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covalent kinase inhibitors

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-52101A
    FMK
    3 Publications Verification

    		 Ribosomal S6 Kinase (RSK) Cancer
    FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.
    FMK
  • HY-12679
    PF-06658607

    		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-122913
    Borussertib

    		Akt Cancer
    Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Akt wt .
    Borussertib
  • HY-112166
    (E)-Rilzabrutinib

    (E)-PRN1008

    		 Btk Metabolic Disease Cancer
    Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
    (E)-Rilzabrutinib
  • HY-138825
    NCGC00188636

    		Pyk2 Metabolic Disease
    NCGC00188636 is a novel covalent pyruvate kinase (PYK) inhibitor. NCGC00188636 blocks nucleotide binding to the active site of pyruvate kinase. NCGC00188636 can be used for the research of the metabolism of many organisms and cell types.
    NCGC00188636
  • HY-163267
    ZNL0325

    		Fluorescent Dye Others
    ZNL0325 is a covalent probe based on pyrazolopyrimidine. ZNL0325 features an acrylamide side chain at the C3 position, which is capable of forming covalent bonds with multiple kinases that possess a cysteine at the αD-1 position, including BTK, EGFR, BLK, and JAK3. ZNL0325 can be used in the research of creating structurally distinct covalent kinase inhibitors .
    ZNL0325
  • HY-150022
    GRK5-IN-4

    CCG-265328

    		 G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GRK5-IN-4 (Compound 16d, CCG-265328) is a potent and and selective covalent GRK5 (G protein-coupled receptor kinase 5) inhibitor, with an IC50 of 1.1 μM. GRK5-IN-4 shows 90-fold selectivity over GRK2. GRK5-IN-4 can be used for heart failure research . GRK5-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    GRK5-IN-4
  • HY-119935
    JAK3 covalent inhibitor-1

    		JAK Inflammation/Immunology
    JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs .
    JAK3 covalent inhibitor-1
  • HY-116533
    RMM-46

    		MAPKAPK2 (MK2) Cancer
    RMM-46 is a selective and reversible covalent inhibitor for MSK/RSK-family kinases .
    RMM-46
  • HY-150717
    RSK2-IN-3

    		Ribosomal S6 Kinase (RSK) Cancer
    RSK2-IN-3 (Compound 26) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase .
    RSK2-IN-3
  • HY-144308
    RMS-07

    		Mps1 Others
    RMS-07 is a covalent Monopolar Spindle Kinase 1 (MPS1/TTK) inhibitor, with an apparent IC50 of 13.1 nM. RMS-07 targets a poorly conserved cysteine in the kinase's hinge region .
    RMS-07
  • HY-43521
    Ibrutinib-MPEA

    		Btk Cancer
    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-100338
    CNX-500

    		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-169231
    BCR-ABL-IN-10

    		Bcr-Abl Cancer
    BCR-ABL-IN-10 (compound B4) is a covalent and aryl vinyl sulfate (AVS)-containing BCR-ABL inhibitor with an IC50 of 43.1 nM for ABL kinase. BCR-ABL-IN-10 forms a covalent and stable adduct with ABL kinase, leading to sustained inhibition of endogenous BCR-ABL activities. BCR-ABL-IN-10 can be used for the study of chronic myeloid leukemia (CML) .
    BCR-ABL-IN-10
  • HY-W143698
    PDGFRα kinase inhibitor 2

    		Bcr-Abl c-Kit PDGFR Cancer
    PDGFRα kinase inhibitor 2 (compound 1), an Imatinib (HY-15463) analogue, is a covalent and irreversible kinase inhibitor with IC50s of 6.95 μM, 2.45 μM, 1.39 μM for ABL1 wt, KIT wt, PDGFRR wt .
    PDGFRα kinase inhibitor 2
  • HY-162785
    XC219

    		CDK Infection
    XC219 (compound 43) is a cyclin-dependent kinase CDK) inhibitor, that covalently binds to CDK active site Lys. XC219 can be used in antifungal research .
    XC219
  • HY-163565
    BIIB129

