SEC inhibitor KL-1 (KL-1) 是一种拟肽先导化合物，有效的选择性 SEC 抑制剂，通过破坏 SEC 支架蛋白 AFF4 和 P-TEFb 之间的相互作用，导致 Pol II 从启动子近端暂停位点的释放受损并且进行性转录延伸的平均速率降低。SEC inhibitor KL-1 剂量依赖性地抑制 AFF4-CCNT1 相互作用，Ki 值为 3.48 μM。
货号:ajcx14254
CAS:900308-84-1
分子式:C18H16ClNO4
分子量：345.78
溶解度:DMSO: 41.67 mg/mL (120.51 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

SEC inhibitor KL-1 (KL-1), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-1 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 3.48 μM[1].

[1]. Liang K, et al. Targeting Processive Transcription Elongation via SEC Disruption for MYC-Induced CancerTherapy. Cell. 2018 Oct 18;175(3):766-779.