Kinase Inhibitors

A cell-permeable thiourea compound that selectively inhibits the kinase activity of ATM and ATR (IC 50 = ~200 nM) without significant effect against other PIKK family members (PI 3-K, mTOR, and DNA-PK) or kinases that are known to phosphorylate p53

A cell-permeable aminopyrazinyl-sulfone compound that acts as a potent, reversible and ATP-competitive inhibitor of ATR kinase (IC 50 = 12 nM K i = 6 nM) with excellent selectivity over ATM, DNA-PK (IC 50 &gt8 &#181M) and in a 50-kinase panel (%

A cell-permeable triazolylsulfonamido compound that acts a reversible, ATP-competitive kinase inhibitor with selectivities towards Aurora kinases (IC 50 = 11 and 15 nM for Aurora-A, Aurora-B, respectively) and Cdk&#8242s (IC 50 = 9, 4, and 3 nM

A cell-permeable chlorophenylpropionate compound that is superior to its structural analog 4PB (Cat. No.

A cell-permeable tricyclic quinoline-acrylamide analog of BMX-IN-1 ( &gtCat. No.

Synonym(s): Thr-Thr-Tyr-Ala-Asp-Phe-Ile-Ala-Ser-Gly-Arg-Thr-Gly-Arg-Arg-Asn-Ala-Ile-His-Asp Formula: C94H148N32O31 Formula weight: 2222.40 CAS Number: 99534-03-9 Harmonized Tariff Code:  2933.99

A cell-permeable pyrazolopyrimidinylamino compound that acts as a potent, ATP-competitive and reversible inhibitor of CKI&#949 with ~22-fold greater potency over CKI&#948 (IC 50 = 32 and 711 nM, respectively) and displays excellent selectivity

A cell-permeable triaryl substituted imidazolo compound that acts as a potent, reversible and relatively specific ATP-competitive inhibitor of CK1 (IC 50 = 0.2 &#181M from S.

A cell-permeable benzotriazolo compound that acts as a highly selective, ATP/GTP-competitive casein kinase II (CKII) inhibitor (IC50 = 900 nM and 1.6 &#181M for rat liver and human recombinant CKII, respectively) and DYRK (IC 50 &lt1 &#181M for

A cell-permeable thiazolamide compound that acts as a potent, reversible, and ATP-competitive inhibitor against casein kinase-2/CK2 (IC 50 = 32 and 46 nM against CK2&#945 and CK2&#945&#8242, respectively), as well as DYRK1B and FLt-3 (82% and

A cell-permeable halogenated benzimidazole compound that acts as a selective and ATP competitive inhibitor of casein kinase II (CK2, K i = 70 nM for the active hetero-tetrameric form). However, its effect on free CK2a and CK2a&#8242 subunits is

A potent, reversible, and substrate-competitive inhibitor of Cdk4/cyclin D1 (IC 50 = 200 nM). Displays ~500-fold greater selectivity for Cdk4/cyclin D1 over Cdc2/cyclin A (Cdk1/cyclin A), Cdk2/cyclin A, and Cdk2/cyclin E (IC 50 &gt100 &#181M).