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Pathways Recommended: Protein Tyrosine Kinase/RTK
Targets Recommended: Btk Syk DYRK Pyk2 FAK FLT3 ALK
Results for "

Tyrosine Inhibitors

" in MCE Product Catalog:

309

Inhibitors & Agonists

2

Screening Libraries

1

Biochemical Assay Reagents

1

Peptides

1

MCE Kits

29

Natural
Products

23

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-10421
    Tyrosine kinase inhibitor

    c-Met/HGFR Cancer
    Tyrosine kinase inhibitor is a potent tyrosine kinase inhibitor.
  • HY-Y0444
    D-Tyrosine

    Tyrosinase Metabolic Disease
    D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth.
  • HY-N0473S
    L-Tyrosine D4

    Others Neurological Disease
    L-Tyrosine D4 is a deuterium labeled L-Tyrosine. L-Tyrosine is a non-essential amino acid which can inhibit citrate synthase activity in the posterior cortex.
  • HY-50946
    Imatinib Mesylate

    STI571 Mesylate; CGP-57148B Mesylate

    c-Kit Bcr-Abl PDGFR Autophagy Cancer
    Imatinib Mesylate (STI571 Mesylate) is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-50686
    Tivantinib

    ARQ 197

    c-Met/HGFR Apoptosis Cancer
    Tivantinib is a highly selective c-Met tyrosine kinase inhibitor with a Ki of 355 nM.
  • HY-100315
    Tyrosine kinase-IN-1

    VEGFR PDGFR FGFR Cardiovascular Disease
    Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.
  • HY-101474A
    Zanubrutinib

    BGB-3111

    Btk Cancer
    Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.
  • HY-10159
    Nilotinib

    AMN107

    Bcr-Abl Autophagy Cancer
    Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
  • HY-101756
    SDZ281-977

    SDZ-LAP 977

    Others Cancer
    SDZ 281-977 is a derivative of the EGF receptor tyrosine kinase inhibitor Lavendustin A.
  • HY-50868
    Bafetinib

    INNO-406; NS-187

    Bcr-Abl Autophagy Cancer
    Bafetinib is a Lyn and Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity.
  • HY-W013478
    PTP inhibitor 1

    Phosphatase Cancer
    PTP inhibitor 1 is a protein tyrosine phosphatase (PTP) inhibitor, with anti-angiogenic effect.
  • HY-101429
    RG13022

    Tyrphostin RG13022

    EGFR Cancer
    RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
  • HY-101296
    PD-166866

    FGFR Autophagy Cancer
    PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM.
  • HY-18840
    BBT594

    NVP-BBT594

    RET Cancer
    BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.
  • HY-101474B
    (R)-Zanubrutinib

    (R)-BGB-3111

    Others Others
    (R)-Zanubrutinib is the R enantiomer of Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (BTK) inhibitor.
  • HY-100335
    PCI-33380

    Btk Others
    PCI-33380 is an irreversible and selective Bruton's Tyrosine Kinase (BTK) inhibitor (fluorescent probe).
  • HY-12312
    TCS 401

    Phosphatase Metabolic Disease
    TCS 401 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B).
  • HY-101474
    (±)-Zanubrutinib

    (±)-BGB-3111

    Btk Cancer
    (±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
  • HY-101246
    RPI-1

    RET Cancer
    RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity.
  • HY-D0852
    Sodium orthovanadate

    Phosphatase Cancer
    Sodium orthovanadate is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue.
  • HY-111138
    CZC-8004

    CZC-00008004

    Bcr-Abl Cancer
    CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase.
  • HY-12974
    PRT-060318

    PRT318

    Syk Cancer
    PRT-060318 (PRT318) is a novel selective inhibitor of the tyrosine kinase Syk with an IC50 of 4 nM.
  • HY-N0473
    L-Tyrosine

    Endogenous Metabolite Neurological Disease
    L-Tyrosine is a non-essential amino acid which can inhibit citrate synthase activity in the posterior cortex.
  • HY-15333
    ZK-261991

    VEGFR Inflammation/Immunology
    ZK-261991 is an orally active VEGFR tyrosine kinase inhibitor with an IC50 of 5 nM for VEGFR2.
  • HY-111489A
    LMPTP INHIBITOR 1 hydrochloride

    Phosphatase Metabolic Disease
    LMPTP INHIBITOR 1 (hydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
  • HY-12000
    AG490

    Tyrphostin AG490; Tyrphostin B42

    EGFR STAT JAK Autophagy Cancer
    AG490 (Tyrphostin AG490) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
  • HY-111489B
    LMPTP INHIBITOR 1 dihydrochloride

    Phosphatase Metabolic Disease
    LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
  • HY-N0198
    Nordihydroguaiaretic acid

    NDGA

    Lipoxygenase Autophagy Ferroptosis Cancer Neurological Disease
    Nordihydroguaiaretic acid is a 5-lipoxygenase (5LOX) (IC50=8 μM) and tyrosine kinase inhibitor.
  • HY-12963
    Dubermatinib

    TP-0903

    TAM Receptor Apoptosis Cancer
    Dubermatinib (TP-0903) is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.
  • HY-101793
    BMS-935177

    Btk Inflammation/Immunology
    BMS-935177 is a potent and selective reversible inhibitor of Bruton’s tyrosine kinase (Btk) with an IC50 of 3 nM.
  • HY-18007
    ALW-II-41-27

    Eph receptor Tyrosine kinase inhibitor

    Ephrin Receptor Cancer
    ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC50 of 11 nM for Eph2.
  • HY-18963
    Lavendustin A

    RG-14355

    EGFR Cancer
    Lavendustin A (RG-14355), isolated from Streptomyces Griseolavendus, is a potent, specific and ATP-competitive inhibitor of tyrosine kinase, with an IC50 of 11 ng/mL for EGFR-associated tyrosine kinase. It suppresses VEGF-induced angiogenesis and blocks the induction of LTPGABA-A.
  • HY-130255
    BTK inhibitor 13

    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.
  • HY-N5118
    Chimonanthine

    (-)-Chimonanthine

    Tyrosinase Cancer
    Chimonanthine is an alkaloid of Chimonanthus praecox, inhibits tyrosinase and tyrosine-related protein-1 mRNA expression, amd inhibits melanogenesis.
  • HY-100463
    TPI-1

    Phosphatase Inflammation/Immunology Cancer
    TPI-1, also known as Tyrosine Phosphatase Inhibitor 1, is a SHP-1 inhibitor; inhibits recombinant SHP-1 with an IC50 of 40 nM.
  • HY-10181S
    Dasatinib D8

    BMS-354825 D8

    Bcr-Abl Src Apoptosis Autophagy Cancer
    Dasatinib D8 is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.
  • HY-13804
    PP1

    AGL 1872; EI 275

    Src Apoptosis Cancer
    PP1 is a potent, and Src family-selective tyrosine kinase inhibitor with IC50 of 5 and 6 nM for Lck and Fyn, respectively.
  • HY-101856
    BMS-986142

    Btk Inflammation/Immunology
    BMS-986142 is a potent and highly selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.5 nM.
  • HY-10338
    Foretinib

    XL880; GSK1363089; GSK089; EXEL-2880

    VEGFR c-Met/HGFR Cancer
    Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
  • HY-101053
    Src Inhibitor 1

    Src Kinase Inhibitor 1; Src-l1

    Src Cancer
    Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
  • HY-101766
    Btk inhibitor 2

    BGB-3111 analog

    Btk Inflammation/Immunology
    Btk inhibitor 2 (BGB-3111 analog) is a Bruton's tyrosine kinase (BTK) inhibitor extracted from patent US 20170224688 A1.
  • HY-109082
    Cevidoplenib

    Syk Inflammation/Immunology
    Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities.
  • HY-101820A
    Simotinib hydrochloride

    EGFR Cancer
    Simotinib hydrochloride is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
  • HY-132816
    Gemnelatinib

    c-Met/HGFR Cancer
    Gemnelatinib is a tyrosine kinase inhibitor (WO2018077227, implementation example 1). Gemnelatinib can be used for the research of cancer.
  • HY-101820
    Simotinib

    EGFR Cancer
    Simotinib is a selective, specific, and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 19.9 nM. Antineoplastic activities.
  • HY-19779
    JTT 551

    Phosphatase Metabolic Disease
    JTT 551 is selective a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with Kis of 0.22 μM and 9.3 μM for PTP1B and TCPTP (T-cell protein tyrosine phosphatase), respectively; JTT 551 can be used in the research of type 2 diabetes mellitus.
  • HY-10331S
    Regorafenib D3

    BAY 73-4506 D3

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib D3 (BAY 73-4506 D3) is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor.
  • HY-101474S
    Zanubrutinib D5

    BGB-3111 D5

    Btk Cancer
    Zanubrutinib D5 (BGB-3111 D5) is deuterium labeled Zanubrutinib. Zanubrutinib is a selective Bruton tyrosine kinase (Btk) inhibitor.
  • HY-20878
    Tyrphostin AG 879

    AG 879

    Trk Receptor EGFR Apoptosis Cancer
    Tyrphostin AG 879 (AG 879) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation (IC50 of 10 μM), but not TrKB and TrKC. Tyrphostin AG 879 is also a selective ErbB2 tyrosine kinase inhibitor with an IC50 of 1 μM, and has at least 500-fold higher selectivity to ErbB2 than EGFR. Tyrphostin AG 879 has anticancer activity.
  • HY-110328
    PKI-166 hydrochloride

    EGFR Cancer
    PKI-166 hydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.
  • HY-128576
    DS21360717

    Others Cancer
    DS21360717 is a potent and orally active FER tyrosine kinase inhibitor, with an IC50 of 0.49 nM. Anti-cancer activity.
  • HY-117155
    PKI-166

    EGFR Cancer
    PKI-166 is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.
  • HY-N2506
    Ginsenoside Ra1

    Others Cardiovascular Disease
    Ginsenoside Ra1 is a component from ginseng, inhibits protein tyrosine kinase (PTK) activation induced by hypoxia/reoxygenation.
  • HY-112166
    Rilzabrutinib

    PRN1008

    Btk Cancer Metabolic Disease
    Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
  • HY-112096
    eCF506

    Src Cancer
    eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC50 of less than 0.5 nM.
  • HY-133083
    BAY-474

    c-Met/HGFR Cancer
    BAY-474 is a tyrosine-protein kinase c-Met inhibitor. BAY-474 acts as an epigenetics probe.
  • HY-115496
    7-BIA

    Phosphatase Neurological Disease
    7-BIA is a receptor-type protein tyrosine phosphatase D (PTPRD) inhibitor with an IC50 of ~1-3 μM.
  • HY-50878
    Crizotinib

    PF-02341066

    ALK c-Met/HGFR ROS Autophagy Cancer
    Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.
  • HY-108330
    AG126

    Tyrphostin AG126

    ERK Inflammation/Immunology
    AG126 is a tyrosine kinase inhibitor which can prevent the activation of mitogen-activated protein kinase p42MAPK (ERK2).
  • HY-15656S
    Ceritinib D7

    LDK378 D7

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib D7 (LDK378 D7) is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor.
  • HY-32721
    Neratinib

    HKI-272

    EGFR Cancer
    Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
  • HY-138202
    Lck-IN-1

    Src Inflammation/Immunology
    Lck-IN-1 is a potent lymphocyte protein tyrosine kinase (Lck) inhibitor extracted from patent WO2007013673A1, example 48.
  • HY-10159A
    Nilotinib monohydrochloride monohydrate

    AMN107 monohydrochloride monohydrate

    Bcr-Abl Autophagy Cancer
    Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.
  • HY-100314
    BCR-ABL-IN-1

    Bcr-Abl Cancer
    BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia.
  • HY-100462
    PTP1B-IN-2

    Phosphatase Metabolic Disease
    PTP1B-IN-2 is a potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 50 nM.
  • HY-100625
    BVT948

    Phosphatase Cytochrome P450 Histone Methyltransferase Cancer
    BVT948 is a protein tyrosine phosphatase (PTP) inhibitor which can also inhibit several cytochrome P450 (P450) isoforms and lysine methyltransferase SETD8 (KMT5A).
  • HY-10407
    SU 5402

    VEGFR FGFR PDGFR Cancer
    SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
  • HY-13802
    SC-514

    GK 01140

    IKK Cancer
    SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
  • HY-103097
    ST271

    Phospholipase Others
    ST271 is a potent inhibitor of protein tyrosine kinase (PTK), inhibits phospholipase D activation stimulated by fMet-Leu-Phe and PAF, with IC50s of 6.7 and 9 μM, respectively.
  • HY-10395
    PD173955

    Bcr-Abl Src Apoptosis Cancer
    PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.
  • HY-12806
    AG1557

    EGFR Cancer
    AG1557 is a specific and ATP competitive inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, has a pIC50 value of 8.194.
  • HY-13455
    LDN-192960

    Haspin Kinase DYRK Cancer
    LDN-192960 is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
  • HY-13455A
    LDN-192960 hydrochloride

    Haspin Kinase DYRK Cancer
    LDN-192960 hydrochloride is an inhibitor of Haspin and Dual-specificity Tyrosine-regulated Kinase 2 (DYRK2) with IC50s of 10 nM and 48 nM, respectively.
  • HY-50878A
    Crizotinib hydrochloride

    PF-02341066 hydrochloride

    ALK c-Met/HGFR ROS Autophagy Cancer
    Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition.
  • HY-N1750
    3-(2,4-Dihydroxyphenyl)propanoic acid

    Tyrosinase Others
    3-(2,4-Dihydroxyphenyl)propanoic acid (DPPacid) is a potent and competitive tyrosinase inhibitor, inhibits L-Tyrosine and DL-DOPA with an IC50 and a Ki of 3.02 μM and 11.5 μM, respectively.
  • HY-131669
    Dasatinib metabolite M6

    Dasatinib carboxylic acid

    Drug Metabolite Others
    Dasatinib metabolite M6 (Dasatinib carboxylic acid) is an oxidative metabolite of Dasatinib (HY-10181). Dasatinib is a potent and orally active dual Bcr-Abl and Src family tyrosine kinase inhibitor.
  • HY-14596
    Genistein

    NPI 031L

    EGFR Autophagy Apoptosis Endogenous Metabolite Cancer
    Genistein, a soy isoflavone, is a multiple tyrosine kinases (e.g., EGFR) inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.
  • HY-10260B
    Vandetanib hydrochloride

    ZD6474 hydrochloride

    VEGFR Autophagy Apoptosis Cancer
    Vandetanib hydrochloride (D6474 hydrochloride) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib hydrochloride also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
  • HY-10260
    Vandetanib

