| 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. |
| M58129 | BIIB129 | BIIB129 is a covalent, selective inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier. BIIB129 inhibits the activity of BTK by covalently binding to Cys481 in BTK, thereby affecting the function of B cells and myeloid cells. |
| M55647 | (R)-NX-2127 | (R)-NX-2127 (compound 28) is a first-in-class, orally bioavailable Bruton’s Tyrosine Kinase (Btk) degrader. (R)-NX-2127 mediates the degradation of transcription factors IKZF1 and IKZF3 through molecular glue interactions with the cereblon E3 ubiquitin ligase complex. NX-2127 degrades common BTK resistance mutants, including BTKC481S. |
| M43813 | NX-2127 | NX-2127 is an orally active, potent BTK inhibitor that induces degradation of mutant BTKC481S in cells, as well as inhibits the proliferation of BTKC481S mutant TMD8 cells. In addition, NX-2127 stimulates T cell activation and increases IL-2 production in primary human T cells. |
| 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. |
| 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 first-in-class, highly selective, non-covalent, next-generation BTK inhibitor with an IC50 of 5.69 nM in WT BTK HEK cells.Pirtobrutinib's selectivity for BTK more than 300 times more selective than other 370 kinases. Pirtobrutinib can be used in studies related to chronic lymphocytic leukemia (CLL). |
| M10500 | Remibrutinib | 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 with Kiapp values of 8.2, 4.6, and 2.5 nM for BTK, Lck, and Lyn, respectively, and has only modest inhibitory activity against Itk, another Tec family kinase. In addition, PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP binding site of ABCG2. |
| M9628 | Branebrutinib | Branebrutinib (BMS-986195) is a potent, covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with IC50 of 0.1 nM. |
| M9166 | BMS-986142 | BMS-986142 is a potent, selective, reversible BTK inhibitor, shows BTK IC50 = 0.5nM; human WB IC50 = 90 nM. |
| M8941 | Fenebrutinib | GDC-0853 (Fenebrutinib) is a potent, selective and non-covalent bruton tyrosine kinase (Btk) inhibitor with a Ki value of 0.91 nM against BRK. |
| M8887 | Btk inhibitor 2 | Btk inhibitor 2 (BGB-3111) is a Brutons tyrosine kinase (BTK) inhibitor. |
| M7536 | BMS-935177 | BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective. |
| M6907 | (Z)-LFM-A13 | LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM. |
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