Supplier: Enzo Life Sciences

Inhibits PKCα (IC50=43 µM) and PKCγ (IC50=50 µM) without inhibiting the δ, βI and βII isotypes.

Supplier: Enzo Life Sciences

AG-490 is a potent inhibitor of the JAK-2 tyrosine kinase. In acute lymphoblastic leukemia (ALL) cells, which abundantly express JAK-2, AG-490 dose-dependently inhibited DNA synthesis, blocked cell growth and induced apoptosis. At 5 µM, AG-490 almost completely blocked the growth of all pre-B ALL cells but had no significant effect on the growth of mitogen-stimulated normal B or T cells, B-cell lymphoma or T-cell leukemia cells. AG-490 does not significantly inhibit other kinases such as Lck, Lyn, Btk, Syk and Src. It blocks interleukin-7-induced JAK kinase activity in T-cells (JAK-1, JAK-3) and the consequent phosphorylation of PI-3 kinase. AG-490 is cell permeable and is a valuable tool for studying the cellular role of JAK kinases in signal transduction.

Supplier: Enzo Life Sciences

Inhibits ERK2 (Ki = 525nM). Also inhibits adenosine kinase (Ki = 30nM), CK1 and CK2 and insulin receptor kinase (IC50 ranging from 0.4-28µM).

Supplier: Enzo Life Sciences

Potent and specific inhibitor of the protein kinase c-Raf (IC50=70nM). Has no significant effect on many other protein kinases tested (even at 50µM) with the exception of p38 (SAPK2a) (IC50=2µM) and SAPK2b (p38β) (IC50=2µM). Induces a paradoxical >100-fold activation of c-Raf in whole cells.

Supplier: Enzo Life Sciences

Src kinase inhibitor

Supplier: Enzo Life Sciences

Member of the tyrphostin family of tyrosine kinase inhibitors. Selective inhibitor of the PDGF receptor kinase (IC50=20µM) vs. the EGF receptor kinase (IC50=820µM). Inhibits PDGF-induced mitogenesis in human bone marrow fibroblasts.

Supplier: Enzo Life Sciences

Phospholipase inhibitor

Supplier: Enzo Life Sciences

Inhibits Rho kinase (ROCK; Ki=0.33μM). Selective protein kinase A and G inhibitor (both Ki’s = 1.6μM). Inhibits agonist-induced activation of NADPH oxidase in human neutrophils (IC50=15μM). Inhibitor of myosin light chain kinase and Ca2+/calmodulin-dependent protein kinase II. Inhibits translocation of PKCβI, PKCβII and PKCζ. Cell permeable Ca2+ antagonist with antivasospastic properties.

Supplier: Enzo Life Sciences

MPTP inhibitor

Supplier: Enzo Life Sciences

A cell-permeable cGMP analog which is more resistant to phosphodiesterases than cGMP and which preferentially activates cGMP-dependent protein kinase. It inhibits thrombin stimulated arachidonic acid release in human platelets.

Supplier: Enzo Life Sciences

Macrolide antibiotic that acts as a potent and selective inhibitor of vacuolar-type H⁺-ATPase (V-type) (IC₅₀=004 - 0.4 nmol/mg). Valuable tool for distinguishing among different types of ATPases. Inhibitor of endosomal acidification. Blocks lysosomal cholesterol trafficking in macrophages. Blocks pH regulation in brain cells.

Supplier: Enzo Life Sciences

Clinically useful diuretic. Clopamide selectively inhibits the chloride the sodium chloride cotransporter.

Supplier: Enzo Life Sciences

Selectively inhibits monoacylglycerol (MAG) lipase (IC50=28µM) via a noncompetitive mechanism. Does not inhibit FAAH, DAG lipase or COX-2. URB-602 selectively raises levels of 2-arachidonoylglycerol with no change in anandamide concentrationsin cells and tissues. In the same way anandamide levels were markely elevated by the FAAH inhibitor URB597 at 1µM.

Supplier: Enzo Life Sciences

ADP-ribosylation factor inhibitor

Supplier: Enzo Life Sciences

A useful tool for affinity purification of HSP-90 and HSP-90 dependent client proteins.

Supplier: Enzo Life Sciences

NF-kappaB inhibitor

Supplier: Enzo Life Sciences

VEGF receptor tyrosine kinase inhibitor. Inhibits KDR (IC50=100nM) and Flt (IC50=2µM) tyrosine kinases.

Supplier: Enzo Life Sciences

Retinoic acid analog which acts as a selective RARα agonist with no affinity for RXRs. Induces differentiation in leukemia cell lines and inhibits angiogenesis in chick embryos.

Supplier: Enzo Life Sciences

Blocks agonist and antagonist binding to G protein-coupled receptors.

Supplier: Enzo Life Sciences

Phospholipase inhibitor

Supplier: Enzo Life Sciences

Precursor to a large family of eicosanoids. Acts as a second messenger independent of metabolism. Retrograde messenger in long-term potentiation in the nervous system. Inhibits ras-GAP. Activator for several protein kinase C (PKC) isotypes.

Supplier: Enzo Life Sciences

PPAR ligand.

Supplier: Enzo Life Sciences

Beneficial effect in cardiovascular diseases and inflammation. Inhibits PGE2 formation from arachidonic acid in 3T3 fibroblats.

Supplier: Enzo Life Sciences

A potent and selective 15-lipoxygenase inhibitor which lacks significant nonspecific antioxidant properties. It suppresses atherogenesis and limits atherosclerotic lesion development in the rabbit. It reduces oxidant stress-induced apoptosis in endothelial cells and inhibits proliferation in 15-LO overexpressing PC3 cells.

Supplier: Enzo Life Sciences

PD-98059 is a potent and selective inhibitor of MAP kinase kinase (MEK). It selectively blocks the activation of MEK thereby inhibiting the phosphorylation and the activation of MAP kinase. PD-98059 is cell permeable. In PC12 pheochromocytoma cells, it completely blocked the increase in MAP kinase activity produced by NGF, IC50=2µM. Enhances self-renewal of embryonic stem cells PD-98059 is an invaluable tool to help elucidate the role of the MAPK cascade in a variety of biological systems. Inhibits cell growth and proliferation in acute myelogenous leukemia cell lines by causing cell arrest.

Supplier: Enzo Life Sciences

GEF inhibitor

Supplier: Enzo Life Sciences

A myristate analog which has similar chain length but reduced hydrophobicity compared to myristate. Inhibits replication of HIV-1. Its specific mechanism of action is not clear but it is believed to either inhibit the activity of N-myristoyltransferase or modulate the function of target acylated proteins.

Supplier: Enzo Life Sciences

HMG-CoA reductase inhibitor

Supplier: Enzo Life Sciences

Active against Gram-positive bacteria. Clindamycin binds to the 50S subunit of bacterial ribosomes and suppresses protein synthesis.

Supplier: Enzo Life Sciences

ATPase inhibitor