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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
19 Results for "
G2M checkpoint
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "G2M checkpoint" in MCE Product Catalog:
37
37 Publications Verification
Cat. No.: HY-16954
CAS No.: 1818885-28-7
Target:
PROTACs Epigenetic Reader Domain c-Myc Polo-like Kinase (PLK) CDK JAK STAT Pim Bcl-2 Family PAK Wnt β-catenin Caspase PARP Apoptosis Reactive Oxygen Species (ROS)
Research Areas:
ARV-825 is a BET protein PROTAC degrader that recruits cereblon, and it targets BRD2, BRD3, and BRD4 for degradation via the ubiquitin-proteasome pathway. ARV-825 downregulates c-MYC, PLK1, MYCN, CDK4/6, JAK2, pSTAT3/5, PIM1, and Bcl-xL, upregulates p21 and p27, and modulates H3K27Ac-mediated transcription, the G2/M checkpoint, the Wnt/β-catenin pathway, and amino acid transport pathways. ARV-825 induces G1 phase cell cycle arrest, caspase 3/PARP-mediated apoptosis, DNA damage, and reactive oxygen species (ROS) production, reduces mitochondrial respiration, and simultaneously inhibits cell proliferation, clonogenic growth, and cell migration. ARV-825 is used in research on gastric cancer, leukemia, neuroblastoma, and cholangiocarcinoma .
27
27 Cited Publications
Synonyms: VE-822; VX-970; M6620
Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
27
27 Cited Publications
Cat. No.: HY-13902A
CAS No.: 1428935-04-9
Synonyms: VE-822 hydrochloride; VX-970 hydrochloride; M6620 hydrochloride
Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib hydrochloride blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib hydrochloride induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib hydrochloride can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
11
11 Cited Publications
Cat. No.: HY-19959
CAS No.: 1198097-97-0
Mirin is a potent Mre11-Rad50-Nbs1 (MRN) complex inhibitor. Mirin prevents MRN-dependent activation of ATM (IC50=12 μM) without affecting ATM protein kinase activity, and it inhibits Mre11-associated exonuclease activity. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Mirin prevents ATM activation in response to DNA double-strand breaks (DSBs) and blocks homology-directed repair (HDR) in mammalian cells .
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GNE-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 .
Cat. No.: HY-178190
WEE1-IN-13 (Compound 10) is a highly selective WEE1 kinase inhibitor (IC50=0.7 nM). WEE1-IN-13 abrogates the G2/M checkpoint and induces tumor cell apoptosis. WEE1-IN-13 is promising for research of solid tumors (e.g., non-small cell lung cancer, ovarian cancer) .
Cat. No.: HY-146792
CAS No.: 2622273-55-4
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PLK1-IN-4 is a potent and selective PLK1 inhibitor with IC50 < 0.508 nM. PLK1-IN-4 has broad antiproliferative activity against a variety of cancer cell lines. PLK1-IN-4 induces mitotic arrest at the G2/M phase checkpoint, leading to cancer cell apoptosis. PLK1-IN-4 can be used for researching hepatocellular carcinoma .
Cat. No.: HY-W015940
CAS No.: 1455-77-2
Target:
Guanazole is a ribonucleotide reductase (RNR) inhibitor that blocks replicative DNA synthesis by inhibiting deoxyribonucleotide biosynthesis. Guanazole selectively inhibits DNA synthesis in rapidly proliferating tissues, induces replication stress and G2/M phase arrest in Schizosaccharomyces pombe, and exhibits myelosuppressive, immunosuppressive, and anti-L1210 leukemia activities. Guanazole does not induce DNA repair and only shows slight mutagenicity towards Salmonella typhimurium TA102. Guanazole serves as an alternative tool to Hydroxyurea (HY-B0313) for replication checkpoint studies in Schizosaccharomyces pombe. Guanazole can be applied in research related to leukemia and solid tumors .
Cat. No.: HY-112347
CAS No.: 244148-46-7
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Research Areas:
Isogranulatimide 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 .
Cat. No.: HY-156916
CAS No.: 93326-70-6
Research Areas:
WAY-230563 (ST045945) is a serine/threonine kinase inhibitor that can block CHK1/CHK2-mediated cell cycle checkpoints. WAY-230563 can induce G2/M phase arrest and DNA damage in tumor cells .
