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SEC inhibitor KL-2

产品编号: DC11392 Featured
SEC inhibitor KL-2
结构式
900308-51-2
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中国地区超过5000个高品质化合物库存
应用领域
SEC inhibitor KL-2 (KL-2) 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-2 剂量依赖性地抑制 AFF4-CCNT1 相互作用，Ki 值为 1.50 μM。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 900308-51-2
名称:
别名: KL2,KL-2,KL 2
SMILES: C1=CC(F)=CC=C1C(CC(C(=O)NC1=CC(Cl)=CC=C1C)=O)=O
分子式: C17H13ClFNO3
分子量: 333.06
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: The super elongation complex (SEC) is required for robust and productive transcription through release of RNA polymerase II (Pol II) with its P-TEFb module and promoting transcriptional processivity with its ELL2 subunit. Malfunction of SEC contributes to multiple human diseases including cancer.KL-2 is a novel super elongation complex (SEC) inhibitor, disrupting 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. KL-1 and its structural homolog KL-2, which disrupt 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 is required for induction of heat-shock genes and treating cells with KL-1 and KL-2 attenuates the heat-shock response from Drosophila to human. SEC inhibition downregulates MYC and MYC-dependent transcriptional programs in mammalian cells and delays tumor progression in a mouse xenograft model of MYC-driven cancer, indicating that small-molecule disruptors of SEC could be used for targeted therapy of MYC-induced cancer.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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