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BTK Inhibitor

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10997
    Ibrutinib
    Maximum Cited Publications
    126 Publications Verification

    PCI-32765

    Btk Ligands for Target Protein for PROTAC Infection Inflammation/Immunology Cancer
    Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM .
    Ibrutinib
  • HY-131328
    Pirtobrutinib
    5 Publications Verification

    LOXO-305

    Btk Cancer
    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 .
    Pirtobrutinib
  • HY-128757
    Remibrutinib
    5 Publications Verification

    LOU064

    Btk Inflammation/Immunology Cancer
    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 .
    Remibrutinib
  • HY-129390
    Orelabrutinib
    3 Publications Verification

    ICP-022

    Btk Cancer
    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 .
    Orelabrutinib
  • HY-112215
    Nemtabrutinib
    4 Publications Verification

    ARQ-531; MK-1026

    Btk Inflammation/Immunology Cancer
    Nemtabrutinib (ARQ 531) 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.
    Nemtabrutinib
  • HY-11999
    CGI-1746
    5+ Cited Publications

    Btk Autophagy Inflammation/Immunology
    CGI-1746 is a potent and highly selective inhibitor of the Btk with IC50 of 1.9 nM.
    CGI-1746
  • HY-156640

    LP-168

    EGFR Cancer
    Rocbrutinib is an orally available, highly selective Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 of 0.11 nM against wild-type BTK and an IC50 of 1.0 nM against C481S-mutated BTK. Rocbrutinib reduces the viability of leukemia cells, induces cytotoxicity and inhibits cell migration. Rocbrutinib can be used in research related to chronic lymphocytic leukemia, non-Hodgkin's lymphoma and mantle cell lymphoma .
    Rocbrutinib
  • HY-109143
    Elsubrutinib
    2 Publications Verification

    ABBV-105

    Btk Inflammation/Immunology
    Elsubrutinib (ABBV-105) is an orally active, potent, selective and irreversible Bruton's tyrosine kinase (BTK) inhibitor. The IC50 of Elsubrutinib for BTK catalytic domain is 0.18 μM. Elsubrutinib can be used for the research of inflammatory disease .
    Elsubrutinib
  • HY-160167

    DZD8586

    Src Btk Inflammation/Immunology Cancer
    Birelentinib (DZD8586) is an orally effective, selective, non-covalent inhibitor targeting LYN tyrosine kinase and BTK tyrosine kinase, capable of penetrating the blood-brain barrier. Birelentinib exhibits concentration-dependent antiproliferative effects in RI-1 cells and diffuse large B-cell lymphoma (DLBCL) cell lines carrying BTK resistance mutations (such as C481X, V416L, etc.). Birelentinib blocks both BTK-dependent and independent signaling of the B-cell receptor (BCR), thereby inhibiting tumor cell proliferation and inducing cell death. Birelentinib can be used in research to overcome resistance to existing covalent and non-covalent BTK inhibitors in B-cell non-Hodgkin lymphoma (B-NHL) .
    Birelentinib
  • HY-10644

    Src Inflammation/Immunology
    Lck inhibitor 2 is a multi-target tyrosine kinase inhibitor with IC50s of 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively.
    Lck inhibitor 2
  • HY-13943
    CNX-774
    2 Publications Verification

    Btk Cancer
    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 .
    CNX-774
  • HY-15427
    GDC-0834
    1 Publications Verification

    Btk Inflammation/Immunology
    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.
    GDC-0834
  • HY-160142

    PROTACs Btk Syk MEK ERK Cancer
    UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers .
    UBX-382
  • HY-100338

    Btk Cancer
    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-12679

    Btk Cancer
    PF-06658607 is an alkynylated irreversible Brutons tyrosine kinase (BTK) inhibitor that covalently reacts with active site cysteines in the ATP-binding pocket. PF-06658607 can be used to detect "off "-targets for covalent kinase inhibitors in cancer cells. The alkyne moiety allows for azide-based detection probe via copper-catalyzed click chemistry .
    PF-06658607
  • HY-101941

    SNS062 analog

    Btk Inflammation/Immunology Cancer
    BTK IN-1 (SNS062 analog) is a potent BTK inhibitor, with an IC50 of <100 nM.
    BTK IN-1
  • HY-163565

    Btk Neurological Disease
    BIIB129 is a covalent, selective, small molecule inhibitor of Bruton's tyrosine kinase (BTK) capable of penetrating the blood-brain barrier. BIIB129 inhibits the activity of BTK by covalently binding to Cys481 in BTK, thereby affecting the function of B cells and myeloid cells. BIIB129 can be used in multiple sclerosis (MS) research .
    BIIB129
  • HY-132879

    Btk Inflammation/Immunology
    TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.
    TAK-020
  • HY-128403

    Btk Inflammation/Immunology
    BTK inhibitor 8 (Compound 27) is a Btk inhibitor with an IC50 of 0.11 nM. BTK inhibitor 8 inhibits Btk activity. BTK inhibitor 8 suppresses B cell activation. BTK inhibitor 8 is applicable to research related to arthritis and asthma .
    BTK inhibitor 8
  • HY-101766

    Btk Inflammation/Immunology
    Btk inhibitor 2 is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
    Btk inhibitor 2
  • HY-174850

    Btk Cancer
    CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27  nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
    CFON-026
  • HY-130983

    Btk Ligands for Target Protein for PROTAC Cancer
    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-149391

    PROTACs Btk Inflammation/Immunology
    PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6) .
    PROTAC BTK Degrader-6
  • HY-136531

    Btk Apoptosis Cancer
    XMU-MP-3 is a potent non-covalent BTK inhibitor with IC50s of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation in the presence of 10 μM ATP, respectively. XMU-MP-3 also induces apoptosis .
    XMU-MP-3
  • HY-131328A

    (R)-LOXO-305

    Btk Others
    (R)-Pirtobrutinib ((R)-LOXO-305) is a less active enantiomer of Pirtobrutinib. Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations .
    (R)-Pirtobrutinib
  • HY-130255

    Btk Inflammation/Immunology
    BTK inhibitor 13 (compound 8) is a potent and selective Bruton's tyrosine kinase (BTK) inhibitor with an IC50 of 1.2 nM .
    BTK inhibitor 13
  • HY-145373

    Btk Inflammation/Immunology
    BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases .
    BMS-986143
  • HY-152212

    Btk Inflammation/Immunology
    BTK-IN-19 (Compound 51) is a reversible BTK inhibitor with an IC50 of <0.001 μM .
    BTK-IN-19
  • HY-174129

    Btk Apoptosis Cancer
    TM471-1 is an orally active and covalent Bruton's tyrosine kinase (BTK) inhibitor with IC50 values of 1.3 nM (BTK WT), >40,000 nM (BTK C481S), 7.9 nM (TEC) and 12.4 nM (TXK). TM471-1 inhibits cell growth in vivo and in vitro, arrests cell cycle at G0/G1 phase and induces cell apoptosis .
    TM471-1
  • HY-131705

    Btk Inflammation/Immunology
    BTK inhibitor 17 is a potent and orally active irreversible BTK inhibitor with an IC50 of 2.1 nM. BTK inhibitor 17 can be used for rheumatoid arthritis research .
    BTK inhibitor 17
  • HY-139881

    Btk Cancer
    BTK inhibitor 19 is a highly selective, covalent BTK inhibitor (IC50 = 2.7 nM).
    BTK inhibitor 19
  • HY-125997

    Btk Inflammation/Immunology
    BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment .
    BTK inhibitor 10
  • HY-170324

    Btk Others
    BTK-IN-40 (compound 375) is a BTK inhibitor .
    BTK-IN-40
  • HY-147580

    Btk Cancer
    BTK-IN-10 is a potent BTK inhibitor with IC50s of <5 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022012509A1; example 111) .
    BTK-IN-10
  • HY-148832

    Btk Inflammation/Immunology Cancer
    BTK-IN-20 (compound 283) is a BTK tyrosine kinase inhibitor and a 1H-pyrazolo[3,4-d]pyrimidine derivative. BTK-IN-20 can be used for the research of cancer and inflammation .
    BTK-IN-20
  • HY-162280

    PROTACs RANKL/RANK Nuclear Factor of activated T Cells (NFAT) Btk Cancer
    PROTAC BTK Degrader-9 (compound 23) is a PROTAC degrader that effectively targets BTK. PROTAC BTK Degrader-9 downregulates the BTK-PLCγ2-Ca 2+-NFATc1 signaling pathway activated by RANKL. Thus, PROTAC BTK Degrader-9 was able to inhibit osteoclastogenesis and attenuate alveolar bone resorption in a mouse periodontitis model .
    PROTAC BTK Degrader-9
  • HY-177103

    Btk Cancer
    Midobrutinib (Example 13) is a BTK inhibitor (IC50: 0.813 nM). Midobrutinib can be used for research of diseases involving BTK, particularly cancer .
    Midobrutinib
  • HY-168963

    PROTACs Btk Itk p38 MAPK Inflammation/Immunology Cancer
    PROTAC BTK Degrader-13 (Compound 25) is the PROTAC degrader for BTK with a DC50 of 0.27 μM. PROTAC BTK Degrader-13 inhibits the activity of BTK with an IC50 of 0.44 μM, inhibits IL-2-induced T cell kinase (ITK) with an IC50 of 2.16 μM. PROTAC BTK Degrader-13 inhibits p38 MAPK signaling pathway, block the activation of the BCR (B cell receptor) signaling pathway . (Pink: ligand for target protein BTK ligand 15 (HY-168965); Black: linker (HY-Y0524); Blue: ligand for E3 ligase cereblon (HY-103596))
    PROTAC BTK Degrader-13
  • HY-147584

    Btk Inflammation/Immunology Cancer
    BTK-IN-14 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-14 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022057894A1, compound 1) .
    BTK-IN-14
  • HY-164002

    Btk Others
    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 .
    PF-303
  • HY-151961

    Btk FLT3 Cancer
    RSH-7 is a potent BTK and FLT3 inhibitor with IC50s of 47, 12 nM, respectively. RSH-7 induces apoptosis and shows antiproliferative activities. RSH-7 inhibits BTK and FLT3 signaling and shows anti-tumor activity .
    RSH-7
  • HY-110013

    Btk Antibiotic Infection Inflammation/Immunology
    Terreic acid, a quinone epoxide antibiotic, acts as an effective Btk inhibitor. Terreic acid blocks the interaction between PKC and the pleckstrin homology domain of Btk. Terreic acid inhibits the binding of GST-BtkPH to PKC in lysates of HMC-1 human mast cells with an IC50 of approximately 100 μM .
    Terreic acid
  • HY-132196

    Btk Inflammation/Immunology
    BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC50 of 142 nM. BTK inhibitor 18 has anti-inflammatory activities .
    BTK inhibitor 18
  • HY-143730

    Btk Cancer
    BTK inhibitor 20 is a potent BTK inhibitor with an IC50 of 8 nM .
    BTK inhibitor 20
  • HY-162257

    Btk Cancer
    BTK-IN-34 (compound 9h) is a selective BTK inhibitor. BTK-IN-34 shows antiproliferative activity in RAMOS cells through selective inhibition of pBTK (Tyr223) without affecting Lyn and Syk, upstream proteins in the BCR signaling pathway .
    BTK-IN-34
  • HY-153705

    Btk Cancer
    BTK-IN-25 (compound 71) is a potent inhibitor of BTK, and inhibits BTK(C481S) with an IC50 value of 0.77 nM. BTK-IN-25 inhibits BTK in DOHH2 cells with an IC50 value of 1 nM .
    BTK-IN-25
  • HY-162081

    Btk Cancer
    BTK-IN-32 (compound C2) is a potent inhibitor of BTK. BTK-IN-32 activates full-length BTK and smaller multidomain BTK fragments instead of the isolated kinase domain .
    BTK-IN-32
  • HY-150752

    Btk Pyroptosis Cancer
    BTK-IN-15 (compound 42) is a potent Bruton's tyrosine kinase (BTK) inhibitor with high oral absorption. BTK-IN-15 inhibits BTK with an IC50 value of 0.7 nM. BTK-IN-15 displays excellent kinase selectivity, antitumor activity, and induces apoptosis .
    BTK-IN-15
  • HY-141689

    Btk Cancer
    BTK-IN-3 (example 1) is an inhibitor of BTK. BTK-IN-3 can used to study cancer .
    BTK-IN-3
  • HY-157159

    Btk Cancer
    BTK-IN-28 (compound PID-4) is a potent BTK inhibitor with anticancer activity. BTK-IN-28 has inhibitory effects on BTK and downstream signaling cascades and selectively inhibits Burkitt lymphoma RAMOS proliferation. BTK-IN-28 has no significant cytotoxicity towards non-tumor cells .
    BTK-IN-28

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