Cat. No.: HY-178150
CAS No.: 2803921-87-9
WEE1-IN-14 (Compound 14) is a selective WEE1 inhibitor (IC50: 0.5 nM in L-RB-FEP calculations, 1.0 nM in ADP-Glo kinase assay). Inhibition of Wee1 in cancer cells disrupts the G2-M checkpoint, removes the regulatory controls on the cell cycle, and leads to early onset of mitotic failure followed by apoptosis of tumor cells. Therefore, WEE1-IN-14 is a useful tool for studying cancer biology .
Cat. No.: HY-168739
CAS No.: 2413582-45-1
Target:
Topoisomerase Reactive Oxygen Species (ROS) Apoptosis Survivin Bcl-2 Family IAP DNA/RNA Synthesis
Research Areas:
Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice .
Cat. No.: HY-160948
CAS No.: 622855-60-1
Target:
Research Areas:
DB07006 (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 .
Cat. No.: HY-108343R
CAS No.: 622855-37-2
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Research Areas:
WEE1-IN-4 (Standard) is the analytical standard of WEE1-IN-4 (HY-108343). This product is intended for research and analytical applications. WEE1-IN-4 (Compound 15) is a potent checkpoint Wee1 Kinase inhibitor with an IC50 of 0.011 μM. Wee1 inhibitors can abrogate the G2/M checkpoint .
Cat. No.: HY-189062
ZJC-11 is a CDK7 inhibitor with an IC50 of 5.4 nM. ZJC-11 binds covalently to CDK7, inhibits CDK7-dependent phosphorylation of RNAPII at Ser2, Ser5 and Ser7 sites, and suppresses transcriptional processes. ZJC-11 acts as a cell cycle inhibitor, inhibits the G2/M checkpoint pathway, and induces G2/M phase arrest. ZJC-11 induces DNA damage-driven cellular senescence and cell death. ZJC-11 exhibits antiproliferative activity against triple-negative breast cancer both in vitro and in vivo. ZJC-11 can be used for research related to triple-negative breast cancer
Cat. No.: HY-184732
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Research Areas:
ERα-IN-3 is a ERα inhibitor with an IC50 of 74.48 μM. ERα-IN-3 induces cell cycle arrest at the G0/G1 and G2/M checkpoints and triggers Apoptosis. ERα-IN-3 exhibits anticancer effects against ER-positive breast cancer. ERα-IN-3 can be used for the research of ERα-positive breast cancer .
Cat. No.: HY-183547
CAS No.: 3055032-68-0
WEE1/PKMYT1-IN-4 is a selective WEE1/PKMYT1 inhibitor, with IC50 values of 0.185 μM and 2.2 nM for human WEE1 and PKMYT1, respectively. WEE1/PKMYT1-IN-4 inhibits phosphorylation of CDK1 at T14 and Y15, disrupting the G2/M cell cycle checkpoint. WEE1/PKMYT1-IN-4 can be used for the research of colorectal cancer and amplified breast cancer .
Cat. No.: HY-13902R
CAS No.: 1232416-25-9
Synonyms: VE-822 (Standard); VX-970 (Standard); M6620 (Standard)
Berzosertib (Standard) is the analytical standard of Berzosertib (HY-13902). This product is intended for research and analytical applications. Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR Kinase inhibitor. Berzosertib blocks ATR Kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
Cat. No.: HY-183118
CAS No.: 3064485-16-8
Research Areas:
CID-078 is an orally active macrocyclic cyclin A and cyclin B inhibitor. CID-078 binds cyclin hydrophobic patches, disrupting interactions of cyclin A-Cdk2 with E2F1 and cyclin B-Cdk1 with Myt1, and selectively targets RxL binding motifs to block complex-substrate interactions. CID-078 induces DNA damage, G2/M cell cycle arrest, apoptosis, mitotic catastrophe, spindle assembly checkpoint activation, and neomorphic cyclin B-CDK2 complex formation, driving synthetic lethality in E2F-driven cancer cells. CID-078 can be used for the research of small cell lung cancer, non-small cell lung cancer, triple negative breast cancer, advanced solid tumors, luminal HR +/HER 2- breast cancer, RB1-altered solid tumors, and neuroblastoma .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
