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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BMX Kinase-IHMT-15137
IHMT-15137

Chemical Structure : IHMT-15137

CAS No.:

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IHMT-15137 (IHMT15137)

货号: PC-26499Not For Human Use, Lab Use Only.

IHMT-15137 is a potent and selective, irreversible BMX inhibitor with IC50 of 26.97 nM, overcomes chemoresistance in SCLC.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

IHMT-15137 is a potent and selective, irreversible BMX inhibitor with IC50 of 26.97 nM, overcomes chemoresistance in SCLC.
IHMT-15137 displays potent anti-proliferative activity with GI50 of 0.83 nM in TEL-BMX-BaF3 cells.
IHMT-15137 significantly stabilized the BMX protein in cellular thermal shift assay (CETSA) assays, protected BMX from proteolysis in a dose-dependent manner in cell lysates from H446DDPR and H69AR cells.
IHMT-15137 (0-10 uM) effectively inhibited the phosphorylation of BMX (Tyr566) in a dose-dependent manner in TEL-BMX-BaF3 cells, also induced dose-dependent decrease in the phosphorylation levels of BMX (Tyr566), ERK1/2 (Thr202/Tyr204), and STAT3 (Tyr705) in chemoresistant SCLC cells, H446DDPR and H69AR.
IHMT-15137 effectively overcomes chemoresistance in SCLC through multiple mechanisms, including suppressing cell proliferation, inducing apoptosis, inhibiting metastasis, and impairing DNA repair, which are mediated through disruption of the BMX-ERK1/2-Cyclin D1/CDK4/6-E2F1 signaling axis.
IHMT-15137 overcomes cisplatin resistance in SCLC PDC models.

物理化学性质&存储条件

分子量 446.43
分子式 C21H21F3N6O2
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-acryloylpiperidin-3-yl)-N-(3-(5-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)acetamide

参考文献

1. Wu T, et al. Signal Transduct Target Ther. 2026 Apr 8;11(1):125.

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