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DNA Damage/DNA Repair DNA-PK

DNA-PK

DNA-dependent protein kinase, catalytic subunit, also known as DNA-PKcs, is an enzyme that in humans is encoded by the gene designated as PRKDC or XRCC7. DNA-PKcs belongs to the phosphatidylinositol 3-kinase-related kinase protein family. The DNA-Pkcs protein is a serine/threonine protein kinase comprising a single polypeptide chain of 4,128 amino acids.DNA-PKcs is the catalytic subunit of a nuclear DNA-dependent serine/threonine protein kinase called DNA-PK. The second component is the autoimmune antigen Ku. On its own, DNA-PKcs is inactive and relies on Ku to direct it to DNA ends and trigger its kinase activity. DNA-PKcs is required for the non-homologous end joining (NHEJ) pathway of DNA repair, which rejoins double-strand breaks. It is also required for V(D)J recombination.
Cat No. product name
T1826 Voxtalisib Analogue Voxtalisib (SAR245409, XL765)Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ ,also inhibits DNA-PK and mTOR.
T1859 AZD8055HOT AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.
T2083 PI3065 PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
T2084 ETP46464 ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
T2287 PIK-75 hydrochloride PIK-75 Hydrochloride is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inh...
T2377 XL147 analogue XL147 analogue is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ.
T2433 NU7026 NU7026 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...
T2616 PIK-93 PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
T2667 PIK75 PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).
T2685 KU55933 KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
T3351 CC-223 CC-223 is an orally available mTOR inhibitor with potential antitumor activity. CC-223 inhibits the activity of mTOR, which may result in the induction of tumor...
T3541 CC-115 CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
T3586 Compound 401 Compound 401 is a synthetic DNA-PK inhibitor (IC50 = 0.28 μM) that also targets mTOR but not PI3K.
T3986 SF2523 SF2523 is a highly selective and potent inhibitor.
T6045 Torin 1 Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
T6087 AZD6482 AZD 6482 is a potent and selective p110β inhibitor with IC50 of 0.69 nM and a PI3Kβ inhibitor with IC50 of 10 nM.
T6100 Torin 2 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 proper...
T6143 PI-103HOT 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).
T6276 NU7441HOT NU7441 (KU-57788) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM).
T6319 OSI-027 OSI-027 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 PI...
T6557 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 I...
T6612 NU6027 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-amino...
T6883 LY3023414 LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. LY3023414 has been used in trials studying the treatment of Neopl...
T7014 Voxtalisib Voxtalisib (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.
T4339 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.
T7122 AZD-7648 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.
TQ0031 Nedisertib Nedisertib (M3814) is a specific inhibitor of DNA-dependent Protein Kinase (DNA-PK, IC50: <3 nM).
T2461 PIK-90 PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .
T6283 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM, with little selectivity within the PI3K family. Also blocks autophagosome formation and pot...
T5166 Leniolisib Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor (IC50: 11 nM).
T2008 LY294002HOT LY294002 is an inhibitor of PI3K (IC50s: 0.5/0.57/0.97 μM for PI3Kα/δ/β in cell-free assays). It also blocks autophagosome formation.
T2414 TorkinibHOT Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).
T12672 (Rac)-Nedisertib (Rac)-Nedisertib is a racemate of Nedisertib, a potent inhibitor of DNA-PK(IC50 of <3 nM).
T13448 (R)-(-)-Rolipram (R)-(-)-Rolipram is the R-enantiomer of Rolipram. Rolipram is a selective inhibitor of phosphodiesterases PDE4(IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B,...
T15799 LY-2940094 LY-2940094 decreases ethanol self-administration in animal models. LY-2940094 is an effective, selective, and orally available nociceptin receptor antagonist wi...
Voxtalisib Analogue
T1826CAS 1349796-36-6
Voxtalisib (SAR245409, XL765)Analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ ,also inhibits DNA-PK and mTOR.
AZD8055 HOT
T1859CAS 1009298-09-2
AZD8055 is an ATP-competitive mTOR inhibitor (IC50: 0.8 nM in MDA-MB-468 cells). It is ~1,000-fold selective for mTOR over all PI3K isoforms.
