DNA Damage/DNA Repair

<p>PPARα agonist 1 is a complete and potent PPARα agonist.</p>

<p>L2H2-6OTD is a telomerase inhibitor with G-quadruplex loops; IC50: 15 nM.</p>

<p>DNA Crosslinker 4 binds DNA's minor groove, inhibits NCI-H460, A2780, MCF-7 cancer cells, and is used in cancer research.</p>

<p>15-keto-Prostaglandin E2, an endogenous metabolite, inhibits STAT3 activation through binding to Cys259 and regulates breast cancer cell growth and progression.</p>

<p>2-Ethylhexyl diphenyl phosphate is an organophosphorus flame retardant (OPFRs) and acts as a PPARG agonist (EC20: 2.04 µM). Additionally, it inhibits the transcriptional activity of ERRγ (IC50: 1.3 µM) and enhances the expression of 3β-HSD1, human chorionic gonadotropin (hCG), and progesterone secretion. This compound is applicable in studies related to female reproduction and fetal development.</p>

<p>SARS-CoV-2 nsp14-IN-1 inhibits Nsp14 Mtase with an IC50 of 0.061 μM, affecting multiple substrates.</p>

<p>PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binding agent (IC50: 24 nM) with antidiabetic effects.</p>

<p>Intoplicine is an inhibitor of DNA topoisomerase I and II.</p>

<p>Gimatecan (STI481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.</p>

<p>Compound 1a inhibits Topoisomerase I/II, shrinks mouse liver tumors, IC50: 6.83/9.82 μM for LM9/Huh7 cells.</p>

<p>GSK1820795A: Telmisartan analog, selective hGPR132a antagonist, blocks yeast activation by N-acylamides, angiotensin II antagonist, partial PPARγ agonist.</p>

<p>Topotecan acetate is an inhibitor of topoisomerase.</p>

<p>DNA-PK-IN-8: Potent, selective oral DNA-PK inhibitor, IC50 = 0.8 nM, boosts anti-cancer effects with Doxorubicin.</p>

<p>Namitecan is an effective inhibitor of topoisomerase I. It has antitumor property.</p>

<p>Topoisomerase II inhibitor 5 (Compound E24) is a DNAtopoisomerase II inhibitor with anticancer effects.</p>

<p>HDAC8-IN-12 (compound 5k), a non-hydroxamic acid derivative, serves as a selective HDAC8 inhibitor with an IC 50 of 0.12 nM and demonstrates potent efficacy against breast cancer. This compound enhances anti-tumor immunity by activating T cells, elevating M1 macrophage levels, and reducing M2 macrophage proportions. In an orthotopic mouse model of breast cancer, HDAC8-IN-12, administered at 50 mg/kg, effectively suppresses tumor growth.</p>

<p>Levofloxacin mesylate is an orally active antibiotic effective against both Gram-positive and Gram-negative bacteria. It inhibits DNA gyrase and topoisomerase IV enzymes. Levofloxacin mesylate is employed in research related to chronic periodontitis, airway inflammation, and BK viremia. Additionally, it possesses anti-Orthopoxvirus activity.</p>

<p>PPARα/γ agonist 1 is a potent and dual PPARα/γ partial agonist which is a promising prototype for the research of dyslipidemia and diabetes.</p>

<p>NU5455 is a potent DNA-PKcs inhibitor, oral, boosts doxorubicin in liver tumors, amplifies topoisomerase inhibitors, no adverse effects.</p>

<p>Lys(CO-C3-p-I-Ph)-O-tBu, a pharmacokinetic modifier (PK modifier), enhances the pharmacokinetic properties of PSMA ligand molecules by increasing their residence time in plasma through improved binding to albumin and reducing absorption by the salivary glands, potentially extending the active compound's half-life. Moreover, Ac-PSMA-trillium is an effective PSMA-targeting compound for various biological applications when modified with different radioactive isotopes. When labeled with 111 In, it serves as a DOTA chelating agent and imaging agent. Alternatively, when labeled with 225 Ac, it acts as a Macropa chelator for targeted radionuclide therapy (TRT) in researching metastatic castration-resistant prostate cancer (mCRPC) [1] [2].</p>