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
-
Chk1 Related Products (71)
Related Products (71)
-
Recombinant Proteins (2)
-
Antibodies (3)
-
BEN-28010
0 ImagesCat. No.: HY-186085CAS No.: 3033961-38-2BEN-28010 is a selective, orally active, blood-brain barrier permeable CHK1 inhibitor with an IC50 of 4.0 nM. BEN-28010 functions as a radiosensitizer, exhibits antitumor efficacy in GBM models. BEN-28010 can be used for the research of glioblastoma.
-
Tubulozole
0 ImagesCat. No.: HY-119169CAS No.: 84697-22-3Synonyms: R 46846Tubulozole (R 46846) is an orally active inhibitor of tubulin polymerization with an ID50 of 0.34 μM. Tubulozole induces activation of the Chk1 kinase and phosphorylation of ERK1/2, which is required for microtubule formation. Tubulozole arrests Mitosis at the metaphase stage. Tubulozole causes cells to accumulate in the radiosensitive mitotic phase of the cell cycle. Tubulozole exerts anticancer activity against colon cancer. Tubulozole produces a radiosensitizing effect in mouse tumor models and enhances the tumor growth delay effect when combined with γ-ray irradiation. Tubulozole is used in studies related to colon cancer, fascioliasis, MO4 fibrosarcoma, and Lewis lung carcinoma.
-
CBP-501 acetate
0 ImagesCat. No.: HY-16129APurity: 99.75%CBP-501 acetate, 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 acetate is used for various types of cancer.
-
DHI1
0 ImagesCat. No.: HY-175261DHI1 is an anti-leukemia agent with high selectivity for Jurkat (IC50 = 21.83 μM) and HL-60 (IC50 = 19.14 μM) leukemia cells and has low toxicity to non-cancerous cells. DHI1 can induce G2/M phase cell arrest in Jurkat and HL-60 leukemia cells, as well as S phase arrest in HL-60 cells, and has significant effects on cell cycle signaling molecules Wee1, cyclin B1, cdc2 on Tyr15, and Chk1. DHI1 inhibits the migration and invasion of Jurkat and HL-60 cells by disrupting cytoskeletal actin filaments. DHI1 can be used to study hematological malignancies.
-
BBI-355
0 ImagesCat. No.: HY-171759CAS No.: 3017958-71-0BBI-355 (Compound 1) is an orally active, checkpoint kinase 1 (CHK1) inhibitor. BBI-355 is useful for the study of cancers with oncogene amplification.
-
Castalin
0 ImagesCat. No.: HY-N21945CAS No.: 19086-75-0Castalin is a polyphenolic anticancer compound isolated and identified from the bark or nut shells of Castanea sativa Mill. Castalin induces DNA damage by increasing ROS to activate CHK1, while recruiting 53BP1/RIF1 and activating DNA-PKcs to initiate the NHEJ pathway for DNA repair. Castalin can be used in research related to cervical cancer and breast cancer.
-
MA203
0 ImagesCat. No.: HY-179157MA203 is a selective CHK1 PROTAC degrader. MA203 targets activated CHK1 for degradation by recruiting the CRBN E3 ubiquitin ligase, thereby completely abolishing both its catalytic and non-catalytic functions and ultimately triggering DNA replication catastrophe and apoptosis. MA203 can be used in research related to pancreatic ductal adenocarcinoma, colorectal cancer, and acute lymphoblastic leukemia.
-
Chk2-IN-1
0 ImagesCat. No.: HY-112477CAS No.: 724708-21-8Synonyms: Hymenialdisine analogue-1Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect.
-
GDC0575 hydrochloride
0 ImagesCat. No.: HY-112167BCAS No.: 1196504-54-7Synonyms: ARRY-575 hydrochloride; RG7741 hydrochloride
-
CCT241533 dihydrochloride
0 ImagesCat. No.: HY-110331CAS No.: 1962925-28-5CCT241533 dihydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
-
PROTAC ATR degrader-3
0 ImagesCat. No.: HY-182016CAS No.: 3126270-11-6PROTAC ATR degrader-3 is a potent CRBN-based ATR PROTAC degrader with a DC50 of 127 nM. PROTAC ATR degrader-3 also degrades CHK1 with an DC50 of 135 nM. PROTAC ATR degrader-3 inhibits cancer cells proliferation, migration and invasion, triggers apoptosis and induces S phase arrest and DNA damage. PROTAC ATR degrader-3 achieves tumor growth inhibition in LoVo xenograft mouse model without apparent toxicity. PROTAC ATR degrader-3 can be used for the research of colorectal cancer.
-
CHK1-IN-9
0 ImagesCat. No.: HY-161383CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026).
-
CHK1-IN-13
0 ImagesCat. No.: HY-177027CAS No.: 2120398-52-7CHK1-IN-13 (Compound 38) is a checkpoint kinase 1 (Chk1) inhibitor with an IC50 of 10-50 nM. CHK1-IN-13 has anticancer activity, and can be used for the research of cancers, such as breast, ovarian and prostate cancer.
-
Multi-kinase-IN-6
0 ImagesCat. No.: HY-156470CAS No.: 3009081-73-3Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.
-
CHK1-IN-14
0 ImagesCat. No.: HY-177551CAS No.: 1803106-00-4CHK1-IN-14 is a free base form of CHK1 inhibitor. CHK1-IN-14 can be used in research on resistance to chemotherapy and radiotherapy.
-
DB07006
0 ImagesCat. No.: HY-160948CAS No.: 622855-60-1DB07006 (compound 18) is a potent, ATP-cpmpetitive dual inhibitor of Wee1 (IC50 = 0.030 μM) and Chk1 checkpoint kinases (IC50 = 0.018 μM). DB07006 demonstrates effective abrogation of the G2/M checkpoint in combination with DNA-damaging agents in cellular models. DB07006 can be used for cancer research.
-
PROTAC FLT3/CHK1 Degrader-1
0 ImagesCat. No.: HY-178858PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces Apoptosis in cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML).
-
CHK1-IN-12
0 ImagesCat. No.: HY-171785CAS No.: 2871056-82-3CHK1-IN-12 (Compound example 1-5) is an orally active and highly selective checkpoint kinase 1 (CHK1) inhibitor with in vitro enzyme IC50≤10 nM and cellular IC50≤50 nM. CHK1-IN-12 inhibits the phosphorylation activity of CHK1 kinase to block the DNA damage response pathway, inducing tumor cell cycle arrest and apoptosis. CHK1-IN-12 is promising for research of cancers.
