MAIT-203

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。

MAIT-203 

MAIT-203 是一种环戊丙氨酸衍生的拟肽,有效抑制腺瘤性息肉病 (APC) 和 Asef (RhoGEF4) 的相互作用,但不抑制 APC-Sam68 或 APC-striatin 的相互作用。MAIT-203 结合 APC-ARM,Ki 值为 0.015 μM,Kd 值为 0.036 μM。MAIT-203 显着抑制结直肠癌细胞的迁移和侵袭。

MAIT-203

MAIT-203 Chemical Structure

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生物活性

MAIT-203, a cyclopentyalanin-derived peptidomimetic, potently inhibits the interaction of adenomatous polyposis coli (APC) and Asef (RhoGEF4), but not APC-Sam68 or APC-striatin interactions. MAIT-203 binds APC-ARM with a Ki of 0.015 μM and a Kd of 0.036 μM. MAIT-203 significantly represses the migration and invasion of colorectal cancer cells.

体外研究
(In Vitro)

MAIT-203 (10 μM and 25 μM; for 24 h) reduces Asef-APC interaction in a dose-dependent manner in HEK293T cells[1].
MAIT-203 (10 μM) significantly attenuates SW480 and HCT116 cell migration[1].
Incubation of SW480 cells with MAIT-203 (25, 50 μM;for 24 h) results in a dose-dependent decrease in the amount of the active form of CDC42, but not Rac1[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

2517.85

Formula

C106H177N43O29

Sequence Shortening

Z-AGEA-{S-3cyclopentylalamine}-YEGGGGGRKKRRQRRR-NH2

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]. Haiming Jiang, et al. Peptidomimetic Inhibitors of APC-Asef Interaction Block Colorectal Cancer Migration. Nat Chem Biol. 2017 Sep;13(9):994-1001.

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