Btk
Bruton tyrosine kinase
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 plays a crucial role in B cell development and activation through the BCR signaling pathway and represents a new target for diseases characterized by inappropriate B cell activity. Btk is a kinase expressed exclusively in B cells and myeloid cells and has a well characterized, vital role in B cells highlighted by the human primary immune deficiency disease, X-linked agammaglobulinemia (XLA), which results from mutation in the Btk gene. Btk plays an essential role in the BCR signaling pathway. Antigen binding to the BCR results in B cell receptor oligomerization, Syk and Lyn kinase activation, followed by Btk kinase activation. Once activated, Btk forms a signaling complex with proteins such as BLNK, Lyn, and Syk and phosphorylates phospholipase C (PLC)γ2. This leads to downstream release of intracellular Ca2+ stores and propagation of the BCR signaling pathway through extracellular signal-regulated kinase and NF-κB signaling, ultimately resulting in transcriptional changes to foster B cell survival, proliferation, and/or differentiation.
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Btk Related Products (271)
Related Products (271)
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Recombinant Proteins (19)
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Antibodies (3)
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BMX-IN-1
0 ImagesSynonyms: BMX kinase inhibitorBMX-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.
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Ibrutinib Racemate
0 ImagesCat. No.: HY-10997ACAS No.: 936563-87-0Synonyms: PCI-32765 RacemateIbrutinib Racemate (PCI-32765 Racemate) is the racemate of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with IC50 value of 0.5 nM.
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Branebrutinib
0 ImagesSynonyms: BMS-986195Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with an IC50 of 0.1 nM. Branebrutinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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MT-802
0 ImagesMT-802 is a BTK PROTAC degrader. MT-802 degrades wild-type BTK (DC50 = 14.6 nM) and BTK mutants including E41K, C481S (DC50 = 14.9 nM), C481R, C481Y, C481T, C481F, L528W, and inhibits their Y223 phosphorylation. BI-4732 can be used for the study of Ibrutinib (HY-10997)-resistant chronic lymphocytic leukemia (CLL). (Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-141371), E3 ligase ligand-linker conjugate (HY-176340)).
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PROTAC BTK Degrader-1
0 ImagesPROTAC BTK Degrader-1 is a selective, orally active BTK PROTAC degrader with a DC50 of 5.8 nM. PROTAC BTK Degrader-1 induces ubiquitination and degradation of wild-type and mutant (C481S, T316) BTK proteins via the CRBN-mediated pathway. PROTAC BTK Degrader-1 exhibits anticancer activity against diffuse large B-cell lymphoma. PROTAC BTK Degrader-1 can be used in lymphoma-related research.
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Corubrutinib
0 ImagesSynonyms: BIIB091Corubrutinib (BIIB091) is an orally active BTK inhibitor with an IC50 of <0.5 nM, Kd of 0.07 nM, and >500-fold kinome selectivity. Corubrutinib suppresses B cell activation, proliferation, differentiation, antibody production, antigen presentation, cytokine secretion, and myeloid cell effector functions. Corubrutinib exhibits favorable pharmacokinetic and preclinical safety profiles, including low genotoxic potential, minimal hepatotoxicity, and no major transporter or CYP inhibition. Corubrutinib can be used for the research of multiple sclerosis.
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Luxeptinib
0 ImagesSynonyms: CG-806Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells.
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PCI-33380
0 ImagesPCI-33380 is a fluorescent probe ( (Ex=532 nm, Em=555 nm). PCI-33380 consists of a (BTK) inhibitor PCI-32765 (HY-10997) attaching with a Bodipy-FL fluorophore via a piperazine linker. PCI-33380 binds predominantly to Btk in B cell lysates with cell permeable activity. PCI-33380 can be used for imaging live cancer cells such as non-Hodgkin lymphoma research
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Poseltinib
0 ImagesSynonyms: HM71224; LY3337641Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC50 of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis.
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GBD-9
0 ImagesGBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML).
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PF-06658607
0 ImagesPF-06658607 is an alkynylated irreversible Brutons tyrosine kinase (BTK) inhibitor that covalently reacts with active site cysteines in the ATP-binding pocket. PF-06658607 can be used to detect "off "-targets for covalent kinase inhibitors in cancer cells. The alkyne moiety allows for azide-based detection probe via copper-catalyzed click chemistry.
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KIN-8194
0 ImagesKIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice.
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QL47
0 ImagesQL47, a broad-spectrum antiviral agent, inhibits dengue virus and other RNA viruses. QL47 selectively inhibits eukaryotic translation. QL47 is a potent covalent inhibitor of BTK with an IC50 of 7 nM.
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Elsubrutinib
0 ImagesSynonyms: ABBV-105
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Tirabrutinib hydrochloride
0 ImagesSynonyms: ONO-4059 hydrochloride; GS-4059 hydrochlorideTirabrutinib (ONO-4059) hydrochloride is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies.
