CCT367766

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CCT367766 

CCT367766 是一种有效的口服活性蛋白,第三代异功能和基于 Cereblon 配体的 pirin 靶向蛋白降解探针 (PDP,或PROTAC),在低浓度时就可以减少 pirin 蛋白的表达。CCT367766 对 CRBN-DDB1 复合物表现出中等亲和力,其 IC50 值为 490 nM。CCT367766 对重组的 pirin 和 CRBN 具有良好的亲和力,其 Kd 值分别为 55 nM 和 120 nM。CCT367766 阐释了一种有用的的化学工具来研究一些未被开发的蛋白质。

CCT367766

CCT367766 Chemical Structure

CAS No. : 2229856-58-8

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生物活性

CCT367766 is a potent and the third generation heterobifunctional and Cereblon-based pirin targeting protein degradation probe (PDP, or PROTAC), depletes pirin protein expression at low concentration. CCT367766 exhibits a moderate affinity for the CRBN-DDB1 complex with an IC50 value of 490 nM. CCT367766 reveals a good affinity for the recombinant pirin and CRBN with Kd values of 55 nM and 120 nM, respectively. CCT367766 provides a potential chemical tool to study a largely unexplored protein[1].

IC50 & Target[1]

CRBN-DDB1

490 nM (IC50)

体外研究
(In Vitro)

CCT367766 (50-1500 nM; 24 hours) demonstates the depletion of pirin protein as a the time-dependent hook-effect in SK-OV-3 human ovarian cancer cells[1].
CCT367766 (0.5-50 nM; 2 hours) demonstrates the concentration-dependent depletion of pirin protein after 2 h exposure in SK-OV-3 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: SK-OV-3 human ovarian cancer cells
Concentration: 50, 150, 250, 500 and 1500 nM
Incubation Time: 2 hours, 4 hours, 24 hours
Result: Decreased pirin protein expression.

Western Blot Analysis[1]

Cell Line: SK-OV-3 human ovarian cancer cells
Concentration: 0.5, 1, 2.5, 5, 7.5, 10, 25, and 50 nM
Incubation Time: 2 hours
Result: Completely degraded pirin just at 50 nM treatment.

分子量

946.40

Formula

C49H48ClN7O11

CAS 号

2229856-58-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Chessum NEA, et al. Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).J Med Chem. 2018 Feb 8;61(3):918-933.

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