Chemical Structure : IHMT-15137
CAS No.:
IHMT-15137
(IHMT15137)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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446.43
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Formula
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C21H21F3N6O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(1-acryloylpiperidin-3-yl)-N-(3-(5-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)-1H-pyrazol-4-yl)acetamide
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References
1. Wu T, et al. Signal Transduct Target Ther. 2026 Apr 8;11(1):125.
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