PROTAC BCR-ABL1 ligand 1

发表于由

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。

PROTAC BCR-ABL1 ligand 1 

PROTAC BCR-ABL1 ligand 1，化合物 GMB-475， 是靶向蛋白水解的嵌合体 (PROTAC) 的配体，其以变构方式靶向 BCR-ABL1 蛋白并募集 E3 连接酶 Von Hippel-Lindau，从而导致泛素化和随后的 BCR-ABL1 蛋白的降解。

PROTAC BCR-ABL1 ligand 1

PROTAC BCR-ABL1 ligand 1 Chemical Structure

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生物活性

PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1[1].

体外研究
(In Vitro)

GMB-475 (0-10 μM) exhibits cell proferation with IC50 values of 1.11,1.98,0.37 μM for BCR-ABL1 WT, T315I, G250E cells, respectively[1].
GMB-475 (0-30 μM) induces the degradation of BCR-ABL1 and c-ABL1 with concomitant inhibition of downstream signaling via the STAT5 pathway, in a dose- and time-dependent fashion in the context of both K562 and Ba/F3 cells[1].

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

Western Blot Analysis[1]

Cell Line: K562 and Ba/F3 cells
Concentration: 0-30 μM
Incubation Time:
Result: Decreased p-STAT5 expression.

分子量

347.29

Formula

C17H12F3N3O2
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]. Burslem GM, et al. Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-Mediated Targeted Protein Degradation. Cancer Res. 2019 Sep 15;79(18):4744-4753.

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