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Chk

Checkpoint kinase 1, commonly referred to as Chk1, is a serine/threonine-specific protein kinase that, in humans, is encoded by the CHEK1 gene. Chk1 coordinates the DNA damage response (DDR) and cell cycle checkpoint response. Activation of Chk1 results in the initiation of cell cycle checkpoints, cell cycle arrest, DNA repair and cell death to prevent damaged cells from progressing through the cell cycle.

  • CCT245737
    T70801489389-18-5
    CCT245737 (SRA737) is an orally active and selective Chk1 inhibitor (IC50: 1.3 nM); CCT245737 shows much less activity against Chk2 (IC50: 2440 nM).
    • $33
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  • CHK1-IN-4 hydrochloride
    T10792L In house
    CHK1-IN-4 hydrochloride is a potent inhibitor of checkpoint kinase 1 (chk1). CHK1-IN-4 hydrochloride potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity.
    • $197
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  • GDC0575 monohydrochloride
    T274071196504-54-7
    GDC0575 monohydrochloride (ARRY575) is a potent and selective inhibitor of cell cycle checkpoint kinase 1 (Chk1) with an IC50 of 1.2 nM. GDC-0575 specifically binds to and inhibits Chk1; this may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases, which permits the cells to undergo DNA repair prior to entry into mitosis.
    • $63
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  • ANI-7
    T10325931417-26-4In house
    ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells and potently and selectively inhibits the growth of MCF-7 breast cancer cells (GI50: 0.56 μM).
    • $35
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  • CHK1-IN-3
    T107912097252-39-4In house
    CHK1-IN-3 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 0.4 nM).
    • $195
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  • CCT241533
    T107181262849-73-9In house
    CCT241533 is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).
    • $1,520
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  • Rabusertib
    T6084911222-45-2
    Rabusertib (IC-83) is an inhibitor of the cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiating activity. Rabusertib has been used in trials studying the treatment of Cancer, Solid Tumors, Advanced Cancer, Pancreatic Neoplasms, and Non-Small Cell Lung Cancer.
    • $38
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  • BML-277
    T2033516480-79-8
    BML-277 (C 3742) is a selective checkpoint kinase 2 (Chk2) inhibitor.
    • $47
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  • Baricitinib
    T24851187594-09-7
    Baricitinib (INCB028050) is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.
    • $43
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  • SCH900776
    T2517891494-63-6
    SCH900776 (MK-8776) is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.
    • $48
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  • AZD-7762
    T6093860352-01-8
    AZD-7762, an effective and specific inhibitor of Chk1(IC50=5 nM), is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.
    • $32
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  • PHI-101
    T814902127107-15-5
    PHI-101 is an orally available and selective checkpoint kinase 2 (Chk2) inhibitor for the study of refractory acute myelogenous leukemia (AML) and ovarian cancer.
    • $183
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  • CCT241533 hydrochloride
    T10718L1431697-96-9
    CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).
    • $67
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  • VER-00158411
    T172231174664-88-0
    VER-00158411 is a checkpoint kinase 1 and CHK2 inhibitor (IC50: 4.4 nM and 4.5 nM, respectively).
    • $1,820
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  • GDC-0575
    T73001196541-47-5
    GDC-0575 (ARRY-575) is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM).
    • $51
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  • LY2880070
    T92521375637-35-6
    LY2880070 is a new checkpoint kinase 1 (CHK1) inhibitor for cancer therapy.
    • $133
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  • CHK1-IN-4
    T107922120398-41-4
    CHK1-IN-4 is a potent inhibitor of checkpoint kinase 1 (chk1) and potently inhibits chk1 phosphorylation in the tumor cells with anti-tumor activity.
    • $2,270
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  • Prexasertib dihydrochloride
    T43271234015-54-3
    Prexasertib dihydrochloride (LY2606368) is an ATP-competitive CHK1 inhibitor (Ki: 0.9 nmol/L). in the cell-free assay, its IC50 values are 8 nM and 9 nM for CHK2 and RSK, respectively.
    • $38
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  • BX-912
    T1837702674-56-4
    BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc.
