nhej

NHEJ Inhibitor-1 (Compound C2), a trifunctional Pt(II) complex, mitigates non-homologous end joining (NHEJ) homologous recombination (HR)-related double strand break (DSB) repairs, combating Cisplatin resistance in non-small cell lung cancer (NSCLC). It achieves this by inhibiting the damage repair proteins Ku70 and Rad51, thus re-sensitizing tumors to Cisplatin. Additionally, this compound prompts the generation of reactive oxygen species (ROS) and reduces mitochondrial membrane potential (MMP) [1].

VX-984 (M9831) is an oral, selective DNA-PK inhibitor that can cross the blood-brain barrier. VX-984 inhibited the conjugation of non-homologous terminal NHEJ and acted on DSBs to break DNA double strand. VX-984 is commonly seen in glioblastoma (GBM) and non-small cell lung cancer (NSC-LC) studies.

NU7441 (KU-57788 (NU7441)) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM).

DMNB (6-Nitroveratraldehyde) is DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 of 15 μM, an enzyme involved in the non-homologous end-joining (NHEJ) pathway of double-stranded DNA break (DSB) repair in human cells.

PFM01 is an inhibitor of MRE11 endonuclease. PFM01 can regulate double-strand break repair (DSBR) by nonhomologous end-joining (NHEJ) versus homologous recombination (HR).

TMU 35435 is an inhibitor of histone deacetylases (HDAC). It enhances radiosensitivity by inducing the accumulation of misfolded proteins and autophagy (autophagy) in TNBC, and inhibits the NHEJ pathway through ubiquitination of the catalytic subunit of DNA-dependent protein kinase (DNA-PKcs).

SCR7, a specific DNA Ligase IV inhibitor, blocks nonhomologous end-joining (NHEJ).

NSC 617145 (NSC617145) is an inhibitor of WRN helicase that inhibits the ATPase, but not exonuclease, activity of WRN helicase in a concentration-dependent manner.

DDRI-18 is a novel small molecule inhibitor that regulates the DNA damage response with sensitizing and anticancer activities, inhibits non-homologous end-joining (NHEJ) DNA repair and enhances the cytotoxicity of anticancer DNA damage compounds.

YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays.

5-Hydroxy Lansoprazole Sulfide is an inhibitor of fatty acid synthase (FASN). FASN, which is responsible for de-novo synthesis of lipids, has been found to be overexpressed in cancerous tissue. 5-Hydroxy Lansoprazole Sulfide specifically inhibits enoyl reductase, and was found to more effectively inhibit FASN function than lansoprazole and was also more efficient at regulating NHEJ repair of oxidative DNA damage via PARP1.

SCR7 pyrazine (SCR7) enhances CRISPR-Cas9-mediated homology-directed repair (HDR) efficiency in vitro up to 19-fold. Inhibits nonhomologous end-joining (NHEJ).

SCR130 (1,7,9-Triazaspiro[4.5]dec-1-ene-6,10-dione, 2,4-bis(4-chlorophenyl)-8-thioxo-) is enzyme inhibition, antiproliferative effects and antifungal activity.