    ZD6474

    VEGFR Autophagy Apoptosis Cancer
    Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
  • HY-10260A
    Vandetanib trifluoroacetate

    ZD6474 trifluoroacetate

    VEGFR Autophagy Apoptosis Cancer
    Vandetanib trifluoroacetate (D6474 trifluoroacetate) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib trifluoroacetate also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
  • HY-10322
    Falnidamol

    BIBX 1382

    EGFR Cancer
    Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
  • HY-18667
    LTV-1

    Phosphatase Inflammation/Immunology
    LTV-1 is a potent lymphoid tyrosine phosphatase (LYP) inhibitor in T cells with an IC50 of 508 nM. LTV-1 has the potential for autoimmunity treatment.
  • HY-100636
    Gefitinib N-oxide

    EGFR Cancer
    Gefitinib N-oxide is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
  • HY-10159S
    Nilotinib D6

    AMN107 D6

    Bcr-Abl Autophagy Cancer
    Nilotinib D6 (AMN107 D6) is a deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
  • HY-112161
    Branebrutinib

    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.
  • HY-10501
    SU14813

    PDGFR VEGFR c-Kit Cancer
    SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
  • HY-43521
    Ibrutinib-MPEA

    Others 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.
  • HY-10501A
    SU14813 maleate

    PDGFR VEGFR c-Kit Cancer
    SU14813 maleate is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
  • HY-100595
    Sodium stibogluconate

    Stibogluconate trisodium nonahydrate

    Phosphatase Cancer
    Sodium stibogluconate (Stibogluconate trisodium nonahydrate) is a potent inhibitor of protein tyrosine phosphatase. Sodium stibogluconate inhibits 99% of SHP-1, SHP-2 and PTP1B activity at 10, 100, 100 μg/mL, respectively.
  • HY-10644
    Lck inhibitor 2

    Src Inflammation/Immunology
    Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively
  • HY-50683
    JNJ-38877605

    c-Met/HGFR Cancer
    JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.
  • HY-15492
    AG-13958

    AG-013958

    VEGFR Cardiovascular Disease
    AG-13958 (AG-013958), a potent VEGFR tyrosine kinase inhibitor, is used for treatment of choroidal neovascularization associated with age-related macular degeneration (AMD).
  • HY-100024
    NTRC 0066-0

    Others Cancer
    NTRC 0066-0 is a selective threonine tyrosine kinase (TTK) inhibitor (IC50=0.9 nM). NTRC 0066-0 can be used for the research of cancer.
  • HY-80002
    BMX-IN-1

    BMX kinase inhibitor

    Btk BMX Kinase Cancer
    BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys 496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.
  • HY-112345
    PD-089828

    FGFR PDGFR EGFR Src Cancer
    PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.
  • HY-50896S
    Erlotinib D6

    CP-358774 D6; NSC 718781 D6; OSI-774 D6

    EGFR Cancer
    Erlotinib D6 (CP-358774 D6) is a deuterium labeled Erlotinib (CP-358774). Erlotinib is a directly acting inhibitor EGFR tyrosine kinase inhibitor with an IC50 of 2 nM for human EGFR.
  • HY-10981A
    Lenvatinib mesylate

    E7080 mesylate

    VEGFR FGFR PDGFR RET c-Kit Cancer
    Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-10981
    Lenvatinib

    E7080

    VEGFR FGFR PDGFR c-Kit RET Cancer
    Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
  • HY-123390
    DB07107

    Bcr-Abl Akt Cancer
    DB07107 is a potent drug resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM.
  • HY-126319
    SU5204

    VEGFR EGFR Cancer
    SU5204, a tyrosine kinase inhibitor, has IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.
  • HY-130680
    Syk-IN-3

    Syk Cancer
    Syk-IN-3, a potent spleen tyrosine kinase (Syk) inhibitor, extracted from patent WO2011075515A1, compound example 152, has an IC50 of 1 nM.
  • HY-N4185
    Licoflavone A

    Phosphatase Neurological Disease
    Licoflavone A is a flavonoid isolated from the roots of Glycyrrhiza uralensis, inhibits protein tyrosine phosphatase-1B (PTP1B), with an IC50 of 54.5 μM.
  • HY-100867
    TAK-659

    Syk FLT3 Cancer
    TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).
  • HY-100867A
    TAK-659 hydrochloride

    Syk FLT3 Cancer
    TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).
  • HY-118304
    AKN-028

    FLT3 Caspase Cancer
    AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor (IC50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.
  • HY-107145A
    Ningetinib

    TAM Receptor VEGFR c-Met/HGFR Cancer
    Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
  • HY-139300
    Epitinib

    HMPL-813

    EGFR Cancer
    Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer.
  • HY-N6650
    Isotanshinone IIA

    Phosphatase Metabolic Disease
    Isotanshinone IIA, an abietane-type diterpene metabolite, could non-competitively inhibit Protein Tyrosine Phosphatase 1B (PTP1B) activity with an IC50 0f 11.4 μM.
  • HY-50895S
    Gefitinib D8

    ZD1839 D8

    EGFR Autophagy Cancer
    Gefitinib D8 (ZD1839 D8) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
  • HY-N6651
    Isocryptotanshinone

    STAT Phosphatase Cancer
    Isocryptotanshinone is a potent signal transducer and activator of transcription 3 (STAT3) and protein tyrosine phosphatase 1B PTP1B inhibitor, with an IC50 of 56.1 μM for PTP1B.
  • HY-18819
    BCR-ABL-IN-2

    Bcr-Abl Cancer
    BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1 native and ABL1 T315I, respectively.
  • HY-13524
    AG-1478

    Tyrphostin AG-1478; NSC 693255

    EGFR HCV Influenza Virus Cancer Infection Metabolic Disease Cardiovascular Disease
    AG-1478 (Tyrphostin AG-1478) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 has antiviral effects against HCV and encephalomyocarditis virus (EMCV).
  • HY-107145
    Ningetinib Tosylate

    TAM Receptor VEGFR c-Met/HGFR Cancer
    Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
  • HY-13016
    Cabozantinib

    XL184; BMS-907351

    VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis Cancer
    Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
  • HY-19730
    Olmutinib

    HM61713, BI 1482694

    EGFR Cancer
    Olmutinib (HM61713; BI-1482694) is an orally bioavailab and irreversible third EGFR tyrosine kinase inhibitor that binds to a cysteine residue near the kinase domain. Olmutinib is used for NSCLC.
  • HY-128893
    MC-Sq-Cit-PAB-Gefitinib

    Drug-Linker Conjugates for ADC Cancer
    MC-Sq-Cit-PAB-Gefitinib is a drug-linker conjugate for ADC with potent antitumor activity by using Gefitinib (an EGFR tyrosine kinase inhibitor), linked via the ADC linker MC-Sq-Cit-PAB.
  • HY-N0374
    Licochalcone C

    Glucosidase Metabolic Disease
    Licochalcone C could inhibit α-glucosidase, with IC50s of <100 nM and 92.43 μM for α-glucosidase and protein tyrosine phosphatase 1B (PTP1B), respectively.
  • HY-16446
    SAR125844

    c-Met/HGFR Apoptosis Cancer
    SAR125844 is a potent, highly selective, reversible and ATP-competitive MET receptor tyrosine kinase (RTK) inhibitor, with an IC50 of 4.2 nM. Shows inhibition of MET autophosphorylation in cell-based assays.
  • HY-103032
    Multi-kinase inhibitor 1

