更多
5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA. 了解更多
Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively. 了解更多
Cenerimod (ACT-334441) is a potent and orally available sphingosine 1-phosphate 1 receptor (S1P1) agonist extracted from patent WO 2016184939 A1 and WO 2011007324 A1, example 1, with an EC50 of 2.7 nM. 了解更多
Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively. 了解更多
Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
RPR107393 free base is a selective squalene synthase inhibitor, which inhibits rat liver microsomal squalene synthase with an IC50 of 0.8??0.2 nM. 了解更多
PSI-7409 is the active 5'-triphosphate metabolite of Sofosbuvir (PSI-7977). Sofosbuvir (PSI-7977) is a selective and highly active nucleotide analog inhibitor of HCV. 了解更多
Lenampicillin (hydrochloride) is the efficient prodrug of ampicillin (ABPC ) in terms of the enhancement of absorption and decrease of side effects. 了解更多
TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP. 了解更多
Demethoxydeacetoxypseudolaric acid B analog (Compound 13b) is semi-synthesized by efficient routines from Pseudolaric acid B. It has potent activities against HMEC-1, HL-60, A-549, MB-MDA-468, BEL-7402, HCT116, and Hela cells with IC50s ranging from 0.136 to 1.162 μM. 了解更多
E3 ligase Ligand 10 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 10 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins. 了解更多
GSK547 (GSK-547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer. 了解更多
ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor. ZT-12-037-01 effectively blocks oncogenic NRAS-driven melanocyte malignant transformation and melanoma growth in vitro and in vivo. 了解更多
BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCFFbxo3 catalyzed Fbxl2 ubiquitination. 了解更多
Lincomycin hydrochloride is a peptidyl transferase and protein translation inhibitor used to treat bacterial infections. It also inhibits growth of plasmodium. 了解更多
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