DNA-PK Inhibitor

SU-11752 is an inhibitor for DNA-dependent protein kinase (DNA-PK) with an IC₅₀ of 0.13 μM. SU-11752 inhibits PI3K p110γ kinase with IC₅₀ of 1.1 μM. SU-11752 binds competitively for ATP-site in DNA-PK, results in inhibition of intracellular DNA double-strand break repair and increases the sensitivity of cells to radiotherapy.

AZD-7648 (GMP) is AZD-7648 (HY-111783) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC₅₀ of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity.

NU-7031 (compound 10), a coumarin derivative, is a DNA-PK inhibitor with an IC₅₀ of 1.7 μM. NU-7031 can be used for the study of cancer.

Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and potent chemosensitizer that can increase the amount of DNA double strand breaks induced by Doxorubicin (HY-15142A). Multi-target kinase inhibitor 4, is an efficient inhibitor of multidrug resistance (MDR) that exhibits inhibitory activity toward P-glycoprotein-mediated drug efflux. Multi-target kinase inhibitor 4 can be loaded into PEG-coated LNPs.

DNA-PK-IN-3 is a potent inhibitor of DNA-PK. DNA-PK-IN-3 synergistically enhances the effect of radiotherapy and chemotherapy and effectively inhibits tumor growth. DNA-PK-IN-3 also effectively reduces the damage to normal cells and reducing side effects. DNA-PK-IN-3 has the potential for the research of cancer disease (extracted from patent WO2021213460A1, compound 4).

ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC₅₀ of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC₅₀ values of 47, 663 and 5131 nM, respectively.

PP487 is a selective dual inhibitor of Tyrosine kinase/PI3-K, with IC₅₀ values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used in cancer research.

NU7200 is a metabolite of the DNA-PK inhibitor NU7026 (HY-15719).

DNA-PK-IN-1 is a potent inhibitor of DNA-PK. DNA-dependent protein kinase (DNA-PK) is a DNA-PK enzyme complex composed of Ku70/Ku80 heterodimer and DNA-dependent protein kinase catalytic subunit (DNA-PKcs). DNA-PK-IN-1 has the potential for the research of cancer diseases (extracted from patent WO2021136463A1, compound 1).

NU-7107 is a derivative of NU7026 (HY-15719) and a DNA-dependent protein kinase (DNA-PK) inhibitor with an IC₅₀ >10 μM. NU-7107 is applicable for cancer research.

DNA-PK-IN-9 (compound YK6) is a potent DNA-dependent protein kinase (DNA-PK) inhibitor with an IC₅₀ value of 10.47 nM. DNA-PK-IN-9 can be used for researching anticancer.

ZL-2201 free base is a potent DNA-PK inhibitor with an IC₅₀ of 1 nM (WO2021104277A1, compound 5).

eALM1137 is a mTOR inhibitor with an IC₅₀ of 4.8 nM. eALM1137 mediates dual inhibition of the mTORC1 and mTORC2 signaling pathways, and inhibits DNA-PK (IC₅₀=77 nM). eALM1137 exhibits antiproliferative and cytostatic activities, and induces G1 cell cycle arrest. eALM1137 is applicable to the research of glioblastoma multiforme.

DNA-PK-IN-14 (compound 78) is a potent, selective DNA-PK inhibitor with an IC₅₀ value of 7.95 nM. DNA-PK-IN-14 has oral activity and has the potential to be a radiosensitizer for cancer treatment.

DNA-PK-IN-4 is a potent inhibitor of DNA-PK. DNA-PK-IN-4 is a imidazolinone derivative compound. DNA-PK-IN-4 inhibits DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-4 has the potential for the research of cancer disease (extracted from patent WO2021209055A1, compound 27).

DNA-PK-IN-10 is a DNA-PK inhibitor. DNA-PK-IN-10 can be used for the research of breast cancer and non-small cell lung cancer.

Panulisib (P7170; AK151761) is an orally active inhibitor of PI3K (IC₅₀ = 2.2 nM) and mTOR (IC₅₀ = 4.4 nM). Panulisib inhibits ALK1 and DNA-PK, two enzymes that respectively participate in angiogenesis and DNA repair, with IC₅₀ values of 47 nM and 1.5 nM respectively. Panulisib inhibits cell proliferation and apoptosis. Panulisib can be used for research on breast cancer and non-small cell lung cancer.

PP162 is a selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC₅₀ of 53 nM. PP162 selectively inhibits DNA-PK by binding to a conserved hydrophobic pocket. PP162 exhibits weak inhibitory activity against various tyrosine kinases and PI3K family members. PP162 can be used for research on selective kinase targeting.

IC-87361 is a DNA-dependent protein kinase (DNA-PKcs) inhibitor with an IC₅₀ of 35 nM, and radiosensitizer. IC-87361 inhibits the catalytic activity of DNA-PKcs and blocks non-homologous end joining (NHEJ) DNA double-strand break repair. IC-87361 can be used for the research of lung cancer and melanoma.

DNA-PK-IN-16 is an orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC₅₀ of 10.2 nM. DNA-PK-IN-16 induces the upregulation of γH2A.X, a biomarker of DNA double-strand breaks. DNA-PK-IN-16 exhibits antiproliferative activity in various cancer cell lines. DNA-PK-IN-16 enhances the infiltration of CD8⁺ T cells in tumor tissues through synergistic action with anti-PD-L1 monoclonal antibody. DNA-PK-IN-16 is applicable for cancer research.