    PDGFR c-Kit Bcr-Abl Cancer
    Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl.
  • HY-15463S1
    Imatinib D4

    STI571 D4; CGP-57148B D4

    Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib D4 (STI571 D4) is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity.
  • HY-19642
    Glesatinib

    MGCD265

    TAM Receptor c-Met/HGFR Cancer
    Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-19642A
    Glesatinib hydrochloride

    MGCD265 hydrochloride

    TAM Receptor c-Met/HGFR Cancer
    Glesatinib hydrochloride (MGCD265 hydrochloride) is an orally active, potent MET/SMO dual inhibitor. Glesatinib hydrochloride, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).
  • HY-W015007
    Metyrosine

    COX Cardiovascular Disease
    Metyrosine is a selective tyrosine hydroxylase enzyme inhibitor. Metyrosine exerts anti-inflammatory and anti-ulcerative effects. Metyrosine significantly inhibits high COX-2 activity. Metyrosine is a very effective agent for blood pressure control.
  • HY-15463S
    Imatinib D8

    STI571 D8; CGP-57148B D8

    Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib D8 (STI571 D8) is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity.
  • HY-108935
    Lavendustin B

    HIV Integrase GLUT Tyrosinase Cancer
    Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 µM. Lavendustin B is also a weak inhibitor of tyrosine kinases.
  • HY-112800
    cyt-PTPε Inhibitor-1

    Phosphatase Metabolic Disease
    cyt-PTPε Inhibitor-1 is a potent cytosolic protein tyrosine phosphatase epsilon (cyt-PTPε) inhibitor, binds to the catalytic domain of cyt-PTPε, blocks c-Src activation (dephosphorylation of c-Src), and exhibits anti-osteoclastic activity.
  • HY-118532
    Tyrphostin AG30

    AG30

    EGFR Cancer
    Tyrphostin AG30 (AG30) is a potent and selective EGFR tyrosine kinase inhibitor. Tyrphostin AG30 (AG30) selectively inhibits self renewal induction by c-ErbB, and is able to inhibit activation of STAT5 by c-ErbB in primary erythroblasts.
  • HY-101957
    AG 1295

    PDGFR Cardiovascular Disease
    AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor.
  • HY-132549S
    Nilotinib-d3

    Bcr-Abl Autophagy Cancer
    Nilotinib-d3 (AMN107-d3) is the deuterium labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
  • HY-128978
    (E,E)-RAMB4

    Phosphatase Metabolic Disease
    (E,E)-RAMB4 is a potent and selective potent protein tyrosine phosphatase-1B (PTP1B) inhibitor extracted from patent CN103626692A, example 1.
  • HY-139300A
    Epitinib succinate

    HMPL-813 succinate

    EGFR Cancer
    Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer.
  • HY-13979
    DDR1-IN-1

    Discoidin Domain Receptor Cancer
    DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM).
  • HY-12297
    Sulfatinib

    HMPL-012

    FGFR VEGFR Cancer
    Sulfatinib (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50s of in a range of 1 to 24 nM.
  • HY-50898
    Lapatinib

    GW572016; GW2016

    EGFR Autophagy Ferroptosis Cancer
    Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
  • HY-128571
    FLT3-IN-4

    FLT3 Cancer
    FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia.
  • HY-13979A
    DDR1-IN-1 dihydrochloride

    Discoidin Domain Receptor Cancer
    DDR1-IN-1 dihydrochloride is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM).
  • HY-10255A
    Sunitinib

    SU 11248

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-125017
    Bozitinib

    PLB-1001; CBT-101; Vebreltinib

    c-Met/HGFR Cancer
    Bozitinib (PLB-1001) is a highly selective c-MET kinase inhibitor with blood-brain barrier permeability. Bozitinib (PLB-1001) is a ATP-competitive small-molecule inhibitor, binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily.
  • HY-128757
    Remibrutinib

    Btk Inflammation/Immunology
    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.
  • HY-10517
    Orantinib

    SU6668; TSU-68

    PDGFR FGFR VEGFR Apoptosis Cancer
    Orantinib (SU6668; TSU-68) is a multi-targeted receptor tyrosine kinase inhibitor with Kis of 2.1 μM, 8 nM and 1.2 μM for Flt-1, PDGFRβ and FGFR1, respectively.
  • HY-18314
    GW 441756

    Trk Receptor Apoptosis Cancer Neurological Disease
    GW 441756 is a potent and specific nerve growth factor (NGF) receptor tyrosine kinases A (TrkA) inhibitor (IC50=2 nM), which eliminates the BmK NSPK-induced neurite outgrowth.
  • HY-10065
    Axitinib

    AG-013736

    VEGFR PDGFR Cancer
    Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
  • HY-10460
    PF-431396

    Pyk2 FAK Cancer
    PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively.
  • HY-117900A
    (Rac)-PF-06250112

    Others Inflammation/Immunology
    (Rac)-PF-0625011 is a racemate of PF-06250112. PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor and shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC.
  • 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.
  • HY-15511
    Tyrphostin A9

    Tyrphostin 9; Malonoben

    VEGFR Influenza Virus Cancer Infection
    Tyrphostin A9, a PDGFR inhibitor, is a potent inducer of mitochondrial fission. Tyrphostin A9 emerged as the most potent and selective of 51 tyrosine kinase inhibitors tested against the TNF-induced respiratory burst. Tyrphostin A9 has anti-influenza virus activities.
  • HY-12219A
    MSI-1436 lactate

    Trodusquemine lactate; Aminosterol-1436 lactate

    Phosphatase Endocrinology
    MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
  • HY-50898B
    Lapatinib ditosylate

    GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate

    EGFR Autophagy Ferroptosis Cancer
    Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
  • HY-15749
    XL228

    Aurora Kinase Bcr-Abl IGF-1R Src Cancer Endocrinology
    XL228 is a multi-targeted tyrosine kinase inhibitor with IC50s of 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src and Lyn, respectively.
  • HY-13223
    Crenolanib

    CP-868596

    FLT3 PDGFR Autophagy Cancer
    Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
  • HY-12219
    MSI-1436

    Trodusquemine; Aminosterol-1436

    Phosphatase Endocrinology
    MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).
  • HY-113468A
    3-O-Methyldopa

    3-Methoxy-L-Tyrosine; 3-O-Methyl-L-DOPA

    Dopamine Receptor Endogenous Metabolite Neurological Disease
    3-O-Methyldopa (3-Methoxy-L-tyrosine) is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine.
  • HY-50898A
    Lapatinib ditosylate

    GW572016 ditosylate; GW2016 ditosylate

    EGFR Autophagy Ferroptosis Cancer
    Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
  • HY-10255
    Sunitinib Malate

    SU 11248 Malate

    PDGFR VEGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-12044
    Cabozantinib S-malate

    XL184 S-malate; BMS-907351 S-malate

    VEGFR Apoptosis Cancer
    Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
  • HY-125510
    UNC2541

    TAM Receptor Others
    UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor, binds in the MerTK ATP pocket, with an IC50 of 4.4 nM, more selective over Axl, Tyro3 and Flt3. UNC2541 inhibits phosphorylated MerTK (pMerTK; EC50, 510 nM).
  • HY-10991
    MGCD-265 analog

    c-Met/HGFR VEGFR Apoptosis Cancer
    MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2 tyrosine kinases, with IC50s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity.
  • HY-N1549
    Prunin

