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kinase-1

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448

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3

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4

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26

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21

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143

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11

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160

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1

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GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-136270
    Gartisertib
    5 Publications Verification

    VX-803; M4344; ATR inhibitor 2

    ATM/ATR Cancer
    Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity [1] .
    Gartisertib
  • HY-15425
    PF-543
    20+ Cited Publications

    Sphingosine kinase 1 Inhibitor II

    SphK LPL Receptor Apoptosis Autophagy Cardiovascular Disease Inflammation/Immunology Cancer
    PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy [1] .
    PF-543
  • HY-111941
    GSK8612
    25+ Cited Publications

    IKK Neurological Disease Inflammation/Immunology Cancer
    GSK8612 is a highly selective and potent Tank-binding Kinase-1 (TBK1) inhibitor, with a pIC50 of 6.8 for recombinant TBK1 [1].
    GSK8612
  • HY-50877
    GSK461364
    15+ Cited Publications

    GSK461364A

    Polo-like Kinase (PLK) Cancer
    GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM.
    GSK461364
  • HY-12279
    Umbralisib
    5 Publications Verification

    TGR-1202; RP5264

    PI3K Casein Kinase Cancer
    Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach [1] .
    Umbralisib
  • HY-15532
    SCH900776
    10+ Cited Publications

    MK-8776

    Checkpoint Kinase (Chk) Cancer
    SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively [1] .
    SCH900776
  • HY-15425A
    PF-543 Citrate
    20+ Cited Publications

    Sphingosine kinase 1 Inhibitor II Citrate

    SphK LPL Receptor Apoptosis Autophagy Cardiovascular Disease Inflammation/Immunology Cancer
    PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy [1] .
    PF-543 Citrate
  • HY-12045
    HMN-214
    3 Publications Verification

    IVX-214

    Polo-like Kinase (PLK) Cancer
    HMN-214, an orally bioavailable proagent of HMN-176, is an inhibitor of polo-like kinase-1 (plk1), with antitumor activity.
    HMN-214
  • HY-W011109
    CKI-7
    1 Publications Verification

    Casein Kinase CDK SGK Ribosomal S6 Kinase (RSK) Cancer
    CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases .
    CKI-7
  • HY-114371

    DNL-758; SAR-443122

    RIP kinase Inflammation/Immunology
    Eclitasertib (DNL-758) is a potent receptor-interacting protein kinase 1 (RIPK1) inhibitor with an IC50 of 0.0375 µΜ [1].
    Eclitasertib
  • HY-148297

    LY3871801; R 552

    RIP kinase Inflammation/Immunology
    Ocadusertib is a potent Serine/Threonine kinase receptor-interacting protein kinase 1 (RIPK1) inhibitor [1].
    Ocadusertib
  • HY-133028
    CKI-7 free base
    1 Publications Verification

    Casein Kinase CDK SGK Ribosomal S6 Kinase (RSK) Cancer
    CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases .
    CKI-7 free base
  • HY-12892
    SKI-178
    1 Publications Verification

    SphK Apoptosis Cancer
    SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines [1] .
    SKI-178
  • HY-14440
    MP7
    2 Publications Verification

    PDK1 inhibitor

    PDK-1 Cancer
    MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
    MP7
  • HY-19566
    NQDI-1
    5+ Cited Publications

    MAP3K Apoptosis Cancer
    NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a Ki of 500 nM and an IC50 of 3 μM.
    NQDI-1
  • HY-13647

    Polo-like Kinase (PLK) Mitosis Cancer
    HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1), without significant effect on tubulin polymerization.
    HMN-176
  • HY-148455

    Casein Kinase Neurological Disease
    Casein kinase 1δ-IN-3 (Compound 23a) is a casein kinase 1 delta (CK1d) inhibitor with a pIC50 of 6.5376 M [1].
    Casein kinase 1δ-IN-3
  • HY-117291A
    XMD-17-51 TFA
    1 Publications Verification

    Mps1 ERK Polo-like Kinase (PLK) Bcr-Abl AMPK Trk Receptor Others
    XMD-17-51 TFA is a pyrimido-diazepinone compound that is able to modulate protein kinases .
    XMD-17-51 TFA
  • HY-148251