    		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-147784
    HZ-A-005

    		Btk Cancer
    HZ-A-005 is a potent, selective, and covalent Bruton’s tyrosine kinase (BTK) inhibitor. HZ-A-005 markedly decreases tumor growth in xenograft mouse models .
    HZ-A-005
  • HY-80013A
    THZ1 Hydrochloride
    Maximum Cited Publications
    82 Publications Verification

    		 CDK Cancer
    THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression .
    THZ1 Hydrochloride
  • HY-80013
    THZ1
    Maximum Cited Publications
    82 Publications Verification

    		 CDK Cancer
    THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression .
    THZ1
  • HY-129288
    GW837016X

    NEU-391

    		 EGFR Paraptosis Mitosis Infection
    GW837016X (NEU-391) is an orally active ErbB-2 kinase covalent inhibitor. GW837016X also is a potent antitrypanosome agent. GW837016X inhibits mitosis and cytokinesis .
    GW837016X
  • HY-139504
    Gamcemetinib

    CC-99677

    		 MAPKAPK2 (MK2) Inflammation/Immunology
    Gamcemetinib (CC-99677) is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). Gamcemetinib is extracted from patent WO2020236636, compound 1 .
    Gamcemetinib
  • HY-149354
    Aurora kinase-IN-4

    		Aurora Kinase Cancer
    Aurora kinase-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). Aurora kinase-IN-4 inhibits cell proliferation in SJSA-1, MDA-MB-231, A54, HeLa cells with IC50s of 4.27, 1.54, 3.08, 6.99 μM. Aurora kinase-IN-4 can be used for research of triple negative breast cancer (TNBC) .
    Aurora kinase-IN-4
  • HY-47573
    CCG273441
    1 Publications Verification

    		 G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease Cancer
    CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC50 value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC50=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle .
    CCG273441
  • HY-15816A
    Ulixertinib hydrochloride
    30+ Cited Publications

    BVD-523 hydrochloride; VRT752271 hydrochloride

    		 ERK Cancer
    Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
    Ulixertinib hydrochloride
  • HY-169230
    BCR-ABL-IN-9

    		Bcr-Abl Cancer
    BCR-ABL-IN-9 (Compound B1) is a BCR-ABL inhibitor that achieves sustained BCR-ABL suppression by forming stable covalent bonds with the ABL kinase. BCR-ABL-IN-9 is also effective in inhibiting the activity of the ABL kinase (IC50 = 1.2 nM). BCR-ABL-IN-9 possesses anticancer activity .
    BCR-ABL-IN-9
  • HY-136430
    JCN037

    JGK037

    		 EGFR Cancer
    JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively .
    JCN037
  • HY-153244
    MFH290

    		CDK Cancer
    MFH290 is a potent and highly selective cyclin-dependent kinase 12/13 (CDK12/13) covalent inhibitor. MFH290 forms a covalent bond with Cys-1039 of CDK12 and exhibits excellent kinome selectivity and inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II). MFH290 is used for cancer research .
    MFH290
  • HY-150643
    RSK2-IN-2

    		Ribosomal S6 Kinase (RSK) Cancer
    RSK2-IN-2 (Compound 25) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase. RSK2-IN-2 is also described to inhibit MSK1, MSK2 and RSK3 .
    RSK2-IN-2
  • HY-124645
    QL-X-138

    		Flavivirus Dengue Virus Btk MNK Infection Cancer
    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-144448
    FAK-IN-2

    		FAK Apoptosis Cancer
    FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis .
    FAK-IN-2
  • HY-144283
    BLK-IN-1

    		Btk Cancer
    BLK-IN-1 (compound 1) is a selective and covalent inhibitor of B-Lymphoid tyrosine kinase (BLK) and BTK, with IC50s of 18.8 nM and 20.5 nM, respectively. BLK-IN-1 can be used for the research of cancer .
    BLK-IN-1
  • HY-112215
    Nemtabrutinib
    3 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-15816
    Ulixertinib
    30+ Cited Publications

