Activators & Inhibitors

Activity: Retinoid RAR agonist . Function/Pharmacology: All−trans−Retinoic acid (ATRA; a metabolite of Vitamin A) is an endogenous ligand for the retinoic acid receptor (RAR). The binding of retinoic acid to the RAR and retinoid X (RXR) heterodimer causes conformation changes in RAR that affects the binding of other proteins that regulate the growth and differentiation of a variety of both normal and malignant cells.1 ATRA promotes differentiation of embryonic stem cells (ESCs) into a variety of cell types in vitro.2-4 Chemical Name: 3,7-Dimethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2E,4E,6E,8E,-nonatetraenoic acid

Activity: Calcium channel blocker . Function/Pharmacology: A non-dihydropyridine-type blocker of L-type Ca2+ channels1,2.Reduces Ca2+ oscillations in subcellular compartments in vascular smooth muscle cells3. Also blocks P-type Ca2+ channels in freshly dissociated rat cerebellar Purkinje neurons4. Clinically useful antihypertensive agent5. Cell permeable. Chemical Name: (2S-cis)-3-(Acetyloxy)-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(methoxyphenyl)-1,5-benzothiazepin-4-(5H)-one hydrochloride

Activity: Dopamine D2/D4 antagonist . Function/Pharmacology: Dopamine D4 and D2 receptor antagonist. High affinity for the cloned rat dopamine D4 receptor (Ki < 20 nM).1 Atypical neuroleptic agent.2 Antagonist at 5HT2A, 5HT2C, 5HT3, 5HT6 and 5HT7 receptors.3,4 Chemical Name: 8-Chloro-11-(4-methyl-1-piperazinyl)-5/H-dibenzo[b,e]diazepine

Activity: LOX and COX inhibitor .

Activity: DPPIV inhibitor . Function/Pharmacology: Potent and selective inhibitor of dipeptidyl peptidase IV (DPPIV) (Ki=130 nM). May be used in cell cuture (1-10 μM) or in vivo (10 mg/kg orally). Cell permeable. Experimental anti-diabetic agent. This product not approved for human therapeutic use. Chemical Name: (2S,3S)-2-Amino-3-methyl-1-(thiazolidin-3-yl)pentan-1-one hemi-fumarate

Activity: TRPA1 agonist . Function/Pharmacology: TRPA1 agonist (EC50=400 nM)1. A naturally occurring drimane sesquiterpene dialdehyde found in a variety of plant species including water pepper (Polygonum hydropiper). Has been used in folk medicine for a variety of indications. Displays analgesic activity via desensitization of sensory neurons2. Chemical Name: (1R,4aS,8aS)-5,5,8a-Trimethyl-1,4,4a,6,7,8-hexahydronaphthalene-1,2-dicarboxaldehyde

Activity: MetAP-2 inhibitor . Function/Pharmacology: Fumagillin is a natural product isolated from the microbial organism Aspergillus fumigatus and used as an antimicrobial for honey bees. It covalently binds and inhibits methionine aminopeptidase-2.1 Fumagillin also inhibits endothelial cell proliferation in vitro and tumor-induced angiogenesis in vivo.2 Chemical Name: (2E,4E,6E,8E)-Mono[(3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methyl-2-butenyl)oxiranyl]-1- oxaspiro[2.5]oct-6-yl] 2,4,6,8-decatetraenedioic acid ester

Activity: Cyclopamine analog . Function/Pharmacology: Veratramine is a teratogenic steroidal alkaloid found in the corn lily (Veratrum sp.)1,2. It is an analog of cyclopamine which can inhibit the hedgehog signaling pathway-dependent proliferation in NIH/3T3 cells at 8 μM1. Cell permeable. SPECIAL HANDLING PRECAUTIONS: This product is teratogenic. Women who are, or may be pregnant should not handle this compound. Chemical Name: (3β, 23β)-14,15,16,17-Tetrahydroveratraman-3,23-diol

Activity: EGFR-Kinase inhibitor . Function/Pharmacology: Potent and selective EGFR kinase inhibitor (IC50 = 23-79 nM)1. Inhibits EGFR autophosphorylation and inhibits tumor growth in vivo2. Enhances efficacy of cytotoxic agents3. Inhibits growth factor production and angiogenesis4. Clinically useful anticancer agent. Chemical Name: N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine