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Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombinationrepair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research .
TDRL-551 is a potent replication protein A (RPA) inhibitor (IC50=18 µM). TDRL-551 inhibits RPA-DNA interaction and increases the efficacy of Platinum (Pt)-based chemotherapy in lung and ovarian cancer. RPA plays essential roles in both nucleotide excision repair (NER) and homologous recombination (HR), along with its role in DNA replication and DNA damage checkpoint activation .
AZ3391 is a potent inhibitor of PARP. AZ3391 is a quinoxaline derivative. PARP family of enzymes play an important role in a number of cellular processes, such as replication, recombination, chromatin remodeling, and DNA damage repair. AZ3391 has the potential for the research of diseases and conditions occurring in tissues in the central nervous system, such as the brain and spinal cord (extracted from patent WO2021260092A1, compound 23) .
AOH1160 is a potent oral small molecule proliferating cell nuclear antigen (PCNA) inhibitor that interferes with DNA replication, blocks homologous recombination-mediated DNA repair, leads to cell cycle arrest and induces apoptosis .
PFM01, N-alkylated Mirin derivative, is a MRE11 endonuclease inhibitor. PFM01 can regulate double-strand break repair (DSBR) by nonhomologous end-joining (NHEJ) versus homologous recombination (HR) .
KWWCRW is a Holliday linker inhibitory peptide with anticancer activity. KWWCRW inhibits homologous recombinationrepair (HDR) during DNA repair by binding to the reactive Holliday linker intermediate and preventing its degradation, and inhibits site-specific recombination by bacteriophage in vitro .
BRCA2-RAD51-IN-2 (compound S-35d) is a BRCA2-RAD51 inhibitor and inhibits homologous recombinationrepair in combination with 10 µM olaparib (HY-10162) .
ATR-IN-8 is a potent inhibitor of ATR. ATR is a key enzyme in the homologous recombinationrepair pathway and belongs to the PIKK family. ATR-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021143821A1, compound 3) .
NHEJ inhibitor-1 (Compound C2) is a trifunctional Pt(II) complex, alleviates the non-homologous end connection (NHEJ)/homologous recombination (HR)-related double strand breaks (DSBs) repairs to evade Cisplatin-resistance in non-small cell lung cancer (NSCLC). NHEJ inhibitor-1 inhibits the damage repair proteins Ku70 and Rad51 to make tumors re-sensitive to Cisplatin. NHEJ inhibitor-1 also induces ROS generation and MMP deduction .
PARP-1/Proteasome-IN-1 (compound 42i) is a dual PARP-1 and proteasome inhibitor with significant inhibitory effects on breast cancer. PARP-1/Proteasome-IN-1 can downregulate the expression of BRCA1 and RAD51 to inhibit homologous recombinationrepair function and induce apoptosis .
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) .
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 .
NSC15520 is a small molecular inhibitor of Replication Protein A (RPA). NSC15520 specifically recognizes the RPA N-terminal DNA binding domain (DBD), and blocks the interaction of RPA with p53 or RAD9. NSC15520 also inhibtis helix destabilization of a duplex DNA (dsDNA) oligonucleotide, involves in DNA replication, DNA repair, DNA recombination, and DNA damage response signaling .
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 .
TNG348 is an orally available allosteric inhibitor of the ubiquitin-specific protease USP1. TNG348 specifically and efficiently inhibits the activity of USP1, inhibiting its deubiquitination of proliferative PCNA and FANCD2, thereby disrupting the DNA repair process. TNG348 has inhibitory activity against breast and ovarian cancers carrying BRCA1/2 mutations and other homologous recombination defects (HRD) .
D-G23 is a selective RAD52 inhibitor. D-G23 disrupts RAD52-mediated DNA repair pathways and suppresses the growth of BRCA1- and BRCA2-deficient cancer cells. D-G23 is promising for research of homologous recombination-related cancers, such as hereditary breast cancer and ovarian cancer caused by BRCA1/2 mutations .
BER-IN-1 is a base excision repair (BER) inhibtor, targeting DNA abasic sites. BER-IN-1 cleaves abasic sites via β- and β,δ-elimination mechanisms, disrupts the base excision repair (BER) pathway and leads to DNA double-strand breaks (DSBs). BER-IN-1 can enhance the effectiveness of the PARP inhibitor Olaparib (HY-10162) in homologous recombination (HR)-proficient cancer cells (MDA-MB-231, HeLa, and SKOV3). BER-IN-1 induces an S-phase arrest and apoptosis companied with Olaparib. BER-IN-1 can be used for the research of cancer, such as breast, cervical and ovarian cancer .
