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DNA Damage/DNA Repair

DNA Alkylator/Crosslinker

Nucleoside Antimetabolite/Analog

PI3K/Akt/mTOR signaling

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.

Filter HomeSignaling PathwaysPI3K/Akt/mTOR signaling-DNA Damage/DNA RepairDNA-PK

LY294002

SF 1101, NSC 697286, LY 294002

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.

Apoptosis Autophagy Casein Kinase DNA-PK PI3K

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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.

Apoptosis ATM/ATR DNA-PK PI3K

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VX-984

M9831

T110671476074-39-1

VX-984 (M9831) is an oral, selective DNA-PK inhibitor that can cross the blood-brain barrier. VX-984 inhibited the conjugation of non-homologous terminal NHEJ and acted on DSBs to break DNA double strand. VX-984 is commonly seen in glioblastoma (GBM) and non-small cell lung cancer (NSC-LC) studies.

DNA-PK

$126

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Wortmannin

SL-2052, KY-12420

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.

Antibiotic ATM/ATR Autophagy DNA-PK PI3K PLK Serine/threonin kinase

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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).

Apoptosis DNA-PK PI3K

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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.

Autophagy DNA-PK mTOR PI3K

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STL127705

Compound L, 7-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]-3-(3-fluorophenyl)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione

T130171326852-06-5In house

STL127705 (Compound L) is a potent inhibitor of the Ku 70/80 heterodimer protein, disrupting Ku70/80-DNA interaction with an IC50 of 3.5 μM, and inhibiting Ku-dependent DNA-PKCS kinase activation with an IC50 of 2.5 μM.

Apoptosis DNA-PK

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Onatasertib

CC-223, CC223, CC 223

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).

Apoptosis c-Fms DNA-PK FLT mTOR PI3K

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KU-55933

ATM Kinase Inhibitor

T2685587871-26-9

KU-55933 (ATM Kinase Inhibitor) is an ATM inhibitor (IC50=12.9 nM; Ki=2.2 nM) that is selective and ATP-competitive. KU-55933 induces apoptosis and has antitumor effects.

ATM/ATR Autophagy DNA-PK mTOR PI3K

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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.

Apoptosis ATM/ATR Autophagy DNA-PK mTOR

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KU-57788

NU7441

T6276503468-95-9

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

CRISPR/Cas9 DNA-PK

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AZD 6482

KIN 193, AZD6482

T60871173900-33-8

AZD 6482 (KIN-193) is a potent and selective inhibitor of p110β and PI3Kβ with IC50 values of 0.69nM and 10nM, respectively. AZD 6482 is particularly effective in blocking AKT signaling and tumor growth dependent on p110β activation or PTEN loss.

Autophagy DNA-PK PI3K

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Samotolisib

LY3023414, GTPL8918

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.

Autophagy DNA-PK mTOR PI3K

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PI-103

PI103, 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).

Apoptosis Autophagy DNA-PK mTOR PI3K

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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) .

DNA-PK PI3K

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NU 7026

NU7026, LY293646, DNA-PK Inhibitor II

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.

Apoptosis ATM/ATR DNA-PK PI3K

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LY-294002 hydrochloride

LY294002 hydrochloride, LY 294002 hydrochloride

T4079934389-88-5

LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.

Apoptosis Casein Kinase DNA-PK PI3K

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KU-0060648

KU0060648

T6557881375-00-4

KU-0060648 is a dual inhibitor of DNA-PK and PI3Kα, PI3Kβ, PI3Kδ with IC50 values of 8.6 nM, 4 nM, 0.5 nM, and 0.1 nM respectively, and demonstrates less inhibition of PI3Kγ with an IC50 of 0.59 μM.

DNA-PK mTOR PI3K

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Leniolisib

CDZ173

T51661354690-24-6

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

DNA-PK PI3K

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OSI-027

OSI027, ASP4786

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.

Autophagy DNA-PK mTOR PI3K

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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.

ATM/ATR CDK DNA-PK

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SF2523

T39861174428-47-7

SF2523 is a highly selective and potent inhibitor (SF2523) with improved physicochemical properties, excellent aqueous solubility, and biological efficacy. It is typically used in genome editing [CRISPR/Cas Solution] technology and can effectively enhance the efficiency of this process.

DNA-PK Epigenetic Reader Domain mTOR PI3K

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BAY-8400

T9498

BAY-8400 is a potent, selective, and orally active DNA-dependent protein kinase (DNA-PK) inhibitor (IC50 = 81 nM) that demonstrates synergistic efficacy when combined with targeted alpha therapies. BAY-8400 is applicable for cancer research [1].

DNA-PK

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