常用名：TL12-186

产品描述：

TL12-186 is a Cereblon-dependent kinase degrader that degrades CDK, BTK, FLT3, Aurora and other kinases.TL12-186 inhibits CDK2/cyclin A and CDK9/cyclin T1 with IC50s of 73 and 55 nM, respectively.

靶点活性 CDK2-CyclinA:73 nM (IC50), CRBN:12nM, CDK9-CyclinT1:55 nM (IC50)

体外活性 TL12-186 demonstrates over 90% inhibition against 193 kinases at a screening concentration of 1 μM[1]. Utilizing AlphaScreen binding assays, it exhibits potent binding to CRBN with an IC50 of 12 nM[1]. Displaying CRBN-dependent pharmacological effects, TL12-186 (1-10000 nM; 2 days) exerts 13 to 15 times stronger inhibition of cell survival in WT cells compared to CRBN-/- cells[1]. Moreover, at concentrations ranging from 10 to 10000 nM for 4 hours, TL12-186 selectively inhibits STAT1 phosphorylation without inducing degradation of JAK1/2[1].

别名 TL12 186, TL12186

分子量 931.46

分子式 C44H51ClN10O9S

CAS No. 2250025-88-6

存储

keep away from direct sunlight　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 200 mg/mL (214.72 mM), Sonication is recommended.

PROteolysis TArgeting Chimeras (PROTACs) 通过将靶蛋白和 E3 连接酶结合起来，从而“劫持”细胞的泛素-蛋白酶体系统（UPS）来实现蛋白质的降解。由于 PROTACs 只需具有高选择性地结合其靶标（而不是抑制靶蛋白的酶活性），目前有许多努力将先前无效的抑制剂分子改造为 PROTACs，用作下一代药物。

产地：西安

用途：科研！

厂家：西安齐岳生物科技有限公司

温馨提示：仅用于科研，不能用于人体实验！

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