CAY10576

CAY10576 is a multi-kinase inhibitor.^1,2,3 It inhibits TANK-binding kinase 1 (TBK1), polo-like kinase 1 (Plk1), and IKKβ (IC₅₀s =0.093, 0.63, and 0.79 µM, respectively) and is selective for these kinases over IKKε, Aurora B kinase, and cyclin-dependent kinase 2 (Cdk2; IC₅₀s = 5, >5.32 and >30 µM, respectively).^1,2,3 CAY10576 also inhibits Rho-associated kinase1 (ROCK1) and ROCK2 (IC₅₀s = 1.8 and 0.04 µM, respectively).⁴

WARNING This product is not for human or veterinary use.

1. Bamborough, P., Christopher, J.A., Cutler, G.J., et al. 5-(1H-benzimidazol-1-yl)-3-alkoxy-2-thiophenecarbonitriles as potent, selective, inhibitors of IKK-ε kinase. Bioorg. Med. Chem. Lett. 16(24), 6236-6240 (2006).

2. Xie, H.-Z., Liu, L.-Y., Ren, J.-X., et al. Pharmacophore modeling and hybrid virtual screening for the discovery of novel IκB kinase 2 (IKK2) inhibitors. J. Biomol. Struct. Dyn. 29(1), 165-179 (2011).

3. Johannes, J.W., Chuaqui, C., Cowen, S., et al. Discovery of 6-aryl-azabenzimidazoles that inhibit the TBK1/IKK-ε kinases. Bioorg. Med. Chem. Lett. 24(4), 1138-1143 (2014).

4. Wang, P., Yang, Y., Shao, Q., et al. Selective inhibition of ROCK kinase isoforms to promote neuroregeneration after brain surgery. Med. Chem. Res. 25, 40-50 (2016).

Huh, J.Y., Reilly, S.M., Abu-Odeh, M., et al. TANK-binding kinase 1 regulates the localization of acyl-CoA synthetase ACSL1 to control hepatic fatty acid oxidation. Cell Metab. 32(6), 1012-1027 (2020).