Catalog No.
Product Name
Application
Product Information
Citations
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PLK inhibitor
BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations.- Kyohei Matsuhashi, .et al. , Nat Commun, 2025, Sep 8;16:7799 PMID: 40921755
- Masae Ikura, .et al. , J Biochem, 2025, Jul 31;178(2):97-107 PMID: 40441713
- Ryuzaburo Yuki, .et al. , Eur J Pharmacol, 2024, Jan 15:963:176229 PMID: 38072041
- Nuria Gallisa-Sune, .et al. , Nat Commun, 2023, Apr 27;14(1):2434 PMID: 37105961
- Kei K Ito, .et al. , J Cell Biol, 2021, Mar 1;220(3):e202005153 PMID: 33492359
- Ryuzaburo Yuki, .et al. , J Cell Mol Med, 2021, Feb;25(3):1677-1687 PMID: 33465289
- Yamagishi A, .et al. , Int J Mol Sci, 2020, Feb 5;21(3) PMID: 32033461
- Bucko PJ, .et al. , Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
- Watanabe K, .et al. , Nat Commun, 2019, Feb 25;10(1):931 PMID: 30804344
- Valérian Pasche, .et al. , Parasit Vectors, 2018, 11: 298 PMID: 29764454
- Takeshi Wakida, .et al. , eLife, 2017, 6: e29953 PMID: 29254517
- Majid Momeny, .et al. , Sci Rep, 2017, 7: 4204 PMID: 28646172
- Ifuji A, .et al. , Exp Cell Res, 2017, Nov 15;360(2):347-357 PMID: 28942021
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PLK Inhibitor
BI6727 is a highly potent and selective polo-like kinase (PLK) 1 inhibitor (enzyme IC50 = 0.87 nM, EC50 = 11-37 nM on a panel of cancer cell lines).- Kishan Shamjibhai Italiya, .et al. , Ultrasound in Medicine & Biology, 2025, 51(7): 1124-1133
- Xiaofei Xin, .et al. , ACS Appl Mater Interfaces, 2019, 2019 PMID: 30933478
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PLK Inhibitor
HMN-214 inhibits polo-like and cyclin-dependent kinase activity, has potent antimicrotubular effects and results in profound apoptosis and antitumor activity in a broad spectrum of human xenografts.- Yao-Yu Hsieh, .et al. , Mol Oncol, 2023, Oct 16 PMID: 37842807
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PLK Inhibitor
ON-01910 is selectively cytotoxic for chronic lymphocytic leukemia cells through a dual mechanism of action involving PI3K/AKT inhibition and induction of oxidative stress. -
Chk inhibitor
LY2603618 is a chk2 inhibitor that binds to and inhibits the activity of chk2, which may prevent the repair of DNA caused by DNA-damaging agents.- Hayakawa K, .et al. , Biochem Biophys Res Commun, 2018, Dec 2;506(4):983-989 PMID: 30404732
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Chk1 inhibitor
SCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. It specifically binds to and inhibits Chk1, which may result in tumor cells bypassing Chk1-dependent cell cycle arrest in the S and G2/M phases to undergo DNA repair prior to entry into mitosis; tumor cells may thus be sensitized to the DNA-damaging effects of ionizing radiation and alkylating chemotherapeutic agents.
- Hong Yang, .et al. , Research Square, 2022, May 9th
- Motofumi Suzuki, .et al. , Int J Radiat Oncol Biol Phys, 2021, May 25;S0360-3016(21)00361-8 PMID: 34112559
- Min Wu, .et al. , Haematologica, 2019, 104 PMID: 30975911
- Permata TBM, .et al. , Oncogene, 2019, Feb 12 PMID: 30755733
- Hiro Sato, .et al. , Nat Commun, 2017, 8: 1751 PMID: 29170499
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PLK1/PLK3 inhibitor
GW843682X is a selective inhibitor of polo-like kinase 1 (PLK1) and polo-like kinase 3 (PLK3) (IC50 values are 2.2 and 9.1 nM respectively).- Kanada F, .et al. , Sci Rep, 2019, Dec 27;9(1):20085 PMID: 31882756
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PLK1 inhibitor
MLN0905 is a potent, selective small-molecule PLK1 inhibitor. MLN0905 inhibits cell proliferation in a broad range of human tumor cells including DLBCL cell lines.- Reyhane Piri, .et al. , Invest New Drugs, 2025, Apr;43(2):348-356 PMID: 40278989
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CHK1 Inhibitor
SCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. -
PLK inhibitor
NMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. -
Chk2, KDR, FGFR, Aurora A & Cdk2 inhibitor
R1530 is a pyrazolobenzodiazepine small molecule with potential antiangiogenesis and antineoplastic activities. R1530 is also a mitosis-angiogenesis inhibitor (MAI) that inhibits multiple receptor tyrosine kinases involved in angiogenesis, such as vascular endothelial growth factor receptor (VEGFR)-1, -2, -3, platelet-derived growth factor receptor (PDGFR) beta? FMS-like tyrosine kinase (Flt)-3, and fibroblast growth factor receptor (FGFR) -1, -2.- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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Chk1 inhibitor
LY2606368 is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.- Yuri Tozaki, .et al. , Cancers (Basel), 2023, Jan 25;15(3):735 PMID: 36765693
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PLK inhibitor
SBE 13 HCl is a selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). -
