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Chk1 inhibitor

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-128766A
    CHK1-IN-4 hydrochloride

    		Checkpoint Kinase (Chk) Cancer
    CHK1-IN-4 hydrochloride (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity .
    CHK1-IN-4 hydrochloride
  • HY-139901
    Chk1-IN-6

    		Checkpoint Kinase (Chk) Cancer
    Chk1-IN-6 is a potent, selective, and orally bioavailable CHK1 inhibitor candidate.
    Chk1-IN-6
  • HY-128601
    CHK1-IN-3

    		Checkpoint Kinase (Chk) Cancer
    CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM .
    CHK1-IN-3
  • HY-14720
    Rabusertib
    10+ Cited Publications

    LY2603618; IC-83

    		 Checkpoint Kinase (Chk) Autophagy Cancer
    Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.
    Rabusertib
  • HY-131446
    Chk1-IN-5

    		Checkpoint Kinase (Chk) Cancer
    Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model .
    Chk1-IN-5
  • HY-128766
    CHK1-IN-4

    		Checkpoint Kinase (Chk) Cancer
    CHK1-IN-4 (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 has anti-tumor activity .
    CHK1-IN-4
  • HY-111369
    CHK1-IN-2

    		Checkpoint Kinase (Chk) Cancer
    CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.
    CHK1-IN-2
  • HY-161383
    CHK1-IN-9

    		Checkpoint Kinase (Chk) Cancer
    CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026) .
    CHK1-IN-9
  • HY-103367
    CHK1-IN-7

    		Checkpoint Kinase (Chk) Cancer
    CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer .
    CHK1-IN-7
  • HY-162367
    FLT3/CHK1-IN-2

    		FLT3 Checkpoint Kinase (Chk) Cancer
    FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC50s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML) .
    FLT3/CHK1-IN-2
  • HY-U00345
    CHK-IN-1

    		Checkpoint Kinase (Chk) Cancer
    CHK-IN-1 is an inhibitor of CHK1 and CHK2, with anti-proliferative activities.
    CHK-IN-1
  • HY-18958
    CCT245737
    2 Publications Verification

    SRA737

    		 Checkpoint Kinase (Chk) Cancer
    CCT245737 (SRA737) is an orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM.
    CCT245737
  • HY-10992
    AZD-7762
    Maximum Cited Publications
    22 Publications Verification

    		 Checkpoint Kinase (Chk) Cancer
    AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
    AZD-7762
  • HY-10992A
    AZD-7762 hydrochloride
    Maximum Cited Publications
    22 Publications Verification

    		 Checkpoint Kinase (Chk) Cancer
    AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
    AZD-7762 hydrochloride
  • HY-112927
    MU380

    		Checkpoint Kinase (Chk) Cancer
    MU380 is a potent and selective CHK1 inhibitor that induces apoptosis and has anticancer activity .
    MU380
  • HY-112167A
    GDC-0575 dihydrochloride
    5+ Cited Publications

    ARRY-575 dihydrochloride; RG7741 dihydrochloride

    		 Checkpoint Kinase (Chk) Cancer
    GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.
    GDC-0575 dihydrochloride
  • HY-18958A
    (S)-CCT245737

    (S)-SRA737

    		 Checkpoint Kinase (Chk) Others
    (S)-CCT245737 ((S)-SRA737) is a potent and selective oral inhibitor of checkpoint kinase 1 (CHK1).
    (S)-CCT245737
  • HY-124731
    PD-321852

    		Checkpoint Kinase (Chk) Cancer
    PD-321852 is a Chk1 inhibitor, with IC50 of 5 nM. PD-321852 can be used in anti-cancer research .
    PD-321852
  • HY-107407
    SB-218078
    4 Publications Verification

    		 Checkpoint Kinase (Chk) CDK PKC Apoptosis Cancer
    SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest .
    SB-218078
  • HY-112167
    GDC-0575
    5+ Cited Publications

