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>

<p>Edotecarin is a potent topoisomerase I inhibitor. It can decrease single-strand DNA cleavage (IC50: 50 nM).</p>

<p>Karenitecin (Cositecan) is an inhibitor of topoisomerase I. It has potent anti-cancer activity.</p>

<p>ATR-IN-17 is a potent inhibitor of ATR kinase with good anti-cancer effects in LoVo cells (IC50: 1 nM).</p>

<p>OSUAB-0284 is an inhibitor of bacterial topoisomerase. It exhibits significant activity against staphylococci, particularly methicillin-resistant Staphylococcus aureus (MRSA). The compound exerts its antibacterial effect by inhibiting bacterial topoisomerase and may be used in research on infections caused by drug-resistant bacteria, including MRSA.</p>

<p>ATM Inhibitor -4: selective, potent (IC50: 0.32 nM), inhibits PI3K family, stable, stops mTOR at 1 μM.</p>

<p>PARP-1/HDAC-IN-1 is a PARP-1 and HDAC6 inhibitor with anticancer, antimigratory, and antiangiogenic activities and is used in tumor research.</p>

<p>KU 59403 is an effective ATM inhibitor (IC50: 3 nM, 9.1 μM, and 10 μM for ATM, DNA-PK, and PI3K, respectively).</p>

<p>PPARγ agonist 2 is a highly effective compound that acts as a partial agonist for PPARγ.</p>

<p>SPR719 is an inhibitor of gyrase B, has bactericidal activity.</p>

<p>ATR-IN-14: potent ATR kinase inhibitor; 98.03% inhibition at 25 nM; IC50 of 64 nM in LoVo cells.</p>

<p>WSD0628 is a brain-penetrant and potent ATM inhibitor with a significant radiosensitizing effect [1].</p>

<p>DNA-PK-IN-9 (YK6) is a potent DNA-PK inhibitor with an IC50 of 10.47 nM, important in cancer research.</p>

<p>Topoisomerase II inhibitor 18 (Compound IV), a Quinoxaline derivative, exhibits an IC 50 of 7.5 μM in inhibiting topoisomerase II. It impedes PC-3 cell proliferation, arrests the cell cycle at the S phase, and induces apoptosis. Moreover, this compound demonstrates substantial antitumor activity against cancer [1].</p>

<p>PPARγ agonist17 (Compound C1) is an orally active PPARγ agonist. It enhances PPARγ activity, arrests the cell cycle of HT-29 cells at the G2/M phase, inhibits cell migration, and induces apoptosis. PPARγ agonist17 exhibits broad-spectrum antiproliferative activity against cancer cells with relatively low toxicity to normal cells and does not cross the blood-brain barrier.</p>

<p>Anti-NASH agent 2 (compound 21) is an inhibitor of neolipogenesis activity and α-SMA gene expression. It improves hepatic steatosis, edema, inflammatory infiltration, and liver fibrosis in NASH mouse models.</p>

<p>SP-C01 is an orally active soluble epoxide hydrolase (sEH) inhibitor and a partial agonist of PPARγ. It can inhibit the phosphorylation of Ser273.</p>

<p>Topoisomerase inhibitor 5 (compound 158) is an inhibitor of bacterial topoisomerase, with a minimum inhibitory concentration of 0.125 μg/mL, and exhibits anti-tuberculosis activity.</p>

<p>Compound 5h (Topoisomerase I/II inhibitor 7) is a Topoisomerase I/II inhibitor.</p>

<p>DNA-PK-IN-6 inhibits DNA-PKcs, disrupting tumor DNA repair and triggering apoptosis; enhances radiotherapy and targets various tumors (WO2021197159A1).</p>

<p>MC3138 is a selective SIRT5 activator showing anti-tumor effects in PDAC cells.</p>

<p>LP-284 is a DNA alkylating agent effective against solid tumors and hematologic cancers like MCL.</p>

<p>Simmitecan hydrochloride is a camptothecin derivative, a topoisomerase I inhibitor with anticancer activity, which can be used to study is solid tumors.</p>

<p>KU-60019 is a specific inhibitor of ATM kinase (IC50: 6.3 nM).</p>

<p>BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase ( DNA-PK ) inhibitor ( IC 50 =81 nM) which shows synergistic efficacy in</p>

<p>OBI-3424, a highly selective prodrug, is converted by aldo-keto reductase family 1 member C3 (AKR1C3) to a potent DNA-alkylating agent.</p>

<p>YF438 is an HDAC inhibitor that demonstrates potent anti-cancer activity both in vitro and in vivo. It inhibits the growth and metastasis of triple-negative breast cancer (TNBC) cells by blocking the interaction between HDAC and MDM2, inducing the dissociation of MDM2 from MDMX, and promoting the degradation of MDM2.</p>

<p>Merbarone is a Type II DNA topoisomerase inhibitor. Merbarone inhibits the catalytic activity of human topoisomerase IIalpha by blocking DNA cleavage. Merbarone induces activation of caspase-activated DNase and excision of chromosomal DNA loops from the n</p>

<p>NSC61610 is anti-inflammatory that activates PPARγ in vitro via LANCL2 and adenylate cyclase/cAMP-dependent pathways, thereby improving experimental colitis.</p>

<p>Zabofloxacin hydrochloride is a potent and seletive bacterial type II and IV topoisomerases inhibitor, has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia.</p>

<p>Phenanthriplatin, also known as cis-[Pt(NH3)2-(phenanthridine)Cl]NO3, is a new drug candidate. It belongs to a family of platinum(II)-based agents which includes cisplatin, oxaliplatin and carboplatin. Phenanthriplatin Acts As a Covalent Poison of Topoiso</p>

<p>SR-4370 is an HDAC inhibitor. SR- 4370 exhibited IC50 values of 0.5 μM, 0.1 μM and 0.06 μM towards HDAC1, HDAC2 and HDAC3, resp.</p>

<p>Mavodelpar free acid (REN001 free acid) is an selective agonist of PPARδ.</p>

<p>Fotemustine: antineoplastic, chloroethylates DNA, blocks synthesis, causes cell arrest/apoptosis, lipophilic, crosses blood-brain barrier.</p>

<p>ATR-IN-24 (Compound 1) is an ATR inhibitor with demonstrated anticancer activity [1].</p>

<p>Lerzeparib is a PARP (ADP-ribose polymerase) inhibitor that exhibits antineoplastic activity [1].</p>

<p>MDL-811, an allosteric activator of SIRT6, markedly enhances the deacetylation of histone H3 at lysine residues 9, 18, and 56 (H3K9Ac, H3K18Ac, and H3K56Ac),</p>

<p>Antitumor Agent-104 (Compound 9) serves as an antineoplastic by impeding DNA repair mechanisms in tumor cells, primarily through the inhibition of PARP1 enzyme</p>

<p>PARP7-IN-16 free base is the freebase form of PARP7-IN-16. As a selective oral inhibitor of PARP-1/2/7, it demonstrates IC50 values of 0.94, 0.87, and 0.21 nM, respectively. This compound is utilized in the research of breast and prostate cancer.</p>