Activators & Inhibitors

Activity: Natural sphingolipid . Function/Pharmacology: Displays antibacterial activity1. Can be taken up by E. coli and S. aureus and induce ultrastructural damage2. Chemical Name: (2S,3R,4R)-Octadecane-1,2,3,4-tetraol

Activity: Intracellular Zn2+ chelator . Function/Pharmacology: TPEN is a cell permeable metal chelator. Frequently used to study effects of zinc depletion on cellular processes.1,2 Chemical Name: N,N,N’,N’-Tetrakis(2-pyridylmethyl)ethylenediamine

Activity: Calmodulin antagonist . Function/Pharmacology: Binds to and inhibits calmodulin in a calcium-dependent and irreversible manner (IC50= ca. 1 μM)1. A classical irreversible α adrenergic antagonist2. A useful tool for irreversible inhibition of calmodulin. Cell permeable. Chemical Name: N-(2-Chloroethyl)-N-(1-methyl-2-phenoxyethyl)benzylamine hydrochloride

Activity: PARP inhibitor . Function/Pharmacology: Inhibits endogenous poly-ADP-ribosyltransferases1. Inhibits nitric oxide-induced apoptosis but not differentiation in HL-60 cells2. Inhibits stress-induced apoptosis3. Protects cells from oxygen radical and nitric oxide toxicity4. Chemical Name: null

Activity: Protein kinase inhibitor . Function/Pharmacology: Apigenin is a plant flavonoid with antioxidant properties. It has been reported to have myriad effects on biochemical pathways including kinase inhibition (CK2, PKC, ERK)1-3, CYP2CP inhibition4, inhibition of cellular proliferation via G2/M cell cycle arrest3,5, reduction of HIF-1 and VEGF expression6, and inhibition of nitric oxide and PGE2 synthesis7. Chemical Name: 5,7-Dihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one

Activity: PKC activator . Function/Pharmacology: Selective activator of protein kinase C which displays antileukemic activity mediated via PKC1 In contrast, it provides a strong survival signal to resting and activated human T cells via activation of PKC and downstream activation of NFB.2 Treatment of subcutaneous tumors results in anti-cancer CD8 T cells, also displays adjuvant activity and synergizes with cancer immunotherapies.3 Induces senescence-like growth arrest in solid tumor cells.4 Inhibits HIV-1 infection at an early pathway of viral entry.5 Chemical Name: null

Activity: Na+ K+ ATPase inhibitor . Function/Pharmacology: Selective inhibitor of Na+ K+-ATPase isolated from Strophanthus gratus1. Endogenous ouabain is found in human circulation2. Displays cardiotonic and diuretic activity. May be used to induce hypertensive rat model3. Cell permeable and active in vivo. Chemical Name: 3-[(6-Deoxy-α-L-mannopyranosyl)oxy]-1,5,11α,14,19-pentahydoxycard-20(22)-enolide octahydrate

Activity: ER antagonist; GPR30 agonist . Function/Pharmacology: Estrogen receptor antagonist/partial agonist. Induces oxidative stress and apoptosis in estrogen receptor-negative cancer cell lines1. Displays neuroprotective effects in permanent focal ischemia2. Inhibits PKC3. Potent agonist at GPR30 (membrane estrogen receptor)4. Clinically useful breast cancer agent5. Chemical Name: (2)-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethanamine citrate

Activity: Dihydrofolate reductase inhibitor . Function/Pharmacology: A synthetic folic acid analog with immunosuppressant and cancer chemotherapeutic activity.1 Inhibits thymidylate synthetase and de novo purine synthesis.2,3 Displays beneficial effects in rheumatoid arthritis by inhibiting the production of cytokines induced by T-cell activation4 and stimulation of adenosine release5. It is the classic disease-modifying antirheumatic drug (DMARD).6 Chemical Name: N-[4-[[(2,4-Diamino-6-pteridinyl)methyl]methylamino]benzoyl]-L-glutamic acid