Description | K00546, a potent inhibitor of both cyclin-dependent kinase (CDK1 and CDK2) and CDC2-like kinase (CLK1 and CLK3), demonstrates high specificity with IC50s of 0.6 nM and 0.5 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. Additionally, it inhibits CLK1 and CLK3 with IC50s of 8.9 nM and 29.2 nM, respectively [1] [2] [3]. |
In vitro | K00546 binds to the SLK ATP-binding site and forms three hydrogen bonds with the kinase hinge residues E109 and C111. The sulphamoyl moiety of K00546 also interacts with the main chain of L40 [1]. K00546 (compound 3n) also inhibits PKA, casein kinase-1, MAP kinase (ERK-2), calmodulin kinase, VEGF-R2, GSK-3 and PDGF-Rβ with IC 50 values of 5.2 μM, 2.8 μM, 1.0 μM, 8.9 μM, 0.032 μM, 0.14 μM and 1.6 μM, respectively [2]. |
molecular weight | 425.44 |
Molecular formula | C15H13F2N7O2S2 |
CAS | 443798-47-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |