Search Result

Results for "

γ-H2AX

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (2) AMPK (2) Antibody-Drug Conjugates (ADCs) (1) Apoptosis (26) ATM/ATR (1) Autophagy (1) Bacterial (1) Bcl-2 Family (6) c-Met/HGFR (2) c-Myc (3) Caspase (9) CDK (3) Checkpoint Kinase (Chk) (1) DNA Alkylator/Crosslinker (2) DNA Methyltransferase (2) DNA-PK (3) DNA/RNA Synthesis (22) EGFR (2) Eukaryotic Initiation Factor (eIF) (1) FABP (1) FAK (2) Fluorescent Dye (1) GLUT (2) HDAC (3) Histone Demethylase (1) Histone Methyltransferase (4) HSP (1) IAP (3) IFNAR (2) JNK (1) MDM-2/p53 (11) Mitochondrial Metabolism (1) Mitosis (1) MMP (1) Molecular Glues (1) mTOR (1) PAK (1) PARP (7) PERK (1) PI3K (2) RAD51 (3) Reactive Oxygen Species (ROS) (10) Reference Standards (1) SOD (1) Src (1) STING (1) Survivin (1) TOPK (1) Topoisomerase (9) VEGFR (1) Virus Protease (1) Wee1 (1)
By Research Areas:	Cancer (49) Cardiovascular Disease (2) Infection (2) Inflammation/Immunology (2) Metabolic Disease (1)

By Targets:

Akt (2)

AMPK (2)

Antibody-Drug Conjugates (ADCs) (1)

Apoptosis (26)

ATM/ATR (1)

Autophagy (1)

Bacterial (1)

Bcl-2 Family (6)

c-Met/HGFR (2)

c-Myc (3)

Caspase (9)

CDK (3)

Checkpoint Kinase (Chk) (1)

DNA Alkylator/Crosslinker (2)

DNA Methyltransferase (2)

DNA-PK (3)

DNA/RNA Synthesis (22)

EGFR (2)

Eukaryotic Initiation Factor (eIF) (1)

FABP (1)

FAK (2)

Fluorescent Dye (1)

GLUT (2)

HDAC (3)

Histone Demethylase (1)

Histone Methyltransferase (4)

HSP (1)

IAP (3)

IFNAR (2)

JNK (1)

MDM-2/p53 (11)

Mitochondrial Metabolism (1)

Mitosis (1)

MMP (1)

Molecular Glues (1)

mTOR (1)

PAK (1)

PARP (7)

PERK (1)

PI3K (2)

RAD51 (3)

Reactive Oxygen Species (ROS) (10)

Reference Standards (1)

SOD (1)

Src (1)

STING (1)

Survivin (1)

TOPK (1)

Topoisomerase (9)

VEGFR (1)

Virus Protease (1)

Wee1 (1)

By Research Areas:

Cancer (49)

Cardiovascular Disease (2)

Infection (2)

Inflammation/Immunology (2)

Metabolic Disease (1)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-172085

SH514	IFNAR DNA/RNA Synthesis c-Myc CDK	Cancer
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 .

HY-171124

Tilatamig samrotecan AZD9592	Antibody-Drug Conjugates (ADCs) EGFR c-Met/HGFR Topoisomerase DNA/RNA Synthesis	Cancer
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] .

HY-19939S

VX-984 4 Publications Verification M9831	DNA-PK	Cancer
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium ^[2] .

HY-122181

OTS186935 4 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-163944

LL-K12-18	DNA/RNA Synthesis Molecular Glues CDK Apoptosis RAD51 ATM/ATR PARP	Cancer
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].

HY-N2445

Flavokawain C 4 Publications Verification	Apoptosis Akt JNK PERK Caspase PARP MDM-2/p53 IAP Reactive Oxygen Species (ROS) SOD FABP Autophagy AMPK mTOR GLUT EGFR PI3K HSP VEGFR FAK	Cancer
Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway . Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and *HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR* signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases *γ-H2AX* levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer ^[2] .

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

HY-N7271

Solanidine 1 Publications Verification	RAD51 MDM-2/p53	Cardiovascular Disease Cancer
Solanidine is an orally active cholestane alkaloid. Solanidine can be isolated from potato. Solanidine decreases RAD51 and increases *γH2AX* and p53. Solanidine has anti-tumor effects on LLC tumors and lung cancer. Solanidine promotes breast cancer cell proliferation. Solanidine reduces neovascularization. Solanidine causes abortion in some pregnant mice ^[2] .

HY-139621

Colibactin 742	DNA Alkylator/Crosslinker	Cancer
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] .

HY-122181B

OTS186935 hydrochloride 4 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-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-160005

LMP517 NSC 781517	Topoisomerase DNA/RNA Synthesis	Cancer
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].

HY-163942

GSK_WRN4	DNA/RNA Synthesis	Cancer
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 .

HY-N0857

Deoxyandrographolide 1 Publications Verification	GLUT HDAC Virus Protease PI3K AMPK Akt Histone Demethylase MDM-2/p53 IFNAR Reactive Oxygen Species (ROS)	Infection Metabolic Disease Inflammation/Immunology
Deoxyandrographolide is an orally active lactone found in the Andrographis paniculata Nees. Deoxyandrographolide shows a K_D of 38.4 μM of HDAC1. Deoxyandrographolide enhances GLUT4 plasma membrane translocation, activates PI3K and AMPK-dependent signaling pathways, suppresses fasting blood glucose, serum insulin, triglycerides, and LDL-cholesterol levels. Deoxyandrographolide enhances HDAC1 expression via inhibited ubiquitination degradation, represses H3K4me3, improves chromosome stability, and restrains aging biomarkers p16, p21, *γH2A.X, p53* and ROS production. Deoxyandrographolide interacts with Foot-and-Mouth Disease Virus 3Cpro active site, inhibits protease and IFN-antagonist activity, derepresses ISG expression, and inhibits viral replication. Deoxyandrographolide can be used for the researches of type 2 diabetes mellitus, vascular senescence and virus infection .

HY-153339

E235	Eukaryotic Initiation Factor (eIF)	Cancer
E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research .

HY-175700

YCJ-02	Topoisomerase Apoptosis	Cancer
YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC) .

HY-122860

SKLB-C05	TOPK Apoptosis c-Myc MDM-2/p53 FAK Src Mitosis	Cancer
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 .

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-178909

Y502-2304	c-Myc Apoptosis Reactive Oxygen Species (ROS)	Cancer
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 .

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-W414334

ICR-191 dihydrochloride	DNA/RNA Synthesis Fluorescent Dye	Cancer
ICR-191 dihydrochloride enhances Cisplatin (HY-17394)- DNA binding and sensitizes cells to cisplatin. ICR-191 dihydrochloride induces a significant increase in the expression of phosphorylated H2AX (γH2AX), particularly in DNA-replicating cells. ICR-191 dihydrochloride can be used for the study of leukemia ^[2].

HY-178373

Topoisomerase I-IN-18	Topoisomerase DNA/RNA Synthesis Reactive Oxygen Species (ROS) MDM-2/p53 Caspase	Cancer
Topoisomerase I-IN-18, a derivative of Thiosemicarbazide (HY-Y0032), is a Topoisomerase I inhibitor. Topoisomerase I-IN-18 can disrupt DNA synthesis and transcription. Topoisomerase I-IN-18 inhibits tumor cell proliferation by inducing S-phase cell cycle arrest. Topoisomerase I-IN-18 can enhance mitochondria-mediated apoptosis, suppress cell migration, and increase intracellular Reactive Oxygen Species (ROS) levels. Topoisomerase I-IN-18 can increase p53 protein expression, *γH2AX* phosphorylation, upregulate Bax expression, downregulate Bcl-2 expression, and activate the caspase cascade. Topoisomerase I-IN-18 can be used for the study of lung cancer .

HY-178032

PARP1-IN-44	PARP Apoptosis Reactive Oxygen Species (ROS) DNA/RNA Synthesis STING	Cancer
PARP1-IN-44, an Olaparib (HY-10162) derivative, is an orally active PARP1 inhibitor (IC₅₀ = 0.6 nM), and also inhibits *PARP2* (IC₅₀ = 1.0 nM) and PARP7 (IC₅₀ = 7.5 nM). PARP1-IN-44 has selective antiproliferative activity against BRCA-deficient cancer cells with minimal toxicity to normal cells. PARP1-IN-44 induces G2/M phase arrest, promotes apoptosis, elevates ROS levels, disrupts mitochondrial membrane potential. PARP1-IN-44 suppresses PARylation while increasing γH2AX accumulation. PARP1-IN-44 activates the cGAS-STING pathway, upregulating IFN-β and CXCL10 expression. PARP1-IN-44 enhancing CD8+ T cell infiltration in a CT26 tumor mouse model, demonstrating robust in vivo antitumor efficacy .

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-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-168877

FMP	MDM-2/p53 Reactive Oxygen Species (ROS) 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-172537

Indolimine-214	DNA/RNA Synthesis	Inflammation/Immunology Cancer
Indolimine-214 is a metabolite of M. morganii Indolimine-214 increases the level of *γH2AX* in HeLa cells. Indolimine-214 can be used in the study of inflammatory bowel disease (IBD) and colorectal cancer (CRC) .

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-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-N7271R

Solanidine (Standard)	Reference Standards RAD51 MDM-2/p53	Cardiovascular Disease Cancer
Solanidine (Standard) is the analytical standard of Solanidine. This product is intended for research and analytical applications. Solanidine is an orally active cholestane alkaloid. Solanidine can be isolated from potato. Solanidine decreases RAD51 and increases *γH2AX* and p53. Solanidine has anti-tumor effects on LLC tumors and lung cancer. Solanidine promotes breast cancer cell proliferation. Solanidine reduces neovascularization. Solanidine causes abortion in some pregnant mice ^[2] .

HY-170937

Urease-IN-20	Bacterial Apoptosis Reactive Oxygen Species (ROS)	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-119892

Batracylin NSC 320846; BAY-H 2049	Topoisomerase	Cancer
Batracylin (NSC320846) is a potent DNA Topoisomerases I and DNA Topoisomerases II inhibitor. Batracylin shows cytotoxicity and antiproliferative activity. Batracylin induces DNA breaks .

HY-178348

PARP1/c-Met-IN-2	PARP c-Met/HGFR DNA/RNA Synthesis	Cancer
PARP1/c-Met-IN-2 is a highly potent, orally active, PARP1 (IC₅₀ = 21.8 nM) and c-Met (IC₅₀ = 30.2 nM) dual inhibitor. PARP1/c-Met-IN-2 can elevate the expression level of *γH2AX, cause DNA damage. PARP1/c-Met-IN-2 exhibits remarkable anti-tumor efficacy in the Olaparib (HY-10162)-resistant HCT116 (HCT116OR) xenograft models. PARP*1/c-Met-IN-2 can be used for the study of Colon Cancer .

HY-124731

PD-321852	Checkpoint Kinase (Chk)	Cancer
PD-321852 is a Chk1 inhibitor, with IC₅₀ of 5 nM. PD-321852 can be used in anti-cancer research .

HY-149972

Antitumor agent-96	Apoptosis	Cancer
Antitumor agent-96 (Compound D34) is a potent MRE11 inhibitor. Antitumor agent-96 down-regulates the HR pathway by binding with MRE11 and suppressing its endonuclease functions. Antitumor agent-96 induces CM cells apoptosis .

