dna-pk-in-1

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].

DNA-PK-IN-12 (compound 31t), an orally active inhibitor of DNA-PK, demonstrates potent inhibition with an IC 50 of 0.1 nM. It effectively impedes Hct116 cell growth and colony formation, displaying an IC 50 of 33.28 μM, and exhibits antitumor activity in vivo [1].

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

DNA-PK-IN-14 (compound 78) is a potent and selective DNA-PK inhibitor with an IC50 value of 7.95 nM. It exhibits oral activity and is a promising radiosensitizer for cancer treatment.

BAY-8400 is a potent, selective, and orally active DNA-dependent protein kinase (DNA-PK) inhibitor (IC50 = 81 nM) that demonstrates synergistic efficacy when combined with targeted alpha therapies. BAY-8400 is applicable for cancer research [1].

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

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].

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

Canfosfamide (TLK-286, TER286), a glutathione analogue prodrug, becomes activated by glutathione S-transferase P1-1 to induce apoptosis and inhibit DNA-dependent protein kinase's (DNA-PK) catalytic kinase activity. Upon activation, it generates an anticancer alkylating agent and a glutathione derivative, making it useful in researching malignancies [1] [2] [3].

Yhhu6669 is an anti-HBV agent that suppresses viral DNA and replication by promoting DNA-free capsid assembly, effectively reducing HBV DNA and HBcAg levels in AAV HBV-infected mice and demonstrating favorable pharmacokinetic (PK) properties [1].

QLT0267 is an inhibitor targeting integrin-linked kinase (ILK; IC50= 26 nM), showing over 10-fold selectivity against cyclin-dependent kinases 1, 2, and 5 (Cdk1, Cdk2, and Cdk5), and over 1,000-fold selectivity against C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2) at a concentration of 10 mg/ml. This compound effectively inhibits the proliferation of NPA187 papillary thyroid cancer cells with an IC50 of approximately 3 µM and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo studies reveal that QLT0267, administered at 100 mg/kg, significantly reduces tumor growth in a DRO mouse xenograft model and diminishes both tumor volume and intratumoral vascularization in a U87MG glioblastoma mouse xenograft model, showcasing its potential for therapeutic applications in cancer treatment.

DNA-PK Inhibitor IV is an active molecule that can be used in life science related research. The CAS number of DNA-PK Inhibitor IV is 70362-07-1.

PP487 is a dual tyrosine kinase PI(3)K inhibitor, exhibiting 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. It is applicable in cancer research [1].