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γH2AX

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Aldehyde Dehydrogenase (ALDH) (1) Apoptosis (14) Bacterial (1) Bcl-2 Family (2) Caspase (3) DNA-PK (1) DNA/RNA Synthesis (7) HDAC (3) Histone Methyltransferase (4) IAP (1) MDM-2/p53 (1) Microtubule/Tubulin (1) Mitochondrial Metabolism (1) PARP (2) Reactive Oxygen Species (5) Survivin (1) Topoisomerase (3)
By Research Areas:	Cancer (21) Infection (1) Inflammation/Immunology (1)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-137843

NSC 80467	DNA/RNA Synthesis	Cancer
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 .

HY-147356

ERCC1-XPF-IN-2	DNA/RNA Synthesis	Cancer
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 .

HY-122181

OTS186935 3 Publications Verification	Histone Methyltransferase	Cancer
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 .

HY-122181B

OTS186935 hydrochloride 3 Publications Verification	Histone Methyltransferase	Cancer
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 .

HY-157954

WRN inhibitor 6	DNA/RNA Synthesis Apoptosis	Cancer
WRN inhibitor 6 (compound 3ci) is a potent WRN inhibitor. WRN inhibitor 6 induces apoptosis. WRN inhibitor 6 increases the expression of p-p53, P-Chk2, γH2AX expression .

HY-121777

SFOM-0046	DNA/RNA Synthesis	Cancer
SFOM-0046 arrests cell cycle in S-phase and causes DNA replication stress leading to the phosphorylation of H2AX into γ-H2AX. SFOM-0046 induces DNA damages. SFOM-0046 is a potent anticancer agent .

HY-122181A

OTS186935 trihydrochloride	Histone Methyltransferase	Cancer
OTS186935 trihydrochloride is a protein methyltransferase *SUV39H2* inhibitor with an IC₅₀ of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .

HY-123786

NSC745887	Apoptosis Caspase	Cancer
NSC745887 (compound 25) is an inhibitor that targets DNA topoisomerase cleavage, activates the caspase-8/9-caspase-3-poly (ADP-ribose) polymerase cascade, and induces apoptosis in cancer cells. NSC745887 enhances γH2AX expression and causes DNA fragmentation leading to DNA damage ^[2].

HY-158166

DNA-PK-IN-13	DNA-PK	Inflammation/Immunology Cancer
DNA-PK-IN-13 (Compound SK10) is a DNA-PK inhibitor that exhibits potent inhibitory activity (IC₅₀= 0.11 nM). DNA-PK-IN-13 regulates tumor cell proliferation by decreasing the expression level of *γH2A.X* and enhancing the sensitivity of tumor cells to chemotherapeutic agents. DNA-PK-IN-13 is suitable for oncology studies .

HY-168877

FMP	MDM-2/p53 Reactive Oxygen Species Apoptosis Caspase PARP Bcl-2 Family	Cancer
FMP is a Platinum(IV) complexe. FMP significantly upregulates the expression of *γ-H2AX* and p53. FMP increases the production of ROS. FMP markedly upregulates the expressions of Apoptosis-related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP shows antiproliferative activity against breast cancer .

HY-171124

Tilatamig samrotecan AZD9592	Topoisomerase DNA/RNA Synthesis	Cancer
Tilatamig samrotecan (AZD9592) is an antibody-drug conjugate (ADC) used to deliver topoisomerase I inhibitors (TOP1i), targeting the epidermal growth factor receptor (EGFR) and c-MET, with anti-tumor activity. Tilatamig samrotecan (AZD9592) can induce DNA double-strand breaks, increase the expression of pRAD50 and γH2AX, and inhibit the growth of non-small cell lung cancer ^[2].

HY-170937

Urease-IN-20	Bacterial Apoptosis Reactive Oxygen Species	Infection
Urease-IN-20 (compound XBP2) is an inhibitor of Helicobacter pylori (H. pylori). Urease-IN-20 inhibits H. pylori with an IC₅₀ of 0.14 μM. Urease-IN-20 reduces cell Apoptosis and decreases ROS and γH2AX in GES-1 cells infected with H. pylori. Urease-IN-20 exhibits significant gastric mucosal protective effects. Urease-IN-20 shows the potential for H. pylori research .

HY-122182

OTS193320	Histone Methyltransferase Apoptosis	Cancer
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 (DOX; HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .

HY-117688

WJ35435	HDAC Topoisomerase Apoptosis	Cancer
WJ35435 is a dual-targeted anticancer hybrid that induces anti-HDAC (in particular HDAC1 and HDAC6) and anti-topoisomerase I activities that causes DNA damage associated with a low DNA repair capability and induces cell cycle arrest at G1- and G2-phase to apoptosis. WJ35435 induces histone H3 acetylation and phosphorylation, α-tubulin acetylation and γ-H2AX formation to achieve anti-HDAC effect. WJ35435 is promising for research of cancer .

HY-145289

Antitumor agent-37	Apoptosis	Cancer
Antitumor agent-37 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-37 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-37 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-37 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .

HY-145288

Antitumor agent-36	Apoptosis	Cancer
Antitumor agent-36 possesses potent anti-proliferative and anti-metastasis activities. Antitumor agent-36 induces serious DNA damage and further leads to high expression of γ-H2AX and p53. Antitumor agent-36 promotes apoptosis of tumor cells through mitochondrial apoptotic pathway Bcl-2/Bax/caspase3. Antitumor agent-36 significantly improves immune response through restraining the expression of PD-L1 to increase CD3+ and CD8+ T infiltrating cells in tumor tissues .

HY-168739

Topoisomerase I inhibitor 17	Topoisomerase Reactive Oxygen Species Apoptosis Survivin Bcl-2 Family IAP DNA/RNA Synthesis	Cancer
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 .

HY-159111

KS124	Aldehyde Dehydrogenase (ALDH) Apoptosis Reactive Oxygen Species	Cancer
KS124 (compound 3) is a potent ALDH inhibitor. KS124 shows inhibition for ALDH1A1, ALDH1A3, ALDH3A1. KS124 shows antiproliferative activity. KS124 induces apoptosis and ROS production .

HY-150765

PARP1-IN-12	PARP Apoptosis	Cancer
PARP1-IN-12 is a potent PARP1 inhibitor with an IC₅₀ of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells .

HY-109109

Alteminostat CKD-581	HDAC Apoptosis	Cancer
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 .

HY-15586

L67 1 Publications Verification DNA Ligase Inhibitor	DNA/RNA Synthesis Caspase Apoptosis Reactive Oxygen Species	Cancer
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].

HY-150772

Tubulin/HDAC-IN-1	Microtubule/Tubulin HDAC Apoptosis Mitochondrial Metabolism	Cancer
Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC₅₀: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia .

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γH2AX

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