PI3065
T2083CAS 955977-50-1
PI-3065 is a novel potent and selective PI3K p110δ inhibitor.
ETP46464
T2084CAS 1345675-02-6
ETP-46464 is an effective and specific ATR inhibitor (IC50: 25 nM).
PIK-75 hydrochloride
T2287CAS 372196-77-5
PIK-75 Hydrochloride is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inh...
XL147 analogue
T2377CAS 956958-53-5
XL147 analogue is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ.
NU7026
T2433CAS 154447-35-5
NU7026 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...
PIK-93
T2616CAS 593960-11-3
PIK-93 is the first potent, synthetic PI4K inhibitor with IC50 of 19 nM; inhibits PI3Kα with IC50 of 39 nM.
PIK75
T2667CAS 372196-67-3
PIK-75, a DNA-PK and PI3K inhibitor, suppresses DNA-PK(IC50=2 nM), p110α(IC50=5.8 nM) and p110γ(IC50=76 nM).
KU55933
T2685CAS 587871-26-9
KU-55933 (ATM Kinase Inhibitor) is a potent and specific ATM inhibitor.
CC-223
T3351CAS 1228013-30-6
CC-223 is an orally available mTOR inhibitor with potential antitumor activity. CC-223 inhibits the activity of mTOR, which may result in the induction of tumor...
CC-115
T3541CAS 1228013-15-7
CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).
Compound 401
T3586CAS 168425-64-7
Compound 401 is a synthetic DNA-PK inhibitor (IC50 = 0.28 μM) that also targets mTOR but not PI3K.
SF2523
T3986CAS 1174428-47-7
SF2523 is a highly selective and potent inhibitor.
Torin 1
T6045CAS 1222998-36-8
Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.
AZD6482
T6087CAS 1173900-33-8
AZD 6482 is a potent and selective p110β inhibitor with IC50 of 0.69 nM and a PI3Kβ inhibitor with IC50 of 10 nM.
Torin 2
T6100CAS 1223001-51-1
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 proper...
PI-103 HOT
T6143CAS 371935-74-9
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).
NU7441 HOT
T6276CAS 503468-95-9
NU7441 (KU-57788) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM).
OSI-027
T6319CAS 936890-98-1
OSI-027 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 PI...
KU-0060648
T6557CAS 881375-00-4
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 I...
NU6027
T6612CAS 220036-08-8
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-amino...
LY3023414
T6883CAS 1386874-06-1
LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. LY3023414 has been used in trials studying the treatment of Neopl...
Voxtalisib
T7014CAS 934493-76-2
Voxtalisib (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.
YU238259
T4339CAS 1943733-16-1
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.
AZD-7648
T7122CAS 2230820-11-6
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.
Nedisertib
TQ0031CAS 1637542-33-6
Nedisertib (M3814) is a specific inhibitor of DNA-dependent Protein Kinase (DNA-PK, IC50: <3 nM).
PIK-90
T2461CAS 677338-12-4
PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) .
Wortmannin
T6283CAS 19545-26-7
Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM, with little selectivity within the PI3K family. Also blocks autophagosome formation and pot...
Leniolisib
T5166CAS 1354690-24-6
Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor (IC50: 11 nM).
LY294002 HOT
T2008CAS 154447-36-6
LY294002 is an inhibitor of PI3K (IC50s: 0.5/0.57/0.97 μM for PI3Kα/δ/β in cell-free assays). It also blocks autophagosome formation.
Torkinib HOT
T2414CAS 1092351-67-1
Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).
(Rac)-Nedisertib
T12672CAS 1637542-34-7
(Rac)-Nedisertib is a racemate of Nedisertib, a potent inhibitor of DNA-PK(IC50 of <3 nM).
(R)-(-)-Rolipram
T13448CAS 85416-75-7
(R)-(-)-Rolipram is the R-enantiomer of Rolipram. Rolipram is a selective inhibitor of phosphodiesterases PDE4(IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B,...
LY-2940094
T15799CAS 1307245-86-8
LY-2940094 decreases ethanol self-administration in animal models. LY-2940094 is an effective, selective, and orally available nociceptin receptor antagonist wi...