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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.- Giuseppe Madaro, .et al. , Neurogastroenterol Motil, 2026, Feb;38(2):e70259 PMID: 41639608
- 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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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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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).- Jianguo Huang, .et al. , JCI Insight, 2026, Jun 30:e192686 PMID: 42378032
- Kishan Shamjibhai Italiya, .et al. , Ultrasound in Medicine & Biology, 2025, 51(7): 1124-1133 PMID: 40234152
- Xiaofei Xin, .et al. , ACS Appl Mater Interfaces, 2019, 2019 PMID: 30933478
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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
LY2606368 is an inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity.- Rina Kato, .et al. , Pediatr Res, 2026, June 02 PMID: 42230907
- Yuri Tozaki, .et al. , Cancers (Basel), 2023, Jan 25;15(3):735 PMID: 36765693
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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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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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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. -
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. -
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
Isogranulatimide is a selective inhibitor of checkpoint kinase 1 (Chk1) with an IC50 value of 0.1 μM. It effectively inhibits the G2/M checkpoint, demonstrating the ability to impede the growth of p53-mutant tumor cells. This compound shows promise for research applications focused on tumors that are linked to DNA damage response mechanisms. -
CHK1 Inhibitor
BEN-28010 is a selective CHK1 inhibitor that demonstrates potent inhibitory activity with an IC50 of 4.0 nM. This compound is orally active and effectively penetrates the blood-brain barrier, making it a valuable tool in cancer research. BEN-28010 acts as a radiosensitizer and exhibits antitumor efficacy in glioblastoma models, providing a promising avenue for investigation into glioblastoma therapies. -
Chk1/Wee1 Inhibitor
PD 407824 is a selective inhibitor of checkpoint kinase Chk1 and WEE1, exhibiting IC50 values of 47 nM and 97 nM, respectively. This compound enhances the sensitivity of cells to low concentrations of BMP4, positioning it as a valuable tool for studying BMP signaling pathways and cellular responses to DNA damage. PD 407824 is applicable in cancer research and therapeutic development targeting cell cycle regulation and stress response mechanisms. -
CHK1 Inhibitor
LY2880070 is a potent, orally active CHK1 inhibitor with an IC50 of less than 1 nM. This reagent demonstrates significant biological activity in cancer cell lines, making it a valuable tool for investigating cancer therapies, particularly in combination with DNA-damaging agents. Its application in preclinical research facilitates the exploration of CHK1's role in DNA repair and cellular response to genotoxic stress. -
Chk2 Inhibitor
PV-1019 (NSC 744039) is a selective inhibitor of Chk2 with an IC50 value of 24 nM. This compound effectively inhibits Chk2 autophosphorylation induced by Topotecan, demonstrating its potential to modulate cellular responses to DNA damage. PV-1019 is valuable for research applications related to cancer biology and therapeutic strategies targeting DNA damage response mechanisms. -
ChK1 Inhibitor
GDC-0425 is a potent, oral small molecule inhibitor targeting check-point kinase 1 (ChK1). This selective inhibitor demonstrates significant activity in disrupting ChK1-mediated signaling pathways, making it valuable for research into various malignancies. Its application in cancer studies may enhance the understanding of tumor response to DNA damage and inform therapeutic strategies. -
Chk1 Inhibitor
Chk1-IN-5 is a potent inhibitor of checkpoint kinase 1 (Chk1), effectively blocking its phosphorylation activity. This compound demonstrates significant antitumor efficacy by inhibiting tumor growth in colon cancer xenograft models. Chk1-IN-5 is valuable for research applications focusing on cell cycle regulation and cancer therapeutics. -
Chk Inhibitor
AZD-7762 hydrochloride is a potent ATP-competitive inhibitor of checkpoint kinases, specifically demonstrating an IC50 of 5 nM for Chk1. This compound is primarily utilized in research focused on cell cycle regulation and DNA damage response mechanisms. Its ability to inhibit Chk1 makes it valuable for investigating therapeutic strategies in cancer treatment and enhancing the efficacy of DNA-damaging agents. -
CHK1 Inhibitor
