ULK1-IN-2

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。

ULK1-IN-2 

ULK1-IN-2 (化合物 3s) 是一种有效的 ULK1 抑制剂。ULK1-IN-2 对癌细胞具有最高的细胞毒作用,A549 中 IC50 值为 1.94 μM。ULK1-IN-2 可诱导细胞凋亡同时阻断自噬,可用于研究非小细胞肺癌。

ULK1-IN-2

ULK1-IN-2 Chemical Structure

CAS No. : 2497409-01-3

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生物活性

ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer)[1].

IC50 & Target

ULK1

 

体外研究
(In Vitro)

ULK1-IN-2 (compound 3s) (10 μM, 24 h) shows strong anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7[1].
ULK1-IN-2 (0-8 μM, 24 h) blocks autophagy via inhibiting ULK1 in A549 cells[1].
ULK1-IN-2 (0-8 μM, 24 h) induces apoptosis via the mitochondrial pathways in A549 cells in dose department manner[1].
ULK1-IN-2 (0-8 μM, 24 h) inhibits ULK1 and p-ULK1ser317 expression in a concentration-dependent manner, remarkably decreases Bcl-2 expression, increases Bax and the active form of Caspase-3 expression.[1].

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

Cell Proliferation Assay

Cell Line: Human cancer cell lines A549, U937, HL60, MDA-MB-468 and MCF-7[1]
Concentration: 10 μM
Incubation Time: 24 h
Result: Significantly improved anti-proliferative activity against A549, U937, HL60, MDA-MB-468 and MCF-7, with kinase inhibitory activity of 99.15% and IC50 values of 1.94, 12.92, 10.89, 16.83, and 19.60 μM, respectively.

Cell Autophagy Assay

Cell Line: A549 cells[1]
Concentration: 0, 2, 4, 8 μM
Incubation Time: 24 h
Result: Blocked autophagy of A549 cells via inhibiting ULK.

Western Blot Analysis

Cell Line: A549 cells[1]
Concentration: 0, 2, 4, 8 μM
Incubation Time: 24 h
Result: Inhibited expression of ULK1 and p-ULK1ser317 in a concentration-dependent manner. Increased the autophagy substrate P62, reduced LC3-I conversion to LC3-II, and decreased the levels of Beclin1. Remarkably decreased Bcl-2 expression, increased Bax and the active form of Caspase-3 expression.

分子量

495.26

Formula

C19H16BrFN4O6

CAS 号

2497409-01-3

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]. Sun D, Yang Z, Zhen Y, et al. Discovery of 5-bromo-4-phenoxy-N-phenylpyrimidin-2-amine derivatives as novel ULK1 inhibitors that block autophagy and induce apoptosis in non-small cell lung cancer. Eur J Med Chem. 2020;208:112782.

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