    Casein Kinase Cancer
    MU1742 is a probe for CK1δ and CK1ε protein kinases .
    MU1742
  • HY-12279C
    Umbralisib hydrochloride
    5 Publications Verification

    TGR-1202 hydrochloride; RP5264 hydrochloride

    PI3K Casein Kinase Cancer
    Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach [1] .
    Umbralisib hydrochloride
  • HY-15532B

    MK-8776 S-isomer

    Drug Isomer Cancer
    SCH900776 S-isomer is the S-isomer of SCH900776. SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with IC50 of 3 nM.
    SCH900776 (S-isomer)
  • HY-135892
    GNE-1858
    3 Publications Verification

    MAP4K Inflammation/Immunology
    GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively [1].
    GNE-1858
  • HY-15159

    Polo-like Kinase (PLK) Cancer
    Cyclapolin 9 is a potent, selective and ATP-competitive polo-like kinase 1 (PLK1) inhibitor with an IC50 of 500 nM. Cyclapolin 9 is inactive against other kinases .
    Cyclapolin 9
  • HY-115868

    AAK1 Neurological Disease
    BMS-911172 is an adaptor associated kinase 1 (AAK1 kinase) inhibitor (IC50 = 35 nM).
    BMS-911172
  • HY-148233S

    Casein Kinase Others
    JNJ-6204 is a dual inhibitor for CSNK1D (Casein Kinase 1 Delta) and CSNK1E (Casein Kinase 1 Epsilon) (CSNK1D IC50=2.3 nM; CSNK1E IC50=137 nM). JNJ-6204 shows good brain exposure [1] .
    JNJ-6204
  • HY-19635A
    G-5555 hydrochloride
    5+ Cited Publications

    PAK Cancer
    G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
    G-5555 hydrochloride
  • HY-151539

    LIM Kinase (LIMK) Neurological Disease
    TH470 is a highly selective LIMK1/2 (LIM kinase1/2) inhibitor (LIMK1 IC50=9.8 nM; LIMK2 IC50=13 nM), and can be used in orphan disease research [1].
    TH470
  • HY-148112

    Casein Kinase Neurological Disease
    Casein kinase 1δ-IN-1 is an inhibitor of casein kinase 1δ (CK1δ). Casein kinase 1δ-IN-1 can be used for the research of neurodegenerative diseases such as tauopathies [1].
    Casein kinase 1δ-IN-1
  • HY-134911

    IRAK CDK Inflammation/Immunology Cancer
    HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity [1].
    HS-243
  • HY-117393
    Bisindolylmaleimide III
    1 Publications Verification

    PKC Cancer
    Bisindolylmaleimide III is a potent and selective inhibitor of protein kinase C (PKC). Bisindolylmaleimide III selectively interacts with either PKCα or ribosomal S6 protein kinase 1 after activation of these kinases .
    Bisindolylmaleimide III
  • HY-15425B

    Sphingosine kinase 1 Inhibitor II hydrochloride

    SphK LPL Receptor Apoptosis Autophagy Cardiovascular Disease Inflammation/Immunology Cancer
    PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy [1] .
    PF-543 hydrochloride
  • HY-101805
    SK1-IN-1
    2 Publications Verification

    SphK Inflammation/Immunology Cancer
    SK1-IN-1 is a potent sphingosine kinase 1 (SPHK1) inhibitor with an IC50 of 58 nM.
    SK1-IN-1
  • HY-130433

    Fluorescent Dye Others
    NBD Sphingosine (NBD-Sph), a fluorochrome, is a fluorescence-labeled sphingosine. NBD Sphingosine can be uesd for fluorescence assay for sphingosine kinases .
    NBD Sphingosine
  • HY-117809

    PDK-1 Cancer
    PDK1-IN-2 is a small molecule inhibitor of 3-phosphoinositol-dependent protein kinase-1 (PDK1). PDK1-IN-2 inhibits the binding of PDK1 to its substrate by competitively binding to the PIF pocket of PDK1, thereby inhibiting the kinase activity and downstream signaling of PDK1. PDK1-IN-2 can be used for cell survival and proliferation in cancer [1].
    PDK1-IN-2
  • HY-P0200

    Src Inflammation/Immunology
    RR-SRC is a substrate for src-tyrosine-specific protein kinase .
    RR-SRC
  • HY-P5450

    PDK-1 Others
    PDKtide, a biological active peptide is a substrate for Phosphatidylinositide-Dependent Kinase 1 (PDK1) [1].
    PDKtide
  • HY-P5450A

    PDK-1 Others
    PDKtide TFA, a biological active peptide, is a substrate for phosphatidylinositide-dependent kinase 1 (PDK1) [1].
    PDKtide TFA
  • HY-P4520

    Amino Acid Derivatives Others
    (Trp4)-Kemptide is a peptide substrate for adenosine 3',5'-cyclic monophosphate-dependent protein kinase .
    (Trp4)-Kemptide
  • HY-145107

    MAP4K Inflammation/Immunology Cancer
    HPK1-IN-19 (Compound I-47) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor [1].
    HPK1-IN-19
  • HY-133850

    Pim Cancer
    10-DEBC is a selective Akt inhibitor. 10-DEBC shows strong inhibitory activity against Moloney murine leukemia virus (Pim) kinase-1 (IC50=1.28 μM) [1].
    10-DEBC
  • HY-177913

    PDK-1 Cancer
    OSU-02067 is a selective 3-phosphoinositide-dependent protein kinase-1 (PDK-1) inhibitor (IC50=9 μM). OSU-02067 is promising for research of solid tumors (e.g., prostate, breast, colorectal cancers) [1].
    OSU-02067
  • HY-12470A

    Casein Kinase Cancer
    PF-4800567 hydrochloride is a potent and selective inhibitor of?casein kinase?1? (CK1?), with an?IC50?of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 hydrochloride is useful in probing unique roles between these two kinases in multiple signaling pathways [1].
    PF-4800567 hydrochloride
  • HY-E70868

    TNK1 Cancer
    Thirty-eight-negative kinase-1 (TNK1) is a member of the ACK family of NRTKs, which includes only two human kinases, TNK1 and TNK2 (also called ACK1). TNK1 Recombinant Human Active Protein Kinase is a recombinant TNK1 protein that can be used to study TNK1-related functions [1].
    TNK1 Recombinant Human Active Protein Kinase
  • HY-132150A

    MAP4K FLT3 Src Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    HPK1-IN-2 dihydrochloride is a potent and orally active hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50<0.05 μΜ) with antitumor activity. HPK1-IN-2 dihydrochloride also inhibits Lck (0.05 μΜ<IC50<0.5 μΜ) and Flt3 (IC50<0.05 μΜ) kinase activities [1].
    HPK1-IN-2 dihydrochloride
  • HY-153904

    Casein Kinase Neurological Disease
    Casein kinase 1δ-IN-5 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 47 nM. Casein kinase 1δ-IN-5 shows neuroprotective and anti-inflammatory properties both in vitro. Casein kinase 1δ-IN-5 has the potential for neurodegenerative diseases research.
    Casein kinase 1δ-IN-5
  • HY-153905

    Casein Kinase Neurological Disease
    Casein kinase 1δ-IN-6 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 23 nM. Casein kinase 1δ-IN-6 shows neuroprotective and anti-inflammatory properties both in vitro and in vivo. Casein kinase 1δ-IN-6 is a promising drug candidate and can be used for neurodegenerative diseases research.
    Casein kinase 1δ-IN-6
  • HY-P2298

    PKC Neurological Disease
    TAT-P4-(DATC5)2 is a high-affinity peptide inhibitor of the PICK1 (protein interacting with C kinase-1) PDZ domain, with a Ki of 1.7 nM. TAT-P4-(DATC5)2 can inhibit addiction in rats [1].
    TAT-P4-(DATC5)2
  • HY-P2298A

    PKC Neurological Disease
    TAT-P4-(DATC5)2 TFA is a high-affinity peptide inhibitor of the PICK1 (protein interacting with C kinase-1) PDZ domain, with a Ki of 1.7 nM. TAT-P4-(DATC5)2 TFA can inhibit addiction in rats [1].
    TAT-P4-(DATC5)2 TFA
  • HY-14986

    JAK Others
    JAK-IN-32 (XC) is a bi-aryl meta-pyrimidine inhibitor of JAK kinase .
    JAK-IN-32
  • HY-117291

    AMPK Ser/Thr Protease Others
    XMD-17-51 is a pyrimido-diazepinone compound that is able to modulate protein kinases .
    XMD-17-51

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