DNA Damage/DNA Repair

Atiratecan (TP300), a CH0793076-based camptothecin prodrug, combats BCRP+/- tumors; doesn't affect AChE.

Fonadelpar is an agonist of PPARδ. It also is used in the research of neuroparalytic keratopathy.

Gepotidacin (GSK-2140944) is a potent DNA topoisomerase inhibitor, a novel antibacterial efficacious against various anaerobes.

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.

ATM Inhibitor -2 is a potent and selective inhibitor of ATM (IC50<1 nM).

MC3138 is a selective SIRT5 activator showing anti-tumor effects in PDAC cells.

TMU 35435 is an inhibitor of histone deacetylases (HDAC). It enhances radiosensitivity by inducing the accumulation of misfolded proteins and autophagy (autophagy) in TNBC, and inhibits the NHEJ pathway through ubiquitination of the catalytic subunit of DNA-dependent protein kinase (DNA-PKcs).

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

O6BTG-C8-αGlu is an O6-methylguanine-DNA methyltransferase (MGMT) inhibitor with an IC50 of 0.45 μM. At a concentration of 0.1 μM, it fully inhibits MGMT in HeLaS3 cells and demonstrates no cytotoxicity even at prolonged high doses (up to 20 μM). This compound is suitable for research on MGMT-related cancers.

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].

Topotecan acetate is an inhibitor of topoisomerase.

ATRkinase-IN-3 (Compound I-G-28) is an inhibitor of the ATR protein kinase, exhibiting a Ki value ranging from 0.01 to 1 μM, and is utilized in cancer research.

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

TERT ligand-1 is a PROTAC target protein ligand used in the synthesis of PROTAC NU-PRO-1. NU-PRO-1 can induce the degradation of TERT in cancer cells.

<p>TH1338 is an orally active camptothecin derivative with significant blood-brain barrier permeability and cytotoxicity, used in cancer research.</p>

Aleglitazar (R1439) (R1439) is a potent dual PPARα/γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively.

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

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

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

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