rad51

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

PU-H71 HCl (Zelavespib HCl) is a novel Hsp90 inhibitor, a novel purine-based analog, and a radiosensitizer that may be a promising agent for CIRT. PU-H71 HCL shows antitumor activity in many preclinical models of malignancy. PU-H71 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.

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].

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].

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

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

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.

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

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

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

D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. It specifically inhibits RAD52-dependent single-chain annealing (SSA) and D-loop formation, with IC50 values of 5 µM and 8 µM, respectively. D-I03 also inhibits the growth of BRCA1 and BRCA2 deficient cells and prevents the formation of damage-induced RAD52 foci, but does not affect RAD51 foci induced by Cisplatin.

CAM 833 is an effective positivity inhibitor, which can inhibit the interaction between BRCA2 and RAD51. The Kd of ChimRAD51 protein is 366 nM. CAM 833 inhibited the oligocoagulation of RAD51 and promoted the process of apoptosis in G2 M cells.

DIDS, an anion exchange inhibitor, acts by blocking reversibly and later irreversibly, exchangers such as chloride-bicarbonate exchanger. It is also a RAD51 inhibitor.

BRC4wt, an acetylated peptide originating from the BRC4 repeat within human BRCA2 (1521-1536), acts as an inhibitor of the BRCA2 and RAD51 protein-protein interaction. When linked to the cationic cell-penetrating peptide (Arg)9, it effectively shortens DNA replication tract lengths and diminishes the frequency of homologous repair of camptothecin-induced DNA damage in vitro. Additionally, BRC4wt enhances the efficacy of the poly(ADP-ribose) polymerase (PARP) inhibitor olaparib in inducing cell death in HeLa human cervical cancer and U2OS human osteosarcoma cells, albeit it does not affect non-cancerous hTERT RPE-1, MRC-5, or MCF-10A cells.

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].

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.

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

Phosphoramide mustard cyclohexanamine is the active metabolite of cyclophosphamide, an alkylating agent that cross-links DNA strands, organizes cell division and causes cell death, and has antitumor activity.

Halenaquinone is a phosphatidylinositol 3-kinase inhibitor. Halenaquinone specifically inhibits the secondary DNA binding of RAD51. Halenaquinone inhibits RANKL-induced osteoclastogenesis. Halenaquinone induces apoptosis in PC12 cells.

PARP1 BRD4-IN-3 (compound HF4) is an effective inhibitor of BRD4 and PARP1, with IC50 values of 1210 nM and 2019 nM respectively. The compound exhibits antiproliferative activity, induces apoptosis (apoptosis) and cell cycle arrest at the G0 G1 phase. Additionally, PARP1 BRD4-IN-3 causes DNA damage and reduces the expression of the Rad51 protein, demonstrating anti-tumor activity.

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

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.