    • $48
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  • Monalizumab
    T766911228763-95-8
    Monalizumab is a novel immune checkpoint inhibitor targeting natural killer cell population 2A (NKG2A). Monalizumab is a humanized monoclonal antibody against NKG2A that induces IFN-γ production, thereby activating natural killer cell function. Monalizumab has antitumor activity and can be used to study neck squamous cell carcinoma (HNSCC).
    • $438
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  • CHIR-124
    T6350405168-58-3
    CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2, 000-fold selectivity against Chk2, 500- to 5, 000-fold less activity against Cdc2 and CDK2/4.
    • $35
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  • CHK-IN-1
    T131481278405-51-8
    CHK-IN-1 is a dual inhibitor of CHK1 and CHK2 with antiproliferative activity.
    • $700
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  • CCT244747
    T149041404095-34-6
    CCT244747 is a CHK1 inhibitor (IC50: 7.7 nM) and also abrogates G2 checkpoint (IC50: 29 nM).
    • $76
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  • BX795
    T1830702675-74-9
    BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.
    • $54
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  • CHK1-IN-2
    T10790912367-45-4
    CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 6 nM).
    • $2,420
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  • SCH900776 (S-isomer)
    T3700891494-64-7
    SCH900776 S-isomer (MK-8776 S-isomer) is an effective, specific and orally bioavailable inhibitor of checkpoint kinase Chk1 (IC50: 3 nM). It also inhibitors Chk2 (IC50: 1500 nM) and cyclin-dependent kinase CDK2 (IC50: 160 nM).
    • $45
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  • SAR-020106
    T213311184843-57-9
    SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme.
    • $44
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  • Prexasertib
    T43101234015-52-1
    Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.
    • $48
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  • PD 407824
    T16446622864-54-4
    PD 407824 is a chemical BMP sensitiser that promotes increased cellular sensitivity to subthreshold amounts of BMP4.PD 407824 is a potent inhibitor of the checkpoint kinases Chk1 and WEE1 (IC50s: 47 and 97 nM, respectively).
    • $65
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  • Tuvusertib
    T104061613200-51-3
    Tuvusertib (M1774) is an orally available ataxia telangiectasia and Rad3-related (ATR) kinase inhibitor (Ki< 1 µΜ) with selective and potentially antitumor activity.Tuvusertib selectively inhibits ATR activity and blocks downstream phosphorylation of serine/threonine protein kinase checkpoint kinase 1 (CHK1), thereby inhibits DNA damage checkpoint activation, disrupting DNA damage repair and inducing apoptosis in tumor cells.
    • $68
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  • GNE-900
    T712591200126-26-6
    GNE-900 is an ATP-competitive ChK1 inhibitor with selective and oral activity.GNE-900 inhibits ChKl and ChK2 with IC50 values of 0.0011 and 1.5 µM, respectively.GNE-900 enhances DNA damage and induces apoptosis. GNE-900 has antitumor activity.
    • $67
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  • SB-218078
    T16848135897-06-2
    SB-218078 is less potently inhibits Cdc2 (IC50: 250 nM) and PKC (IC50: 1000 nM). SB-218078 is a potent, ATP-competitive, and cell-permeable checkpoint kinase 1 inhibitor that inhibits Chk1 phosphorylation of cdc25C (IC50: 15 nM).
    • $353
    35 days
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  • PF 477736
    T6028952021-60-2
    PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.
    • $45
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  • CHK1 inhibitor
    T107932097938-64-0
    CHK1 inhibitor (GDC-0575 analog) is a CHK1 inhibitor.
    • $2,270
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  • PD0166285
    T6931185039-89-8
    PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.
    • $52
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  • M443
    T159431820684-31-8
    M443 is a potent small molecule inhibitor of MRK that inhibits radiation-induced activation of p38 and Chk2 and can be used in cancer research.
    • $199
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  • A-443654
    T14072552325-16-3
    A-443654 is a pan-Akt inhibitor. A-443654 has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).
    • $84
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  • MBM-55
    T119602083622-09-5
    MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM. MBM-55 effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis.
    • $187
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  • 4-Demethyldeoxypodophyllotoxin
    T833213590-93-0
    4-Demethyldeoxypodophyllotoxin, an aryl tetrahydronaphthalenyl lignan analog from the roots of Podophyllum peltatum, has anticancer activity and modulates the Chk-2 signaling pathway in MCF-7 breast cancer cells.
    • $122
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