    Naringenin 7-0-glucoside

    Enterovirus Phosphatase Infection Metabolic Disease
    Prunin is a potent inhibitor of human enterovirus A71 (HEVA71). Prunin shows strong inhibitory activity against protein tyrosine phosphatase 1B (PTP1B), with an IC50 of 5.5 µM.
  • HY-N4143
    Cyanidin 3-arabinoside

    Phosphatase Metabolic Disease
    Cyanidin 3-arabinoside is a selective and reversible protein tyrosine phosphatase 1B (PTP1B) inhibitor, with an IC50 of 8.91 μM. Cyanidin 3-arabinoside is potential for the research of type 2 diabetes.
  • HY-19981
    Derazantinib

    ARQ-087

    FGFR Cancer
    Derazantinib (ARQ-087) is an orally bioavailable, ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
  • HY-13524A
    AG-1478 hydrochloride

    Tyrphostin AG-1478 hydrochloride; NSC 693255 hydrochloride

    EGFR HCV Influenza Virus Cancer Infection Metabolic Disease Cardiovascular Disease
    AG-1478 hydrochloride (Tyrphostin AG-1478 hydrochloride) is a selective EGFR tyrosine kinase inhibitor with IC50 of 3 nM. AG-1478 hydrochloride has antiviral effects against HCV and encephalomyocarditis virus (EMCV).
  • HY-109061
    Lazertinib

    YH25448; GNS-1480

    EGFR Cancer
    Lazertinib (YH25448) is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer.
  • HY-109143
    Elsubrutinib

    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.
  • HY-14435
    Pyridone 6

    JAK Cancer
    Pyridone 6 is a pan-JAK inhibitor, which potently inhibits the JAK kinase family, with IC50s of 1 nM for JAK2 and TYK2, 5 nM for JAK3, and 15 nM for JAK1, while displaying significantly weaker affinities (130 nM to >10 mM) for other protein tyrosine kinases.
  • HY-10260S1
    Vandetanib-d4

    VEGFR Autophagy Apoptosis Cancer
    Vandetanib-d4 (ZD6474-d4) is the deuterium labeled Vandetanib. Vandetanib (ZD6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
  • HY-101549
    MRX-2843

    UNC2371

    FLT3 Cancer
    MRX-2843 (UNC2371) is an orally active, ATP-competitive dual MERTK and FLT3 tyrosine kinases inhibitor (TKI) with enzymatic IC50s of 1.3 nM for MERTK and 0.64 nM for FLT3, respectively.
  • HY-N2451
    Aloe-emodin-8-O-β-D-glucopyranoside

    Phosphatase Endocrinology Metabolic Disease
    Aloe-emodin-8-O-β-D-glucopyranoside, a compound isolated from Saussrurea lappa, is a moderate inhibitor of human protein tyrosine phosphatase 1B (hPTP1B) with an IC50 of 26.6 μM.
  • HY-W008452
    H-Tyr(3-I)-OH

    Endogenous Metabolite Metabolic Disease
    H-Tyr(3-I)-OH is a potent and effective tyrosine hydroxylase inhibitor. H-Tyr(3-I)-OH is an intermediate in the production of thyroid hormones and has a role as a human or mouse metabolite.
  • HY-136179
    ZAP-180013

    Tyrosinase Inflammation/Immunology
    ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs).
  • HY-19981A
    Derazantinib Racemate

    ARQ-087 Racemate

    FGFR Cancer
    Derazantinib Racemate (ARQ-087 Racemate) is the racemate of Derazantinib. Derazantinib is an orally bioavailable, ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
  • HY-123846
    MLS-0437605

    Phosphatase Cardiovascular Disease
    MLS-0437605 is a selective dual-specificity phosphatase 3 (DUSP3) inhibitor with an IC50 of 3.7 μM. MLS-0437605 is more selective for DUSP3 than DUSP22 and other protein tyrosine phosphatases (PTPs).
  • HY-10205
    Cediranib

    AZD2171

    VEGFR Autophagy PDGFR Cancer
    Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
  • HY-103018
    Gusacitinib

    ASN-002

    JAK Syk Cancer
    Gusacitinib (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Gusacitinib has anti-cancer activity in both solid and hematological tumor types.
  • HY-10234
    Saracatinib

    AZD0530

    Src Autophagy Cancer
    Saracatinib (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib shows high selectivity over other tyrosine kinases.
  • HY-128758
    DYRKs-IN-1

    DYRK Cancer
    DYRKs-IN-1 is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 has antitumor activity.
  • HY-108372
    Boc-C5-O-C5-O-C6-Cl

    PROTAC Linker 2

    PROTAC Linker Cancer
    Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.
  • HY-128758A
    DYRKs-IN-1 hydrochloride

    DYRK Cancer
    DYRKs-IN-1 hydrochloride is a potent DYRKs (Dual-specificity tyrosine-phosphorylation-regulated kinases) inhibitor with IC50s of 5 nM and 8 nM for DYRK1A and DYRK1B, respectively. DYRKs-IN-1 hydrochloride has antitumor activity.
  • HY-117900
    PF-06250112

    Btk Inflammation/Immunology
    PF-06250112 is a potent, highly selective, orally bioavailable BTK inhibitor with an IC50 of 0.5 nM, shows inhibitory effect toward BMX nonreceptor tyrosine kinase and TEC with IC50s of 0.9 nM and 1.2 nM, respectively.
  • HY-112215
    ARQ 531

    MK-1026

    Btk Cancer Inflammation/Immunology
    ARQ 531 (MK-1026) 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.
  • HY-50867
    Lestaurtinib

    CEP-701; KT-5555

    JAK FLT3 Trk Receptor Cancer
    Lestaurtinib (CEP-701;KT-5555) is an ATP-competitive multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.
  • HY-16590
    X-376

    ALK c-Met/HGFR Cancer
    X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity.
  • HY-118203
    SU4984

    FGFR PDGFR Insulin Receptor Cancer
    SU4984 is a protein tyrosine kinase inhibitor, with an IC50 of 10-20 μM for fibroblast growth factor receptor 1 (FGFR1). SU4984 is also inhibits platelet-derived growth factor receptor, and insulin receptor. SU4984 can be used for the research of cancer.
  • HY-121515A
    DPM-1001 trihydrochloride

    Phosphatase Metabolic Disease
    DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property.
  • HY-121515
    DPM-1001

    Phosphatase Metabolic Disease
    DPM-1001 is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 has anti-diabetic property.
  • HY-13314
    Tesevatinib

    XL-647; EXEL-7647; KD-019

    EGFR VEGFR Ephrin Receptor Cancer
    Tesevatinib (XL-647; EXEL-7647; KD-019) is an orally available, multi-target tyrosine kinase inhibitor; inhibits EGFR, ErbB2, KDR, Flt4 and EphB4 kinase with IC50s of 0.3, 16, 1.5, 8.7, and 1.4 nM.
  • HY-107367
    Epertinib

    S-22611

    EGFR Cancer
    Epertinib (S-22611) is a potent, oral, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib shows potent antitumor activity.
  • HY-32721S
    Neratinib-d6

