Endonuclease Inhibitor

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).

FEN1-IN-SC13 is a potent DNA fragmentation endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-SC13 interferes with DNA replication and repair in vitro and in cells.

NSC 45576 is a selective inhibitor of XendoU endoribonuclease and an inhibitor of CREB-CRE interaction, with an IC₅₀ value of 29 μM against Xenopus laevis XendoU. NSC 45576 binds to the active sites of XendoU and PP11, and inhibits CREB-CRE interaction. NSC 45576 can be used in cancer-related research such as breast cancer and gastric cancer.

MU262 is a MUS81 inhibitor with an IC₅₀ value of 0.87 μM. MU262 directly inhibits the catalytic activity of MUS81 without interfering with DNA binding, induces genomic instability in tumor cells, and specifically inhibits the HR/BIR repair pathway. The combination of MU262 with Cisplatin (HY-17394) significantly enhances the chemotherapeutic killing effect. MU262 serves as a chemical biology tool for studying MUS81 function, and also acts as a lead compound for the development of anticancer therapies that exploit DNA repair defects in cancer cells.

Deoxyribonuclease II (DNase II) is an endonuclease that hydrolyzes the phosphodiester bonds of deoxyribonucleotides in native and denatured DNA, producing 3' phosphate and 5'-hydroxyl termini. Deoxyribonuclease II works best at acidic pH and is commonly used in biochemical research.

PFM39, a Mirin analog, is a potent and selective MRE11 exonuclease inhibitor. PFM39 inhibits phosphate rotation for dsDNA exonuclease activity. PFM39 does not inhibit TmMre11 or human MRE11/MRN endonuclease activity.

MU147 is an MRE11 nuclease inhibitor and chemical probe with anticancer activity, which is lethal to Ehrlich ascites tumor cells both in vitro and in vivo. MU147 also eliminates the double-strand break repair mechanism dependent on the MRE11 nuclease activity without impairing the activation of ATM. MU147 also impairs the degradation of nascent strands of stalled replication FOX and selectively affects brca2-deficient cells.

PFM03 is a MRE11 Endonuclease inhibitor. PFM03 regulates DNA double-strand break repair (DSBR) by nonhomologous end-joining (NHEJ).

MUS81-IN-1 (compound 23) is a MUS81 inhibitor. MUS81-IN-1 can be used in cancer research.

PNR-3-80 is an endonuclease G (ENDOG) inhibitor with an IC₅₀ of 0.67 μM. As a non-competitive binder to the ENDOG-substrate complex, PNR-3-80 specifically inhibits the endonuclease activity of ENDOG. PNR-3-80 reduces cell death induced by Cisplatin (HY-17394) and Docetaxel (HY-B0011), and inhibits DNA damage and autophagy (autophagy) induced by Etoposide (HY-13629). PNR-3-80 can be used in studies related to cell injury.

PNR-3-82 is a highly selective inhibitor of endonuclease G (EndoG) with an IC₅₀ value of 0.61 μM against EndoG. As a non-competitive inhibitor, PNR-3-82 blocks EndoG-mediated DNA fragmentation. PNR-3-82 enhances the in vivo delivery efficiency of plasmid DNA and exhibits bioprotective effects against drug-related injuries and other cell/tissue damages. PNR-3-82 can be used in studies related to prostate cancer.

MU1409 is an inhibitor of MRE11 nuclease with an IC₅₀ of 12.1 μM. Additionally, MU1409 also inhibits FEN1 and EXO1, with IC₅₀ values of 24.2 and 176.4 μM, respectively. MU1409 affects DNA repair in cells, preventing the degradation of stalled replication forks in BRCA2-deficient cells, making it a promising candidate for research on BRCA2 mutation-induced cancers.

AV5116 is a cap-dependent endonuclease inhibitor (CENI) that binds to the active site of the cap-dependent endonuclease (CEN) located in the N-terminal domain of the polymerase acidic. AV5116 exhibits potent inhibitory activity against influenza viruses (influenza A, B, and C viruses). AV5116 can be used for the study of influenza virus infections.

Cusculine (FAC21) is an oropouche virus (OROV) endonuclease inhibitor with an IC₅₀ of 1.4 μM. Cusculine strongly interacts with OROV endonuclease, possibly limiting viral RNA interaction with other proteins, intercalates into double-stranded RNA (a viral replication intermediate), and efficiently inhibits OROV viral replication in vitro. Cusculine can be used for the research of oropouche fever.

AD16 (Acetamide) is a LINE-1 retrotransposon endonuclease inhibitor with the IC₅₀ of 4.7 μM. AD16 (Acetamide) reduce LINE-1 retrotransposition, L1-induced DNA damage, and inflammation reinforced by L1 in senescent cells.

MU876 (Compound 32) is a MUS81 inhibitor with an IC₅₀ of 0.5  μM. MU876 effectively inhibits MUS81-dependent homologous recombination (HR) and break-induced replication (BIR) pathways. MU876 sensitizes cancer cells to DNA-damaging agents, such as Cisplatin (HY-17394), through impairing their ability to repair DNA lesions. MU876 can be used for cancers chemotherapy research.

CGCG/CGG ligand 1 (compound 10), an anthracenone derivative, is a CGCG or CGG short spacer-ligand. CGCG/CGG ligand 1 can protect cleavable sites of DNA with the multiple CGCG or continuous CGG sites from the restriction enzyme.

Suraxavir marboxil (GP681; Cap-dependent endonuclease-IN-3) is a PA subunit cap-dependent endonuclease inhibitor with antiviral activity. Suraxavir marboxil inhibits PA subunit cap-dependent endonuclease activity and inhibits influenza A and/or influenza B viral replication. Suraxavir marboxil can be used alone or in combination with other anti-influenzal agents for the prevention of influenza A and/or influenza B viral infectious diseases. Suraxavir marboxil can be used for the research of influenza A and/or influenza B viral infectious diseases.

3'-O-Acetylthymidine, a purine nucleoside analog, is an inhibitor of ribonuclease A.

PAN endonuclease-IN-3 is a potent PAN endonuclease inhibitor that against influenza virus polymerase complexes with an IC₅₀ of 17.4 nM. PAN endonuclease-IN-3 demonstrates potent inhibitory activities against PAN endonuclease. PAN endonuclease-IN-3 demonstrates robust antiviral activities against multiple current and different influenza virus strains while showing minimal cytotoxicity in MDCK cells. PAN endonuclease-IN-3 significantly suppresses viral replication in an A/WSN/33 infected mouse model.