BMX Kinase
The TEC kinases are the second-largest family within the nonreceptor tyrosine kinases of the human genome. The family comprises the five members: tyrosine kinase expressed in hepatocellular carcinoma (TEC), Bruton’s tyrosine kinase (BTK), IL-2 inducible T-cell kinase (ITK), tyrosine–protein kinase TXK (TXK), and bone marrow kinase on chromosomeX (BMX).Bone marrow kinase on chromosome X (BMX) is a cytosolic tyrosine kinase and a member of the TEC kinase family. BMX is expressed in hematopoietic cells of the myeloid lineage where it participates in the immune response. BMX differs from other TEC kinases as its TH domain lacks the proline-rich region and, in addition, its SH3 domain shows a slightly differing sequence.
BMX is expressed in cells of the myeloid lineage, such as granulocytes and monocytes, as well as in the endocardium and the cardiac endothelium. BMX expression has also been demonstrated in several types of cancer, including prostate and breast. In the inflammatory response BMX regulates the secretion of proinflammatory cytokines induced by TNFα, IL-1β, and TLR agonists. It is required for the activation of the MAP kinase and NFκB pathways and acts at the level of the essential TAK1/TAB complex. Cellular regulation of the IL-8 promoter by BMX is dependent on membrane localization mediated by its pleckstrin homology domain, as well as on BMX kinase activity. BMX deficiency confers protection from arthritis in a mouse model known to be dependent on macrophages and IL-1β. Genetic replacement of BMX with a kinase-inactive allele surprisingly restored susceptibility to arthritis, suggesting that in vivo BMX kinase activity can be dispensable.
References
1.Cenni B,et al. Int Rev Immunol. 2012 Apr;31(2):166-73.
BMX is expressed in cells of the myeloid lineage, such as granulocytes and monocytes, as well as in the endocardium and the cardiac endothelium. BMX expression has also been demonstrated in several types of cancer, including prostate and breast. In the inflammatory response BMX regulates the secretion of proinflammatory cytokines induced by TNFα, IL-1β, and TLR agonists. It is required for the activation of the MAP kinase and NFκB pathways and acts at the level of the essential TAK1/TAB complex. Cellular regulation of the IL-8 promoter by BMX is dependent on membrane localization mediated by its pleckstrin homology domain, as well as on BMX kinase activity. BMX deficiency confers protection from arthritis in a mouse model known to be dependent on macrophages and IL-1β. Genetic replacement of BMX with a kinase-inactive allele surprisingly restored susceptibility to arthritis, suggesting that in vivo BMX kinase activity can be dispensable.
References
1.Cenni B,et al. Int Rev Immunol. 2012 Apr;31(2):166-73.
Tyrosine Kinase
BMX Kinase
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CTN06
产品货号 : M16983
cas no: ——
CTN06 是一种有效的 Etk (BMX) 和 Btk 双重抑制剂,IC50 分别为 200 和 50 nM。 -
CHMFL-BMX-078
产品货号 : M12769
cas no: 1808288-51-8
CHMFL-BMX-078 是一种高选择性、有效的 II 型不可逆 BMX 激酶抑制剂,IC50 为 11 nM。 -
BMX-IN-1
产品货号 : M11829
cas no: 1431525-23-3
BMX-IN-1 (CAS 1431525-23-3) 是一种有效、选择性、不可逆的 BMX 激酶抑制剂,IC50 为 8 nM。 -
CTA095
产品货号 : M11112
cas no: 1265823-05-9
CTA095 (CTA-095) 是一种有效的 Etk (BMX) 和 Src 双重抑制剂,IC50 分别为 60 和 120 nM。