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BTK

BTK

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.

BTK related products

Structure Cat No. Product Name CAS No. Product Description
(R)-Acalabrutinib V87996 (R)-Acalabrutinib 1952316-43-6 (R)-Acalabrutinib ((R)-ACP-196) is an isomer of Acalabrutinib.
(R)-NX-2127 V87995 (R)-NX-2127 3024312-52-2 (R)-NX-2127 (compound 28) is an orally active Bruton's tyrosine kinase (Btk) degrader.
(Z)-LFM-A13 V0647 (Z)-LFM-A13 244240-24-2 (Z)-LFM-A13 (LFM-A1-3) is a novel, potent and specific Brutons tyrosine kinase (BTK) inhibitor with potential anticancer activity.
ABBV-992 V89055 ABBV-992 2792171-84-5 ABBV-992 is a potent and selective BTK inhibitor.
BIIB129 V87994 BIIB129 2770960-52-4 BIIB129 is a covalent, selective, blood-brain barrier-penetrating small molecule inhibitor of Bruton's tyrosine kinase (BTK).
BTK inhibitor 27 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.
Btk substrate peptide V99657 Btk substrate peptide The Btk substrate peptide is a peptide substrate corresponding to residues 217-229 of human Bruton's tyrosine kinase (Btk), of which the tyrosine at residue 223 is the major autophosphorylation site of Btk.
BTK-IN-36 V87993 BTK-IN-36 2502301-31-5 BTK-IN-36 (S-016) is a BTK inhibitor with IC50 of 0.5 nM.
BTK-IN-38 V93724 BTK-IN-38 2758410-51-2 BTK-IN-38 (Example 125) is a potent BTK inhibitor.
CGI1746 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.
CNX-774 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.
I-As-1 V87992 I-As-1 I-As-1 is a potent inhibitor of Bruton's tyrosine kinase (BTK) with IC50 of 2.35 nM.
Nemtabrutinib (ARQ-531) 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.
ONO-4059系列物 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.
Poseltinib 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.
QL47B TFA V87991 QL47B TFA QL47B TFA is a biotinylated analog of QL47 and is a potent BTK inhibitor with an IC50 of 1.3 μM.
RN486 V0648 RN486 1242156-23-5 RN486 (RN-486) is a novel, potent, reversible and selective BTK (Brutons tyrosine kinase) inhibitorwith potential anti-inflammatory activity.
sofnobrutinib (AS-0871) 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.
WS-11 V94049 WS-11 2759280-09-4 WS-11 is a non-covalent, reversible BTK inhibitor with IC50 values of 3.9 nM and 2.2 nM for wild-type and C481S mutant BTK, respectively.
依鲁替尼 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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