ELMO2 inhibitor C52

Chemical Structure : ELMO2 inhibitor C52

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货号: PC-26567Not For Human Use, Lab Use Only.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

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生物&药学活性

ELMO2 inhibitor C52 is a specific small-molecule Engulfment and cell motility 2 (ELMO2) inhibitor, binds to ELMO2 with a dissociation constant (KD) of 1.0 uM, effectively kills ELMO3-low lung cancer cells and EGFR inhibitor-resistant cells.
C52 shows no binding was observed with the ELMO2 His435Ala (H435A) mutant, suggesting the critical role of HIS-435 in the interaction.
C52 specifically suppressed the viability of mesenchymal ARTICLE IN PRESS ARTICLE IN PRESS like cells compared with epithelial-like cells.
ELMO3 over-expression rescued the cell death phenotype induced by C52 treatment.
Similar to ELMO2 knockdown, C52 suppressed FAK phosphorylation in a concentration-dependent and time-dependent manner, induced autophagy-dependent cell death in NCI-H1299 and A549.
C52 exhibited a significant synergistic effect for suppression lung cancer cell proliferation with FAK inhibitor Defactinib.
C52 significantly suppressed tumor growth in mesenchymal-like A549 xenograft mice, but showed no significant growth inhibition in epithelial-like PC-9 xenograft mice, also failed to suppress the growth of tumors expressing the ELMO2-H435A mutant in vivo.

物理化学性质&存储条件

分子量	464.57
分子式	C29H28N4O2
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-(3-benzyl-4-oxo-3,4-dihydro-5H-pyrimido[5,4-b]indol-5-yl)-N-(4-phenylbutan-2-yl)acetamide

参考文献

1. Li M, et al. Nat Commun. 2026 Apr 17. doi: 10.1038/s41467-026-72062-y.