    EGFR Cancer
    Neratinib-d6 (HKI-272-d6) is the deuterium labeled Neratinib. Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.
  • HY-50896
    Erlotinib

    CP-358774; NSC 718781; OSI-774

    EGFR Autophagy Cancer
    Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer.
  • HY-114356
    BPI-9016M

    c-Met/HGFR Cancer
    BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma.
  • HY-50896S1
    Erlotinib-13C6

    CP-358774-13C6; NSC 718781-13C6; OSI-774-13C6

    EGFR Autophagy Cancer
    Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR.
  • HY-10255AS
    Sunitinib D10

    SU 11248 D10

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-12736
    GSK143

    Syk PERK Cancer Inflammation/Immunology
    GSK143 is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
  • HY-12736A
    GSK143 dihydrochloride

    Syk PERK Cancer Inflammation/Immunology
    GSK143 dihydrochloride is an orally active and highly selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.5. GSK143 dihydrochloride inhibits phosphorylated Erk (pErk: pIC50=7.1). GSK143 dihydrochloride reduces inflammation and prevents recruitment of immune cells in the intestinal muscularis in mice.
  • HY-101084
    NSC 228155

    EGFR Histone Acetyltransferase Epigenetic Reader Domain Cancer
    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.
  • HY-107459
    (E/Z)-AG490

    (E/Z)-Tyrphostin AG490; (E/Z)-Tyrphostin B42

    EGFR STAT JAK Cancer
    (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
  • HY-50895
    Gefitinib

    ZD1839

    EGFR Autophagy Cancer
    Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-50895A
    Gefitinib hydrochloride

    ZD-1839 hydrochloride

    EGFR Cancer
    Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity.
  • HY-16018
    Ilorasertib

    ABT-348

    Aurora Kinase VEGFR PDGFR RET Cancer
    Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively.
  • HY-N8200
    Cassiaside B2

    Phosphatase Monoamine Oxidase 5-HT Receptor Inflammation/Immunology
    Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a 5-HT2C receptor agonist...
  • HY-12768
    Sotuletinib

    BLZ945

    c-Fms Cancer
    Sotuletinib (BLZ945) is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs.
  • HY-13896
    PD168393

    EGFR Autophagy Apoptosis Cancer
    PD168393 is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC.
  • HY-15756
    PTP1B-IN-4

    Phosphatase Metabolic Disease
    PTP1B-IN-4 is a non-competitive allosteric inhibitor of the protein tyrosine phosphatase PTP1B, with an IC50 of 8 μM. PTP1B-IN-4 is potentail for the research of obesity and diabetes.
  • HY-107367A
    Epertinib hydrochloride

    S-22611 hydrochloride

    EGFR Cancer
    Epertinib hydrochloride (S-22611 hydrochloride) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER2 and HER4, with IC50s of 1.48 nM, 7.15 nM and 2.49 nM, respectively. Epertinib hydrochloride shows potent antitumor activity.
  • HY-101466A
    E7090 succinate

    FGFR Cancer
    E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively.
  • HY-101964
    SPI-112

    Phosphatase Cancer
    SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively.
  • HY-W013857
    Lavendustin C

    CaMK EGFR Src Cancer
    Lavendustin C is a potent Ca 2+ calmodulin-dependent kinase II (CaMK II) inhibitor with an IC50 of 0.2 µM. Lavendustin C inhibits EGFR-associated tyrosine kinase (IC50=0.012 µM) and pp60 c-src(+) kinase (IC50=0.5 µM) .
  • HY-129390
    Orelabrutinib

    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.
  • HY-10330
    Toceranib

    SU11654; PHA 291639E

    PDGFR VEGFR c-Kit Cancer
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
  • HY-10330A
    Toceranib phosphate

    SU11654 phosphate; PHA 291639E phosphate

    PDGFR VEGFR c-Kit Cancer
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors .
  • HY-110193
    SPP-86

    RET Cancer
    SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
  • HY-10331
    Regorafenib

    BAY 73-4506

    VEGFR Autophagy PDGFR Raf RET Cancer
    Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
  • HY-N7599
    Chrysophanol triglucoside

    Phosphatase Glucosidase Metabolic Disease
    Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia, inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC50s of 80.17 and 197.06 µM, respectively. Chrysophanol triglucoside has the potential for diabetes research.
  • HY-10255AS1
    Sunitinib-d4

    VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis Cancer
    Sunitinib-d4 (SU 11248-d4) is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
  • HY-139481
    TL-895

    Btk Cancer Infection
    TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible bruton’s tyrosine kinase (BTK) inhibitor. TL-895 is used be for JAKi-relapsed/refractory myelofibrosis, acute myeloid leukemia, COVID-19 and cancer research.
  • HY-112299
    TAS6417

    CLN-081

    EGFR Apoptosis Cancer
    TAS6417 (CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM.
  • HY-15838
    ID-8

    DYRK Cancer
    ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs.
  • HY-119757
    Tyrphostin AG1433

    SU1433; AG1433

    PDGFR VEGFR Cancer
    Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation.
  • HY-15656A
    Ceritinib dihydrochloride

    LDK378 dihydrochloride

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency.
  • HY-14674
    CP-724714

    EGFR Apoptosis Cancer
    CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities.
  • HY-15656
    Ceritinib

    LDK378

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency.
  • HY-15463
    Imatinib

    STI571; CGP-57148B

    Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
  • HY-N6856
    4-Hydroxycoumarin

    Endogenous Metabolite Bacterial Infection
    4-Hydroxycoumarin, a coumarin derivative, is one of the most versatile heterocyclic scaffolds and is frequently applied in the synthesis of various organic compounds. 4-Hydroxycoumarin possesses both electrophilic and nucleophilic properties. 4-Hydroxycoumarin derivatives are employed as the anticoagulant, antibacterial, antifungal, antiviral, antitumor, antiprotozoal, insecticidal, antimycobacterial, antimutagenic, antioxidant, anti-inflammatory agents, HIV protease inhibitors and tyrosine kinase inhibitors.
  • HY-10704
    PTP1B-IN-1

    PTP1B inhibitor

    Phosphatase Metabolic Disease
    PTP1B-IN-1 is a potent protein tyrosine phosphatase-1B (PTP1B) inhibitor with IC50 of 1.6 mM; 1,2,5-thiadiazolidin-3-one-1,1-dioxide scaffold for derivatives synthesis.
  • HY-16018A
    Ilorasertib hydrochloride

    ABT-348 hydrochloride

    Aurora Kinase PDGFR RET VEGFR Cancer
    Ilorasertib (ABT-348 hydrochloride) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib (ABT-348 hydrochloride) also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively.
  • HY-133779
    Gefitinib impurity 5

    Others Others
    Gefitinib impurity 5 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-131257
    Gefitinib impurity 1

    Others Others
    Gefitinib impurity 1 is the impurity of Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-118567
    Bis(maltolato)oxovanadium(IV)

    BMOV

    Phosphatase Metabolic Disease
    Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer.
  • HY-P1111
    Lyn peptide inhibitor

    Src Interleukin Related Inflammation/Immunology
    Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of  asthma, allergic, and other eosinophilic disorders.
  • HY-16576A
    (Z)-SMI-4a

    Pim Cancer
    (Z)-SMI-4a is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 µM. (Z)-SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. (Z)-SMI-4a has anticancer activity.
  • HY-100663
    Gefitinib impurity 2

