Chk

CCT245737 (SRA737) is an orally active and selective Chk1 inhibitor (IC50: 1.3 nM); CCT245737 shows much less activity against Chk2 (IC50: 2440 nM).

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.

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.

CHK1-IN-3 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 0.4 nM).

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).

CCT241533 is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).

BML-277 (C 3742) is a selective checkpoint kinase 2 (Chk2) inhibitor.

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.

Baricitinib (INCB028050) is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.

SCH900776 (MK-8776) is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.

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.

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.

CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).

VER-00158411 is a checkpoint kinase 1 and CHK2 inhibitor (IC50: 4.4 nM and 4.5 nM, respectively).

LY2880070 is a new checkpoint kinase 1 (CHK1) inhibitor for cancer therapy.

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.

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).

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.

GDC-0575 (ARRY-575) is a highly-selective oral small-molecule Chk1 inhibitor(IC50 of 1.2 nM).

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.

CHK-IN-1 is a dual inhibitor of CHK1 and CHK2 with antiproliferative activity.

CCT244747 is a CHK1 inhibitor (IC50: 7.7 nM) and also abrogates G2 checkpoint (IC50: 29 nM).

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.

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.

CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 6 nM).

SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol L on the isolated human enzyme.

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).

Prexasertib (LY2606368) is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.

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.

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).

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.

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).

CHK1 inhibitor (GDC-0575 analog) is a CHK1 inhibitor.

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.

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.

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.

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.

PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.

A-443654 is a pan-Akt inhibitor. A-443654 has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).