DNA-PKcs (DNA-dependent protein kinase, catalytic subunit) is an enzyme that in humans is encoded by the PRKDC gene. DNA-PKcs belongs to the phosphatidylinositol 3-kinase-related kinase protein family. 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. Many proteins have been identified as substrates for the kinase activity of DNA-PK. Autophosphorylation of DNA-PKcs appears to play a key role in NHEJ and is thought to induce a conformational change that allows end processing enzymes to access the ends of the double-strand break. DNA-PK also cooperates with ATR and ATM to phosphorylate proteins involved in the DNA damage checkpoint.


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15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
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NF-κB >
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PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
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Protein Tyrosine Kinase/RTK >
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Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
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Vitamin D Related >
VD/VDR
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NU5455

NU5455 is a potent, selective, and orally active inhibitor of DNA-PKcs. NU5455 administration increases both the efficacy and the toxicity of a parenterally administered topoisomerase inhibitor. NU5455 enhances the activity of Doxorubicin released locally in liver tumor xenografts without inducing any adverse effect[1].

  • CAS Number: 1257235-99-6
  • MF: C34H33N3O5S
  • MW: 595.71
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VX-984

VX-984 is a potent DNA-PKinhibitor.

  • CAS Number: 1476074-39-1
  • MF: C23H21D2N7O
  • MW: 415.49
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Wortmannin

Wortmannin is a multi-target inhibitor of PI3K and MLCK with IC50s of 3 nM and 200 nM, respectively. Wortmannin is also a potent inhibitor of DNA-PK (IC50, 16 nM) and ATM (IC50, 150 nM). Wortmannin is also a potent inhibitor of Polo-like kinase (Plk).

  • CAS Number: 19545-26-7
  • MF: C23H24O8
  • MW: 428.432
  • Catalog: ATM/ATR
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 615.6±55.0 °C at 760 mmHg
  • Melting Point: 234-240ºC
  • Flash Point: 326.1±31.5 °C

(2R)-L-gamma-Glutamyl-3-((2-((bis(bis(2-chloroethyl)amino)phosphinyl)oxy) ethyl)sulfonyl)- L-alanyl-2-phenylglycine

Canfosfamide (TLK-286, TER286) is a glutathione analogue prodrug that is activated by glutathione S-transferase P1-1 and induces apoptosis. Canfosfamide also inhibits the catalytic kinase activity of DNA-dependent protein kinase (DNA-PK). Canfosfamide produces an anticancer alkylating agent and a glutathione derivative after activation. Canfosfamide can be used to research malignancies[1][2][3].

  • CAS Number: 158382-37-7
  • MF: C26H40Cl4N5O10PS
  • MW: 787.47400
  • Catalog: Apoptosis
  • Density: 1.484g/cm3
  • Boiling Point: 939.8ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 522.2ºC

(Rac)-Nedisertib

Rac-Nedisertib (Rac-M3814) is a racemate of Nedisertib, a potent DNA-PK inhibitor, with an IC50 of <3 nM[1].

  • CAS Number: 1637542-34-7
  • MF: C24H21ClFN5O3
  • MW: 481.91
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

M3814

M3814 is a potent and selective inhibitor of DNA-dependent Protein Kinase (DNA-PK).

  • CAS Number: 1637542-33-6
  • MF: C24H21ClFN5O3
  • MW: 481.91
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(R)-Nedisertib

(R)-Nedisertib ((R)-M3814) is a less active R-enantiomer of Nedisertib, with an IC50 in the range of 7-30 nM for DNA-PK[1].

  • CAS Number: 1637542-32-5
  • MF: C24H21ClFN5O3
  • MW: 481.91
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DNA-PK-IN-10

DNA-PK-IN-10 is a DNA-PK inhibitor. DNA-PK-IN-10 can be used for the research of breast cancer and non-small cell lung cancer[1].