Anti-BRCA1 Antibody (BR64) is a kind of mouse IgG1 κ chimeric antibody, targeting to human BRCA1. Anti-BRCA1 Antibody (BR64) reacts with BRCA1 (Breast cancer susceptibility gene 1) involved in tumor suppression, transcription, genomic stability, DNA repair and recombination. Anti-BRCA1 Antibody (BR64) can be used for the detections of immunofluorescence, western blot, and immunoprecipitation in cancer, such as breast and ovarian cancer .
CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 with a Kd of 366 nM against the ChimRAD51 protein. CAM833 also inhibits RAD51 oligomerization. CAM833 increases the progression of G2/M-arrested cells into apoptosis .
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 recombinationrepair (HR)-deficient cells, thereby inducing apoptosis. Simmiparib exhibits remarkable anticancer activities in cells and nude mice bearing xenografts .
RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM), stabilizes the interaction between RECQL5-RAD51 proteins, causes RAD51 aggregation and homologous recombinationrepair (HRR) inhibition, thereby exhibiting selective cytotoxicity in RECQL5-expressing cancer cells .
A 62176 hydrochloride is a compound that targets DNA topoisomerase II and has the activity of inhibiting purine synthesis in cancer cells. A 62176 hydrochloride interferes with c-MYC mRNA expression by interacting with G-quadruplex. The main mechanism of action of A 62176 hydrochloride is by displacing nucleosomes from the quadruplex of non-template strand rDNA, resulting in rapid redistribution of nucleosomes. The application potential of A 62176 hydrochloride is that it causes DNA damage and relies on BRCA1/2-mediated homologous recombination and DNA-PK-mediated non-homologous end-joining pathways to repair the damage .
AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs. AZD-9574 is an anti-cancer agent and can be used for HRD +?breast cancer and advanced solid malignancies research .
P62-RNF168 agonist-1 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. P62-RNF168 agonist-1 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. P62-RNF168 agonist-1 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner .
BLM-IN-2 is a Bloom's Syndrome Protein (BLM) inhibitor with an IC50 value of 0.8 μM. BLM-IN-2 effectively suppresses the proliferation, invasion, cell cycle arrest and apoptosis of CRC cells. BLM-IN-2 can be used for the reserarch of colorectal cancer (CRC) .
KWWCRW is a Holliday linker inhibitory peptide with anticancer activity. KWWCRW inhibits homologous recombinationrepair (HDR) during DNA repair by binding to the reactive Holliday linker intermediate and preventing its degradation, and inhibits site-specific recombination by bacteriophage in vitro .
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 .
Anti-BRCA1 Antibody (BR64) is a kind of mouse IgG1 κ chimeric antibody, targeting to human BRCA1. Anti-BRCA1 Antibody (BR64) reacts with BRCA1 (Breast cancer susceptibility gene 1) involved in tumor suppression, transcription, genomic stability, DNA repair and recombination. Anti-BRCA1 Antibody (BR64) can be used for the detections of immunofluorescence, western blot, and immunoprecipitation in cancer, such as breast and ovarian 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 .
The MRE11A protein is an important component of the DNA double-strand break repair mechanism and participates in the homologous recombination (HR) pathway. It interacts with RAD50 and NBS1 to form the MRN complex, which is essential for sensing and repairing DNA damage. MRE11A Protein, Human (His, GST) is the recombinant human-derived MRE11A protein, expressed by E. coli , with N-6*His, N-GST labeled tag.
RecO protein, a crucial participant in DNA repair and the RecF pathway, operates as a monomer, contributing to the intricate choreography of DNA repair mechanisms and facilitating recombination. Its monomeric form underscores its singular involvement, highlighting its significance in orchestrating cellular responses to DNA damage and recombination. RecO Protein, E.coli (His-SUMO) is the recombinant E. coli-derived RecO protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag.
BRCA1/BRCA2 containing complex, subunit 5; BRCC 5; BRCC5; DNA repair protein RAD51 homolog 1; DNA repair protein rhp51; HRAD51; HsRad51; HsT16930; MRMV2; Rad 51; RAD51; RAD51 homolog; RecA homolog, E. coli; S. cerevisiae; RAD51 homolog A; RAD51 homolog; RAD51 recombinase; RAD51, S. cerevisiae, homolog of; RAD51_HUMAN; RAD51A; RECA; RecA like protein; RecA, E. coli, homolog of; recombination protein A.
WB
Human, Mouse, Rat, Monkey
Rad51 Antibody (YA5219) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to Rad51.
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