BMX Kinase (inhibitors, antagonists, agonists)-ProbeChem.com

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BMX kinase (also termed ETK) is a member of the TEC family of non-receptor tyrosine kinases (which also includes ITK, TEC, BTK and TXK), and is the major member of this family expressed in epithelial cells, including prostate epithelium. Similar to the SRC family of kinases, the TEC kinases contain core SH3, SH2 and kinase domains, binds to membrane-associated PIPs in a manner similar to Akt.

BMX is further activated by the subsequent phosphorylation of a tyrosine in its kinase domain by membrane-associated SRC. The activation of BMX in response to PI-3K signaling, which is increased in prostate cancer (PCa) due to PTEN loss, suggests a potential role for BMX in PCa. Indeed, BMX expression is increased in PCa, and transgenic over-expression of BMX in mouse prostate epithelium causes hyperplasia and contributes to development of dysplastic lesions resembling human prostate intraepithelial neoplasia (PIN). The irreversible BMX kinase inhibitor, BMX-IN-1, demonstrates antiproliferation efficacy against prostate cancer cells.

References:

1. Liu F, et al. ACS Chem Biol. 2013 Jul 19;8(7):1423-8.

2. Qiu Y, et al. Proc Natl Acad Sci U S A. 1998 Mar 31;95(7):3644-9.

3. Tu T, et al. Cancer Res. 2008 Apr 15;68(8):2861-9.

4. Liang X, et al. J Med Chem. 2017 Mar 9;60(5):1793-1816.

Cat. No.	Product Name	Information
PC-73285	JS25 BMX inhibitor	JS25 is a potent, selective, covalent TEC family of non-receptor tyrosine kinases (BTK, ITK, TXK and BMX) inhibitor with IC50 of 3.5 and 5.8 nM for BMX and BTK, respectively.
PC-35181	CTA095 Etk/Bmx inhibitor, Src inhibitor	CTA095 (CTA-095) is a potent Etk (BMX) and Src dual inhibitor with IC50 of 60 and 120 nM, respectively, shows no significant inhibition on Btk and Yes at 10 uM.
PC-35180	CTN06 BMX/BTK inhibitor	CTN06 is a potent Etk (BMX) and Btk dual inhibitor with IC50 of 200 and 50 nM, respectively.
PC-35179	CHMFL-BMX-078 BMX inhibitor	CHMFL-BMX-078 is a highly selective, potent, type II irreversible BMX kinase inhibitor with IC50 of 11 nM.
PC-46005	BMX-IN-1 BMX inhibitor	BMX-IN-1 (CAS 1431525-23-3) is a potent, selective, irreversible inhibitor of BMX kinase with IC50 of 8 nM.
PC-73286	JS24 BMX inhibitor	JS24 is a potent, selective, covalent TEC family of non-receptor tyrosine kinases (BTK, ITK, TXK and BMX) inhibitor with IC50 of 7.5 and 11.1 nM for BMX and BTK, respectively.

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