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Pathways Recommended: Cell Cycle/DNA Damage
Results for "

double-strand DNA breaks

" in MedChemExpress (MCE) Product Catalog:

54

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2

Biochemical Assay Reagents

2

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6

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1

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1

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-110111
    T2AA
    1 Publications Verification

    		 DNA/RNA Synthesis Cancer
    T2AA is a monoubiquitinated proliferating cell nuclear antigen (PCNA) inhibitor that prevents DNA repair, increases double-strand break (DSB) formation and promotes necroptosis and cell cycle arrest in G1 phase .
    T2AA
  • HY-115531
    UNC-2170

    		DNA/RNA Synthesis Cancer
    UNC-2170 is a functionally active, fragment-like ligand for 53BP1 (IC50=29 µM; Kd=22 µM). UNC-2170 shows at least 17-fold selectivity for 53BP1 as compared to nine other methyl-lysine (Kme) reader proteins. 53BP1 is a Kme binding protein that plays a central role in DNA Damage Repair (DDR) pathways and is recruited to sites of double-strand breaks (DSB) .
    UNC-2170
  • HY-15620
    Methylproamine
    1 Publications Verification

    		 DNA/RNA Synthesis Others
    Methylproamine is a DNA-binding radioprotector, acts by repair of transient radiation-induced oxidative species on DNA. Methylproamine also protects against ionizing radiation by preventing DNA double-strand breaks .
    Methylproamine
  • HY-148078
    PFM03
    1 Publications Verification

    		 Endonuclease Others
    PFM03 is a MRE11 Endonuclease inhibitor. PFM03 regulates DNA double-strand break repair (DSBR) by nonhomologous end-joining (NHEJ) .
    PFM03
  • HY-160424
    DEANO sodium

    Diethylamine NONOate sodium; Diethylamine nitric oxide sodium

    		 Reactive Oxygen Species (ROS) Xanthine Oxidase Others
    DEANO sodium is notric oxide donor. DEANO sodium potentiates the abilitv of hypoxanthine/xanthine oxidase to induce lipid peroxidation as well as DNA single- and double-strand breaks .
    DEANO sodium
  • HY-19609
    Calicheamicin
    5+ Cited Publications

    Calicheamicin γ1

    		 DNA Alkylator/Crosslinker ADC Cytotoxin Bacterial Apoptosis Antibiotic Infection Cancer
    Calicheamicin, an antitumor antibiotic, is a cytotoxic agent that causes double-strand DNA breaks. Calicheamicin is a DNA synthesis inhibitor . Calicheamicin is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Calicheamicin
  • HY-172970
    HQY1428

    		CDK DNA/RNA Synthesis Apoptosis Cancer
    HQY1428 is an orally active CDK12 inhibitor. HQY1428 inhibits DNA replication, causes G2/M arrest in SKOV3 cells, induces DNA double-strand breaks and apoptosis. HQY1428 has anti-tumor activity in the SKOV3 xenograft mouse model. HQY1428 combined with the HER2 inhibitor Lapatinib (HY-50898) in the NCI-N87 xenograft mouse model produces a synergistic therapeutic effect .
    HQY1428
  • HY-D1023
    5-BrdUTP sodium salt

    5-Bromo-2'-deoxyuridine 5'-triphosphate sodium salt

    		 DNA/RNA Synthesis Others
    5-BrdUTP sodium salt is a TdT substrate which can be used to label the DNA double-strand breaks.
    5-BrdUTP sodium salt
  • HY-146095
    p53 Activator 2

    		MDM-2/p53 DNA/RNA Synthesis Apoptosis Cancer
    p53 Activator 2 (compound 10ah) intercalats into DNA and results in significant DNA double-strand break.p53 Activator 2 increases the expression of p53, p-p53, CDK4, p21 to cause cell cycle arrest at G2/M phase.p53 Activator 2 induce apoptosis and significantly down-regulates the anti-apoptosis proteins Bcl-2, Bcl-xL and the levels of cyclin B1.p53 Activator 2 has anti-proliferation activity against MGC-803 cells, with an IC50 of 1.73 µM. p53 Activator 2 displays potent anticancer efficiency against MGC-803 xenograft tumors models .
    p53 Activator 2
  • HY-173458
    NBTIs-IN-7

