Atg4B-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。

Atg4B-IN-2 

Atg4B-IN-2 是一种有效的竞争性 Atg4B 抑制剂,Ki 为 3.1 μM,也具有降低 PLA2 的抑制能力,对 Atg4B 和 PLA2IC50 分别为 11 μM 和 3.5 μM。Atg4B-IN-2 通过细胞自噬 (autophagy) 来增强抗去势抗性前列腺癌药物的抗癌活性。

Atg4B-IN-2

Atg4B-IN-2 Chemical Structure

CAS No. : 2765008-88-4

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生物活性

Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer drugs via autophagy inhibition[1].

IC50 & Target

IC50: 11 μM (Atg4B), 3.5 μM (PLA2)[1]
Ki: 3.1 μM (Atg4B)[1]

体外研究
(In Vitro)

Atg4B-IN-2 (compound 21f) (1-10 μM; 2 hours) restores the p62 expression in cells treated with AF (amino acid-free) in a dose-dependent manner[1].
Atg4B-IN-2 (1 and 5 μM; 2 hours) decreases moderately autophagic vesicles at 1 μM, and almost completely inhibits autophagy at 5 μM[1].
Atg4B-IN-2 (5 μM; 2 hours) inhibits Abi-induced autophagy and significantly augments apoptotic cell death and sensitivity to Abi[1].

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

Western Blot Analysis

Cell Line: LNCaP cells (incubated in AF medium)[1]
Concentration: 1, 2, 5, 10 μM
Incubation Time: 2 hours (then incubated in AFM for 24 or 3 hours)
Result: Restored the p62 expression in cells treated with AF in a dose-dependent manner.

Cell Autophagy Assay

Cell Line: LNCaP cells (incubated in AF medium)[1]
Concentration: 1 and 5 μM
Incubation Time: 2 hours (then incubated in AFM for 24 or 3 hours)
Result: Decreased moderately autophagic vesicles at 1 μM, and almost completely inhibited autophagy at 5 μM.

分子量

330.46

Formula

C21H30O3

CAS 号

2765008-88-4

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]. Kudo Y, Endo S, Fujita M, et al. Discovery and Structure-Based Optimization of Novel Atg4B Inhibitors for the Treatment of Castration-Resistant Prostate Cancer. J Med Chem. 2022;65(6):4878-4892.

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