Btk, a member of the Tec family of kinases, is well-known for its function in B-cell activation and B-cell antigen receptor (BCR) signaling.
Btk is a new target for diseases with abnormal B cell activity because it is essential for B cell development and activation through the BCR signaling pathway. The human primary immune deficiency disease X-linked agammaglobulinemia (XLA), which is caused by a mutation in the Btk gene, highlights the importance of Btk, a kinase that is only expressed in B cells and myeloid cells.The BCR signaling pathway depends on Btk in many ways. B cell receptor oligomerization, Syk and Lyn kinase activation, and Btk kinase activation are all caused by antigen binding to the BCR. When Btk is activated, it joins forces with proteins like BLNK, Lyn, and Syk to form a signaling complex that phosphorylates phospholipase C (PLC)2. This results in transcriptional changes that promote B cell survival, proliferation, and/or differentiation by releasing intracellular Ca2+ stores downstream and propagating the BCR signaling pathway through extracellular signal-regulated kinase and NF-B signaling.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V5248 | BTK inhibitor 27 | 2230724-66-8 | BTK inhibitor 27, compound 27 in the cited reference below, is apyrrolo[2,3-d]pyrimidine based BTK inhibitor with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM. |
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V0646 | CGI1746 | 910232-84-7 | CGI1746 (CGI-1746) is a reversible/non-covalent and highly selective small-molecule inhibitor of the Brutons tyrosine kinase-Btk with potential anti-inflammatory activity. |
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V0645 | CNX-774 | 1202759-32-7 | CNX-774 (CNX774) is an irreversible/covalent, orally bioavailable, and highly selective inhibitor of BTK (Brutons tyrosine kinase) with potential anticancer activity. |
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V0643 | Ibrutinib (PCI-32765) | 936563-96-1 | Ibrutinib(formerly PCI32765; trade name Imbruvica), an approved anticancer drug, is a covalent/irreversible and orally bioavailableBrutons tyrosine kinase (Btk) inhibitor with potential anti-cancer activity. |
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V0647 | LFM-A13 | 244240-24-2 | LFM-A13 (LFM-A1-3) is a novel, potent and specific Brutons tyrosine kinase (BTK) inhibitor with potential anticancer activity. |
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V4775 | Nemtabrutinib (ARQ-531) | 2095393-15-8 | Nemtabrutinib (ARQ531; ARQ-531; MK-1026) is a novel, potent, orally bioavailable, and reversible / non-covalent BTK (Brutons Tyrosine Kinase) inhibitor with potential antitumor activity. |
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V0649 | ONO-4059 analogue | 1351635-67-0 | ONO-4059 analogue, an analogue of ONO-4059, is a novel, covalent, selective and orally bioavailable BTK inhibitor with potential anticancer and anti-inflammatory activity. |
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V3948 | Pirtobrutinib (LOXO-305) HCl | Pirtobrutinib HCl (formerly known as LOXO-305; RXC 005), the hydrochloride salt ofPirtobrutinib, is a novel, potent, selectivenon-covalent / reversibleBrutons tyrosine kinase (BTK) inhibitor that is under investigation for the treatment of cancer. | |
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V27730 | Poseltinib | 1353552-97-2 | Poseltinib (HM71224; LY3337641; HM-71224; LY-3337641) is a covalent/irreversible BTK (Bruton's tyrosine kinase) tyrosine kinase inhibitor with the potential for the treatment ofrheumatoid arthritis. |
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V32253 | Remibrutinib (LOU064) | 1787294-07-8 | Remibrutinib(LOU-064) is a potent, highly selective and orally bioavailable covalent inhibitor of bruton tyrosine kinase (BTK) with an IC50 of 0.023μM. |
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V2085 | Rilzabrutinib (PRN1008) | 1575596-29-0 | Rilzabrutinib (PRN-1008) is a novel, highly potent, and reversiblecovalentinhibitor ofBTK(Brutons Tyrosine Kinase) being studied for treating rheumatoid arthritis. |
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V0648 | RN486 | 1242156-23-5 | RN486 (RN-486) is a novel, potent, reversible and selective BTK (Brutons tyrosine kinase) inhibitorwith potential anti-inflammatory activity. |
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V83209 | sofnobrutinib (AS-0871) | 1646608-10-7 | Sofnobrutinib (AS0871) is an orally bioactive BTK inhibitor, with IC 50 s of 4.2 nM and 0.39 nM for activated and unactivated BTK, respectively. |
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V0644 | Spebrutinib (CC292; AVL292) | 1202757-89-8 | Spebrutinib (formerly AVL-292; CC-292; SBT) is a covalent/irreversible, orally bioactive, and highly selective inhibitor of Brutons agammaglobulinemia tyrosine kinase/BTK inhibitor with potential antitumor activity. |
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V16484 | Tirabrutinib HCl | 1439901-97-9 | Tirabrutinib HCl (formerly known as ONO-4059;GS4059; ONO-WG-307; Steboronine), the hydrochloride salt of tirabrutinib, is a selective, covalent/irreversible and orally bioavailableBTK inhibitor approved in Japan for cancer treatment. |
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V83231 | ZNL-0325 | ZNL0325 is a covalent kinase probe/inhibitor that inhibits multiple kinases including BTK, EGFR, BLK, and JAK3. |
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