BTK
Bruton's tyrosine kinase (BTK) belongs to the Tec kinases family of tyrosine protein kinases. It is a crucial terminal kinase in the B cell receptor (BCR) signaling pathway, and essential for the development and activation of B cells. Aberrant activation of B cells is found to play a central role in the pathogenesis of B-cell lymphomas and autoimmune diseases. BTK is involved in multiple signaling pathways,and plays an important role in the B-cell receptor (BCR) signal pathway, including the PI3K, MAPK and NF-κB pathways. After BCR is first activated by phosphorylation, phosphorylated BCR recruits spleen tyrosine kinase (SYK) to the membrane, where SYK is phosphorylated and subsequently phosphorylates BTK. Activated BTK can phosphorylate PLCγ2 in Y753 and Y759, which is critical for lipase activity. BTK may be a potential target for therapy of hematological malignancies and autoimmune diseases.
References
1.Feng Y,et al. Expert Opin Ther Pat. 2019 Apr;29(4):217-241.
References
1.Feng Y,et al. Expert Opin Ther Pat. 2019 Apr;29(4):217-241.
Tyrosine Kinase
BTK
-
JAK3/BTK-IN-1
catalog no : M37669
cas no: 2674036-91-8
JAK3/ BTk-in-1 is a dual JAK3/BTK inhibitor that specifically targets and inhibits Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), two important targets in autoimmune diseases. -
TAK-020
catalog no : M37633
cas no: 1627603-21-7
TAK-020 is a potent covalent inhibitor of Btk with potential antitumor activity for the study of rheumatoid arthritis and immune-related diseases. -
BLK degrader 1
catalog no : M36930
cas no: 3049215-64-4
BLK degrader 1 is a selective B lymphoid tyrosine kinase (BLK) degrader with anticancer activity and can be used for cancer research. -
NX-2127
catalog no : M36530
cas no: 2416131-46-7
NX-2127 (ETX2514 Triethylamine) is an orally active BTK inhibitor that induces degradation of mutant BTKC481S in cells.NX-2127 has potent antiproliferative activity and inhibits the proliferation of BTKC481S mutant TMD8 cells. -
BGB-8035
catalog no : M36520
cas no: 2283349-24-4
BGB-8035 is an orally available, selective and potent BTK inhibitor with antitumor activity that inhibits BTK, TEC and EGFR.BGB-8035 is used in the study of tumors and autoimmune diseases.