    		Topoisomerase Infection
    NBTIs-IN-7 (compound 276) is a novel bacterial topoisomerase (NBTIs) inhibitor. NBTIs-IN-7 induces both single- and double-strand DNA strand breaks in the presence of gyrase .
    NBTIs-IN-7
  • HY-13703
    Nimustine

    		Apoptosis DNA Alkylator/Crosslinker DNA/RNA Synthesis p38 MAPK JNK AP-1 Cancer
    Nimustine is an alkylating agent, which induces DNA double-strand breaks (DSBs) and inter-strand crosslinks (ICLs), thereby activating the DNA damage response (DDR) signaling pathway. Nimustine activates p38 MAPK/JNK signaling pathway, and exhibits antitumor activity .
    Nimustine
  • HY-18626
    NK 314

    		Topoisomerase Cancer
    NK 314 is an inhibitor for topoisomerase IIα, which generates the break of DNA double-strand. NK 314 arrests the cell cycle at G2 phase in human acute myeloid leukemia cells, inhibits the proliferation of CEM with IC90 of 55 nM .
    NK 314
  • HY-163942
    GSK_WRN4

    		DNA/RNA Synthesis Cancer
    GSK_WRN4 is a WRN helicase inhibitor (pIC50=7.6) with anticancer activity. GSK_WRN4 selectively inhibits the growth of MSI tumor cells in vitro and in vivo by inducing DNA double-strand breaks, particularly at expanded TA repeats and DNA damage regions .
    GSK_WRN4
  • HY-149348
    DiPT-4

    		Topoisomerase PARP Apoptosis Cancer
    DiPT-4 is a dual TOP1/PARP1 inhibitor that induces massive DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells. DiPT-4 has the potential to overcome cancer drug resistance .
    DiPT-4
  • HY-13703A
    Nimustine hydrochloride
    1 Publications Verification

    ACNU

    		 DNA Alkylator/Crosslinker DNA/RNA Synthesis Apoptosis p38 MAPK JNK AP-1 Cancer
    Nimustine hydrochloride (ACNU) is the hydrochloride salt form of Nimustine (HY-13703). Nimustine hydrochloride is an alkylating agent, which induces DNA double-strand breaks (DSBs) and inter-strand crosslinks (ICLs), thereby activating the DNA damage response (DDR) signaling pathway. Nimustine hydrochloride activates p38 MAPK/JNK signaling pathway, and exhibits antitumor activity .
    Nimustine hydrochloride
  • HY-163918
    N,N-Dimethyl-idarubicin

    		P-glycoprotein Cancer
    N,N-Dimethyl-idarubicin, an Idarubicin (HY-17381) derivative, is a potent histone evictor which does not induce DNA double-strand breaks. N,N-Dimethyl-idarubicin, an anthracycline, is an effective cytotoxic agent for ABCB1-overexpressing, Doxorubicin-resistant cells .
    N,N-Dimethyl-idarubicin
  • HY-126490
    Phleomycin
    1 Publications Verification

    		 Bacterial Antibiotic DNA/RNA Synthesis Infection Cancer
    Phleomycin is a copper-dependent DNA damaging agent and antibiotic with antitumor activity. Phleomycin binds to DNA and produces ROS in the presence of reducing agents (such as dithiothreitol and glutathione), inducing single-strand and double-strand breaks in DNA. Phleomycin can induce cell apoptosis or mutation and is widely used in cancer inhibition, microbial genetic transformation (as a screening marker to improve fungal transformation efficiency) and DNA repair mechanism research .
    Phleomycin
  • HY-114923
    SU-11752

    		DNA-PK PI3K Cancer
    SU-11752 is an inhibitor for DNA-dependent protein kinase (DNA-PK) with an IC50 of 0.13 μM. SU-11752 inhibits PI3K p110γ kinase with IC50 of 1.1 μM. SU-11752 binds competitively for ATP-site in DNA-PK, results in inhibition of intracellular DNA double-strand break repair and increases the sensitivity of cells to radiotherapy .
    SU-11752
  • HY-111183
    Neocarzinostatin
    1 Publications Verification

    Zinostatin; Vinostatin

    		 DNA/RNA Synthesis Bacterial Apoptosis Antibiotic Infection Cancer
    Neocarzinostatin, a potent DNA-damaging, anti-tumor antibiotic, recognizes double-stranded DNA bulge and induces DNA double strand breaks (DSBs). Neocarzinostatin induces apoptosis. Neocarzinostatin has potential for EpCAM-positive cancers treatment .
    Neocarzinostatin
  • HY-103710
    IBR2
    3 Publications Verification

