SAH-SOS1A

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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。

SAH-SOS1A 

SAH-SOS1A 是一种基于肽的 SOS1/KRAS 蛋白相互作用抑制剂。SAH-SOS1A 以纳摩尔亲和力 (EC50=106-175 nM) 与野生型和突变型 KRAS (G12D, G12V, G12C, G12S, and Q61H) 结合，直接和独立地阻断核苷酸结合，损害 KRAS 驱动的癌细胞活力，并通过阻断 KRAS 下游 ERK-MAPK 磷酸化信号级联的机制发挥作用。

SAH-SOS1A

SAH-SOS1A Chemical Structure

CAS No. : 1652561-87-9

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SAH-SOS1A 的其他形式现货产品:

SAH-SOS1A TFA

生物活性

SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS[1].

IC50 & Target[1]

KRAS-SOS1

 

KRas G12C

140 nM (EC50)

KRas G12D

109 nM (EC50)

KRas G12V

154 nM (EC50)

KRas G12S

155 nM (EC50)

KRas Q61H

175 nM (EC50)

K-Ras WT

106 nM (EC50)

体外研究
(In Vitro)

SAH-SOS1A (0.625-40 μM) dose-responsively impairs the viability of cancer cells bearing G12D, G12C, G12V, G12S, G13D, and Q61H mutations with IC50 values in the 5- to 15-μM range. Cancer cells expressing wild-type KRAS, such as HeLa and Colo320-HSR cells, are similarly affected[1].
SAH-SOS1A (5-40 μM; 4 hours) dose-responsively inhibits MEK1/2, ERK1/2, and AKT phosphorylation[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 Viability Assay[1]

Cell Line: Panc 10.05 cells bearing the KRAS G12D mutation
Concentration: 0.625-40 μM
Incubation Time: 24 hours
Result: Dose-responsively impaired the viability of cancer cells bearing KRAS G12D.

Western Blot Analysis[1]

Cell Line: Panc 10.05 cells
Concentration: 5-40 μM
Incubation Time: Indicated doses for 4 h, followed by 15-min stimulation with EGF
Result: Dose-responsively inhibited MEK1/2, ERK1/2, and AKT phosphorylation.

体内研究
(In Vivo)

SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85DV12/ActinGS) treatment notably decreases the phosphorylation state of ERK1/2[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.
分子量

2187.53

Formula

C100H159N27O28
CAS 号

1652561-87-9
Sequence Shortening

RRFFGI{Aaa}LTN{Aaa}LKTEEGN (Covalent bridge:Aaa7-Aaa11)
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]. Leshchiner ES, et al. Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices. Proc Natl Acad Sci U S A. 2015;112(6):1761-1766.

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