DNA-PK

DNA-PK製品

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  • DNA-PK阻害剤 (18)
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S1105 LY294002 LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKcs を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。
Cell Rep Med, 2024, 5(2):101420
Biomed Pharmacother, 2024, 172:116259
Stem Cell Reports, 2024, 19(2):196-210
S2758 Wortmannin Wortmannin 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.
Nat Commun, 2024, 15(1):451
J Exp Med, 2023, 220(9)e20230054
Autophagy, 2023, 19(4):1164-1183
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.
Nucleic Acids Res, 2024, gkad1224
Theranostics, 2024, 14(4):1561-1582
Genes Dev, 2024, 38(1-2):70-94
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.
J Transl Med, 2023, 21(1):89
Anticancer Drugs, 2023, 34(4):519-531
Cancer Cell, 2022, S1535-6108(22)00312-9
S2871 T0070907 T0070907 is a potent inhibitor of PPARγ (peroxisome proliferator activator receptor γ ) that induces G2/M arrest and enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. It also acts as an antagonist of PPARγ that suppresses breast cancer cell proliferation and motility via both PPARgamma-dependent and -independent mechanisms.
Nat Commun, 2024, 15(1):1429
Cell Discov, 2023, 9(1):54
Cell Discov, 2023, 9(1):54
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.
Autophagy, 2023, 19(11):2912-2933
Autophagy, 2023, 19(11):2912-2933
Elife, 2023, 12e74903
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.
Cancer Discov, 2023, 13(4):880-909
Blood Cancer J, 2023, 13(1):42
iScience, 2023, 25(7)
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), 2024, 16(2)370
Cancer Res, 2023, 83(3):456-470
Mol Ther Nucleic Acids, 2023, 31:309-323
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.
Cells, 2024, 13(4)304
Cell Rep, 2023, 42(10):113017
J Biol Chem, 2023, S0021-9258(23)01969-5
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.
Breast Cancer Res, 2022, 24(1):41
Biomedicines, 2021, 9(5)579
Chembiochem, 2021, 22(12):2177-2181
S7891 CC-115 CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity.
Cells, 2024, 13(4)304
Mol Ther Nucleic Acids, 2023, 31:309-323
Biochim Biophys Acta Gene Regul Mech, 2023, 1866(2):194939
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.
Genome Biol, 2024, 25(1):58
bioRxiv, 2024, 2024.01.03.574002
Nat Commun, 2023, 14(1):4761
S8322 Samotolisib (LY3023414) LY3023414 (Samotolisib, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
Exp Ther Med, 2023, 25(1):19
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
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
PLoS One, 2016, 11(10):e0164895
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.
Mol Ther Nucleic Acids, 2023, 31:309-323
Cell Biol Int, 2022, 10.1002/cbin.11833
Oncotarget, 2017, 8(58):98471-98481
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.
Theranostics, 2023, 13(3):1130-1149
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.
Front Oncol, 2023, 13:1287444
Int J Mol Sci, 2021, 22(19)10512
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.
S1105 LY294002 LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKcs を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。
Cell Rep Med, 2024, 5(2):101420
Biomed Pharmacother, 2024, 172:116259
Stem Cell Reports, 2024, 19(2):196-210
S2758 Wortmannin Wortmannin 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.
Nat Commun, 2024, 15(1):451
J Exp Med, 2023, 220(9)e20230054
Autophagy, 2023, 19(4):1164-1183
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.
Nucleic Acids Res, 2024, gkad1224
Theranostics, 2024, 14(4):1561-1582
Genes Dev, 2024, 38(1-2):70-94
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.
J Transl Med, 2023, 21(1):89
Anticancer Drugs, 2023, 34(4):519-531
Cancer Cell, 2022, S1535-6108(22)00312-9
S2871 T0070907 T0070907 is a potent inhibitor of PPARγ (peroxisome proliferator activator receptor γ ) that induces G2/M arrest and enhances the effect of radiation in human cervical cancer cells through mitotic catastrophe. It also acts as an antagonist of PPARγ that suppresses breast cancer cell proliferation and motility via both PPARgamma-dependent and -independent mechanisms.
Nat Commun, 2024, 15(1):1429
Cell Discov, 2023, 9(1):54
Cell Discov, 2023, 9(1):54
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.
Autophagy, 2023, 19(11):2912-2933
Autophagy, 2023, 19(11):2912-2933
Elife, 2023, 12e74903
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.
Cancer Discov, 2023, 13(4):880-909
Blood Cancer J, 2023, 13(1):42
iScience, 2023, 25(7)
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), 2024, 16(2)370
Cancer Res, 2023, 83(3):456-470
Mol Ther Nucleic Acids, 2023, 31:309-323
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.
Cells, 2024, 13(4)304
Cell Rep, 2023, 42(10):113017
J Biol Chem, 2023, S0021-9258(23)01969-5
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.
Breast Cancer Res, 2022, 24(1):41
Biomedicines, 2021, 9(5)579
Chembiochem, 2021, 22(12):2177-2181
S7891 CC-115 CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity.
Cells, 2024, 13(4)304
Mol Ther Nucleic Acids, 2023, 31:309-323
Biochim Biophys Acta Gene Regul Mech, 2023, 1866(2):194939
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.
Genome Biol, 2024, 25(1):58
bioRxiv, 2024, 2024.01.03.574002
Nat Commun, 2023, 14(1):4761
S8322 Samotolisib (LY3023414) LY3023414 (Samotolisib, GTPL8918) is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
Exp Ther Med, 2023, 25(1):19
Cold Spring Harb Mol Case Stud, 2022, 8(1)a006140
Cell, 2021, 184(25):6119-6137.e26
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
PLoS One, 2016, 11(10):e0164895
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.
Mol Ther Nucleic Acids, 2023, 31:309-323
Cell Biol Int, 2022, 10.1002/cbin.11833
Oncotarget, 2017, 8(58):98471-98481
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.
Theranostics, 2023, 13(3):1130-1149
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.
Front Oncol, 2023, 13:1287444
Int J Mol Sci, 2021, 22(19)10512
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.

DNA-PK阻害剤の選択性比較

DNA-PKシグナル伝達経路

DNA-PKシグナル伝達経路
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