    		 RAD51 Apoptosis Cancer
    IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis .
    IBR2
  • HY-161970
    XSJ05

    		Topoisomerase Apoptosis Cancer
    XSJ05 is a camptothecin (CPT) derivative that can inhibit topoisomerase I (Topo I) to exert anti-cancer activity. XSJ05 can trigger DNA double-strand breaks, leading to DNA damage. XSJ05 can inhibit the growth of colorectal cancer (CRC), arrest the cell cycle in G2/M phase, and induce apoptosis .
    XSJ05
  • HY-170907
    HDAC-IN-85

    		HDAC DNA/RNA Synthesis RAD51 Cancer
    HDAC-IN-85 (Compound 1) is a BBB-permeable HDAC inhibitor. HDAC-IN-85 has an inhibitory effect on brain tumor cell lines. HDAC-IN-85 can induce acetylation, leading to DNA double-strand breaks, and induce the ubiquitination of RAD51, disrupting the DNA repair process. HDAC-IN-85 can be used in the research of glioblastoma .
    HDAC-IN-85
  • HY-13767
    Tirapazamine
    10+ Cited Publications

    SR259075; SR4233; Win59075; SML 0552; SR 259075; Tirazone

    		 DNA/RNA Synthesis Cancer
    Tirapazamine (SR259075) is an anticancer agent that shows selective cytotoxicity for hypoxic cells in solid tumors, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death. Tirapazamine is an anticancer and bioreductive agent.Tirapazamine (SR259075) can enhance the cytotoxic effects of ionizing radiation in hypoxic cells .
    Tirapazamine
  • HY-121862
    CM03

    		DNA/RNA Synthesis Cancer
    CM03 is a potent DNA G-quadruplexes (G4s) ligand. CM03 can stabilise G4s, downregulating more G4-containing genes as well as increasing incidence of double-strand break events (DSBs) due to torsional strain on DNA and chromatin structure. CM03 has selective potency for pancreatic cancer cells .
    CM03
  • HY-174151
    XSJ110

    		Topoisomerase Apoptosis Cancer
    XSJ110 is a potent irreversible topoisomerase I (Topo I) inhibitor with an IC50 value of 0.133 μM. XSJ110 blocks DNA topoisomerization, induces DNA double-strand breaks, and triggers cell cycle arrest at G0/G1 phase, inducing tumor cell apoptosis. XSJ110 is promising for research of ampullary carcinoma (AC) .
    XSJ110
  • HY-113064
    Selenocystine
    1 Publications Verification

    		 Endogenous Metabolite Cancer
    Selenocystine is a broad-spectrum anti-cancer agent. Selenocystine induces DNA damage in HepG2 cells, particularly in the form of DNA double strand breaks (DSBs). Selenocystine exhibits great promise as a therapeutic or adjuvant agent targeting DNA repair for cancer treatment .
    Selenocystine
  • HY-100707
    IC 86621

    		DNA-PK Apoptosis Inflammation/Immunology Cancer
    IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis .
    IC 86621
  • HY-123232
    KU-0058684

    		PARP Cancer
    KU-0058684 is a potent PARP inhibitor, with an IC50 of 3.2 nM for PARP-1. KU-0058684 significantly reduces DNA double strand break (DSB) repair .
    KU-0058684
  • 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 .
    VX-984
  • HY-164279
    YTR107

    		DNA/RNA Synthesis Cancer
    YTR107 is a radiation sensitizer. YTR107 binds to nucleophosmin1 (NPM1) and inhibits pentamer formation. YTR107 inhibits recruitment of nucleophosmin to sites of DNA damage, suppresses repair of DNA double strand breaks, and enhances radiosensitization .
    YTR107
  • HY-101570
    Nedisertib
    Maximum Cited Publications
    20 Publications Verification

    Peposertib; M3814

    		 DNA-PK BCRP Cancer
    Nedisertib (Peposertib) is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of less than 3 nM. Nedisertib also acts as a modulator of ABCG2, capable of reversing ABCG2-mediated multidrug resistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity .
    Nedisertib
  • HY-W018326
    Temozolomide acid

