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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
60 Results for "
γH2AX
" in MedChemExpress (MCE) Product Catalog:
Products (60)
60 Results for "γH2AX" in MCE Product Catalog:
4
4 Cited Publications
Target:
Research Areas:
OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
4
4 Cited Publications
Cat. No.: HY-N2445
CAS No.: 37308-75-1
4
4 Cited Publications
Cat. No.: HY-122181B
Purity: 99.58%
Target:
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OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
2
2 Cited Publications
Synonyms: DNA Ligase Inhibitor
Research Areas:
L67 (DNA Ligase Inhibitor) is a competitive DNA ligase inhibitor that effectively inhibits DNA ligases I/III (both IC50 are 10 μM). L67 can cause nuclear DNA damage by reducing levels of mitochondrial DNA and increasing levels of mitochondrially-generated ROS. L67 also activates the Caspase 1-dependent apoptosis pathway in cancer cells, can be used in cancer research [2].
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1
1 Cited Publications
Cat. No.: HY-N0857
CAS No.: 79233-15-1
1
Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research .
1
1 Cited Publications
Cat. No.: HY-117664
CAS No.: 1633660-76-0
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PNR-7-02 is a dual Rev1 and human DNA polymerase η (hpol η) inhibitor, with an IC50 value of 8 μM against hpol η. PNR-7-02 binds to hpol η to disrupt the orientation of template DNA and block the catalytic function of hpol η. When used in combination with Cisplatin (HY-17394), PNR-7-02 induces DNA damage and replication stress in cells with intact hpol η function. PNR-7-02 can be used in mechanism studies related to chronic myeloid leukemia and ovarian cancer [2].
Cat. No.: HY-172085
CAS No.: 3099543-90-2
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SH514 is an orally active IRF4 inhibitor (IC50 = 2.63 μM). SH514 binds to the IRF4-DBD domain, thereby inhibiting the interaction of IRF4 protein with DNA (KD = 1.28 μM). SH514 can inhibit the proliferation of IRF4-high-expressing NCI-H929 and MM.1R cells, and displays no cytotoxicity for normal cells. SH514 significantly downregulates the expression of IRF4 downstream target genes concentration-dependently. SH514 inhibits the expression of cell cycle-related proteins CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC in Multiple Myeloma cells. SH514 can induce DNA damage and increase the expression of γH2AX. SH514 effectively inhibits the proliferation of multiple myeloma tumors .
Cat. No.: HY-171124
Synonyms: AZD9592
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Tilatamig samrotecan (AZD9592) is an anti-EGFR/c-MET antibody-drug conjugate (ADC). Tilatamig samrotecan consists of an anti-EGFR/c-MET antibody with the drug-linker conjugate being AZ14170133 (HY-145399) (a topoisomerase I (TOP1i) inhibitor payload). Tilatamig samrotecan induces multiple DNA damage response pathway markers (like ATM, ATR, γH2AX). Tilatamig samrotecan selectively binds to EGFR and c-MET, delivering the cytotoxic payload. Tilatamig samrotecan exerts anti-tumor activity in vivo. Tilatamig samrotecan can be used for non-small cell lung cancer (NSCLC) and head and neck squamous cell carcinoma (HNSCC) research [2] .
Cat. No.: HY-163944
CAS No.: 3081311-94-3
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LL-K12-18 is a CDK12 kinase inhibitor and a dual-site molecular glue. LL-K12-18 inhibits human CDK12 with an IC50 value of 283.9 nM, and selectively degrades cyclin K via the ubiquitin-proteasome system by stabilizing the CDK12-DDB1 complex. LL-K12-18 downregulates DNA damage response genes, reduces the phosphorylation level of CTD Ser2 in RNA polymerase II, and modulates biomarkers such as ATM, RAD51, γ-H2AX and cleaved PARP, thereby effectively inducing apoptosis and inhibiting proliferation of breast cancer cells. LL-K12-18 exhibits high target selectivity and serves as a research tool for studies on triple-negative breast cancer [2].
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OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .
Cat. No.: HY-139621
CAS No.: 2916559-62-9
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Colibactin 742 is a covalently binding DNA-damaging agent targeting DNA, with an IC50 of 5.2 μM against human cervical cancer cells (HeLa). Colibactin 742 covalently binds to DNA, forming interstrand crosslinks (ICLs), activating the Fanconi anemia DNA repair pathway, inducing γH2AX and FANCD2 foci formation and cell cycle arrest, while exacerbating mismatch repair deficiency (MMRd)-related mutations. Colibactin 742 can mimic the genotoxicity of natural Colibactin while avoiding its instability, and is mainly used in colorectal cancer (CRC) related research, including microbial tumorigenesis mechanisms, DNA damage repair pathways, and mutation signature analysis [2] .
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ERCC1-XPF-IN-2 is a potent ERCC1-XPF endonuclease inhibitor with an IC50 value of 0.6 μM. ERCC1-XPF-IN-2 shows activity in nucleotide excision repair, cisplatin enhancement and γH2AX assays .
Cat. No.: HY-160005
CAS No.: 1883730-99-1
Synonyms: NSC 781517
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LMP517 (NSC 781517) is a potent and non-camptothecin Topoisomerase I and II (TOP1 and TOP2) dual inhibitor. LMP517 can induce TOP1 and TOP2 cleavage complexes (TOP1ccs and TOP2ccs). LMP517 can induce cancer cells DNA damage and γH2AX production. LMP517 can be used for the research of cancer, such as small cell lung cancer [2].
Cat. No.: HY-163942
CAS No.: 2923008-66-4
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GSK_WRN4 is an orally active WRN helicase inhibitor (pIC50=7.6). GSK_WRN4 induces DNA damage markers (p21, p-γH2AX, p-KAP1). GSK_WRN4 selectively inhibits microsatellite-unstable tumor growth in vitro and in vivo by inducing DNA double-strand breaks, particularly at expanded TA repeats and regions of DNA damage .
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NSC 80467, a DNA damaging agent, selectively inhibits survivin. NSC 80467 preferentially inhibits DNA synthesis and results in induction of γH2AX and pKAP1, two markers of DNA damage .
Cat. No.: HY-P990947
CAS No.: 2868265-50-1
Synonyms: AZD9592 Antibody
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Cat. No.: HY-122860
CAS No.: 2300981-68-2
SKLB-C05 is a novel selective, orally active TOPK inhibitor, with an IC50 of 0.5 nM. SKLB-C05 selectively inhibit TOPK kinase. SKLB-C05 induces Apoptosis, downregulates c-Myc, γ-H2AX, activates p53, blocks FAK/Src medicated migration-related signaling. SKLB-C05 disturbs cell mitosis. SKLB-C05 shows anticancer activity only against TOPK-positive colorectal cancer .
Cat. No.: HY-178909
CAS No.: 741278-95-5
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Y502-2304 is a c-Myc G-quadruplex stabilizer. Y502-2304 exhibits potent antiproliferative activity in multiple myeloma (MM) cells. Y502–2304 downregulates c-Myc mRNA and protein expression. Y502-2304 induces apoptosis in MM cells, characterizes by elevated γH2AX levels, increases reactive oxygen species (ROS) generation, and mitochondrial dysfunction. Y502-2304 significantly inhibits tumor growth in a xenograft MM model. Y502-2304 can be used for the study of multiple myeloma .
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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
