rad51

RAD51 Inhibitor B02 (B02) (B02) is an inhibitor of human RAD51 with an IC50 of 27.4 μM.

Rad51-in-1 is a derivative of B02 and an effective inhibitor of Rad51.

IBR2 (Isoquinoline) is a potent and specific RAD51 inhibitor known for its ability to suppress RAD51-mediated DNA double-strand break repair. By interfering with RAD51 multimerization, accelerating proteasome-mediated RAD51 protein degradation, inhibiting cancer cell growth, and inducing apoptosis, IBR2 has proved to be an effective compound in these aspects.

Emzadirib (RAD51-IN-2) is a potent inhibitor of RAD51, showing potential anticancer activity and useful for studying DNA damage repair.

RI-1 (RAD51 inhibitor 1) is a RAD51 inhibitor (IC50: 5-30 μM).

Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.

RI-2 is an optimized RAD51 inhibitor with an IC50 of 44.17 μM in the standard DNA binding assay; specifically inhibits HR(Homologous recombination) repair in human cells.

Zelavespib HCl is a novel Hsp90 inhibitor, a novel purine-based analog, and a radiosensitizer that may be a promising agent for CIRT. Zelavespib HCl shows antitumor activity in many preclinical models of malignancy. Zelavespib HCl has an inhibitory effect on the protein expression levels of Rad51 and Ku70, which may be associated with the double chain break repair in the homologous recombination pathway and non-homologous end-joining pathway.

RS-1 is a RAD51 activator. RS-1 also increases CRISPR/Cas9-mediated knock-in efficiencies.

Bractoppin is a drug-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem (t)BRCT domain (IC50 = 0.074 μM), which selectively inhibits substrate binding with nanomolar potency in vitro. Structure-activity exploration suggests that Bractoppin engages BRCA1 tBRCT residues recognizing pSer in the consensus motif, pSer-Pro-Thr-Phe, plus an abutting hydrophobic pocket that is distinct in structurally related BRCT domains, conferring selectivity.

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.

RAD51-IN-9 (Compound 3a) is an inhibitor of RAD51, specifically blocking its binding to ssDNA, with an IC50 of 17.85 μM. The compound has an LD50 of 40.21 μM in HEK293 cells and can sensitize cells to mitomycin C.

BRCA2-RAD51-IN-2 (compound S-35d) is a BRCA2-RAD51 inhibitor that, when combined with 10 µM Olaparib, can inhibit homologous recombination repair.

BRCA2-RAD51-IN-3 is an inhibitor of the RAD51-BRCA2 protein interaction, exhibiting an EC50 of 29.35 μM and a Kd of 75.14 μM. It disrupts the binding of RAD51 to BRCA2, impairing homologous recombination in cancer cells and inducing synthetic lethality. BRCA2-RAD51-IN-3 is effective against human pancreatic cancer cells, with no activity in normal pancreatic cells, and is applicable in pancreatic cancer research.

RAD51-IN-3, a Rad51 inhibitor, is chemically identified as (8aR,9R)-11'-chloro-6',8'-dihydroxy-2H,2'H-[3,8'-bi-1H-benzo[f]indene]-1,3,5',7'(4H,6H)-tetraone.

RAD51-IN-8, a new RAD51 binder, is a RAD51-BRCA2 inhibitor that disrupts the RAD51 BRCA2 protein-protein interaction in the micromolar range. This protein-protein interaction (PPI) inhibitor also demonstrates inhibitory activity for H4A4 with an EC50 value of 19 μM [1].

RAD51-IN-7 is a potent inhibitor of RAD51, a eukaryotic gene, with demonstrated research potential for mitochondrial deficiency disorders.

RAD51-IN-6 is a potent inhibitor of RAD51 (a eukaryotic gene) and has demonstrated potential for the study of mitochondrial deficiency disorders.

RAD51-IN-5, a potent inhibitor of RAD51, exhibits potential for studying mitochondrial deficiency disorders.

RAD51-IN-4 is a potent RAD51 inhibitor targeting a eukaryote gene critical for research on conditions associated with mitochondrial defects.

BRCA2-RAD51-IN-1, also known as Compound 46, is an inhibitor of BRCA2-RAD51 with an EC50 value of 28 μM, showcasing antitumor properties [1].

CAY10760 is a novel RAD51-BRCA2 protein–protein interaction inhibitor (EC₅₀ = 19 μM) that interferes with the homologous recombination process.

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. D-I03 inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation, with IC₅₀ values of 5 µM and 8 µM, respectively. D-I03 exerts significant growth inhibition on BRCA1/2-deficient cancer cells but has no effect on RAD51. D-I03 can be used in combination therapy studies for tumors with DNA damage repair defects.

CAM 833 is an effective orthosteric inhibitor of the BRCA2-RAD51 interaction, inhibiting RAD51 aggregation, enhancing DNA damage-induced apoptosis, increasing 4N cell cycle arrest, and disrupting homologous DNA repair (HDR), and can be used for cancer therapy.