DNA-PK

<p>STL127705 inhibits Ku 70/80 protein &amp; DNA-PKCS kinase, IC50s: 3.5 μM &amp; 2.5 μM.</p>

<p>LTURM34 is an inhibitor of DNA-PK with IC50 of 34 nM.</p>

<p>Multi-target kinase inhibitor 4 (Compound 2) is a PI3K/DNA-PK inhibitor and a potent chemosensitizer that enhances the number of DNA double-strand breaks induced by Doxorubicin. It serves as an effective multidrug resistance (MDR) inhibitor, demonstrating inhibitory activity against P-glycoprotein (P-gp) mediated drug efflux. Multi-target kinase inhibitor 4 can be encapsulated in PEG-coated lipid nanoparticles.</p>

<p>A unique collection of xnum DNA Damage &amp;amp; Repair related compounds for high throughput screening (HTS) and high content screening (HCS);</p>

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

<p>IC 86621: DNA-PK ATP-competitive inhibitor, IC50 120 nM, enhances DSB antitumor effects, EC50 68 µM for repair.</p>

<p>AMA-37 is a selective, reversible, and ATP-competitive DNA-PK inhibitor.</p>

<p>PIK-75 hydrochloride (PIK-75 HCl) is a p110α inhibitor, isoform-specific mutants at Ser773, and potently inhibits DNA-PK with IC50 of 2 nM in cell-free assay.</p>

<p>PI-3065 is a novel potent and selective PI3K p110δ inhibitor.</p>

<p>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.</p>

<p>LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM).</p>

<p>PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50s: 2/3/3/15/30/23 nM for p110α/β/δ/γ, mTOR, and DNA-PK).</p>

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

<p>NU 7026 (DNA-PK Inhibitor II) is an effective DNA-PK inhibitor (IC50: 0.23 μM, in cell-free assays), 60-fold selective for DNA-PK than PI3K and no inhibition</p>

<p>AZD 6482 (KIN-193) is a potent and selective inhibitor of p110β and PI3Kβ with IC50 values ​​of 0.69nM and 10nM.Cost-effective and quality-assured.</p>

<p>Compound 401 (2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one) is a synthetic DNA-PK inhibitor (IC50 = 0.28 μM) that also targets mTOR but not PI3K.</p>

<p>PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .</p>

<p>DMNB (6-Nitroveratraldehyde) is DNA-dependent protein kinase (DNA-PK) inhibitor, an enzyme involved in the NHEJ pathway of DSB repair in human cells.</p>

<p>CC-115 hydrochloride: potent DNA-PK/mTOR inhibitor; IC50s: 13 nM and 21 nM; blocks mTORC1/C2 pathways.</p>

<p>NU7441 (KU-57788 (NU7441)) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM).</p>

<p>Torin 2: mTOR inhibitor, IC50=0.25 nM, 800x more selective than PI3K, with EC50=28/35/118 nM for ATM/ATR/DNA-PK.</p>

<p>Leniolisib (CDZ173) (CDZ173) is a potent and selective PI3Kδ inhibitor (IC50: 11 nM).</p>

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

<p>Samotolisib (LY3023414) inhibits PI3K, DNA-PK, mTOR; tested for solid tumors including breast and colon cancer.</p>

<p>Voxtalisib (XL765) (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR. Phase 1/2.</p>

<p>ETP-45658 (ETP45658) is a PI 3-kinase inhibitor (IC50 values are 22, 30, 129 and 710 nM for PI 3-Kα, PI 3-Kδ, PI 3-Kβ and PI 3-Kγ respectively).</p>

CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).

YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays.

<p>KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 of 8.6 nM and 4 nM, 0.5 nM, 0.1 nM respectively, less inhibition of PI3Kγ.</p>

<p>LY-294002 HCl (NSC 697286) is a stable PI3K inhibitor (IC50: 0.5-0.97 µM) and prevents autophagosome formation.</p>

<p>SF2523 is a highly selective and potent inhibitor.</p>

<p>PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).</p>

<p>NU-7163 is a potent and selective inhibitor of ATP-competitive DNA-PK.</p>

<p>DNA-PK-IN-1 is a potent inhibitor of DNA-PK. DNA-PK-IN-1 has potential for cancer disease research.</p>

DNA-PK-IN-5: potent DNA-PK inhibitor, reduces tumor repair, induces apoptosis, enhances radiotherapy, overcomes resistance.

<p>DNA-PK-IN-3 is a potent DNA-PK inhibitor, enhancing radio/chemotherapy and reducing tumors with limited side effects.</p>

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

<p>DNA-PK-IN-4, an imidazolinone, targets DNA-PKcs to hinder tumor DNA repair and induce apoptosis, showing cancer research potential.</p>

(R)-(-)-Rolipram ((-)-Rolipram) is an R-enantiomer of Rolipram which is a PDE4 inhibitor.

<p>ZL-2201 is a potent inhibitor of DNA-PK, demonstrating an IC50 value of 1 nM.</p>

<p>SU-11752 selectively inhibits DNA-PK by competing with ATP, enhances ionizing radiation sensitivity without affecting cell cycle or ATM activity.</p>

<p>DNA-PK-IN-10 is a DNA-PK inhibitor utilized in the research of breast cancer and non-small cell lung cancer [1].</p>

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

<p>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].</p>

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

<p>DNA-PK-IN-9 (YK6) is a potent DNA-PK inhibitor with an IC50 of 10.47 nM, important in cancer research.</p>

<p>NU5455 is a potent DNA-PKcs inhibitor, oral, boosts doxorubicin in liver tumors, amplifies topoisomerase inhibitors, no adverse effects.</p>

<p>DNA-PK-IN-2 is an inhibitor of the DNA-PK enzyme complex, useful in cancer research.</p>

<p>DNA-PK-IN-6 inhibits DNA-PKcs, disrupting tumor DNA repair and triggering apoptosis; enhances radiotherapy and targets various tumors (WO2021197159A1).</p>

<p>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</p>