homologous

DFP00173 is a potent and selective aquaporin 3 (AQP3) inhibitor, with an IC50 of approximately 0.1-0.4 μM for both mouse and human AQP3. It demonstrates selectivity for AQP3 compared to homologous AQP subtypes AQP7 and AQP9.

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

ART558 is a potent, selective, low molecular weight, allosteric DNA polymerase activity of Polθ inhibitor (IC50=7.9 nM). ART558 can be used for the research of cancer.

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.

NRX-2663 enhances the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP and increases the binding affinity of β-catenin to β-TrCP (Kd: 54.8 nM, EC50: 22.9 nM).

NRX-103094 is a potent enhancer of the interaction between β-catenin and the homologous E3 ligase SCFβ-TrCP, increasing the affinity of pSer33/Ser37 β-catenin for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM.

NRX-252114 (NRX252114) induces degradation of mutant β-catenin NRX-252114 is a potent enhancer of the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP, and is able to enhance the binding of pSer33/S37A β-catenin to β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. Kd is 0.4 nM.

NRX-103095 is a potent enhancer of the interaction of β-catenin with the homologous E3 ligase SCFβ-TrCP and enhances the affinity of pSer33 Ser37 β-catenin for β-TrCP with an EC50 of 163 nM.

ARB-272572 hydrochloride is a small molecule PD-L1 inhibitor with an IC50 value of 400 pM for PD-1 PD-L1 HTRF.ARB-272572 hydrochloride inhibits PD-1 PD-L1 cell signaling by inducing homologous interactions with PD-L1 proteins.

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.

IRBP acetate(211426-18-5 free base) (Interphotoreceptor Retinoid Binding Protein Fragment IRBP) is a 20-residue peptide, which is a major pathogenic epitope. It exists in the first homologous repeat of interstitial visual pigment Binding Protein peptide (IRBP 161-180) and can induce post-uveitis (EAU).

CRTh2 antagonist 3 is a powerful chemokine receptor homologous molecule expressed on Th2 cell (CRTh2) antagonists. CRTh2 antagonist 3 enhanced the activity of PDK1 on short peptide substrates with EC50 of 2 μM and Kd of 8.4 μM. CRTh2 antagonist 3 has the

DCZ0415 induces antimyeloma activity in vitro, in vivo and in primary cells of drug-resistant myeloma patients. DCZ0415 is a potent TRIP13 inhibitor that can impair the repair of non-homologous end junctions and inhibit NF-κB activity.

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.

BI-671800 (AP-761) is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2 CRTH2). With IC50 values of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has the potential to treat poorly controlled asthma[2].

LBG20304 (compound 2s) serves as a ligand for the homologous GluK5 receptor, demonstrating an IC50 of 432 nM and exhibiting over 40-fold selectivity against the GluK1-3 isoforms. At concentrations below 10 μM, LBG20304 shows neither agonistic nor antagonistic effects on heterologous GluK2 5 receptors. However, at concentrations above 10 μM, it displays minimal agonist activity in neuronal slices (rat).

TA-5707F is an inhibitor specifically targeting IgE-induced homologous PCA (passive cutaneous anaphylaxis).

Ran-IN-1 (Compound M36) is an orally active and selective inhibitor of Ran GTPase. It binds allosterically with high specificity to the switch II pocket of GDP-bound Ran (RanGDP), stabilizing its inactive state and reducing the formation of active Ran-GTP. Ran-IN-1 induces apoptosis in epithelial ovarian cancer (EOC) cells and inhibits DNA repair pathways such as homologous recombination (HR) and non-homologous end joining (NHEJ). This compound shows potential for research in epithelial ovarian cancer, particularly in high-grade serous carcinoma.

D-G23 is a selective RAD52 inhibitor. It disrupts RAD52-mediated DNA repair pathways and suppresses the growth of cancer cells deficient in BRCA1 and BRCA2. D-G23 shows promise for research into homologous recombination-related cancers caused by BRCA1/2 mutations, such as hereditary breast and ovarian cancers.

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

BUR1 is a selective BMP upregulator that acts by increasing the expression of Inhibitor of DNA binding 1 and inducing BMP2 and PTGS2 expression.

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.

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(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].