NSC-658497

发表于由

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。

NSC-658497 

NSC-658497 是一种有效的 SOS1 抑制剂。NSC-658497 与 SOS1 结合，竞争性抑制 SOS1-Ras 相互作用，并呈剂量依赖性抑制 SOS1-GEF 活性。NSC-658497 在抑制 Ras、下游信号活动和相关细胞增殖方面显示出剂量依赖性功效。

NSC-658497

NSC-658497 Chemical Structure

CAS No. : 909197-38-2

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生物活性

NSC-658497 is an effective inhibitor of Ras-GEF, SOS1. NSC-658497 binds to SOS1, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity. NSC-658497 showed dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation[1].

体外研究
(In Vitro)

NSC-658497 (0-20 μM; 2 hours; NIH/3T3 cells) dose-dependently inhibits EGF (50 ng/mL)-stimulated Ras, but not EGFR activation[1].
Concomitant to Ras inhibition, NSC-658497 (0-100 μM; 2 hours; NIH/3T3 cells) dose-dependently inhibited the EGF activated, Ras downstream targets ERK1/2 and AKT[1].
Consistent with these results, NSC-658497 dose-dependently suppressed Ras signaling mediated by the overexpression of an active SOS1 mutant (W729L), originally identified in Noonan’s Syndrome, in human embryonic kidney cells[1].
NSC-658497 dose-dependently inhibits 50 nM SOS1-cat mediated GDP/GTP nucleotide exchange upon 2 μM H-Ras (aa. 1-166) in the BODIPYFL-GDP dissociation assay (IC50=15.4μM)[1].
NSC-658497 (0-60 μM; 3 days; PC-3 and DU-145 cells) inhibits proliferation of prostate cancer cells[1].
NSC-658497 (0-60 μM; 2 hours; PC-3 and DU-145 cells) dose-dependently inhibits Ras-GTP activity and the downstream p-ERK1/2 and p-Akt activities[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: PC-3 and DU-145 cells
Concentration: 0-60 μM
Incubation Time: 3 days
Result: Dose-dependently inhibited proliferation of PC-3 and DU-145 cells.

Western Blot Analysis[1]

Cell Line: PC-3 and DU-145 cells
Concentration: 0-60 μM
Incubation Time: 2 hours
Result: Dose-dependently inhibited Ras-GTP activity and the downstream p-ERK1/2 and p-Akt activities.

分子量

438.43

Formula

C20H10N2O6S2
CAS 号

909197-38-2
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]. Evelyn CR, et al. Rational design of small molecule inhibitors targeting the Ras GEF, SOS1. Chem Biol. 2014;21(12):1618-1628.

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