ULK1-IN-2

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ULK1-IN-2

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2497409-01-3

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。

生物活性

ULK1-IN-2 (compound 3s) is a potentULK1inhibitor. ULK1-IN-2 shows highest cytotoxic effect againstcancercell lines, withIC₅₀of 1.94 μM in A549. ULK1-IN-2 can induceapoptosisand simultaneously blockautophagy, 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 inhibitingULK1in 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) inhibitsULK1andp-ULK1^ser317expression 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 IC₅₀values 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-ULK1^ser317in 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

性状

Solid

Formula

C₁₉H₁₆BrFN₄O₆

CAS 号

2497409-01-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)