Activators & Inhibitors

Activity: H2S synthase inhibitor . Function/Pharmacology: Irreversible inhibitor of the hydrogen sulfide biosynthesis enzyme, cystathione-γ-lyase. It inhibits H2S production in rat liver preparations (IC50=55 μM) and inhibits the rise in plasma H2S in rats with hemorrhagic shock2. It reduces inflammation in a rodent carrageenan-induced hindpaw edema model3. Ameliorates gentamycin-induced nephrotoxicity1. Chemical Name: 2-Amino-4-pentynoic acid

Activity: Inhibits autophagy by inhibiting USP 10 and 13 . Function/Pharmacology: A specific and potent autophagy inhibitor. Spautin-1 promotes the degradation of Vps34 PI3 kinase complexes by inhibiting two ubiquitin-specific proteases USP10 and USP13 which target the Beclin-1 subunit of Vps34 complexes1. Deranges dengue virion maturation2. Inhibits autophagy in a Beclin-1 independent manner in primary epithelial ovarian cancer cells3. Selectively induces cell death of mutant p53-expressing cancer cell lines under confluency4. Cell permeable. Chemical Name: 6-Fluoro-N[(4-fluorophenyl)methyl]-4-quinazolinamine

Activity: Aspartic protease inhibitor . Function/Pharmacology: Selective inhibitor of aspartyl proteases.1 Inhibits human pepsin, human gastricsin, renin, cathepsin D and E and bovine chymosin.2 Does not inhibit thiol proteases, neutral proteases or serine proteases.3 It suppresses RANKL-induced osteoclast differentiation.4 Chemical Name: N-isovaleryl-L-valyl-L-valyl-3-hydroxy-6-methyl-γ-aminoheptanoyl-L-alanyl-3-hydroxy-6-methyl-γ-amino heptanoic acid

Activity: PDGFRβ inhibitor . Function/Pharmacology: A potent and selective inhibitor of PDGFRβ, IC50=80 nM. Greater than 100-fold more selective compared to EGFR, erb-B2, p56, PKA and PKC. Cell permeable. Chemical Name: 5,7-Dimethoxy-3-(4-pyridinyl)quinolone dihydrochloride

Activity: β-catenin inhibitor . Function/Pharmacology: A selective CRT (β-catenin-responsive transcription) inhibitor.1 IC50=18 nM for Wnt responsive STF16 luciferase. Acts via interfering with the β-catenin, TCF4 interaction.1 Displays poor inhibition of cell proliferation in triple-negative breast cancer cells.2 Increases the surface expression of MHCII, CD80 and CD86 on unstimulated dendritic cells (DCs) with no detrimental effects on immune-phenotype of stimulated DCs.3 Modulators of Wnt signaling show great promise in animal models of several cancers.4 Cell permeable. Chemical Name: 4-[5-(3,4-Dimethoxy-benzylidene)-4-oxo-2-thioxo-thiazolidin-3-yl]-butyric acid

Activity: Induces chrondrocyte differentiation . Function/Pharmacology: Promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes (EC50 = 100 nM). Displays chrondroprotective effects in vitro and is efficacious in two animal models of osteoarthritis. Cell permeable. Chemical Name: 2-[(1,1’-Biphenyl)-4-ylcarbamoyl]benzoic acid

Activity: Autophagy inducer . Function/Pharmacology: Specifically induces autophagic cell death in VHL (von Hippel-Lindau)-deficient renal carcinoma cells both in vitro (IC50=625 nM) and in vivo. Renal cell carcinoma cell lines were radiosensitized by induction of autophagy following treatment with STF-62247. Cell permeable Chemical Name: N-(3-Methylphenyl)-4-(4-pyridinyl)-2-thiazolamine

Activity: Tyrosine kinase inhibitor . Function/Pharmacology: An ultra-potent inhibitor of epidermal growth factor receptor tyrosine kinase (EGFRK), with an IC50 of 25 pM. Inhibits other tyrosine kinases at micromolar or higher concentrations. It selectively blocks EGF-mediated cellular processes including mitogenesis, early gene expression and oncogenic transformation1. Inhibits the growth of a number of cancer cell lines2. An extremely useful tool for exploring EGF-mediated cellular signaling3. Chemical Name: 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline hydrochloride

Activity: Autophagy inhibitor . Function/Pharmacology: Hydroxychloroquine sulfate is a lysosomotropic agent which inhibits autophagy and triggers apoptosis in a variety of cell types.1,2 Augments the anticancer activity of DNA-damaging chemotherapy.3 Antiinflammatory activity. Decreases cell surface expression of TNFα receptors in U937 cells.4 Hydroxychloroquine sulfate has been used to treat alopecia successfully5 and is a clinically useful antimalaria agent. Cell permeable and active in vivo. Chemical Name: 7-Chloro-4-[4-(N-ethyl-N-b-hydroxyethylamino)-1-methylbutylamino]quinolone sulfate