Activators & Inhibitors

Activity: Leukocyte elastase inhibitor . Function/Pharmacology: Potent and selective leukocyte elastase inhibitor, IC50 = 44 nM1. Displays no activity at a variety of other proteases. Inhibits NF-κB activation2 and LTB4-induced neutrophil migration in vitro3. Significantly attenuates ischemia-induced spinal cord injury, decreases serum cytokine levels and reduces acute inflammatory lung injury in vivo4. Chemical Name: N-{2-[({4-[(2,2-Dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}glycine sodium

Activity: FKBP inhibitor . Function/Pharmacology: FK-506 induces immunosuppression by inhibiting T cell proliferation. Inhibits FKBP12 and calcineurin (IC50 ~ 1 nM). Cell permeable.

Activity: mTOR inhibitor . Function/Pharmacology: Clinically useful immunosuppressant. Inhibits the response to interleukin-2 blocking activation of T- and B-cells.1 Rapamycin forms a complex with cytosolic FK-binding protein 12 (FKB12) that binds to mTOR Complex1(mTORC1) inhibiting the mammalian target of rapamycin (mTOR).2 Also binds to mTORC2 leading to decreased glucose tolerance and insensitivity to insulin.3 Induces autophagy.4

Activity: Protein kinase inhib (pan spec.) . Function/Pharmacology: Broad spectrum kinase inhibitor. Inhibited kinases include, but are not limited to; PKA, PKC, S6 Kinase, KDR, PKC, Akt, EGFR, VEGFR, PDGFR, c-kit, and FLT-3. Acute myeloid leukemia related mutant forms of FLT-3 are also inhibited both in vitro and in vivo. PKC-412 has been demonstrated to induce apoptosis and shows broad antiproliferative activity in various tumor cell lines. Cell Permeable Chemical Name: 4’-N-Benzoyl staurosporine

Activity: Phospholipase A2 inhibitor . Function/Pharmacology: Reversible inhibitor of Ca2+-independent phospholipase A2 (PLA2), IC50=7 M for guinea pig lung PLA2.1 Inhibits epinephrine-induced thromboxane production in platelets.1 Inhibition of PLA2 by ONO-RS-032 disrupts endosome tubule formation and maintenance of the Golgi complex.2-4 Prevents Xenopus oocyte maturation at stage V.5 Chemical Name: 2-(4-Pentylcinnamoyl)amino-4-chlorobenzoic acid

Activity: GPR40 agonist . Function/Pharmacology: Selective agonist at the free fatty acid receptor, FFA1/4, (GPR40 and GPR120).1 Displays anti-allodynic and anti-hyperalgesic effects in mouse inflammatory and neuropathic pain models.2 Inhibits LPA-induced proliferation of DU145 and PC-3 cells.3 Decreases hepatic lipid accumulation in a high fat diet steatosis mouse model.4 Promotes brown adipose tissue thermogenesis.5 Chemical Name: 4-(3-Phenoxybenzylamino)phenylpropionic acid

Activity: NAD biosynth inhibitor . Function/Pharmacology: Nicotinamide phosphoribosyltransferase inhibitor (Ki=0.4 nM). Induces tumor cell apoptosis. Extends lifespan of human cells. Cell permeable.

Activity: Free radical scavenger . Function/Pharmacology: U-74389G is an antioxidant and Inhibits iron-mediated lipid peroxidation.1 It has also been shown to reduce free radical-mediated injury after ischemia and reperfusion.2,3 Chemical Name: 21-[4-(2,6-Di-1-pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl]pregna-1,4,9[11]-triene-3,20-dione maleate salt

Activity: L-type Ca channel blocker . Function/Pharmacology: Clinically useful L-type calcium channel blocker.1 It is also used as an inhibitor of drug efflux pump proteins.2 Chemical Name: 5-[N-(3,4-Dimethoxyphenylethyl)methylamino]-2-(3,4-dimethoxyphenyl)-2-isopropylvaleronitrile hydrochloride