HY-168739

Topoisomerase I inhibitor 17	Topoisomerase Reactive Oxygen Species (ROS) 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-181678

DNA-PK/HDAC6-IN-1	DNA-PK HDAC Apoptosis Mitochondrial Metabolism DNA/RNA Synthesis	Cancer
DNA-PK/HDAC6-IN-1 is a selcetive and orally active dual DNA-PK and HDAC6 inhibitor with IC₅₀ values of 84.2 and 64.8 nM. DNA-PK/HDAC6-IN-1 suppresses cancer cells proliferation, induces cancer cell cycle G2/M arrest, apoptosis, and decreases the mitochondrial membrane potential. DNA-PK/HDAC6-IN-1 induces DNA damage and elevates γ-H2AX levels. DNA-PK/HDAC6-IN-1 exhibits antitumor efficacy in AML animal mouse model. DNA-PK/HDAC6-IN-1 can be used for the research of acute myeloid leukemia .

HY-181557

SY-589	DNA Alkylator/Crosslinker DNA/RNA Synthesis Apoptosis	Cancer
SY-589 is an orally active DNA polymerase Polθ helicase domain inhibitor (IC₅₀=2.29 nM) and DNA damage inducer. SY-589 inhibits the ATPase activity of the Polθ helicase domain and blocks the Polθ-mediated microhomology-mediated end joining (MMEJ) DNA repair pathway (IC₅₀=0.85 nM). SY-589 also induces the accumulation of DNA double-strand breaks by increasing *γ-H2AX* levels. SY-589 exerts antiproliferative effects on BRCA2-deficient cells and is used in the research of HR-deficient tumors .

HY-181018

Topo I/DDX5-IN-1	Topoisomerase PAK Bcl-2 Family IAP Reactive Oxygen Species (ROS) Apoptosis	Cancer
Topo I/DDX5-IN-1 (Compound A10) is a Topo I and DDX5 inhibitor. Topo I/DDX5-IN-1 inhibits Topo I activity, binds to DDX5, and suppresses DDX5 function. Topo I/DDX5-IN-1 increases expression of *γ-H2AX* and p21, suppresses the expression of antiapoptotic proteins (Bcl-2 and XIAP), stimulates ROS generation, and triggers Apoptosis. Topo I/DDX5-IN-1 exhibits anticancer activity against pancreatic cancer, non-small cell lung cancer, skin cancer, and colorectal cancer .

HY-183330

Topo I/II-IN-3	Topoisomerase Reactive Oxygen Species (ROS) Apoptosis MDM-2/p53 Caspase Bcl-2 Family	Cancer
Topo I/II-IN-3 is a dual inhibitor of topoisomerase I/II (topoisomerase I/II), with an IC₅₀ of 8.99 μM against Topo I and an IC₅₀ of 26.92 μM against Topo II. Topo I/II-IN-3 induces DNA damage, elevates intracellular ROS levels, activates the mitochondrial apoptosis pathway, and exerts cytotoxicity against cancer cells. Topo I/II-IN-3 upregulates the expression of *γ-H2AX, p53, activated caspase-9, Bax* and activated caspase-3, while downregulating the expression of *Bcl-2*. Topo I/II-IN-3 can be used in research related to breast cancer, liver cancer and gastric cancer .

HY-182790

BAA-065	Wee1	Cancer
BAA-065 is a selective and orally active PKMYT1 inhibitor with an IC₅₀ of <50 nM. BAA-065 inhibits cancer cells proliferation, induces γH2AX expression and DNA damage. BAA-065 inhibits tumor growth in OVCAR3 xenograft mice. BAA-065 can be used for the research of cancer, such as ovarian cancer .

HY-181060

Apoptosis inducer 56	Apoptosis DNA/RNA Synthesis Caspase Bcl-2 Family MDM-2/p53	Cancer
Apoptosis inducer 56 is an apoptosis inducer. Apoptosis inducer 56 induces DNA damage (upregulation of γH2AX and p-ATM expression) by minor groove binding. Apoptosis inducer 56 induces intrinsic apoptosis (upregulation of p53 and *Bax/Bcl-2* ratio, cleaved caspase-7) via S-phase cell cycle arrest. Apoptosis inducer 56 shows selectivity for cancer cells over normal breast epithelial cells. Apoptosis inducer 56 can be used for the research of breast cancer .

