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JH-RE-06
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
JH-RE-06图片
CAS NO:1361227-90-8
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
JH-RE-06, 有效的 REV1-REV7 互作抑制剂 (IC50=0.78 μM; Kd=0.42 μM)，靶向与 POLζ 的 REV7 亚基相互作用的 REV1。JH-RE-06 通过阻止诱变 POLζ 的募集来破坏诱变性跨损伤合成 (TLS)。JH-RE-06 增强顺铂诱导的细胞毒性，改善化疗效果。
Cas No.1361227-90-8
Canonical SMILESO=C1C(C(CC(C)C)=O)=C(NC2=CC=C(Cl)C=C2Cl)NC3=C1C([N+]([O-])=O)=CC=C3Cl
分子式C20H16Cl3N3O4
分子量468.72
溶解度DMSO: 5 mg/mL (10.67 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 enhances Cisplatin-induced cytotoxicity and improves chemotherapy[1][2]. IC50: 0.78 μM (REV1-REV7)[1]Kd: 0.42 μM (REV1-REV7)[1]

JH-RE-06 unexpectedly induces dimerization of the REV1 CTD at its REV7-binding surface and blocks the REV1-REV7 interaction[1].

JH-RE-06 inhibits mutagenic TLS and enhances cisplatin-induced toxicity in cultured human and mouse cell lines[1]. Co-administration of JH-RE-06 with cisplatin suppresses the growth of xenograft human melanomas in mice[1].

[1]. Wojtaszek JL, et al. A Small Molecule Targeting Mutagenic Translesion Synthesis Improves Chemotherapy. Cell. 2019 Jun 27;178(1):152-159.e11. [2]. REV1-POLς Inhibition Enhances Cisplatin-Induced Cytotoxicity. Cancer Discov. 2019 Aug;9(8):OF17.