CHK1-IN-7 is a selective inhibitor of checkpoint kinase 1 (CHK1), targeting key signaling pathways involved in cell cycle regulation. This compound has demonstrated the ability to enhance the antiproliferative effects of Gemcitabine in both prostate and breast cancer cell lines, indicating its potential utility in combination therapies. CHK1-IN-7 is suitable for research applications focusing on cancer biology, particularly in understanding the mechanisms of resistance to chemotherapy and improving therapeutic efficacy. -
Chk1 Inhibitor
Chk1-IN-6 is a selective checkpoint kinase 1 (Chk1) inhibitor, exhibiting an IC50 of 16.1 nM. It demonstrates notable antiproliferative activity against MV-4-11 cells and provides effective therapeutic responses in MV-4-11 xenograft mouse models. Additionally, Chk1-IN-6 has shown a synergistic anticancer effect in combination with Gemcitabine. This compound is valuable for research focused on acute myeloid leukemia and colorectal adenocarcinoma. -
CHK1 Inhibitor
MU380 is a selective CHK1 inhibitor that targets the checkpoint kinase 1 (CHK1) pathway. It demonstrates potent pro-apoptotic effects, leading to the induction of apoptosis in cancer cells. This compound is primarily utilized in cancer research to explore mechanisms of tumorigenesis and to evaluate potential therapeutic strategies aimed at enhancing the efficacy of existing treatment modalities. -
Chk2 Inhibitor
VRX0466617 is a selective, ATP-competitive inhibitor of Chk2 with an IC50 of 120 nM and a Ki of 11 nM. It exhibits specificity by not inhibiting Chk1 activity. This compound is valuable for research focused on cancer mechanisms and the modulation of DNA damage repair pathways. -
Chk1/Chk2 Inhibitor
VER-00158411 is a potent inhibitor of checkpoint kinase 1 (CHK1) and CHK2, exhibiting IC50 values of 4.4 nM and 4.5 nM, respectively. This compound is a valuable tool for studying cell cycle regulation and DNA damage response mechanisms. Its inhibitory effects on CHK1 and CHK2 make it suitable for research applications in cancer biology, particularly in combination therapies targeting replication stress in tumor cells. -
Checkpoint Kinase (Chk) Inhibitor
CHK1-IN-4 is a selective inhibitor of checkpoint kinase 1 (Chk1), effectively blocking Chk1 phosphorylation in tumor cells. This compound demonstrates significant anti-tumor activity, making it a valuable tool for cancer research. Its ability to disrupt cell cycle regulation positions CHK1-IN-4 as a potential candidate for investigating therapeutic strategies in oncology. -
Chk2 Inhibitor
PV1115 is a highly selective Chk2 inhibitor with a low IC50 of 0.14 nM, demonstrating significant potency against Chk2 while exhibiting much weaker activity against Chk1 and RSK2 (IC50s of 66000 nM and >100000 nM, respectively). This compound operates by binding within the ATP-binding pocket of Chk2, making it an invaluable tool for research involving DNA damage response and cancer therapeutics. PV1115 is suitable for studies investigating Chk2's role in cell cycle regulation and its implications in tumor biology. -
Chk1 Inhibitor
PD-321852 is a selective Chk1 inhibitor with an IC50 of 5 nM. It effectively interferes with checkpoint kinase 1 activity, promoting cell cycle arrest and apoptosis in cancerous cells. This reagent is valuable for anti-cancer research, particularly in studies exploring the modulation of DNA damage response and therapeutic susceptibility in tumor cells. -
Chk2 Inhibitor
Chk2-IN-2 is a selective inhibitor of CHK2, a key regulator in the DNA damage response pathway. This compound exhibits potent anticancer activity by hindering cell cycle progression in response to DNA damage. It is primarily utilized in research applications focused on cancer cell biology and the development of targeted therapies for tumors with defective DNA repair mechanisms. -
CHK1 Inhibitor
MCL1020 is a potent CHK1 inhibitor, characterized by an IC50 of 1.61 μM. This compound effectively occupies the ATP binding pocket through interactions with multiple sites on the CHK1 kinase. MCL1020 is useful for investigating mechanisms in hematologic malignancies, facilitating research into potential therapeutic strategies targeting this protein. -
CHK1 Inhibitor
CHK1-IN-11 is a selective checkpoint kinase 1 (CHK1) inhibitor that exhibits oral bioactivity. This compound demonstrates significant potential in targeting cancers characterized by oncogene amplification. CHK1-IN-11 may be employed in research to explore the mechanisms of tumor cell proliferation and response to therapeutic agents in cancer models. -
Chk Kinase Inhibitor
CBP501 Affinity Peptide is a Chk kinase inhibitor that effectively disrupts G2 cell cycle arrest triggered by DNA-damaging agents. This reagent is valuable for cancer research, enabling studies on cell cycle regulation and therapeutic responses to genotoxic stress. Its application can facilitate the investigation of DNA damage repair pathways and their implications in oncogenesis. -
