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DNA-PK

The DNA-dependent protein kinase (DNA-PK) is a serine/threonine protein kinase consisting of a catalytic subunit (DNA-PKcs) and a Ku heterodimer that is made up of the Ku70 and Ku80 subunits. DNA-PK was accidentally discovered after researchers studying translation found that double-stranded DNA (dsDNA) contaminated their preparations, leading to the phosphorylation of specific proteins.

  • LY294002
    T2008154447-36-6
    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.
    • $34
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  • Nedisertib
    TQ00311637542-33-6
    Nedisertib (M3814) (M3814) is a specific inhibitor of DNA-dependent Protein Kinase (DNA-PK, IC50: <3 nM).
    • $58
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  • PIK-75
    T2667372196-67-3
    PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).
    • $38
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  • IC 86621
    T9760404009-40-1
    IC 86621 is a selective and reversible ATP-competitive inhibitor of DNA-PK with an IC50 of 120 nM. IC 86621 increases DNA double-strand break(DSB)-induced antitumor activity with an EC50 of 68 µM for DNA-PK mediated cellular DSB repair.
    • $35
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  • STL127705
    T130171326852-06-5In house
    STL127705 (Compound L) is a potent Ku 70/80 heterodimer protein inhibitor and inhibits Ku70/80-DNA interaction with IC50 of 3.5 μM. STL127705 inhibits the activation of Ku-dependent DNA-PKCS kinase with IC50 of 2.5 μM.
    • $116
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  • Wortmannin
    T628319545-26-7
    Wortmannin (SL-2052) is a PI3K inhibitor (IC50=3 nM) that is covalent and irreversible. Wortmannin is also an inhibitor of PlK1 and PlK3 (IC50=5.8/48 nM) that blocks autophagy.
    • $32
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  • OSI-027
    T6319936890-98-1
    OSI-027 (ASP4786) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.
    • $35
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  • Torin 2
    T61001223001-51-1
    Torin 2(IC50=0.25 nM), a specific and effective mTOR inhibitor, is the 800-fold greater specific activity for mTOR than PI3K and improves pharmacokinetic properties. The EC50 of Torin 2 for ATM/ATR/DNA-PK inhibition is 28 nM/35 nM/118 nM, respectively.
    • $35
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  • Torin 1
    T60451222998-36-8
    Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
    • $30
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  • KU-57788
    T6276503468-95-9
    NU7441 (KU-57788 (NU7441)) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM).
    • $34
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  • KU-55933
    T2685587871-26-9
    KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
    • $43
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  • Compound 401
    T3586168425-64-7
    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.
    • $34
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  • DMNB
    T863720357-25-9
    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.
    • $41
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  • NU6027
    T6612220036-08-8
    NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.
    • $38
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  • CC-115
    T35411228013-15-7
    CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
    • $38
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  • Voxtalisib
    T7014934493-76-2
    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.
    • $32
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  • KU-0060648
    T6557881375-00-4
    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.
    • $54
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  • PIK-90
    T2461677338-12-4
    PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .
    • $39
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  • AZD 6482
    T60871173900-33-8
    AZD 6482 (AZD6482) is a potent and selective p110β inhibitor with IC50 of 0.69 nM and a PI3Kβ inhibitor with IC50 of 10 nM.
    • $31
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  • ZL-2201
    T786452865115-39-3
    ZL-2201 is a potent inhibitor of DNA-PK, demonstrating an IC50 value of 1 nM.
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  • Samotolisib
    T68831386874-06-1
    Samotolisib (LY3023414) is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. Samotolisib (LY3023414) has been used in trials studying the treatment of Neoplasm, Solid Tumor, COLON CANCER, BREAST CANCER, and Advanced Cancer, among others.
    • $30
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  • AZD-7648
    T71222230820-11-6
    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.
    • $34
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  • PI3K-IN-1
    T18261349796-36-6
    PI3K-IN-1 (Voxtalisib Analogue) is a dual inhibitor of mTOR/PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR.
    • $30
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  • Pictilisib dimethanesulfonate
    T11381957054-33-0
    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).
    • $32
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  • PI-103
    T6143371935-74-9
    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).
    • $52
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  • (Rac)-Nedisertib
    T126721637542-34-7
    (Rac)-Nedisertib is a racemate of Nedisertib, a potent inhibitor of DNA-PK(IC50 of <3 nM).
    • $1,520
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  • LTURM34
    T157891879887-96-3
    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 .
    • $64
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  • ETP-45658
    T253991198357-79-7
    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). Also inhibits DNA-PK and mTOR (IC50 values are 70.6 and 152 nM respectively).
    • $64
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  • PI-3065
    T2083955977-50-1
    PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
    • $32
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  • SF2523
    T39861174428-47-7
    SF2523 is a highly selective and potent inhibitor.
    • $31
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  • DNA-PK-IN-10
    T791652919315-89-0
    DNA-PK-IN-10 is a DNA-PK inhibitor utilized in the research of breast cancer and non-small cell lung cancer [1].
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  • NU 7026
    T2433154447-35-5
    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 against both ATM and ATR.
    • $33
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  • BAY-8400
    T9498
    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 combination with targeted alpha therapies. BAY-8400 can be used for the research of cancer [1].
    • $128
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  • PIK-93
    T2616593960-11-3
    PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
    • $37
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  • Onatasertib
    T33511228013-30-6
    Onatasertib (CC223) is an orally available mTOR inhibitor with potential antitumor activity. Onatasertib inhibits the activity of mTOR, which may result in the induction of tumor cell apoptosis and a decrease in tumor cell proliferation. Onatasertib is a potent mTOR kinase inhibitor (IC50: 16 nM), with >150-fold sensitivity than the related lipid kinase PI3Kα (IC50: 4 μM).
    • $35
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  • Pilaralisib analogue
    T2377956958-53-5
    Pilaralisib analogue (XL147 analogue) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ.
    • $32
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  • Leniolisib
    T51661354690-24-6
    Leniolisib (CDZ173) (CDZ173) is a potent and selective PI3Kδ inhibitor (IC50: 11 nM).
    • $72
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  • (R)-(-)-Rolipram
    T1344885416-75-7
    (R)-(-)-Rolipram ((-)-Rolipram) is an R-enantiomer of Rolipram which is a PDE4 inhibitor.
    • $39
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  • YU238259
    T43391943733-16-1
    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.
    • $40
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  • PIK-75 hydrochloride
    T2287372196-77-5
    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.
    • $36
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  • ETP-46464
    T20841345675-02-6
    ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
    • $34
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