MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC 50 =0.9 μM for CK1δ) and CHK1 (IC 50 =0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation.
性状
Solid
IC50 & Target[1][2]
CKIδ 0.9 μM (IC50) Chk1 0.23 μM (IC50
体外研究(In Vitro)
MRT00033659 (5-40 μM; 48 hours) is sufficient to significantly reduce cell number of 5 μM. MRT00033659 (1-80 μM; 48 hours) induces substantial cell death from 5 μM. MRT00033659 (0.2-80 μM; 48 hours) induces a robust and sustained stabilisation of p53, MDM2 and p21 proteins, as well as E2F-1 destabilisation from 0.2 μM to 5 μM. MRT00033659 does not inhibit p38α MAPK. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 83.33 mg/mL (312.92 mM; Need ultrasonic)配制储备液