2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Btk

Btk

Bruton tyrosine kinase

Btk

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15771A
    Tirabrutinib hydrochloride
    		Inhibitor 99.66%
    Tirabrutinib (ONO-4059) hydrochloride 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 hydrochloride irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib hydrochloride can be used in studies of autoimmune diseases and hematological malignancies.
    Tirabrutinib hydrochloride
  • 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.
    Poseltinib
  • HY-18010
    PCI 29732
    		Inhibitor 99.86%
    PCI 29732 is a potent, orally active, reversible BTK inhibitor with Kiapp 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.
    PCI 29732
  • HY-147943
    PROTAC BTK Degrader-1
    		98.87%
    PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth. PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    PROTAC BTK Degrader-1
  • 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.
    BLK-IN-2
  • HY-160141
    Catadegbrutinib
    		Degrader
    BGB-16673 (BGB-16673; BTK-IN-29) is an orally active, selectively chimeric degradation activator compound (CDAC), targeting BTK (IC50=0.69 nM). BGB-16673 ligates BTK to E3 ubiquitin ligase, causing BTK to undergo polyubiquitination, which is then recognized and degraded by the proteasome, thereby exerting efficient BTK degradation activity. BGB-16673 can be used in the research of B-cell malignancies such as chronic lymphocytic leukemia, small lymphocytic lymphoma, and mantle cell lymphoma.
    Catadegbrutinib
  • 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.
    Ibrutinib-MPEA
  • 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.
    N-piperidine Ibrutinib hydrochloride
  • 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.
    KIN-8194
  • 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).
    NRX-0492
  • 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.
    CNX-500
  • 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.
    QL-X-138
  • 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 Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research.
    RN486
  • 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.
    Avitinib maleate
  • HY-101941
    BTK IN-1
    		Inhibitor 98.09%
    BTK IN-1 (SNS062 analog) is a potent BTK inhibitor, with an IC50 of <100 nM.
    BTK IN-1
  • 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].
    L18I
  • 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.
    IBT6A
  • HY-17600S
    Acalabrutinib-d4
    		Inhibitor 99.50%
    Acalabrutinib-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.
    Acalabrutinib-d<sub>4</sub>
  • 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.
    Larotinib mesylate hydrate
  • 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.
    BI-1622
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Cat. No. Product Name / Synonyms Application Reactivity