    ARRY-575; RG7741

    		 Checkpoint Kinase (Chk) Cancer
    GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2 nM.
    GDC-0575
  • HY-18942
    VER-00158411

    		Checkpoint Kinase (Chk) Cancer
    VER-00158411 is a checkpoint kinase 1 (CHK1) and CHK2 inhibitor with IC50 values of 4.4 nM and 4.5 nM, respectively .
    VER-00158411
  • HY-148962
    LY2880070

    		Checkpoint Kinase (Chk) Cancer
    LY2880070 is an orally active CHK1 inhibitor, IC50 ＜ 1 nM. LY2880070 can be used as an anticancer agent for combination with DNA damaging agents .
    LY2880070
  • HY-15532B
    SCH900776 (S-isomer)

    MK-8776 S-isomer

    		 Others 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-18175
    CCT244747
    3 Publications Verification

    		 Checkpoint Kinase (Chk) Cancer
    CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
    CCT244747
  • HY-10032
    PF 477736
    5 Publications Verification

    PF 00477736

    		 Checkpoint Kinase (Chk) VEGFR Src c-Fms Aurora Kinase FGFR FLT3 RET CDK Cancer
    PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo .
    PF 477736
  • HY-13263
    CHIR-124
    3 Publications Verification

    		 Checkpoint Kinase (Chk) FLT3 PDGFR Apoptosis Cancer
    CHIR-124 is a potent and selective Chk1 inhibitor with IC50 of 0.3 nM, and also potently targets PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.
    CHIR-124
  • HY-100195
    SAR-020106
    1 Publications Verification

    		 Checkpoint Kinase (Chk) Cancer
    SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents .
    SAR-020106
  • HY-19926
    GDC-0425

    RG-7602

    		 Checkpoint Kinase (Chk) Cancer
    GDC-0425 (RG-7602) is an orally available, highly selective small molecule ChK1 inhibitor. GDC-0425 can be used for the research of various malignancies .
    GDC-0425
  • HY-13925
    PD0166285
    5+ Cited Publications

    		 Wee1 Apoptosis Cancer
    PD0166285, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 exhibits an IC50 of 3.433 μM for Chk1 .
    PD0166285
  • HY-13925A
    PD0166285 dihydrochloride

    		Wee1 Apoptosis Cancer
    PD0166285 dihydrochloride, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC50 of 3.433 μM for Chk1 .
    PD0166285 dihydrochloride
  • HY-18961
    PD 407824

    		Checkpoint Kinase (Chk) Wee1 Inflammation/Immunology Cancer
    PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4 .
    PD 407824
  • HY-119699
    PV1115

    		Checkpoint Kinase (Chk) Cancer
    PV1115 is a potent and highly selective Chk2 inhibitor with an IC50 of 0.14 nM, 66000 nM, >100000 nM for Chk2, Chk1 and RSK2, respectively. PV1115 is situated within the ATP-binding pocket of Chk2 .
    PV1115
  • HY-136270
    Gartisertib
    2 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 .
    Gartisertib
  • HY-112167B
    GDC0575 hydrochloride

    ARRY-575 hydrochloride; RG7741 hydrochloride

    		 Checkpoint Kinase (Chk) Inflammation/Immunology Cancer
    GDC0575 (ARRY-575) hydrochloride is a highly-selective and orally active Chk1 (IC50=1.2 nM) inhibitor. GDC0575 (ARRY-575) hydrochloride can be used for colitis-associated cancer (CAC) and colitis research .
    GDC0575 hydrochloride
  • HY-15532
    SCH900776
    5+ 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 .
    SCH900776
  • HY-122198
    ML367

    		Checkpoint Kinase (Chk) Cancer
    ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation .
    ML367
  • HY-155195
    FLT3/CHK1-IN-1

