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 (187)
Recombinant Proteins (3)
Antibodies (3)

By Effects:	Inhibitors (156) Degraders (18)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-109010

Poseltinib	Inhibitor	98.08%
Poseltinib (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.

HY-144288

BLK-IN-2	Inhibitor	98.72%
BLK-IN-2 (compound 25) is a potent and selective irreversible inhibitor of B-Lymphoid tyrosine kinase (BLK), with an IC₅₀ of 5.9 nM. BLK-IN-2 also inhibits BTK (IC₅₀=202.0 nM). BLK-IN-2 shows potent antiproliferative activities against several lymphoma cells.

HY-153803

GBD-9	Inhibitor	99.76%
GBD-9 is a double-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1. GBD-9 effectively inhibits cancer cell growth.

HY-18010

PCI 29732	Inhibitor	99.86%
PCI 29732 is a potent, orally active, reversible BTK inhibitor with K_i^app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2.

HY-130983

N-piperidine Ibrutinib hydrochloride	Inhibitor	98.06%
N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC₅₀s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively. N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC₅₀ of 7.9 nM.

HY-100338

CNX-500	Inhibitor	99.88%
CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC₅₀ of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn.

HY-18018

RN486	Inhibitor	99.87%
RN486 is a potent, selective and orally active Btk inhibitor with an IC₅₀ of 4.0 nM and a K_d of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research.

HY-18951

ONO-4059 analog	Inhibitor	99.54%
ONO-4059 analog is an analogue of ONO-4059, and ONO-4059 (HY-15771) is a highly potent and selective Btk inhibitor.

HY-15427

GDC-0834	Inhibitor	98.05%
GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC₅₀ of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC₅₀ of 1.1 and 5.6 μM in mouse and rat, respectively.

HY-153357

NRX-0492	Degrader	98.16%
NRX-0492 is an orally active PROTAC-class BTK degrader. NRX-0492 catalyzes BTK ubiquitination and proteasome degradation (DC₅₀ ≤ 0.2 nM, DC₉₀ ≤ 0.5 nM). NRX-0492 inhibits B cell receptor (BCR) mediated signaling, transcription programs, and chemokine secretion. NRX-0492 can bind non-covalently to the BTK binding domain and cereblon, which is an adapter protein in the E3 ubiquitin ligase complex. NRX-0492 consists of a target protein ligand (red part) BTK-IN-40 (HY-170324), an E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383), and a PROTAC linker (black part) (3R)-3-Pyrrolidinemethanol (HY-60263). E3 ubiquitin ligase and linker can form Thalidomide 5-pyrrolidine-CHO (HY-49372A); the active control for the target protein ligand is BTK ligand 12 (HY-49421).

HY-101941

BTK IN-1	Inhibitor	98.01%
BTK IN-1 (SNS062 analog) is a potent BTK inhibitor, with an IC₅₀ of <100 nM.

HY-13036A

IBT6A	Inhibitor	99.43%
IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM.

HY-153110A

Larotinib mesylate hydrate	Inhibitor	98.66%
Larotinib mesylate hydrate is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC₅₀ of 0.6 nM.

HY-150023

BI-1622	Inhibitor	98.97%
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC₅₀ of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile.

HY-131342

BIIB068	Inhibitor	99.69%
BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC₅₀ of 1 nM and a K_d of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research.

HY-78727

Ibrutinib deacryloylpiperidine	Inhibitor	99.97%
Ibrutinib deacryloylpiperidine (IBT4A) is an impurity of Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor with an IC₅₀ of 0.5 nM.

HY-124645

QL-X-138	Inhibitor	99.77%
QL-X-138 is a potent and selective BTK/MNK dual kinase inhibitor, exhibits covalent binding to BTK and non-covalent binding to MNK. QL-X-138 shows IC₅₀s of 9.4 nM, 107.4 nM and 26 nM for BTK, MNK1 and MNK2 kinases respectively. QL-X-138 also shows anti-dengue virus 2 activity, with an IC₅₀ of 3.5 μM. QL-X-138 can be used for the research of B-cell malignancies.

HY-101856

BMS-986142	Inhibitor	99.53%
BMS-986142 is a potent and highly selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC₅₀ of 0.5 nM.

HY-10997S

Ibrutinib-d₅	Inhibitor	98.08%
Ibrutinib-d₅ is a deuterium labeled Ibrutinib. Ibrutinib is a selective, irreversible Btk inhibitor[1].

HY-15805

KIN-8194	Inhibitor	98.01%
KIN-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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Btk

Btk

Btk Related Products (187)

Recombinant Proteins (3)

Antibodies (3)

Btk Related Products (187):