RAD51 Inhibitor

DIDS sodium salt (MDL101114ZA) is a dual inhibitor of ABCA1 and VDAC1. DIDS also inhibits RAD51, inhibiting RAD51-mediated homologous pairing and strand exchange reactions. DIDS inhibits anion exchange and binding to red blood cell membranes, inhibits the activation of caspase-3 and -9, and can be used in cancer research.

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

RI-1 is a RAD51 inhibitor, with IC₅₀s ranging from 5 to 30 μM. RI-1 binds covalently to the surface of RAD51 protein at cysteine 319. RI-1 inactivates RAD51 by directly binding to a protein surface that serves as an interface between protein subunits in RAD51 filaments. RI-1 can disrupt homologous recombination in human cells.

IBR2 is a potent and specific RAD51 inhibitor and inhibits RAD51-mediated DNA double-strand break repair. IBR2 disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, inhibits cancer cell growth and induces apoptosis.

PARP1/PRMT5-IN-1 is an inhibitor of PARP1 and PRMT5, with an IC₅₀ of 0.60 nM against PARP1 and an IC₅₀ of 4.67 nM against PRMT5. PARP1/PRMT5-IN-1 downregulates the homologous recombination (HR)-associated factors BRCA1, BRCA2, and RAD51, thereby suppressing homologous recombination function. PARP1/PRMT5-IN-1 induces the accumulation of DNA double-strand breaks. PARP1/PRMT5-IN-1 triggers apoptosis. PARP1/PRMT5-IN-1 is applicable for breast cancer research.

SeSA-HCPT is an orally active dual-target inhibitor integrating Topo I and HDAC inhibition. SeSA-HCPT induces potent DNA damage, apoptosis, S-phase arrest in prostate cancer cells. SeSA-HCPT inhibits cancer cells proliferation and migration. SeSA-HCPT impairs homologous recombination by suppressing KIF4A-RAD51 signaling. SeSA-HCPT markedly inhibits CRPC tumor growth with minimal systemic toxicity.

CAM833 is a potent orthosteric inhibitor of the interaction between BRCA2 and RAD51 with a K_d of 366 nM against the ChimRAD51 protein. CAM833 also inhibits RAD51 oligomerization. CAM833 increases the progression of G2/M-arrested cells into apoptosis.

Bractoppin is a potent and selective agent-like inhibitor of phosphopeptide recognition by the human BRCA1 tandem(t) BRCT domain (binding IC₅₀: 74 nM). Bractoppin diminishes BRCA1 recruitment to DNA breaks, in turn suppressing damage-induced G2 arrest and assembly of the recombinase, RAD51. Bractoppin preferentially inhibits BRCA1 tBRCT-dependent steps in the DNA damage response.

Emzadirib (RAD51-IN-2) is a RAD51 inhibitor extracted from patent WO2019/051465A1.

Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.

Solanidine is an orally active cholestane alkaloid. Solanidine can be isolated from potato. Solanidine decreases RAD51 and increases γH2AX and p53. Solanidine has anti-tumor effects on LLC tumors and lung cancer. Solanidine promotes breast cancer cell proliferation. Solanidine reduces neovascularization. Solanidine causes abortion in some pregnant mice.

RI-2 is a reversible RAD51 inhibitor, with an IC₅₀ of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.

Homologous recombination-IN-1 is a novel RAD51-BRCA2 protein-protein interaction inhibitor (EC₅₀=19 μM). Homologous recombination-IN-1 can interfere with homologous recombination.

RI(dl)-2 TFA is a potent and selective RAD51-mediated D-loop formation inhibitor with an IC₅₀ of 11.1 μM. RI(dl)-2 TFA does not influence RAD51 binding to ssDNA and inhibits homologous recombination (HR) activity in human cells (IC₅₀ of 3.0 μM).

RAD51-IN-1, a derivative of B02, is a potent inhibitor of RAD51. RAD51-IN-1 can be used for cancer research.

RAD51-IN-5 is a potent inhibitor of RAD51. RAD51 is a eukaryote gene. RAD51-IN-5 has the potential for the research of conditions involving mitochondrial defects (extracted from patent WO2021164746A1, compound 3).

(Rac)-IBR120 is the racemate of IBR120 (HY-176549A). IBR120 is a RAD51 inhibitor that has significant growth inhibition activity against MDA-MB-468 cells. (Rac)-IBR120 can be used for the research of difficult-to-treat cancers like triple negative breast cancer.

RAD51-IN-3 (Example 66A) is an inhibitor of Rad51.

Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.

RAD51-IN-4 is a potent inhibitor of RAD51. RAD51 is a eukaryote gene. RAD51-IN-4 has the potential for the research of conditions involving mitochondrial defects (extracted from patent WO2019014315A1, compound R12).