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首页-小分子抑制剂&激动剂-Autophagy-CIM7
CIM7

Chemical Structure : CIM7

CAS No.: 904829-52-3

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CIM7 (CMA Inhibitory Molecule 7)

货号: PC-24817Not For Human Use, Lab Use Only.

CMA Inhibitory Molecule 7 (CIM7) is a potent and selective chaperone-mediated autophagy (CMA) inhibitor with IC50 of 75 nM (A549 cells, 24h), functions by disrupting the NCoR1/RARα interaction and altering the CMA regulatory transcriptional program to suppress CMA.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CMA Inhibitory Molecule 7 (CIM7) is a potent and selective chaperone-mediated autophagy (CMA) inhibitor with IC50 of 75 nM (A549 cells, 24h), functions by disrupting the NCoR1/RARα interaction and altering the CMA regulatory transcriptional program to suppress CMA.
CIM7 potently inhibit CMA activity in additional NSCLC cell lines, H1703 and H23, with IC50 of 355 and 195 nM respectively, which harbor different Kras and TP53 mutation statuses.
CIM7 (5 uM) has no inhibitory effect on CMA activity in various non-tumorigenic cell lines, has no effect on macroautophagy.
CIM7 disrupts the NCoR1/RARα interaction, directly binds recombinant RARα with KD of 2 uM.
CIM7 does not alter the binding of the coactivator SRC to RARα, selectively regulates only co-repressor NCoR1 binding to RARα.
CIM7 is specific to RARα and does not interact with the other RAR family members.
CIM7 treatment preferentially impacted the proteome related to protein folding, chromatin, cytoplasmic translation, and the nucleosome in A549 cells, CIM7 inhibits degradation of a subset of CMA substrates in NSCLC cells.
CIM7 inhibits viable cell population of all NSCLC cell lines with IC50 of 15-24 uM.
CIM7 treatment (25 mg/kg) reduces CMA and NSCLC tumor growth in xenograft mouse model of A549 cells.

物理化学性质&存储条件

分子量 455.43
分子式 C20H17F4N3O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-((1-(4-fluorobenzyl)-5-(hydroxymethyl)-1H-imidazol-2-yl)thio)-N-(4-(trifluoromethoxy)phenyl)acetamide

参考文献

1. McCabe M, et al. EMBO Mol Med. 2025 Jun 9. doi: 10.1038/s44321-025-00254-y.

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