DNA-PK

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DNA-PK Signaling Pathway Map

DNA-PK Signaling Pathways

DNA-PK Products

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  • DNA-PK Inhibitors (18)
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Catalog No. Product Name Information Product Use Citations Product Validations
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cancers (Basel), 2022, 14(6)1575
Int J Mol Sci, 2022, 23(8)4277
S1105 LY294002 LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Immunity, 2022, 55(1):159-173.e9
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.2292.2021
S1205 PIK-75 HCl 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.
Cancers (Basel), 2022, 14(6)1575
Am J Cancer Res, 2022, 12(3):1102-1115
Cell Metab, 2021, S1550-4131(21)00326-0
S2622 PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
Life Sci Alliance, 2021, 4(2)e202000882
PLoS One, 2016, 11(10):e0164895
Biochem Biophys Res Commun, 2015, 465(1):137-44
S2638 NU7441 (KU-57788) NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.
Cell Metab, 2022, S1550-4131(21)00542-8
EMBO Mol Med, 2022, e14501
Clin Cancer Res, 2022, clincanres.1846.2021
S2758 Wortmannin (KY 12420) Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Cancer Res, 2022, canres.2292.2021
Cell Rep, 2022, 38(11):110522
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.1397.2021
Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021
S2871 T0070907 T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ. T0070907 significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells.
Redox Biol, 2022, 50:102256
Front Cell Dev Biol, 2021, 9:745554
J Inflamm Res, 2021, 14:395-411
S2893 NU7026 NU7026 (LY293646) is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. NU7026 enhances G2/M cell arrest and apoptosis.
Sci Signal, 2022, 15(715):eabh2290
J Biol Chem, 2022, S0021-9258(22)00301-5
Nucleic Acids Res, 2021, gkab584
S6506 Compound 401 Compound 401 is a synthetic inhibitor of DNA-PK(IC50=0.28 μM) and mTOR (IC50=5.3 μM). It has no inhibition on p110α/p85α PI3K (>100 μM) and blocks the phosphorylation of S6 kinase 1 Thr389 and Akt Ser473 in COS7 cells.
S7891 CC-115 CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) with IC50 values of 0.013 μM and 0.021 μM, respectively. It has potential antineoplastic activity.
Neoplasia, 2022, 27:100780
Sci Rep, 2021, 11(1):20338
Genes (Basel), 2021, 12(6)925
S8045 KU-0060648 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 with IC50 of 0.59 μM.
Biomedicines, 2021, 9(5)579
Cell, 2019, 176(3):505-519
Cancer Res, 2019, 79(1):99-113
S8322 Samotolisib (LY3023414) Samotolisib (LY3023414, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
J Cell Mol Med, 2021, 25(12):5602-5614
S8379 YU238259 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.
Int J Mol Sci, 2020, 21(16)E5821
S8427 LTURM34 LTURM34 is a specific DNA-PK inhibitor, 170-fold more selective for DNA-PK activity compared to PI3K activity, with IC50 value of 0.034 μM.
Int J Mol Sci, 2021, 22(19)10512
S8586 Nedisertib (M3814) Nedisertib (M3814, Peposertib, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with IC50 of < 3 nM.
bioRxiv, 2021, 10.1101/2021.10.07.463578
S8589 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
Oncotarget, 2017, 8(58):98471-98481
S8843 AZD7648 AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases.
Cancer Cell, 2022, S1535-6108(21)00662-0
Sci Rep, 2022, 12(1):5827
Cell Rep, 2021, 37(2):109815
S1038 PI-103 PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cancers (Basel), 2022, 14(6)1575
Int J Mol Sci, 2022, 23(8)4277
S1105 LY294002 LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Immunity, 2022, 55(1):159-173.e9
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.2292.2021
S1205 PIK-75 HCl 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.
Cancers (Basel), 2022, 14(6)1575
Am J Cancer Res, 2022, 12(3):1102-1115
Cell Metab, 2021, S1550-4131(21)00326-0
S2622 PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
Life Sci Alliance, 2021, 4(2)e202000882
PLoS One, 2016, 11(10):e0164895
Biochem Biophys Res Commun, 2015, 465(1):137-44
S2638 NU7441 (KU-57788) NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits mTOR and PI3K with IC50 of 1.7 μM and 5 μM in cell-free assays, respectively. It reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage.
Cell Metab, 2022, S1550-4131(21)00542-8
EMBO Mol Med, 2022, e14501
Clin Cancer Res, 2022, clincanres.1846.2021
S2758 Wortmannin (KY 12420) Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Cancer Res, 2022, canres.2292.2021
Cell Rep, 2022, 38(11):110522
Proc Natl Acad Sci U S A, 2022, 119(3)e2114134119
S2817 Torin 2 Torin 2 is a potent and selective mTOR inhibitor with IC50 of 0.25 nM in p53−/− MEFs cell line; 800-fold greater selectivity for mTOR than PI3K and improved pharmacokinetic properties. Inhibition of ATM/ATR/DNA-PK with EC50 of 28 nM/35 nM/118 nM,in PC3 cell lines respectively. Torin 2 decreases cell viability and induces autophagy and apoptosis.
Adv Sci (Weinh), 2022, 10.1002/advs.202104055
Cancer Res, 2022, canres.1397.2021
Mol Cancer Ther, 2022, molcanther.MCT-21-0947-A.2021
S2871 T0070907 T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM in a cell-free assay, with a >800-fold selectivity over PPARα and PPARδ. T0070907 significantly decreases the levels of DNA-PKcs and RAD51 proteins in ME-180 and SiHa cells.
Redox Biol, 2022, 50:102256
Front Cell Dev Biol, 2021, 9:745554
J Inflamm Res, 2021, 14:395-411
S2893 NU7026 NU7026 (LY293646) is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR. NU7026 enhances G2/M cell arrest and apoptosis.
Sci Signal, 2022, 15(715):eabh2290
J Biol Chem, 2022, S0021-9258(22)00301-5
Nucleic Acids Res, 2021, gkab584
S6506 Compound 401 Compound 401 is a synthetic inhibitor of DNA-PK(IC50=0.28 μM) and mTOR (IC50=5.3 μM). It has no inhibition on p110α/p85α PI3K (>100 μM) and blocks the phosphorylation of S6 kinase 1 Thr389 and Akt Ser473 in COS7 cells.
S7891 CC-115 CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR) with IC50 values of 0.013 μM and 0.021 μM, respectively. It has potential antineoplastic activity.
Neoplasia, 2022, 27:100780
Sci Rep, 2021, 11(1):20338
Genes (Basel), 2021, 12(6)925
S8045 KU-0060648 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 with IC50 of 0.59 μM.
Biomedicines, 2021, 9(5)579
Cell, 2019, 176(3):505-519
Cancer Res, 2019, 79(1):99-113
S8322 Samotolisib (LY3023414) Samotolisib (LY3023414, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
J Cell Mol Med, 2021, 25(12):5602-5614
S8379 YU238259 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.
Int J Mol Sci, 2020, 21(16)E5821
S8427 LTURM34 LTURM34 is a specific DNA-PK inhibitor, 170-fold more selective for DNA-PK activity compared to PI3K activity, with IC50 value of 0.034 μM.
Int J Mol Sci, 2021, 22(19)10512
S8586 Nedisertib (M3814) Nedisertib (M3814, Peposertib, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with IC50 of < 3 nM.
bioRxiv, 2021, 10.1101/2021.10.07.463578
S8589 SF2523 SF2523 is a highly selective and potent inhibitor of PI3K with IC50 values of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.
Oncotarget, 2017, 8(58):98471-98481
S8843 AZD7648 AZD7648 is a potent inhibitor of DNA-PK with an IC50 of 0.6 nM in biochemical assay and more than 100-fold selective against 396 other kinases.
Cancer Cell, 2022, S1535-6108(21)00662-0
Sci Rep, 2022, 12(1):5827
Cell Rep, 2021, 37(2):109815
Tags: DNA-PK activation | DNA-PK phosphorylation | DNA-PK assay | DNA-PK activity | DNA-PK activation | DNA-PK pathway | DNA-PK inhibitor clinical trial | DNA-PKcs phosphorylation | DNA-PK function | DNA-PK inhibitor review