Signaling Pathway

Btk

Btk

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Bruton's tyrosine kinase (BTK) also known as tyrosine-protein kinase BTK is an enzyme that in humans is encoded by the BTK gene. BTK is a kinase that plays a crucial role in B-cell development. Its exact mechanism of action remains unknown, but it plays a crucial role in B cell maturation as well as mast cell activation through the high-affinity IgE receptor. Btk contains a PH domain that binds phosphatidylinositol (3,4,5)-trisphosphate (PIP3). PIP3 binding induces Btk to phosphorylate phospholipase C, which in turn hydrolyzes PIP2, a phosphatidylinositol, into two second messengers, inositol triphosphate (IP3) and diacylglycerol (DAG), which then go on to modulate the activity of downstream proteins during B-cell signalling.

Btk Inhibitors & Modulators (24)

Product Name Catalog No. Brief Description
Acalabrutinib

HY-17600

Acalabrutinib (ACP-196) is a second-generation, selective, irreversible inhibitor of BTK (Bruton's tyrosine kinase) that has improved pharmacologic features, including favorable plasma exposure, rapid oral absorption, a short half-life, and the absence of irreversible targeting to alternative kinases, such as EGFR,TEC, and ITK.

AVL-292

HY-18012

AVL-292 is a covalent, highly selective, orally active small molecule inhibitor of Btk with IC50 value of 0.5 nM; >1400-fold selectivity over the other kinases assayed.

AVL-292 benzenesulfonate

HY-18012A

AVL-292 benzenesulfonate is a covalent, highly selective, orally active small molecule inhibitor of Btk with IC50 value of 0.5 nM; >1400-fold selectivity over the other kinases assayed.

BMX-IN-1

HY-80002

BMX-IN-1 is a highly selective and potent irreversible inhibitor which target the cysteine residue in the BMX ATP binding domain.

Btk inhibitor 1

HY-13036

Btk inhibitor 1 is a  pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.

Btk inhibitor 1 hydrochloride

HY-13036C

Btk inhibitor 1 Hcl is a  pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.

Btk inhibitor 1 R enantiomer

HY-13036A

Btk inhibitor 1 R enantiomer is a  pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.

Btk inhibitor 1 R enantiomer hydrochloride

HY-13036B

Btk inhibitor 1R enantiomer Hcl is a  pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.

CGI-1746

HY-11999

CGI-1746 is a small-molecule Bruton's tyrosine kinase (Btk) inhibitor.

CNX-774

HY-13943

CNX-774 is a potent, selective, and orally available small molecule inhibitor of Btk (IC50< 1 nM) that forms a ligand-directed covalent bond with Cys-481, a non-conserved amino acid within the active site of the enzyme.

GDC-0834

HY-15427

GDC-0834 is a potent and selective BTK inhibitor with in vitro IC50s of 5.9 and 6.4 nM in biochemical and cellular assays, respectively.

GDC-0834 Racemate

HY-15427A

GDC-0834 Racemate is the racemate form of GDC-0834, which is a potent and selective BTK inhibitor with in vitro IC50s of 5.9 and 6.4 nM in biochemical and cellular assays, respectively.

GDC-0834 S-enantiomer

HY-15427B

GDC-0834 S-enantiomer is the S-enantiomer of GDC-0834.

GDC-0853

HY-19834

GDC-0853 is a potent and orally BTK inhibitor.

Ibrutinib-biotin

HY-100342

Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, extracted from patent WO2014059368A1 Compound 1-5, has an IC50 of 0.755-1.02 nM for BTK.

LFM-A13

HY-18009

LFM-A13 is a potent and selective inhibitor of Btk with IC50 of 17.2 uM; also inhibits PLK3 with IC50 of 7.2 uM.

ONO-4059

HY-15771

ONO-4059 is a highly selective, orally bioavailable BTK inhibitor with a potency (IC50) of 2.2 nM.

ONO-4059 analog

HY-18951

The product is the analog of ONO-4059, ONO-4059 is a highly potent and selective Btk inhibitor with an IC50 in the sub-nM range.

ONO-4059 hydrochloride

HY-15771A

ONO-4059 is a selective and novel inhibitor of BTK with IC50 2.2 nm, ONO-4059 binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development.

PCI 29732

HY-18010

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.