Kinase Inhibitors

A cell-permeable piperidinyl-pyridine compound that acts as a selective inhibitor of IKK-2 activity (IC 50 = 8.5 and 250 nM for IKK-2 and IKK-1, respectively) with little effect towards IKK-3, Syk, and MKK4 (IC 50 &gt20 &#181M).

A cell-permeable BX795 analog ( >Cat. No.

A cell-permeable, tri-substituted pyrazol compound that acts as a potent and specific integrin-linked kinase (ILK) inhibitor (IC 50 = 600 nM). Shown to have high in vitro anti-proliferative potency against prostrate and breast cancer cell lines (IC

A cell-permeable disubstituted pyranone compound that acts as a potent and ATP-competitive inhibitor of ATM kinase (IC 50 = 13 nM K i = 2.2 nM).

A cell-permeable, highly selective, ATP/GTP-competitive casein kinase II (CKII) inhibitor (IC 50 = 900 nM and 1.6 &#181M for rat liver and human recombinant CKII, respectively) and DYRK (IC 50 &lt1 &#181M for DYRK1a).

A potent inhibitor of Janus Protein tyrosine Kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC 50 = 15 nM for murine JAK1), JAK2 IC 50 = 1 nM), JAK3 (K i = 5 nM), and Tyk2 (IC 50 = 1 nM).

A cell-permeable, potent, selective, and ATP-competitive inhibitor of p38 MAP kinase (IC 50 = 380 nM for p38&#945). Shown to effectively suppress LPS-induced cytokine release in vitro (IC 50 = 160 nM for TNF-&#945 release and 39 nM for IL-1&#946

A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK K i = 1.6 nM).

A cell-permeable, potent, selective, reversible, and ATP-competitive inhibitor of TGF-&#946 type I receptor (ALK5 IC 50 = 23 nM, 4 nM and 18 nM for ALK5 binding, ALK5 auto-phosphorylation, and TGF-&#946 cellular assay in HepG2 cells,

A cell-permeable triarylimidazole compound that is shown to effectively inhibit cellular Smad2 phosphorylation (&gt90% inhibition by 10 &#181M inhibitor) upon vector-mediated expression of constitutively active ALK4, ALK5, or ALK7 in NIH 3T3

Application IRAK-1/4 inhibitor I has been used in various studies to inhibit IRAK1 in hepatoma cell lines and head and neck squamous cell carcinoma (HNSCC) cell lines. Biochem/physiol Actions IRAK-1/4 Inhibitor I is a novel benzimidazole that is a

Application IRAK-1/4 inhibitor I has been used in various studies to inhibit IRAK1 in hepatoma cell lines and head and neck squamous cell carcinoma (HNSCC) cell lines. Biochem/physiol Actions IRAK-1/4 Inhibitor I is a novel benzimidazole that is a