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ULK1-IN-2

目录号 : GC68463

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 Chemical Structure

Cas No.:2497409-01-3

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5mg
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10mg
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25mg
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50mg
¥7,650.00
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100mg
¥12,150.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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].

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].

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.

[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.

Chemical Properties

Cas No. 2497409-01-3 SDF Download SDF
分子式 C19H16BrFN4O6 分子量 495.26
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1 mM 2.0191 mL 10.0957 mL 20.1914 mL
5 mM 0.4038 mL 2.0191 mL 4.0383 mL
10 mM 0.2019 mL 1.0096 mL 2.0191 mL
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