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

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].

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

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.

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.

Amuvatinib hydrochloride (MP470 hydrochloride) is an orally administered multi-targeted tyrosine kinase inhibitor effective against mutant forms of c-Kit, PDGFRα, Flt3, c-Met, and c-Ret, and it suppresses DNA repair by inhibiting the RAD51 protein, contributing to its antineoplastic activity[1][2][3][4].

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.

HDAC-IN-85 (Compound 1) is an HDAC inhibitor capable of crossing the blood-brain barrier. It exhibits inhibitory effects on brain tumor cell lines and can induce acetylation, resulting in DNA double-strand breaks and promoting RAD51 ubiquitination, which disrupts the DNA repair process. HDAC-IN-85 is applicable in studies of glioblastoma.

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

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.

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.

RI(dl)-2 TFA is a potent and selective inhibitor of RAD51-mediated D-loop formation, with an IC50 of 11.1 μM, and inhibits homologous recombination (HR) activity in human cells with an IC50 of 3.0 μM [1].