8 products were found matching "Cay13488-%25"!

Puromycin is a derivative of the glomerular epithelial cell toxin puromycin aminonucleoside (Cay-15509) and an inhibitor of protein synthesis that has been found in S. alboniger. Puromycin is structurally similar to the amino acid-bearing end of tRNA, which allows it to enter the ribosome during protein synthesis,...

MS049 is a potent and selective inhibitor of PRMT4 (IC50 = 34 nM) and PRMT6 (IC50 = 43 nM). It is less active against additional type I PRMTs (IC50s = >130, >220, and 1.6 µM for PRMT1, PRMT3, and PRMT8, respectively) and displays no inhibition against type II or type III PRMTs nor any additional methyltransferases...

12(S)-HETrE is produced by 12-lipoxygenase oxidation of dihomo-gamma-linolenic acid (DGLA). 12(S)-HETrE is reported to inhibit agonist-mediated platelet activation (IC50 = 40 µM), alpha granule secretion, integrin alphaIIbbeta3 activation, Rap1 activation, and thrombin-induced clot retraction in vitro.Formal Name:...

DS-1001b is an inhibitor of mutant isocitrate dehydrogenase 1 (IDH1, IC50s = 15 and 130 nM for IDH1R132H and IDH1R132C, respectively). It is selective for mutant IDH1, which converts alpha-ketoglutarate to the oncometabolite 2-hydroxyglutarate (2-HG), over wild-type IDH1 and IDH2, which convert isocitrate to...

Val-Cit-PAB-OH is a peptide linker molecule used in the synthesis of drug conjugates. It is cleaved by cathepsin B, a protease highly expressed in cancer cells, which confers specificity of the drug conjugates to cancer cells. Val-Cit-PAB-OH has been used in the synthesis of antibody-drug conjugates (ADCs)...

Itraconazole is an antifungal agent and inhibitor of hedgehog signaling (IC50 = 800 nM). It binds to 14-alpha sterol demethylase/CYP51 isoform B (AF51B, Kd = 31 nM for A. fumigatus enzyme expressed in E. coli) and inhibits ergosterol biosynthesis in C. neoformans (IC50 = 6 nM after a 16-hour incubation). It inhibits...

RO4987655 is a MEK inhibitor (IC50 = 5 nM). It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and...

The poly(ADP-ribose) polymerases (PARPs) are enzymes with roles in DNA repair, apoptosis, inflammation, and other cellular events, particularly in response to reactive oxygen and nitrogen species. ME0328 is an inhibitor of PARP3 (IC50 = 0.89 µM), which is a regulator of DNA repair and mitotic progression. It...