    Others Others
    Gefitinib impurity 2 is the impurity of Gefitinib. Gefitinib (ZD1839; HY-50895) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-18756A
    NSC-87877 disodium

    Phosphatase Apoptosis Cancer
    NSC-87877 disodium is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).
  • HY-13016S
    Cabozantinib-d6

    VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis Cancer
    Cabozantinib-d6 (XL184-d6) is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
  • HY-10252
    NVP-ADW742

    ADW742; GSK 552602A; ADW

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
  • HY-18756
    NSC-87877

    Phosphatase Apoptosis Others
    NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).
  • HY-131275
    Imatinib Impurity E

    Others Others
    Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
  • HY-P1111A
    Lyn peptide inhibitor TFA

    Src Interleukin Related Inflammation/Immunology
    Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of  asthma, allergic, and other eosinophilic disorders.
  • HY-113468AS
    3-O-Methyldopa D3

    3-Methoxy-L-Tyrosine D3; 3-O-Methyl-L-DOPA D3

    Dopamine Receptor Endogenous Metabolite Neurological Disease
    3-O-Methyldopa D3 (3-Methoxy-L-tyrosine D3) is deuterium labeled 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of l-DOPA and dopamine.
  • HY-13302
    CP-547632

    VEGFR FGFR Cancer
    CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy.
  • HY-B0062
    Dovitinib lactate hydrate

    TKI258 lactate hydrate; CHIR-258 lactate hydrate

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib lactate hydrate (TKI258 lactate hydrate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
  • HY-13302B
    CP-547632 hydrochloride

    VEGFR FGFR Cancer
    CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy.
  • HY-10207
    Dovitinib lactate

    CHIR-258 lactate; TKI-258 lactate

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
  • HY-50898BS
    Lapatinib-d7 ditosylate

    EGFR Autophagy Ferroptosis Cancer
    Lapatinib-d7 (GW572016-d7) ditosylate is the deuterium labeled Lapatinib. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
  • HY-10065S1
    Axitinib-d3

    AG-013736-d3

    VEGFR Cancer
    Axitinib-d3 (AG-013736-d3) is deuterium labeled Axitinib. Axitinib is a multi-targeted tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.6 nM for VEGFR1, VEGFR2, VEGFR3 and PDGFRβ, respectively.
  • HY-109189
    Rezivertinib

    BPI-7711

    EGFR Cancer
    Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity.
  • HY-B0537A
    Pentamidine dihydrochloride

    MP-601205 dihydrochloride

    Parasite Fungal Phosphatase Bacterial Antibiotic Cancer Infection
    Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
  • HY-10185
    TG 100572 Hydrochloride

    Src VEGFR FGFR PDGFR Inflammation/Immunology
    TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-B0537
    Pentamidine

    MP-601205

    Parasite Fungal Phosphatase Bacterial Antibiotic Cancer Infection
    Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
  • HY-10184
    TG 100572

    Src VEGFR PDGFR FGFR Cancer
    TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-101042
    AG-494

    Tyrphostin AG 494

    EGFR CDK Cancer
    AG-494 (Tyrphostin AG 494) is a potent and selective EGFR tyrosine kinase inhibitor (IC50=0.7 μM). AG-494 inhibits the autophosphorylation of EGFR, ErbB2, HER1-2 and PDGF-R with IC50s 1.1, 39, 45 and 6 μM, respectively. AG-494 blocks Cdk2 activation and inhibits EGF-dependent DNA synthesis.
  • HY-78263
    MNS

    NSC 170724; 5-(2-Nitrovinyl)benzodioxole

    Src Syk Cancer
    MNS (NSC 170724), the beta-nitrostyrene derivative, is a potent tyrosine kinase inhibitor and a broad-spectrum antiplatelet agent. MNS completely inhibits U46619, ADP-, arachidonic acid-, collagen-, and thrombin-induced platelet aggregation with IC50 values of 2.1, 4.1, 5.8, 7.0, and 12.7 μM, respectively. MNS inhibits Src, Syk, and FAK with IC50 of 27.3, 2.8, and 97.6 μM, respectively.
  • HY-131088
    N3-PEG8-Phe-Lys-PABC-Gefitinib

    Drug-Linker Conjugates for ADC Cancer
    N3-PEG8-Phe-Lys-PABC-Gefitinib is a drug-linker conjugate for ADC with potent antitumor activity by using the anti-tumor agent, Gefitinib (orally active EGFR tyrosine kinase inhibitor), linked via the cleavable linker N3-PEG8-Phe-Lys-PABC.
  • HY-108263
    3-Hydroxy Midostaurin

    CGP52421

    FLT3 Cancer
    3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50s of approximately 132 nM and 9.8 μM in culture medium and plasma, respectively. 3-Hydroxy Midostaurin is less selective but more cytotoxic than PKC412.
  • HY-122906
    JTE-952

    c-Fms Inflammation/Immunology
    JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis.
  • HY-133146
    DJ001

    Phosphatase Apoptosis Inflammation/Immunology
    DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration.
  • HY-109192
    Tolebrutinib

    SAR442168; PRN2246

    Btk Neurological Disease
    Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).
  • HY-100499
    Tyrphostin AG 528

    Tyrphostin B66; AG 528

    EGFR Cancer
    Tyrphostin AG 528 is an inhibitor of EGFR and ErbB2 with IC50s of 4.9 and 2.1 μM, respectively. Tyrphostin AG 528 (Tyrphostin B66) is a protein tyrosine kinase inhibitor, with IC50s of 4.9 μM for epidermal growth factor receptors (EGFR) and 2.1 μM for ErbB2. Tyrphostin AG 528 is also an anticancer agent.
  • HY-15424
    5-Iodotubercidin

    NSC 113939; 5-ITu

    Adenosine Kinase Cancer
    5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin.
  • HY-18303
    AMG-47a

    Src VEGFR p38 MAPK JAK Inflammation/Immunology
    AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2, p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity.
  • HY-N6732
    K-252a

    SF2370; Antibiotic K 252a; Antibiotic SF 2370

    PKC PKA CaMK Trk Receptor Autophagy Antibiotic Infection Inflammation/Immunology
    K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
  • HY-50895S2
    Gefitinib-d3

    EGFR Autophagy Cancer
    Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity.
  • HY-B0537B
    Pentamidine isethionate

    MP-601205 isethionate

    Parasite Fungal Phosphatase Bacterial Antibiotic Infection Cancer
    Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
  • HY-103441
    JNJ28871063 hydrochloride

    EGFR Cancer
    JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.
  • HY-137092
    IACS-13909

    Phosphatase Cancer
    IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers.
  • HY-13302C
    CP-547632 TFA

    VEGFR FGFR Cancer
    CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy.
  • HY-123931
    ZLDI-8

    Notch Phosphatase Apoptosis Cancer
    ZLDI-8 is a Notch activating/cleaving enzyme ADAM-17 inhibitor and inhibits the cleavage of Notch protein. ZLDI-8 decreases the expression of pro-survival/anti-apoptosis and epithelial-mesenchymal transition (EMT) related proteins. ZLDI-8 is also a competitive and irreversible tyrosine phosphatase (Lyp) inhibitor with an IC50 of 31.6 μM and a Ki of 26.22 μM. ZLDI-8 inhibits the growth of MHCC97-H cells with an IC50 of 5.32 μM.
  • HY-100434
    PD-161570

    FGFR PDGFR EGFR Src TGF-β Receptor Cancer Cardiovascular Disease
    PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
  • HY-108485
    Damnacanthal

    Src Apoptosis Fungal Cancer Infection Inflammation/Immunology
    Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans.
  • HY-10330S
    Toceranib-d8

    PDGFR VEGFR c-Kit Cancer
    Toceranib-d8 (SU11654-d8) is the deuterium labeled Toceranib. Toceranib (SU11654) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively. Toceranib (SU11654) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
  • HY-16558
    Butein

    2’,3,4,4’-tetrahydroxy Chalcone

    EGFR Autophagy Apoptosis Phosphodiesterase (PDE) Cancer
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
  • HY-130854
    Thalidomide-NH-C6-NH-Boc

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A).
  • HY-135334
    ACP-5862

    Drug Metabolite Btk Cytochrome P450 Cancer
    ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM.
  • HY-50905
    Dovitinib

    CHIR-258; TKI258

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively.
  • HY-19834
    Fenebrutinib

    GDC-0853

    Btk Cancer
    Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.
  • HY-10206
    Amuvatinib

    MP470; HPK 56

    c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Apoptosis Cancer
    Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
  • HY-10206A
    Amuvatinib hydrochloride

    MP470 hydrochloride; HPK 56 hydrochloride

    c-Kit PDGFR RAD51 FLT3 c-Met/HGFR RET Cancer
    Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
  • HY-130616
    EGFR-IN-11

    EGFR Apoptosis Cancer
    EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.
  • HY-N2278
    Kushenol A

    Leachianone E

    Tyrosinase Glucosidase Cancer
    Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively. Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase. Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging.
  • HY-112776
    BN82002

    Phosphatase Cancer
    BN82002 is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 displays ~20-fold greater selectivity over CD45 tyrosine phosphatase.
  • HY-13001
    Quizartinib

    AC220

    FLT3 Ligand for Target Protein for PROTAC Apoptosis Autophagy Cancer
    Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis.
  • HY-116624
    MAZ51

    VEGFR Apoptosis Cancer
    MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity.
  • HY-120327
    KY-226

    Phosphatase Metabolic Disease Neurological Disease
    KY-226 is a potent, selective, orally active and allosteric protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 0.25 μM, and without PPARγ agonist activity. KY-226 exerts anti-diabetic and anti-obesity effects by enhancing insulin and leptin signaling, respectively. KY-226 also protects neurons from cerebral ischemic injury.
  • HY-137460
    Vodobatinib

    K0706

    Bcr-Abl Cancer
    Vodobatinib (K0706) is a potent, third generation and orally active Bcr-Abl1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants, and has no activity against BCR-ABL1T315I. Vodobatinib can be used for chronic myeloid leukemia (CML) research.
  • HY-11107
    PHA-665752

    c-Met/HGFR Autophagy Apoptosis Cancer
    PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (Ki=4 nM; IC50=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity.
  • HY-15844
    AG-825

    Tyrphostin AG-825

    EGFR Apoptosis Cancer Inflammation/Immunology Neurological Disease
    AG-825 (Tyrphostin AG-825) is a selective and ATP-competitive ErbB2 inhibitor which suppresses tyrosine phosphorylation, with an IC50 of 0.35 μM. AG-825 displays anti-cancer activity. AG825 significantly accelerates apoptosis of human neutrophils. AG-825 is a potential agent for overcoming Mn-induced neurotoxicity or AD development.
  • HY-10524
    GSK1904529A

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.
  • HY-12972
    Mavelertinib

    PF-06747775

    EGFR Cancer
    Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).
  • HY-N4201
    β-Hydroxyisovalerylshikonin

    EGFR Src Cancer
    Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermium radix, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.
  • HY-B0879A
    Suramin sodium salt

    Suramin hexasodium salt

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase SARS-CoV Parasite Apoptosis Cancer Infection Cardiovascular Disease
    Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
  • HY-B0879
    Suramin

    Phosphatase Sirtuin Reverse Transcriptase Topoisomerase SARS-CoV Parasite Apoptosis Cancer Infection Cardiovascular Disease
    Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor.Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
  • HY-10187
    TG 100801 Hydrochloride

    VEGFR FGFR PDGFR Src Cancer
    TG 100801 Hydrochloride is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-110208
    BRD9876

    Kinesin Microtubule/Tubulin Cancer
    BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research.
  • HY-50751
    Linifanib

    ABT-869; AL-39324

    PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis Cancer
    Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
  • HY-10186
    TG 100801

    VEGFR FGFR PDGFR Src Cancer
    TG 100801 is a prodrug that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
  • HY-135680
    I-OMe-Tyrphostin AG 538

    I-OMe-AG 538

    IGF-1R Cancer Metabolic Disease
    I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
  • HY-109010
    Poseltinib

    HM71224; LY3337641

    Btk BMX Kinase Toll-like Receptor (TLR) Metabolic Disease
    Poseltinib, an orally active, selective and irreversible Bruton’s tyrosine kinase (BTK) inhibitor (IC50 =1.95 nM), with 0.3, 2.3 and 2.4-fold selectivity for BTK over BMX, TEC and TXK, respectively. Poseltinib can covalently bind to the active site (cysteine 481 residue) of BTK, and reveales potent inhibition of B cell receptor (BCR), Fc receptor (FcR), Toll-like receptor (TLR) mediated signaling.
  • HY-10408
    Ki20227

    c-Fms VEGFR c-Kit PDGFR Inflammation/Immunology
    Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.
  • HY-W011266
    JNJ-10198409

    PDGFR Cancer
    JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM).
  • HY-103693
    NAZ2329

    Phosphatase Cancer
    NAZ2329, the first cell-permeable inhibitor of R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs), allosterically and preferentially inhibits PTPRZ (IC50=7.5 µM for hPTPRZ1) and PTPRG (IC50=4.8 µM for hPTPRG) over other PTPs. NAZ2329 binds to the active D1 domain and more potently inhibits PTPRZ-D1 fragment (IC50 of 1.1 µM) than the whole intracellular (D1 + D2) fragment (IC50 of 7.5 µM). NAZ2329 can effectively inhibit tumor growth of the glioblastoma cells and suppress stem cell-like properties.
  • HY-13775
    XL019

    JAK Apoptosis Cancer
    XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.
  • HY-16961
    Sitravatinib

    MGCD516; MG-516

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-50905S
    Dovitinib-D8

    FLT3 c-Kit FGFR VEGFR PDGFR Cancer
    Dovitinib-D8 (CHIR-258-D8) is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively.
  • HY-109041
    Razuprotafib

    AKB-9778

    Phosphatase Inflammation/Immunology
    Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM).
  • HY-136065
    bpV(phen)

    PTEN Phosphatase Parasite Apoptosis Cancer Infection Metabolic Disease Inflammation/Immunology
    bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
  • HY-16961A
    Sitravatinib malate

    MGCD516 malate; MG-516 malate

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-129550
    BI-4020

    EGFR Cancer
    BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties.
  • HY-122818
    bpV(phen) trihydrate

    PTEN Phosphatase Parasite Apoptosis Cancer Infection Metabolic Disease Inflammation/Immunology
    bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
  • HY-112823
    Almonertinib

    HS-10296

    EGFR Cancer
    Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer.
  • HY-112823B
    Almonertinib hydrochloride

    HS-10296 hydrochloride

    EGFR Cancer
    Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer.