DNA Damage/DNA Repair

Retelliptine, a DNA topoisomerase II inhibitor, is used potentially for the treatment of cancer.

Fostriecin inhibits PP2A/PP4 (IC50s = 3.2/3 nM), weakly affects topoisomerase II/PP1 (IC50s = 40/131 μM), doesn't inhibit PP2B, and may modify epigenetics.

Topoisomerase II inhibitor 5 (Compound E24) is a DNAtopoisomerase II inhibitor with anticancer effects.

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

Moflomycin is an anthracycline derivative. It exhibits a higher antileukemic activity compared to other anthracyclines.

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.

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

LMP517 (NSC 781517), an indenoisoquinoline, is a potent dual TOP1 and TOP2 inhibitor that shows better antitumor activity than its parent compound LMP744 against H82 (Small Cell Lung Cancer) xenografts, inducing TOP1 cleavage complexes (TOP1ccs) and TOP2ccs [1].

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].

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

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.

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

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

DNA-PK-IN-15 (compound 6) acts as an inhibitor of DNA-PK, exhibiting an IC50 value of 0.08 nM.

Carbacyclin, a PGI2 analog, is a prostacyclin (PGI2) receptor agonist and vasodilator with potent inhibitory platelet aggregation.

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

PPARγ phosphorylation inhibitor 1, PPARγ agonist (IC50=24 nM), inhibits CDK5-mediated Ser273 phosphorylation, antidiabetic activity.

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

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

5-cis Carbaprostacyclin: a PGI2 stable analog; poor human platelet aggregation inhibitor (IC50: 2.8 μM); weakens rabbit artery relaxation (EC50: 104 μM).