dna-pk

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

DNA-PK-IN-6, a robust DNA-PK inhibitor, effectively hampers the activity of DNA-PKcs, thereby significantly impairing the DNA repair mechanism in tumors and instigating apoptosis in cells. Additionally, DNA-PK-IN-6 amplifies the responsiveness of tumor tissues to radiotherapy, overcomes the challenge of drug resistance, and augments its inhibitory impact on a diverse range of solid and hematological tumors[1].

DNA-PK-IN-9 (also known as compound YK6) is a highly potent inhibitor of DNA-dependent protein kinase (DNA-PK), displaying an IC50 value of 10.47 nM. DNA-PK-IN-9 holds significant potential in anticancer research [1].

DNA-PK-IN-2 is a highly effective inhibitor of DNA-dependent protein kinase (DNA-PK), an enzyme complex comprising the Ku70/Ku80 heterodimer and DNA-PK catalytic subunit (DNA-PKcs). It shows potential applications in cancer research, making it a valuable tool for studying cancer diseases [1].

DNA-PK-IN-3 is a highly potent inhibitor of DNA-PK that exerts a synergistic effect with radiotherapy and chemotherapy, enhancing therapeutic outcomes and significantly inhibiting tumor growth. Additionally, it demonstrates remarkable efficacy in reducing damage to normal cells, thereby minimizing adverse side effects, making it a compound of great potential for cancer research applications[1].

DNA-PK-IN-8 is a potent, selective, and orally active inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 value of 0.8 nM, demonstrating synergistic antiproliferative effects across various cancer cell lines and significantly reducing HL-60 tumor growth when combined with Doxorubicin [1].

DNA-PK-IN-4 (WO2021209055A1, compound 27), an imidazolinone derivative compound, is a highly effective inhibitor of DNA-PK, specifically targeting DNA-PKcs activity. By inhibiting DNA-PKcs, the compound significantly impairs tumor DNA repair mechanisms and triggers apoptosis in cells. With its potential application in cancer research, DNA-PK-IN-4 holds promise for further investigation [1].

DNA-PK-IN-7 is a potent DNA-PK inhibitor (IC50= 1 nM) (WO2021104277A1, compound 5).

DNA-PK-IN-5 is a potent inhibitor of DNA-PK that inhibits DNA-PKcs activity, significantly reduces tumor DNA repair, and induces apoptosis. It enhances tumor tissue sensitivity to radiotherapy, overcomes drug resistance issues, and improves the inhibition of various solid and haematological tumors.

DNA-PK-IN-1, a potent inhibitor of DNA-PK, holds potential for cancer disease research.

DNA-PK-IN-10 is a DNA-PK inhibitor used in breast cancer and non-small cell lung cancer research [1].

LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.

Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.

AZD-7648 is an inhibitor of DNA-dependent protein kinase (DNA-PK) with the IC50 of 0.63 nM in an enzyme assay,has anti-tumor activity.

STL127705 (Compound L) is a potent inhibitor of the Ku 70/80 heterodimer protein, disrupting Ku70/80-DNA interaction with an IC50 of 3.5 μM, and inhibiting Ku-dependent DNA-PKCS kinase activation with an IC50 of 2.5 μM.

PI-3065 is a novel potent and selective PI3K p110δ inhibitor.

DMNB (6-Nitroveratraldehyde) is DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 of 15 μM, an enzyme involved in the non-homologous end-joining (NHEJ) pathway of double-stranded DNA break (DSB) repair in human cells.

VX-984 (M9831) is an oral, selective DNA-PK inhibitor that can cross the blood-brain barrier. VX-984 inhibited the conjugation of non-homologous terminal NHEJ and acted on DSBs to break DNA double strand. VX-984 is commonly seen in glioblastoma (GBM) and non-small cell lung cancer (NSC-LC) studies.

Pictilisib dimethanesulfonate (GDC-0941 2 MeSO3H salt) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

(R)-VX-984 ((R)-M9831) is the (R)-enantiomer of VX-984. VX-984 is a potent inhibitor of DNA-PK.

LTURM34 is an inhibitor of DNA-PK with IC50 of 34 nM. LTURM34 displays effective antiproliferative activity in a wide range of tumor cell lines. LTURM34 shows 170-fold selectivity for DNA-PK over PI3K .

PI3K-IN-1 (Voxtalisib Analogue) is a dual inhibitor of mTOR/PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR.

ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).

PIK-75 hydrochloride (PIK-75 HCl) is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays.