Activators & Inhibitors

Activity: E3 UB ligase inhibitor . Function/Pharmacology: Binds to the E3 ubiquitin ligase complex formed between CRBN, DDB1 and Cul4A, and inhibits the ligase activity. Inhibits TNF synthesis and FGF-induced angiogenesis. Cell permeable. Handle with caution, compound is teratogenic. Chemical Name: N-(2,6-Dioxo-3-piperidinyl)phthalimide, racemic

Activity: L-type Ca channel blocker . Function/Pharmacology: Nifedipine is a clinically useful L-type calcium blocker. Chemical Name: 2,6-Dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid dimethyl ester

Activity: Protein synthesis inhibitor . Function/Pharmacology: Protein synthesis inhibitor. Induces apoptosis. Antifungal activity. Cell permeable. Chemical Name: 4-[2-(3,5-Dimethyl-2-oxo-cyclohexyl)-2-hydroxyethyl]-2,6-piperidinedione

Activity: HDAC inhibitor . Function/Pharmacology: Histone deacetylase (HDAC) inhibitor. Inhibits proliferation, migration and invasion of a number of cancer cell lines. Induces differentiation, and apoptosis. Active in vivo. Chemical Name: 4-Phenylbutyric acid sodium salt

Activity: Mitochondrial permeability pore opening inhibitor . Function/Pharmacology: Immunosupressant. The CsA-cyclophilin complex binds to and inhibits calcineurin, a type 2B phosphatase. Cell permeable.

Activity: Modulates β-catenin-mediated effects . Function/Pharmacology: Metabolite of the cyclooxygenase inhibitor sulindac that induces apoptosis via inhibition of type 5 phosphodiesterases.1 Sulindac sulfone does not inhibit cyclooxygenase at physiological concentrations but does inhibit K-ras-dependent cyclooxygenase-2 expression in colon cancer cells.2 Chemical Name: (Z)-5-Fluoro-2-methyl-1-[p-(methylsulfonyl)benzylidene]indene-3-acetic acid

Activity: Topoisomerase II inhibitor . Function/Pharmacology: Chemotherapeutic agent. Etoposide forms a ternary complex with DNA and topoisomerase II, preventing re-ligation of DNA strands causing DNA cleavage. Blocks the cell cycle in S-phase and G2-phase. Chemical Name: 4′-Demethylepipodophyllotoxin 9-(4,6-O-ethylidene-β-D-glucopyranoside

Activity: Induces melanocyte ablation . Function/Pharmacology: Specifically ablates zebrafish larval melanocytes. Melanocytotoxicity is dependent on tyrosinase activity1,2. A useful tool for elucidating melanocyte stem cell regeneration, recruitment and maintenance3-5. Chemical Name: 4-(4-Morpholinobutylthio)phenol

Activity: PDE1 inhibitor . Function/Pharmacology: Phosphodiesterase PDE1 inhibitor (IC50=21 μM)1. Also blocks voltage-gated Na+ channels, IC50=44.2 μM (potency similar to phenytoin), a mechanism which may contribute to its neuroprotective and anticonvulsant activity2. It reduces inflammatory IL-1β and TNF-α expression in rat hippocampus3. Displays beneficial effects in a rat model of cerebral ischemia-reperfusion injury4. Exerts neuroprotective effects by suppressing microglial inflammation5. Chemical Name: (3α,16α)-Eburnamenine-14-carboxylic acid ethyl ester