IC261 是一种选择性的，ATP 竞争性的CK1抑制剂，可触发有丝分裂检查点控制。对Ckiδ、Ckiε、 Ckiα1 和CDK5的IC50值分别为 1 μM、1 μM 、16 μM和4.5mM。

IC261 is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.

IC261 leads to a p53-dependent arrest of the cells with a DNA content of 4 N. It can produce effects on cell cycle progression that are indistinguishable from an established spindle poison and are dependent on the p53 status of the cells[1].

Intrathecal injection of a CK1 inhibitor IC261 attenuates neuropathic pain behaviors. CK1 inhibitors are found to be effective in reducing spinal excitatory response elicited by the presynaptic electrical stimulation only in neuropathic mice[2]. Targeting CK1 isoforms by IC261 influences both pancreatic tumour cell growth and apoptosis sensitivity in vitro and the growth of induced tumours in vivo[3].

Cultures of MEFs of di?erent genotypes (p53+/+, p53+/7, p537/7) are treated with the inhibitor IC261 in the low micromolar range (1 μM). After 12, 24, 48 hours exposure, the effects of IC261 on cell cycle distribution are measured by flow cytometry.(Only for Reference)

186611-52-9

C18H17NO4

311.337

SU-5607

DMSO:58 mg/mL (186.3 mM)
Ethanol:<1 mgml
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years