HY-181848

DNA-PK-IN-16	DNA-PK Apoptosis	Cancer
DNA-PK-IN-16 is an orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC₅₀ of 10.2 nM. DNA-PK-IN-16 induces the upregulation of *γH2A.X, a biomarker of DNA double-strand breaks. DNA-PK-IN-16 exhibits antiproliferative activity in various cancer cell lines. DNA-PK-IN-16 enhances the infiltration of CD8 ⁺ T cells in tumor tissues through synergistic action with anti-PD-L1* monoclonal antibody. DNA-PK-IN-16 is applicable for cancer research .

HY-179409

MC3817	DNA Methyltransferase Caspase MDM-2/p53 DNA/RNA Synthesis Apoptosis	Cancer
MC3817 is a selective DNMT1 inhibitor. MC3817 inhibits DNMT1 and DNMT3A/3L with IC₅₀s of 0.044 μM and > 10μM, respectively. MC3817 inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage MC3817 elevates cleaved Caspase 3, P53, and *γH2AX*. MC3817 can be used in non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer and histiocytic lymphoma research .

HY-179409A

MC3817 free base	DNA Methyltransferase Caspase MDM-2/p53 DNA/RNA Synthesis Apoptosis	Cancer
MC3817 free base is a selective DNMT1 inhibitor. MC3817 free base inhibits DNMT1 and DNMT3A/3L with IC₅₀s of 0.044 μM and > 10μM, respectively. MC3817 free base inhibits P53-dependent cancer cell proliferation, induces apoptosis and DNA damage. MC3817 free base elevates cleaved Caspase 3, P53, and *γH2AX*. MC3817 free base can be used in non-small cell lung cancer, colon cancer, cervical cancer, triple-negative breast cancer and histiocytic lymphoma research .

HY-180809

YCH3292	PARP	Cancer
YCH3292, a derivative of YCH189 (HY-155993) is a potent, selective and orally active *PARP1/2* inhibitor with IC₅₀ both <0.001 nM. YCH3292 can increase the stability of PARP-DNA complexes. YCH3292 exhibits robust antiproliferative activity. YCH3292 can induce double-strand breaks in DNA, increase the protein levels of *γH2AX, P-RPA32, and P-Chk1* and induce tumor cells S or G2/M phase arrest and apoptosis. YCH3292 can inhibit tumor growth in MC38 xenograft model .

HY-181272

MMP-9-IN-14	MMP Caspase Apoptosis	Cancer
MMP-9-IN-14 is a MMP-9 inhibitor (IC₅₀ = 34.46 μM). MMP-9-IN-14 induces G1-phase cell cycle arrest and caspase-dependent apoptosis in cancer cells. MMP-9-IN-14 promotes the accumulation of phosphorylated *γH2AX. MMP-9-IN-14 inhibits the migration and invasion of cancer cells, and downregulates the expressions of MMP-2, MMP-9* and hTERT in cancer cells. MMP-9-IN-14 inhibits tumor growth and angiogenic spread in animal models. MMP-9-IN-14 can be used for the research of cancers such as lung adenocarcinoma, cervical cancer and colorectal cancer .

HY-179413

Polθ-IN-9	DNA/RNA Synthesis	Cancer
Polθ-IN-9 is an orally active Polθ polymerase inhibitor (IC₅₀ = 9.6 nM, K_d = 47.5 nM). Polθ-IN-9 shows remarkable selectivity with no inhibitory activity against other human DNA polymerases, including Pol α, Pol ε, Pol γ, Pol λ, and Pol μ. Polθ-IN-9 exhibits strong antiproliferative activity in DLD1 BRCA2 KO cells (IC₅₀ = 2.9 μM), and high sensitivity to MDA-MB-436 cells (IC₅₀ = 4.9 μM). Polθ-IN-9 increases DNA damage accumulation, induces γH2AX levels, and inhibits tumor growth in combination with Olaparib (HY-10162), in the MDA-MB-436 xenograft model. Polθ-IN-9 can be used for the research of homologous recombination (HR)-deficient cancers such as breast cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure