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 (218)
Recombinant Proteins (2)
Antibodies (3)

By Effects:	Ligands (3) Inhibitors (171) Substrate (1) Degraders (27)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-108691

PF-06465469	Inhibitor	99.48%
PF-06465469 is a covalent inhibitor of ITK with an IC₅₀ of 2 nM. PF-06465469 also inhibits BTK. PF-06465469 inhibits cell migration in response to CXCL12. PF-06465469 decreases PD-1 and LAG-3 expression. PF-06465469 can be used to study leukemia and T-cell lymphoma.

HY-13036A

IBT6A	Inhibitor	99.59%
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-133137

SJF620	Inhibitor	98.98%
SJF620 is a PROTAC connected by ligands for Cereblon and Btk with a DC₅₀ of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN.

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.

HY-13943

CNX-774	Inhibitor	99.92%
CNX-774 is an orally active, irreversible and selective BTK inhibitor, with an IC₅₀ of < 1 nM. CNX-774 specifically targets Cysteine 481 of Btk for covalent modification.

HY-101474

(±)-Zanubrutinib	Inhibitor	99.70%
(±)-Zanubrutinib ((±)-BGB-3111) is the racemate of Zanubrutinib (HY-101474A). (±)-Zanubrutinib inhibits Bruton's tyrosine kinase (Btk) with an IC₅₀ of 0.63 nM.

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 has antitumor effects against chronic lymphocytic leukemia.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).

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-163962

L18I		99.89%
L18I is a PROTAC targeting Btk that can reduce inflammation in autoimmune diseases such as lupus erythematosus induced by BM12 splenocytes. L18I is composed of PROTAC target protein ligand IBT6A (HY-13036A) (red part), PROTAC Linker Propargyl-PEG3-alcohol (HY-41921) (balck part) and E3 ubiquitin ligase ligand Lenalidomide-Br (HY-43722) (blue part), of which the active control of the target protein ligand is IBT6A-CO-ethyne (HY-163963), and the conjugate of E3 ubiquitin ligase ligand + Linker is Lenalidomide-C3-PEG3-N3 (HY-163964)^{[1]^.}

HY-18018

RN486	Inhibitor	98.91%
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-43521

Ibrutinib-MPEA		99.71%
Ibrutinib-MPEA (Compound 20) is ibrutinib derivative. Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) that has been used to treat haematological malignancies.

HY-101941

BTK IN-1	Inhibitor	98.09%
BTK IN-1 (SNS062 analog) is a potent BTK inhibitor, with an IC₅₀ of <100 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-19816A

Avitinib maleate	Inhibitor	99.86%
Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC₅₀ values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects.

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-163295

BTK degrader-1	Degrader	99.40%
BTK degrader-1 (compound 1) is a Bruton’s tyrosine kinase (BTK) bifunctional degrader that can be conjugated with CD79b. BTK degrader-1 (compound 1) has anti-tumor effect.

HY-144288

BLK-IN-2	Inhibitor	98.61%
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-17600S

Acalabrutinib-d₄	Inhibitor	99.50%
Acalabrutinib-d₄ (ACP-196-d₄) is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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.

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Btk

Btk

Btk Related Products (218)

Recombinant Proteins (2)

Antibodies (3)

Btk Related Products (218):