CCT367766

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CCT367766

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。

CAS NO:

2229856-58-8

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。

生物活性

CCT367766 is a potent and the third generation heterobifunctional andCereblon-basedpirintargeting 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 K_d 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].
CCT367766 (0.5-50 nM; 2 hours) dose-dependently rescuses pirin expression from pretreatment of chlorobisamide in SK-OV-3 cells^[1].

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.