    BVD-523; VRT752271

    		 ERK Cancer
    Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
    Ulixertinib
  • HY-158154
    EGFR-IN-110

    		EGFR Cancer
    EGFR-IN-110 (Compound 6) is a covalent EGFR inhibitor, with pIC50 values of 9.2 and 8.7 for EGFR enzyme and EGFR cell, respectively. EGFR-IN-110 shows high EGFR potency and good kinase selectivity .
    EGFR-IN-110
  • HY-12680
    PRN694
    1 Publications Verification

    		 Itk Inflammation/Immunology
    PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo .
    PRN694
  • HY-131328
    Pirtobrutinib
    3 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-141480
    GSK-3β inhibitor 3

    		GSK-3 Apoptosis Cancer
    GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC50 of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia .
    GSK-3β inhibitor 3
  • HY-158248
    FGFR4-IN-19

    		FGFR Cancer
    FGFR4-IN-19 (compound 8B) is a potent covalent fibroblast growth factor receptor 4 (FGFR4) inhibitor (IC50=1.2 nM). FGFR4-IN-19 achieves high efficiency and isotype selectivity by covalently targeting a rare cysteine (C552) in the FGFR4 kinase domain. FGFR4-IN-19 can be used for hepatocellular carcinoma (HCC) research .
    FGFR4-IN-19
  • HY-164002
    PF-303

    		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-112161
    Branebrutinib
    2 Publications Verification

    BMS-986195

    		 Btk Cancer
    Branebrutinib (BMS-986195) is a highly potent, selective covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), with an IC50 of 0.1 nM . Branebrutinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Branebrutinib
  • HY-150021
    GRK5-IN-3

    		G Protein-coupled Receptor Kinase (GRK) Others
    GRK5-IN-3 is a covalent inhibitor of GRK5 (G Protein-Coupled Receptor Kinase 5). GRK5-IN-3 shows potent inhibitory effect to GRK5 and GRK6 with IC50s of 0.22 μM and 0.41 μM, respectively .
    GRK5-IN-3
  • HY-15771
    Tirabrutinib
    5 Publications Verification

    ONO-4059; GS-4059

    		 Btk Apoptosis Inflammation/Immunology Cancer
    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 .
    Tirabrutinib
  • HY-15771A
    Tirabrutinib hydrochloride
    5 Publications Verification

    ONO-4059 hydrochloride; GS-4059 hydrochloride

    		 Btk Apoptosis Inflammation/Immunology Cancer
    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-100849
    JAK 3i

    		JAK Inflammation/Immunology
    JAK3i is a highly selective JAK3 inhibitor (IC50: 0.43 nM). JAK3i forms a covalent bond with a cysteine in JAK3, but not the closely related kinase domains in JAK1, JAK2, or TYK2. JAK3i abolishes IL-2-driven T-cell proliferation in vivo and has the potential for  autoimmune disease research .
    JAK 3i
  • HY-174129
    TM471-1

    		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-134205A
    CBR-470-1
    2 Publications Verification

    		 Keap1-Nrf2 Neurological Disease Metabolic Disease
    CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP +-induced cytotoxicity through activation of the Keap1-Nrf2 cascade .
    CBR-470-1
  • HY-131014
    FM-479

    		JAK Inflammation/Immunology
    FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases . FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
    FM-479
  • HY-161910
    SH-E4A-66

    		Anaplastic lymphoma kinase (ALK) Cancer
    SH-E4A-66 is a C 2-COUPLr (COvalent Protein Ligator) with carbazole scaffold barring heterogeneous cysteine reactive warheads (acrylamide and chloroacetamide). SH-E4A-66 is capable of coupling with EML4-ALK (EC50=1.5 μM) and inhibiting the activity of EML4-ALK kinase (IC50=2.3 μM) .
    SH-E4A-66
  • HY-101522
    CHMFL-EGFR-202

    		EGFR BMX Kinase Btk MEK Cancer
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .
    CHMFL-EGFR-202

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