    		DNA/RNA Synthesis Cancer
    Temozolomide acid is a carboxylic acid derivative of Temozolomide (HY-17364) with anticancer activity. Temozolomide is a DNA alkylating agent, methylating the guanine and adenine bases of DNA, causing breaks in DNA double strand, cell cycle arrest, and eventually cell death. Temozolomide acid is promising for research of glioblastoma and brain cancer .
    Temozolomide acid
  • HY-103688
    N-Ac-γ-Calicheamicin-AcBut-NHS ester

    		ADC Cytotoxin Cancer
    AcBut-N-Ac-γ-Calicheamicin is an ADC cytotoxic payload that induces cell cycle arrest and apoptosis by causing DNA double-strand breaks. AcBut-N-Ac-γ-Calicheamicin is primarily used in the synthesis of antibody-drug conjugates (ADC) and holds promise for research in the field of cancer, including acute lymphoblastic leukemia (ALL) and other hematological malignancies .
    N-Ac-γ-Calicheamicin-AcBut-NHS ester
  • HY-162568
    7-tert-Butylfascaplysin

    		DNA Stain Cancer
    7-tert-Butylfascaplysin (7-TB) is a derivative of Fascaplysin (HY-112328), that can be isolated from Fascaplysinopsis sp.. 7-tert-Butylfascaplysin induces replication stress, leads to toxic DNA double-strand breaks and apoptosis-like cell death, and thus exhibits cytotoxicity in cancer cells in nanomolar levels. 7-tert-Butylfascaplysin exhibits DNA intercalating activity with EC50 of 3.2 μM .
    7-tert-Butylfascaplysin
  • HY-Q04764
    TI17

    		Thyroid Hormone Receptor Apoptosis Cancer
    TI17 is an inhibitor of the thyroid hormone receptor-interacting protein Trip13 and has anticancer activity. TI17 effectively inhibits multiple myeloma (MM) cell proliferation and induces cell cycle arrest and apoptosis. Trip13 is an AAA-ATPase that mediates double-strand break (DSB) repair; TI17 inhibits Trip13 function and increases DNA damage .
    TI17
  • HY-164062
    LZCap AG(3'Acm) Cas9 mRNA

    		Biochemical Assay Reagents Others
    The Cas9 protein, guided by sgRNA, induces DNA double-strand breaks (DSBs) at specific genomic locations, activating the cell's endogenous DNA repair mechanisms, non-homologous end joining (NHEJ), or homology-directed repair (HDR), for repairing the targeted DSBs, enabling genome DNA target recognition and cleavage. LZCap AG(3'Acm) Cas9 mRNA can be used together with purified sgRNA, where the expressed Cas9 protein acts in conjunction with sgRNA to perform cleavage.
    LZCap AG(3'Acm) Cas9 mRNA
  • HY-103710A
    (R)-IBR2

    		RAD51 Cancer
    (R)-IBR2 is the isomer of IBR2 (HY-103710). IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis .
    (R)-IBR2
  • 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 .
    Tilatamig samrotecan
  • HY-176481
    ML-20

    		Autophagy Apoptosis Cancer
    ML-20, Malabaricone C (HY-N8518) analogue, is a autophagy inhibitor and radiosensitizer. ML-20 inhibits cell growth, induces cell apoptosis . ML-20 induces DNA double-strand breaks, loss of mitochondrial membrane potential (MMP), and lysosomal membrane permeabilization (LMP). ML-20 induces endoplasmic reticulum stress and concurrent inhibition of autophagy flux due to LMP .
    ML-20
  • HY-10180A
    MLN8054 sodium

    		Aurora Kinase Cancer
    MLN8054 sodium is an Aurora A inhibitor with radiosensitivity-enhancing activity. MLN8054 sodium can activate the DNA double-strand break reaction of prostate cancer cells in in vitro experiments. The application of MLN8054 sodium is closely related to accumulation in the G2/M phase of the cell cycle and polyploid formation. In vivo experiments show that MLN8054 sodium can significantly delay the growth of prostate cancer tumors and promote tumor cell apoptosis when used in combination with radiotherapy .
    MLN8054 sodium
  • HY-174143
    EXO1-IN-1

