CSRM617

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。

CSRM617 

CSRM617 是转录因子 ONECUT2 (OC2,雄激素受体 AR 的主要调节剂) 的选择性小分子抑制剂,在 SPR 测定中 Kd 为7.43 uM,直接与 OC2-HOX 结构域结合。CSRM617 通过切割 Caspase-3 和 PARP 诱导细胞凋亡 (apoptosis)。CSRM617 在小鼠的前列腺癌模型中耐受性良好。

CSRM617

CSRM617 Chemical Structure

CAS No. : 787504-88-5

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生物活性

CSRM617 is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 is well tolerated in the prostate cancer mouse model[1]

体外研究
(In Vitro)

CSRM617 (0.01-100 μM; 48 hours) inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells[1].
CSRM617 (10-20 μM; 48 hours) induces apoptosis in 22Rv1 cells results in cell death in a concentration-dependent fashion[1].
CSRM617 (20 μM; 72 hours) induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP[1].

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

分子量

255.23

Formula

C10H13N3O5

CAS 号

787504-88-5

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]. Rotinen M, et al. ONECUT2 is a targetable master regulator of lethal prostate cancer that suppresses the androgen axis. Nat Med. 2018 Dec;24(12):1887-1898.

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