1401731-54-1

MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 μM for CK1δ) and CHK1 (IC50=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation[1].

CKIδ: 0.9 μM (IC₅₀); Chk1: 0.23 μM (IC₅₀)

[1] Huart AS, et al. A Casein kinase 1/Checkpoint kinase 1 pyrazolo-pyridine protein kinase inhibitor as novelactivator of the p53 pathway. Bioorg Med Chem Lett. 2013 Oct 15;23(20):5578-85. DOI:10.1016/j.bmcl.2013.08.046