Bruton tyrosine kinase (Btk) is a member of the Tec family kinases with a well-characterized role in B-cell antigen receptor (BCR)-signaling and B-cell activation.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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V79030 | DBt-10 | DBt-10 is an effective BTK degrader. | |
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V69665 | Dihydrodiol-Ibrutinib (PCI-45227) | 1654820-87-7 | Dihydrodiol-Ibrutinib (PCI-45227) is the dihydrodiol bioactive metabolite of ibrutinib, but its inhibitory effect against BTK is approximately 15 times lower than that of ibrutinib. |
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V69680 | Edralbrutinib (TG-1701) | 1858206-58-2 | Edralbrutinib (TG-1701) is a potent BTK inhibitor. |
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V69661 | Elsubrutinib (ABBV-105) | 1643570-24-4 | Elsubrutinib (ABBV-105) is an orally bioactive, specific and irreversible inhibitor of Bruton's tyrosine kinase (BTK). |
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V2135 | Evobrutinib (M2951) | 1415823-73-2 | Evobrutinib is discontinued due to commercial reason. |
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V4147 | Fenebrutinib (GDC-0853) | 1434048-34-6 | Fenebrutinib (formerly RG-7845;GDC-0853) is a novel, potent, selective, orally bioavailable, and noncovalent (reversible) brutons tyrosine kinase (BTK) inhibitor (Ki = 0.91 nM) with anticancer and anti-inflammatory activity. |
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V4521 | GDC-0834 Racemate | 1133432-46-8 | GDC-0834 Racemate is a novel, potent and selectiveBTKinhibitor with an in vitroIC50of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivoIC50of 1.1 and 5.6 μM in mouse and rat, respectively. |
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V69664 | Ibrutinib deacryloylpiperidine (IBT4A) | 330786-24-8 | Ibrutinib deacryloylpiperidine (IBT4A) is an impurity of Ibrutinib. |
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V69658 | Ibrutinib-MPEA | 1710768-30-1 | Ibrutinib-MPEA is an analogue of Ibrutinib. |
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V69698 | JDB175 | 2635328-79-7 | JDB175 is a selective BTK inhibitor (antagonist) with oral activity and excellent BBB (blood-brain barrier) penetration. |
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V69678 | JNJ-64264681 | 2101524-34-7 | JNJ-64264681 is a potent, orally bioactive, selective, irreversible, covalent BTK inhibitor. |
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V69671 | JS25 | 2411771-95-2 | JS25 is a selective covalent inhibitor of BTK (IC50=5.8 nM), which inactivates BTK by chelating Tyr551. |
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V3569 | MT-802 | 2231744-29-7 | MT-802 is a novel and potent PROTAC-mediated degrader which binds fewer off-target kinases than ibrutinib does, thereby inducing BTK knockdown, and recruiting BTK to the cereblon E3 ubiquitin ligase complex to trigger BTK ubiquitination and degradation via the proteasome. |
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V39041 | N-piperidine Ibrutinib HCl | 2231747-18-3 | N-piperidine Ibrutinib HCl,the hydrochloride salt ofN-piperidine Ibrutinib, is an intermediate used in the synthesis of BTK-targetedPROTACs such as SJF620 (DC50 of 7.9 nM for degrading BTK). |
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V69666 | NRX-0492 | 2416130-57-7 | NRX-0492 is an orally bioavailable BTK degrader. |
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V69657 | NX-2127 | 2416131-46-7 | NX-2127 is an orally bioavailable BTK inhibitor that induces degradation of mutant BTKC481S in cells. |
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V69659 | NX-5948 (BTK-IN-24) | 2649400-34-8 | NX-5948 (compound 195) is a potent BTK inhibitor that degrades BTK through the ubiquitin proteolytic pathway. |
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V38770 | Orelabrutinib | 1655504-04-3 | Orelabrutinib (ICP-022;ICP022;ICP 022) is an oral bioavailable, new generation and irreversible/covalent Brutons tyrosine kinase (BTK) inhibitor with the potential to be used for the treatment of cancer such asB-cell lymphomas and autoimmune indications. |
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V4779 | PCI-29732 | 330786-25-9 | PCI 29732 is a novel, potent, selective and irreversible Btk (Brutons tyrosine kinase) inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay. |
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V4778 | PCI-33380 | 1022899-36-0 | PCI-33380 is a novel and irreversible Bruton's Tyrosine Kinase (BTK) inhibitor that was designed based on the ibrutinib scaffold in combination with a fluorescent probe, and has been used in both cellular and in vivo studies that demonstrated the connection between the inhibitor binding event and phenotypic readouts of cellular responses due to the inhibition of Btk functions. |
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