Chk2 inhibitor
CCT241533 Hcl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM; shows minimal cross-reactivity against a panel of kinases at 1 uM. -
Wee1/Chk inhibitor
PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.- Trang H. Nguyen Vu, .et al. , Cancer Sci, 2023, Dec; 114(12): 4664-4676 PMID: 37724648
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Chk1 inhibitor
GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2?nM. -
PLK4 inhibitor
Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM. -
PLK4 inhibitor
Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM. -
CHK1 inhibitor
GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity. -
PLK1 inhibitor
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. -
ATP-competitive CHK1 inhibitor
Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay. -
CHK1 inhibitor
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. -
FLT3/CHK2 inhibitor
Lasmotinib (PHI-101) is a dual inhibitor of FLT3 and CHK2 with potent activity against FLT3 single activating mutations (ITD or TKD), as well as double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. It synergizes with Venetoclax or Azacytidine to enhance anti-leukemic effects and also demonstrates anticancer activity in ovarian and breast cancer models. -
Chk-α Inhibitor
V-11-0711 is a potent and selective inhibitor of Chk-α, exhibiting an IC50 value of 20 nM. This compound effectively reduces phosphocholine (PCho) levels and induces reversible growth arrest in various cancer cell lines. At elevated concentrations, V-11-0711 can promote apoptosis. It is particularly useful for research related to cervical cancer and triple-negative breast cancer, facilitating the exploration of therapeutic strategies targeting Chk-α pathways. -
CHK1 Inhibitor
Prexasertib Mesylate Hydrate is a selective, ATP-competitive inhibitor of checkpoint kinase 1 (CHK1) with a Ki of 0.9 nM and an IC50 of <1 nM. It also inhibits checkpoint kinase 2 (CHK2) with an IC50 of 8 nM and ribosomal S6 kinase 1 (RSK1) with an IC50 of 9 nM. By inducing double-stranded DNA breakage and replication catastrophe, Prexasertib Mesylate Hydrate promotes apoptotic cell death, exhibiting significant anti-tumor activity. This reagent is primarily utilized in cancer research to explore mechanisms of DNA damage response and therapeutic resistance. -
CHK1 Inhibitor
Prexasertib mesylate is a selective ATP-competitive inhibitor of checkpoint kinase 1 (CHK1), demonstrating a Ki of 0.9 nM and an IC50 of less than 1 nM. It also inhibits CHK2 and RSK1 with IC50 values of 8 nM and 9 nM, respectively. By inducing double-stranded DNA breaks and triggering replication catastrophe, Prexasertib mesylate leads to apoptosis. Its potent anti-tumor activity makes it valuable for cancer research applications, particularly in studies focusing on DNA damage response and cell cycle regulation. -
CHK1 Inhibitor
Prexasertib dimesylate is a selective checkpoint kinase 1 (CHK1) inhibitor that functions as an ATP-competitive agent. With a Ki of 0.9 nM and an IC50 of less than 1 nM, it effectively inhibits CHK2 and RSK1, exhibiting IC50 values of 8 nM and 9 nM, respectively. This compound induces double-stranded DNA breaks and replication catastrophe, leading to apoptosis. Prexasertib dimesylate demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development. -
CHKα Inhibitor
ICL-CCIC-0019 is a potent inhibitor of choline kinase α (CHKα), a key enzyme involved in phosphatidylcholine synthesis and cellular signaling. This compound has been shown to induce a G1 phase cell cycle arrest and promote endoplasmic reticulum stress-mediated apoptosis in various cancer cell lines. ICL-CCIC-0019 is valuable for research applications focused on cancer biology, specifically in studies exploring cell cycle regulation and mechanisms of apoptosis in tumor cells. -
Dual FLT3/CHK1 Inhibitor
FLT3/CHK1-IN-1 is a dual inhibitor targeting both FLT3 and CHK1, demonstrating significant selectivity for c-KIT over other kinases. With an IC50 value of 58.4 μM, it shows reduced affinity for the hERG channel, minimizing potential cardiac side effects. FLT3/CHK1-IN-1 has exhibited efficacy in inhibiting tumor growth in mouse xenotransplantation models with MV-4-11 cells, making it a valuable tool for cancer research and therapeutic development. -
CHK1 Inhibitor
CHK1-IN-12 is a potent and selective checkpoint kinase 1 (CHK1) inhibitor that exerts its effects by significantly reducing CHK1 phosphorylation activity, thereby disrupting the DNA damage response pathway. With an in vitro enzyme IC50 of up to 10 nM and a cellular IC50 of 50 nM, CHK1-IN-12 effectively induces cell cycle arrest and apoptosis in tumor cells. This compound holds potential for cancer research, particularly in studies focused on cell cycle regulation and DNA repair mechanisms.
