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首页-小分子抑制剂&激动剂-Tyrosine Kinase-BMX Kinase-IHMT-15130
IHMT-15130

Chemical Structure : IHMT-15130

CAS No.:

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IHMT-15130 (IHMT15130)

货号: PC-24630Not For Human Use, Lab Use Only.

IHMT-15130 is a potent, selective and irreversible BMX kinase inhibitor with IC50 of 1.47 nM, covalently targets Cys496 of BMX.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

IHMT-15130 is a potent, selective and irreversible BMX kinase inhibitor with IC50 of 1.47 nM, covalently targets Cys496 of BMX.
IHMT-15130 displayed selectivity over CSK kinase (IC50 > 25,000 nM), compare with BTK/BMX dual inhibitor Ibrutinib.
IHMT-15130 achieved 10-fold selectivity of BMX over BTK kinase.
IHMT-15130 has IC50 of 1.8 nM for engineered BaF3 cells stably expressing TEL-fused BMX kinase (BaF3-TEL-BMX).
IHMT-15130 dose-dependently inhibits the phosphorylation of BMX with EC50 of 3.4 nM in Western blotting using BaF3-TEL-BMX cells lines.
IHMT-15130 binds to the Cys496 of BMX in the ATP binding site, exhibits potent binding affinity to BMX kinase with Ki of 24.5 nM.
dose-dependently reduces LPS-activated phosphorylation levels of BMX, also suppresses BMX-induced tyrosine phosphorylation of STAT3, p38, JNK, and NF-κB in RAW264.7 cells.
IHMT-15130 dose-dependently suppresses the secretion of pro-inflammatory cytokines such as IL-1β, IL-6, and TNF-α in both human PBMC and murine BMDM cells.
IHMT-15130 dose-dependently inhibits the phosphorylation of BMX kinase and its downstream MAPK, AKT, S6K, and RPS6 signals.
IHMT-15130 effectively reduced the secretion of inflammatory cytokines, alleviated angiotensin II (Ang II)-induced myocardial hypertrophy in a murine model.

物理化学性质&存储条件

分子量 454.41
分子式 C22H17F3N6O2
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

N-(3-(2-Oxo-2-((3-(5-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)amino)ethyl)phenyl)acrylamide

参考文献

1. Qi S, et al. ACS Chem Biol. 2025 May 19. doi: 10.1021/acschembio.4c00875.

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