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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M1825 | PCI-32765 | PCI-32765 (Ibrutinib) is a potent, selective and orally bioavailable irreversible inhibitor of BTK with IC50 value of 0.46 nM. |
| M21293 | BCPyr | BCPyr is a new candidate BTK degradation agent (DC50 = 800 nM). |
| M21284 | BMS-986143 | BMS-986143 is a potent, reversible inhibitor of tyrosine kinase (BTK), which has been successfully targeted by a number of irreversible tumor compounds. |
| M21222 | BIIB091 | The reversible BTK kinase inhibitor BIIB091 is a highly selective phase I clinical candidate compound for multiple sclerosis. |
| M21189 | TAK-020 | TAK-020 is a highly selective oral covalent BTK inhibitor with a promising safety and tolerability profile for both hematologic malignancies and autoimmune diseases. |
| M20631 | BTK inhibitor 1 (Compound 27) | BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM. |
| M20290 | WYE-175837 | WYE-175837 is a BTK inhibitor |
| M14882 | Ibrutinib-biotin | Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, extracted from patent WO2014059368A1 Compound 1-5, has an IC50 of 0.755-1.02 nM for BTK. |
| M14881 | GDC-0834 Racemate | GDC-0834 Racemate is the racemate form of GDC-0834, which is a potent and selective BTK inhibitor with in vitro IC50s of 5.9 and 6.4 nM in biochemical and cellular assays, respectively. |
| M14880 | BMX-IN-1 | BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity. |
| M14879 | (±)-Zanubrutinib | (±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor. |
| M11431 | Poseltinib | Poseltinib is an orally active, selective, irreversible small-molecule Bruton tyrosine kinase (BTK) inhibitor with an IC50 of 1.95 nM and 0.3, 2.3, and 2.4 fold selective action against BMX, TEC, and TXK, respectively. Poseltinib covalently binds to the active site of BTK (cysteine 481 residue) and effectively inhibits B cell receptor (BCR), Fc receptor (FcR), and Toll-like receptor (TLR) mediated signaling. |
| M10896 | Vecabrutinib | Vecabrutinib (SNS-062) is a potent, non-covalent BTK and ITK inhibitor,Kd The values are 0.3 nM and 2.2 nM, respectively. Vecabrutinib for ITK IC50 The value is 24 nM. |
| M10605 | Rilzabrutinib | Rilzabrutinib, also known as PRN1008, is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK) with IC50 of 1.3 nM. |
| M10604 | Pirtobrutinib (LOXO-305) | Pirtobrutinib (LOXO-305; LY 3527727; RXC-005) is a highly selective and non-covalent next generation BTK inhibitor, which inhibits diverse BTK C481 substitution mutations. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases. |
| M10500 | Remibrutinib (LOU064) | Remibrutinib (LOU064) is a potentially best-in-class "best-in-class" orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM and an IC50 value of 0.23 μM for inhibition of BTK activity in blood. Remibrutinib can be used to study chronic urticaria (CU). |
| M10274 | Tolebrutinib | Tolebrutinib (SAR442168) is a potent, selective, orally active and blood-brain barrier capable bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 0.4 and 0.7 nM in Ramos B cells and HMC microglia, respectively. Tolebrutinib has an effect on central nervous system immunity. Tolebrutinib can be used in multiple sclerosis (MS) studies. |
| M10095 | Orelabrutinib | Orelabrutinib is an orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK). |
| M10025 | Zanubrutinib | Zanubrutinib (BGB-3111) is a potent and highly selective small molecule inhibitor of Bruton's tyrosine kinase (BTK). |
| M9958 | ARQ 531 | ARQ 531 is a potent reversible inhibitor of BTK (IC50 = 0.85 nM), exhibits potent antitumor activity in ibrutinib-resistant diffuse large B-cell lymphoma. |
| M9889 | PCI-29732 | PCI-29732 is a potent, reversible BTK inhibitor. |
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