Brutons Tyrosine Kinase (BTK) Inhibitors: Small Molecules and Peptides
Bruton tyrosine kinase (Btk) is a 75 kDa cytoplasmic protein tyrosine kinase that is widely expressed in hematopoietic cells. Btk is required for B cell receptor signaling and B cell development. Defects in Btk result in X-linked agammaglobulinemia which is characterized by a severely decreased level of circulating antibodies. Like other Tec family kinases, Btk contains a Pleckstrin homology domain, a Tec homology domain, an SH3 domain, an SH2 domain, and a protein kinase domain. Association of the Btk SH2 domain with the B cell linker protein (BLNK) is required for the activation of PLC? by Btk. The autophosphorylation of Tyr223 facilitates the interaction of Btk with activated Syk. Within the SH2 domain (aa 280 - 377), human Btk shares 99% aa sequence identity with mouse and rat Btk.
7 results for "Brutons Tyrosine Kinase (BTK) Inhibitors Small Molecules and Peptides" in Products
7 results for "Brutons Tyrosine Kinase (BTK) Inhibitors Small Molecules and Peptides" in Products
Brutons Tyrosine Kinase (BTK) Inhibitors: Small Molecules and Peptides
Bruton tyrosine kinase (Btk) is a 75 kDa cytoplasmic protein tyrosine kinase that is widely expressed in hematopoietic cells. Btk is required for B cell receptor signaling and B cell development. Defects in Btk result in X-linked agammaglobulinemia which is characterized by a severely decreased level of circulating antibodies. Like other Tec family kinases, Btk contains a Pleckstrin homology domain, a Tec homology domain, an SH3 domain, an SH2 domain, and a protein kinase domain. Association of the Btk SH2 domain with the B cell linker protein (BLNK) is required for the activation of PLC? by Btk. The autophosphorylation of Tyr223 facilitates the interaction of Btk with activated Syk. Within the SH2 domain (aa 280 - 377), human Btk shares 99% aa sequence identity with mouse and rat Btk.
Potent and selective BTK inhibitor
| Chemical Name: | 1-[(3R)-3-[4-Amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one |
| Purity: | ≥98% (HPLC) |
Potent, selective BTK inhibitor
| Chemical Name: | 2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-butenamide |
| Purity: | ≥98% (HPLC) |
Potent BTK inhibitor
| Chemical Name: | 1-Cyclopentyl-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine |
| Purity: | ≥99% (HPLC) |
Potent, reversible BTK inhibitor
| Chemical Name: | N-[3-[4,5-Dihydro-4-methyl-6-[[4-(4-morpholinylcarbonyl)phenyl]amino]-5-oxo-2-pyrazinyl]-2-methylphenyl]-4-(1,1-dimethylethyl)benzamide |
| Purity: | ≥97% |
Potent and selective BTK Degrader (PROTAC®)
| Chemical Name: | 4-(1,1-Dimethylethyl)-N-[3-[6-[[4-[[4-[6-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]acetyl]amino]hexyl]-1-piperazinyl]carbonyl]phenyl]amino]-4,5-dihydro-4-methyl-5-oxo-2-pyrazinyl]-2-methylphenyl]benzamide |
| Purity: | ≥98% (HPLC) |
Potent c-SRC kinase inhibitor; also inhibits DDR2, BTK and Syk
| Chemical Name: | 3-[[2-[3-(4-Morpholinylmethyl)phenyl]thieno[3,2-b]pyridin-7-yl]amino]phenol dihydrochloride |
| Purity: | ≥98% (HPLC) |
Potent ITK inhibitor; also inhibits BTK
| Chemical Name: | (R)-3-(1-(1-Acryloylpiperidin-3-yl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-N-(3-methyl-4-(1-methylethyl))benzamide |
| Purity: | ≥95% (HPLC) |
