Chk1
Chk1 (checkpoint kinase 1) mediates the DNA damage response and normal cell-cycle regulation through checkpoint activation, cell-cycle arrest, DNA repair, and cell death control[1]. Mechanistically, Chk1 functions as a key transducer in genome-integrity checkpoints, especially within ATR-linked responses to stalled replication and genotoxic stress[2][3]. In cancer research, this role makes Chk1 relevant to replication stress, BRCA wild-type ovarian cancer models, and studies combining checkpoint inhibition with DNA-damaging therapy[4][5]. Compared with Chk2, Chk1 shows distinct activation biology and experimentally separable checkpoint functions, while Chk1-S acts as an endogenous splice-variant inhibitor that regulates Chk1-dependent checkpoints[2][6]. For experimental applications, Chk1 inhibitors such as prexasertib/LY2606368 induce replication catastrophe and have been tested in tumor models and recurrent high-grade serous ovarian cancer[7][8].
References:
- [1]. Patil M, et al. Checkpoint kinase 1 in DNA damage response and cell cycle regulation. Cell Mol Life Sci. 2013 Nov;70(21):4009-21. [Content Brief]
- [2]. Bartek J, et al. Chk1 and Chk2 kinases in checkpoint control and cancer. Cancer Cell. 2003 May;3(5):421-9. [Content Brief]
- [3]. Dai Y, et al. New insights into checkpoint kinase 1 in the DNA damage response signaling network. Clin Cancer Res. 2010 Jan 15;16(2):376-83. [Content Brief]
- [4]. Rabezanahary H, et al. Live virus neutralizing antibodies against pre and post Omicron strains in food and retail workers in Québec, Canada. Heliyon. 2024 May 21;10(10):e31026. [Content Brief]
- [5]. Nair J, et al. Resistance to the CHK1 inhibitor prexasertib involves functionally distinct CHK1 activities in BRCA wild-type ovarian cancer. Oncogene. 2020 Aug;39(33):5520-5535. [Content Brief]
- [6]. Pabla N, et al. Checkpoint kinase 1 (Chk1)-short is a splice variant and endogenous inhibitor of Chk1 that regulates cell cycle and DNA damage checkpoints. Proc Natl Acad Sci U S A. 2012 Jan 3;109(1):197-202. [Content Brief]
- [7]. King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-13. [Content Brief]
- [8]. Lee JM, et al. Prexasertib, a cell cycle checkpoint kinase 1 and 2 inhibitor, in BRCA wild-type recurrent high-grade serous ovarian cancer: a first-in-class proof-of-concept phase 2 study. Lancet Oncol. 2018 Feb;19(2):207-215. [Content Brief]
All Product Categories
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Chk1 Related Products (73)
Related Products (73)
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Recombinant Proteins (2)
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Antibodies (3)
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Chk1-IN-5
0 ImagesChk1-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.
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GNE-900
0 ImagesGNE-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.
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AZD-7762 hydrochloride
0 ImagesAZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
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Abd110
0 ImagesAbd110 is a selective ATR PROTAC degrader. Abd110 recruits Cereblon to induce the proteasomal degradation of ATR, and reduces the levels of phosphorylated ATR and downstream phosphorylated CHK1. Abd110 can be used for research on pancreatic cancer and cervical cancer.
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CHK1-IN-3
0 ImagesCHK1-IN-3 is a potent and selective CHK1 inhibitor with an IC50 of 0.4 nM. CHK1-IN-3 effectively inhibits the growth of malignant hematopathy cell lines and displays low affinity for hERG (IC50 > 40 μM). CHK1-IN-3 significantly suppresses the tumor growth in vivo. CHK1-IN-3 can be used for the study of hematologic malignancies.
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Chk1-IN-6
0 ImagesChk1-IN-6 is a selective and orally active Chk1 inhibitor with an IC50 of 16.1 nM. Chk1-IN-6 shows antiproliferative activity of MV-4-11 cells. Chk1-IN-6 exerts effective response in the MV-4-11 xenograft mouse model. Chk1-IN-6 exhibits synergistic anticancer effect with Gemcitabine (HY-17026). Chk1-IN-6 can be used in the research of cancers such as acute myeloid leukemia and colorectal adenocarcinoma.
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PROTAC Chk1 degrader-1
0 ImagesPROTAC Chk1 degrader-1 is a Chk1-targeting PROTAC.PROTAC Chk1 degrader-1 recruits the Cereblon E3 ligase to induce ubiquitination and proteasomal degradation of Chk1.PROTAC Chk1 degrader-1 exhibits Chk1 degradation activity in malignant melanoma cells without showing a hook effect.PROTAC Chk1 degrader-1 can be used for the research of malignant melanoma.
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CCT241533
0 ImagesCat. No.: HY-14715CAS No.: 1262849-73-9CCT241533 is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
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Prexasertib Mesylate Hydrate
0 ImagesCat. No.: HY-18174BCAS No.: 1234015-57-6Synonyms: LY2606368 Mesylate Hydrate; LY2940930Prexasertib 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.
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CBP-501
0 ImagesCat. No.: HY-16129CAS No.: 565434-85-7CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of cancer.
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BBI-2779
0 ImagesCat. No.: HY-155798CAS No.: 2871057-47-3BBI-2779 is a highly selective, orally active CHK1 inhibitor with a CHK1 IC50 of 0.3 nM. BBI-2779 leverages transcription-replication conflicts on extrachromosomal DNA (ecDNA) to induce synthetic lethality, replication stress, DNA damage and cell death in ecDNA-positive tumor cells. BBI-2779 blocks ecDNA-mediated acquired resistance to targeted therapies and inhibits tumor growth in mouse models of gastric cancer. BBI-2779 is applicable to ecDNA-positive cancer-related research.
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CHK1-IN-4 hydrochloride
0 ImagesCat. No.: HY-128766ACHK1-IN-4 hydrochloride is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC50 ≤ 1 nM. The IC50 value of CHK1-IN-4 hydrochloride against Chk2 ranges from 50 to 100 nM. CHK1-IN-4 hydrochloride inhibits cancer cell proliferation and exhibits antitumor activity in colon cancer xenograft models. CHK1-IN-4 hydrochloride can be used for the research of colon cancer and breast cancer.
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Prexasertib mesylate
0 ImagesCat. No.: HY-18174CCAS No.: 1234015-55-4Synonyms: LY2606368 mesylatePrexasertib 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.
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VER-00158411
0 ImagesCat. No.: HY-18942CAS No.: 1174664-88-0VER-00158411 is a checkpoint kinase 1 (CHK1) and CHK2 inhibitor with IC50 values of 4.4 nM and 4.5 nM, respectively.
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CHK1-IN-2
0 ImagesCat. No.: HY-111369CAS No.: 912367-45-4CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.
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Isogranulatimide
0 ImagesCat. No.: HY-112347CAS No.: 244148-46-7Isogranulatimide is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC50 value of 0.1 μM. Isogranulatimide inhibits the G2/M checkpoint and inhibits the growth of p53-mutant tumor cells. Isogranulatimide is promising for research of tumors associated with DNA damage response.
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PD-321852
0 ImagesCat. No.: HY-124731CAS No.: 622856-21-7PD-321852 is a Chk1 inhibitor, with IC50 of 5 nM. PD-321852 can be used in anti-cancer research.
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MCL1020
0 ImagesCat. No.: HY-159707CAS No.: 2309309-69-9