    		Others Cancer
    EXO1-IN-1 (Compound F684) is a potent and selective inhibitor of exonuclease 1 (EXO1) (IC50= 15.7 μM). EXO1-IN-1 suppresses DNA end resection, promotes the accumulation of DNA double-strand breaks, and triggers S-phase PARylation, disrupts DNA repair pathways in homologous recombination-deficient (HRD) cancer cells, and selectively kills tumor cells with defects in HR genes like BRCA1/2. EXO1-IN-1 is promising for research of homologous recombination-deficient cancer (such as BRCA-related tumors) .
    EXO1-IN-1
  • HY-N4327
    Eurycomalactone

    		NF-κB Apoptosis Akt Bcl-2 Family Infection Inflammation/Immunology
    Eurycomalactone is an active quassinoid could be isolated from Eurycoma longifolia Jack. Eurycomalactone is a potent NF-κB inhibitor with an IC50 value of 0.5 μM. Eurycomalactone inhibits protein synthesis and depletes cyclin D1. Eurycomalactone enhances radiosensitivity through arrest cell cycle at G2/M phase and delayed DNA double-strand break repair. Eurycomalactone inhibits the activation of AKT/NF-κB signaling, induces apoptosis and enhances chemosensitivity to Cisplatin (HY-17394) .
    Eurycomalactone
  • HY-115552
    Simmiparib

    		PARP Cancer
    Simmiparib is a highly potent and orally active PARP1 and PARP2 inhibitor with IC50 values of 1.75 nM and 0.22 nM, respectively. Simmiparib has more potent PARP1/2 inhibition than its parent Olaparib (HY-10162). Simmiparib induces DNA double-strand breaks (DSB) accumulation and G2/M arrest in homologous recombination repair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts .
    Simmiparib
  • HY-155246
    PARP1-IN-15

    		Apoptosis PARP Cancer
    PARP1-IN-15 (Compound 6) is a PARP1 inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations .
    PARP1-IN-15
  • HY-118897
    UNC-2170 maleate

    		DNA/RNA Synthesis Cancer
    UNC-2170 maleate is the maleate salt form of UNC-2170 (HY-115531). UNC-2170 maleate is a selective inhibitor for the methyl-lysine binding protein 53BP1, with IC50 of 29 µM and Kd of 22 µM. UNC-2170 maleate shows at least 17-fold selectivity for 53BP1 as compared to nine other methyl-lysine (Kme) reader proteins. 53BP1 is a Kme binding protein that plays a central role in DNA Damage Repair (DDR) pathways and is recruited to sites of double-strand breaks (DSB) .
    UNC-2170 maleate
  • HY-126972
    RI(dl)-2

    		RAD51 Cancer
    RI(dl)-2 blocks RAD51’s D-loop activity in biochemical systems with an IC50 value of 11.1 µM and inhibits homologous recombination (HR) activity with an IC50 value of 3.0 µM. RI(dl)-2 inhibits HR-mediated repair of DNA double strand breaks and sensitizes different cancer cell lines .
    RI(dl)-2
  • HY-172771
    Multi-target kinase inhibitor 4

    		PI3K DNA-PK P-glycoprotein Cancer
    Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and potent chemosensitizer that can increase the amount of DNA double strand breaks induced by Doxorubicin (HY-15142A). Multi-target kinase inhibitor 4, is an efficient inhibitor of multidrug resistance (MDR) that exhibits inhibitory activity toward P-glycoprotein-mediated drug efflux. Multi-target kinase inhibitor 4 can be loaded into PEG-coated LNPs .
    Multi-target kinase inhibitor 4
  • HY-176165
    CDK9/EZH2-IN-1

    		CDK Histone Methyltransferase Cancer
    CDK9/EZH2-IN-1 (Compound D16) is a CDK9/EZH2 dual-target inhibitor (IC50: 83.9/108.6 nM). CDK9/EZH2-IN-1 induces apoptosis and DNA double-strand breaks (DSBs). CDK9/EZH2-IN-1 inhibits the proliferation activity of MKN45, MDA-MB-453 and SW620 cancer cells (IC50 values are 136.3, 171.3 and 315.7 nM, respectively) .
    CDK9/EZH2-IN-1
  • HY-19959
    Mirin
    5 Publications Verification

    		 ATM/ATR Apoptosis Cancer
    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 .
    Mirin
  • 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 .
    PARP1-IN-12

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