    		Others Cancer
    FLT3/CHK-IN-1 (Compound 18) is a dual inhibitor of FLT3/CHK1. FLT3/CHK-IN-1 is more than 1700 times more selective to c-KI T and greatly reduces hERG affinity with an IC50 value of 58.4 μM. FLT3/CHK-IN-1 inhibits tumor growth in mouse xenotransplantation models inoculated with MV-4-11 cells .
    FLT3/CHK1-IN-1
  • HY-114302
    CCB02
    1 Publications Verification

    		 Microtubule/Tubulin Cancer
    CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC50 of 689 nM, and shows potent anti-tumor activity. CCB02 shows no inhibition on the cell cycle- and centrosome-related kinases, or the phosphorylation status of Aurora A, Plk1, Plk2, CDK2, and CHK1 .
    CCB02
  • HY-117857
    MRT00033659

    		Casein Kinase Checkpoint Kinase (Chk) MDM-2/p53 Early 2 Factor (E2F) Cancer
    MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 μM for CK1δ) and CHK1 (IC50=0.23 μM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation .
    MRT00033659
  • HY-18174
    Prexasertib
    20+ Cited Publications

    LY2606368

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity .
    Prexasertib
  • HY-18174A
    Prexasertib dihydrochloride
    20+ Cited Publications

    LY2606368 dihydrochloride

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity .
    Prexasertib dihydrochloride
  • HY-18174B
    Prexasertib Mesylate Hydrate

    LY2606368 Mesylate Hydrate; LY2940930

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity .
    Prexasertib Mesylate Hydrate
  • HY-18174C
    Prexasertib mesylate

    LY2606368 mesylate

    		 Checkpoint Kinase (Chk) DNA/RNA Synthesis Apoptosis Cancer
    Prexasertib mesylate (LY2606368 mesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib mesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity .
    Prexasertib mesylate
  • HY-112477
    Chk2-IN-1

    		Checkpoint Kinase (Chk) Cancer
    Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect .
    Chk2-IN-1
  • HY-15883
    GNE-900

    		Checkpoint Kinase (Chk) Apoptosis Cancer
    GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .
    GNE-900
  • HY-18174E
    Prexasertib dimesylate
    20+ Cited Publications

    LY2606368 dimesylate

    		 Checkpoint Kinase (Chk) Apoptosis Cancer
    Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity .
    Prexasertib dimesylate
  • HY-15882
    GNE-783

    		Others Cancer
    GNE-783 is a selective CHK1 inhibitor that enhances the activity of gemcitabine. GNE-783 improves the efficacy of anti-metabolite DNA damage drugs by inactivating S-phase and G2-phase cell cycle checkpoints following DNA damage. GNE-783 selectively enhances the chemical synergy of certain drugs in different tumor types, for example, enhancing the activity of temozolomide only in melanoma cell lines .
    GNE-783
  • HY-18174H
    Prexasertib lactate

    LY2606368 lactate

    		 Checkpoint Kinase (Chk) Apoptosis DNA/RNA Synthesis Cancer
    Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib lactate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity .
    Prexasertib lactate
  • HY-13661
    7-Hydroxystaurosporine

    UCN-01; KRX-0601

    		 Akt PKC CDK Apoptosis Cancer
    7-Hydroxystaurosporine (UCN-01) is a synthetic derivative of Staurosporine (HY-15141) with antitumor activity. 7-hydroxystaurosporine inhibits serine/threonine kinase AKT and calcium-dependent protein kinase C activity. 7-hydroxystaurosporine also activates indirectly cyclin-dependent kinases (CDKs). 7-hydroxystaurosporine arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis .
    7-Hydroxystaurosporine
  • HY-156470
    Multi-kinase-IN-6

    		Trk Receptor Anaplastic lymphoma kinase (ALK) c-Kit EGFR Pim Casein Kinase Checkpoint Kinase (Chk) CDK Apoptosis Cancer
    Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
    Multi-kinase-IN-6

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