Btk

Bruton tyrosine kinase

Btk

Related Products

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.

Btk Related Products (182)
Recombinant Proteins (3)
Antibodies (3)

By Effects:	Inhibitors (155) Degraders (16)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-10997

Ibrutinib	Inhibitor	99.97%
Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM.

HY-17600

Acalabrutinib	Inhibitor	99.88%
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-131328

Pirtobrutinib	Inhibitor	99.88%
Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations. Pirtobrutinib causes regression of BTK-dependent lymphoma tumors in mouse xenograft models. Pirtobrutinib is also more than 300-fold selective for BTK versus 370 other kinases tested and shows no significant inhibition of non-kinase off-targets at 1 μM.

HY-101474A

Zanubrutinib	Inhibitor	99.71%
Zanubrutinib (BGB-3111) is a selective and orally active Bruton tyrosine kinase (Btk) inhibitor (IC₅₀: 0.3 nM).

HY-19834

Fenebrutinib	Inhibitor	99.42%
Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with K_is of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.

HY-161876

GSTO1-IN-2	Inhibitor
GSTO1-IN-2 (Compound B-9) is a dual covalent inhibitor of GSTO1/BTK with IC₅₀ values of 441 nM and 6.2 nM respectively.

HY-164002

PF-303	Inhibitor
PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC₅₀=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation.

HY-169228

WS-11	Inhibitor
WS-11 is a non-covalent reversible BTK inhibitor with IC₅₀s of 3.9 nM and 2.2 nM for wild type, C481S mutation BTK, respectively. WS-11 can form strong π-π interaction with PHE540 and form p-π interaction with LYS430 within the active pocket, besides the strong hydrogen bonds.

HY-128757

Remibrutinib	Inhibitor	99.76%
Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC₅₀ value of 1 nM. Remibrutinib inhibits BTK activity with an IC₅₀ value of 0.023 μM in blood. Remibrutinib has the potential for Chronic urticaria (CU) treatment.

HY-109192

Tolebrutinib	Inhibitor	99.79%
Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC₅₀s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).

HY-153220

NX-2127	Inhibitor	99.72%
NX-2127 is a a PROTAC targeting Bruton’s Tyrosine Kinase (Btk) with oral activity. NX-2127 is composed of PROTAC target protein ligand BTK ligand 10 (HY-168302) (red part), E3 ligase ligand Thalidomide 5-fluoride (HY-W087383) (blue part) and PROTAC Linker (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304). NX-2127 inhibits proliferation of BTK^C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells.

HY-112166

Rilzabrutinib	Inhibitor	99.37%
Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC₅₀ of 1.3 nM.

HY-129390

Orelabrutinib	Inhibitor	99.90%
Orelabrutinib (ICP-022) is a potent, orally active, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Orelabrutinib prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.

HY-15771

Tirabrutinib	Inhibitor	99.65%
Tirabrutinib (ONO-4059) 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 irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.

HY-112215

Nemtabrutinib	Inhibitor	98.64%
ARQ 531 (MK-1026) is a reversible non-covalent and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC₅₀s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.

HY-153321

NX-5948	Degrader	99.33%
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker).

HY-132842

Sunvozertinib	Inhibitor	99.92%
Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC₅₀s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52).

HY-18012

Spebrutinib	Inhibitor	99.62%
Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC₅₀ of 0.5 nM.

HY-100342

Ibrutinib-biotin	Inhibitor	99.93%
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.

HY-122562

MT-802	Inhibitor	98.94%
MT-802 is a potent BTK degrader based on Cereblon ligand, with a DC₅₀ of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia (CLL).

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Btk

Btk

Btk Related Products (182)

Recombinant Proteins (3)

Antibodies (3)

Btk Related Products (182):