Chk2 Inhibitor
NSC 109555 ditosylate is a selective, ATP-competitive inhibitor of checkpoint kinase 2 (Chk2) with an IC50 of 240 nM. This compound is primarily utilized in cancer research to investigate mechanisms of cell cycle regulation and DNA damage response. Its specificity towards Chk2 makes it valuable in studying potential therapeutic strategies for cancer treatment. -
Chk2 Inhibitor
Chk2-IN-1 is a selective inhibitor of checkpoint kinase 2 (Chk2), demonstrating an IC50 of 13.5 nM for Chk2 and 220.4 nM for Chk1. This compound effectively enhances ATM-dependent Chk2-mediated radioprotection, making it a valuable tool for studying DNA damage response mechanisms. Chk2-IN-1 is applicable in cancer research, particularly in investigations of cell cycle regulation and therapeutic resistance. -
Chk1 Inhibitor
GDC0575 hydrochloride is a highly selective and orally active inhibitor of Chk1, with an IC50 of 1.2 nM. This compound exhibits significant activity in disrupting cell cycle regulation and DNA damage response pathways. GDC0575 is primarily utilized in research related to colitis-associated cancer (CAC) and provides a valuable tool for studying the mechanisms underlying colitis and its implications in oncogenesis. -
CHK2 Inhibitor
CCT241533 dihydrochloride is a highly selective ATP-competitive inhibitor of CHK2, exhibiting an IC50 of 3 nM and a Ki of 1.16 nM. This compound has significant potential in cancer research due to its ability to modulate DNA damage responses and cell cycle regulation. It is particularly valuable for studies investigating the role of CHK2 in tumor biology and therapeutic sensitivity. -
CHK1 Inhibitor
CHK1-IN-13 is a selective checkpoint kinase 1 (CHK1) inhibitor with an IC50 range of 10-50 nM. This compound exhibits significant anticancer activity, making it a valuable tool for research focused on various cancers, including breast, ovarian, and prostate cancers. Its role in modulating the cell cycle checkpoint pathways provides insights into the mechanisms of cancer cell proliferation and therapeutic resistance. -
CHK1 Inhibitor
CHK1-IN-14 is a potent CHK1 inhibitor that selectively disrupts checkpoint kinase 1 activity. This compound is primarily utilized in research focused on understanding mechanisms of resistance to chemotherapy and radiotherapy in cancer cells. Its application provides valuable insights into potential therapeutic strategies aimed at improving the efficacy of cancer treatments. -
Dual Wee1/Chk1 Inhibitor
DB07006 is a potent dual inhibitor targeting Wee1 and Chk1 kinases. It exhibits ATP-competitive inhibition, with IC50 values of 0.030 μM for Wee1 and 0.018 μM for Chk1. This compound effectively abrogates the G2/M checkpoint when used in conjunction with DNA-damaging agents in cellular models, making it a valuable tool for cancer research and therapeutic strategies aimed at enhancing the efficacy of DNA-damage response inhibitors. -
Checkpoint Kinase (Chk) Inhibitor
(S)-CCT245737 is a selective inhibitor of checkpoint kinase 1 (CHK1), primarily targeting cell cycle regulation. This compound exhibits potent inhibitory activity, making it a valuable tool for studying the role of CHK1 in DNA damage response and replication stress. Its applications extend to cancer research, particularly in investigating therapeutic strategies for tumors with defective DNA repair mechanisms. -
Chk Inhibitor
XL-844 is an inhibitor of checkpoint kinases Chk1 and Chk2, leading to the induction of apoptosis in tumor cells by disrupting cell cycle arrest. Additionally, XL-844 demonstrates inhibitory effects on vascular endothelial growth factor receptors VEGFR1 and VEGFR3. This compound is primarily applied in anti-cancer research to explore its potential in enhancing therapeutic efficacy against various malignancies. -
Chk1 Inhibitor
CHK1-IN-8 is a selective Chk1 inhibitor with an IC50 value of less than 10 nM for human Chk1. This compound is valuable for investigating the role of Chk1 in cell cycle regulation and DNA damage response mechanisms in cancer research. Its potent inhibition of Chk1 makes it a useful tool for exploring therapeutic strategies in cancer treatment. -
Chk2 Inhibitor
PV1162 is a selective Chk2 inhibitor that functions by preventing ATP binding to Chk2, specifically targeting the gatekeeper-dependent hydrophobic pocket situated behind the ATP-binding site. With an IC50 of 0.29 nM, PV1162 effectively inhibits the phosphorylation activity of Chk2. This compound demonstrates significant potential for research applications in cancer therapy, particularly in the study of checkpoint regulation and tumor progression.
