Bruton's Tyrosine Kinase
Bruton's Tyrosine Kinase (BTK) is member of the Tec family that is critically important for the growth, differentiation and activation of myeloid-, mast- and B-cells. BTK is initially activated by membrane localization which is stimulated by the generation of PIP3.
Bruton's Tyrosine Kinase Inhibitors |
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|---|---|
| Cat. No. | Product Name / Activity |
| 6965 | CGI 1746 |
| Potent, reversible BTK inhibitor | |
| 6813 | Ibrutinib |
| Potent and selective BTK inhibitor | |
| 5592 | LCB 03-0110 dihydrochloride |
| Potent BTK inhibitor; also inhibits c-Src, DDR2 and Syk | |
| 1300 | LFM-A13 |
| Potent, selective BTK inhibitor | |
| 5012 | PCI 29732 |
| Potent BTK inhibitor | |
| 4710 | PF 06465469 |
| Potent inhibitor of interleukin-2 inducible T cell kinase (ITK). Also inhibits BTK | |
Degraders |
|
| Cat. No. | Product Name / Activity |
| 7160 | DD 03-171 |
| Potent and selective BTK Degrader | |
| 8856 | NX 5948 New |
| Potent and selective BTK Degrader (PROTAC®) | |
Bruton's Tyrosine Kinase (BTK) is member of the Tec family that is critically important for the growth, differentiation and activation of myeloid-, mast- and B-cells. BTK is activated firstly by membrane localization stimulated by PIP3 generation, and subsequently, by transphosphorylation of Tyr-551 by Src family kinases.
Activated BTK is involved in the phosphorylation of a number of signaling molecules involved in the PLCγ, JNK and p38 MAPK pathways, leading to Ca2+ mobilization, mRNA stabilization and the induction of NF-κB and AP-1 transcription factors. BTK activity is negatively regulated by a number of proteins including inhibitor of BTK (IBTK), Sab and c-Cbl. Mutations in this enzyme are known in humans and result in the immunological disorder X-linked agammaglobulemia.