TL12-186,2250025-88-6

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TL12-186

CAS No. : 2250025-88-6

MCE 国际站：TL12-186

产品活性：TL12-186 是一种依赖于 Cereblon 的多激酶 PROTAC 降解剂。包括 CDK，BTK，FLT3，Aurora激酶，TEC，ULK，ITK 等。TL12-186 抑制 CDK2/cyclin A 和 CDK9/cyclin T1，IC₅₀ 分别为 73 和 55 nM。

研究领域：PROTAC  |  Cell Cycle/DNA Damage

作用靶点：PROTACs  |  CDK

In Vitro: TL12-186 displays >90% inhibition of 193 kinases at a screening concentration of 1 μM.
?TL12-186 displays potent binding to CRBN (IC₅₀=12 nM) using an AlphaScreen engagement assay.
?TL12-186 (1-10000 nM; 2 days) exhibits a CRBN-dependent pharmacological effect, displaying 13 to 15-fold more potent inhibition of survival of the WT cells than the CRBN^-/- cells.
?TL12-186 (10-10000 nM; 4 hours) inhibits STAT1 phosphorylation without causing JAK1/2 degradation.

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