  • CAS Number: 2919315-89-0
  • MF: C25H28N6O2
  • MW: 444.53
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ATR-IN-15

ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC50 of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC50 values of 47, 663 and 5131 nM, respectively[1].

  • CAS Number: 2756665-52-6
  • MF: C19H22N8O
  • MW: 378.43
  • Catalog: ATM/ATR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AMA-37

AMA-37, an Arylmorpholine analog, is ATP-competitive DNA-PK inhibitor, with IC50 values of 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ), respectively[1][2].

  • CAS Number: 404009-46-7
  • MF: C17H17NO3
  • MW: 283.32200
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NU7026

NU 7026 is a novel specific DNA-PK inhibitor with IC50 of 0.23±0.01 μM, also inhibits PI3K with IC50 of 13±3 μM.

  • CAS Number: 154447-35-5
  • MF: C17H15NO3
  • MW: 281.306
  • Catalog: DNA-PK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 459.9±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 231.9±28.7 °C

ZL-2201

ZL-2201 is a potent DNA-PK inhibitor with an IC50 of 1 nM (WO2021104277A1, compound 5)[1].

  • CAS Number: 2865115-39-3
  • MF: C20H25N9O5S
  • MW: 503.53
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

YU238259

YU238259 is an inhibitor of homology-dependent DNA repair (HDR), used for cancer research.

  • CAS Number: 1943733-16-1
  • MF: C22H22ClN3O4S
  • MW: 459.9525
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1-(2-hydroxy-4-morpholin-4-ylphenyl)ethanone

IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis[1][2].

  • CAS Number: 404009-40-1
  • MF: C12H15NO3
  • MW: 221.252
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 425.5±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 211.1±28.7 °C

CC-115

CC-115 is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.

  • CAS Number: 1228013-15-7
  • MF: C16H16N8O
  • MW: 336.35100
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PIK-75

PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM)[1][2]. PIK-75 induces apoptosis[3].

  • CAS Number: 372196-67-3
  • MF: C16H14BrN5O4S
  • MW: 452.283
  • Catalog: Apoptosis
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ETP-45658

ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer[1][2].

  • CAS Number: 1198357-79-7
  • MF: C16H17N5O2
  • MW: 311.34
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Compound L

STL127705 (Compound L) is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM. STL127705 also inhibits Ku-dependent activation of DNA-PKCS kinase (IC50, 2.5 μM)[1].

  • CAS Number: 1326852-06-5
  • MF: C22H20FN5O4
  • MW: 437.42
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AZD-7648

AZD-7648 is a potent and selective DNA-PK inhibitor. Anti-tumour activity[1].

  • CAS Number: 2230820-11-6
  • MF: C18H20N8O2
  • MW: 380.40
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NU7441 (KU-57788)

KU-57788 is a potent and selective inhibitor of DNA-PK with an IC50 of 13 nM, with selectivity over a range of kinases including mTOR, PI 3-K, ATM and ATR.

  • CAS Number: 503468-95-9
  • MF: C25H19NO3S
  • MW: 413.488
  • Catalog: CRISPR/Cas9
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 646.9±55.0 °C at 760 mmHg
  • Melting Point: 246.28° C
  • Flash Point: 345.0±31.5 °C

SF2523

SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

  • CAS Number: 1174428-47-7
  • MF: C19H17NO5S
  • MW: 371.414
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Compound 401

Compound 401 is a synthetic inhibitor of DNA-PK (IC50 = 0.28 μM) that also targets mTOR but not PI3K in vitro.

  • CAS Number: 168425-64-7
  • MF: C16H15N3O2
  • MW: 281.309
  • Catalog: DNA-PK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 456.9±55.0 °C at 760 mmHg
  • Melting Point: 214 °C
  • Flash Point: 230.1±31.5 °C

DNA-PK-IN-7

DNA-PK-IN-7 is a potent DNA-PK inhibitor with an IC50 of 1 nM (WO2021104277A1, compound 5)[1].

  • CAS Number: 2646592-18-7
  • MF: C19H21N9O2
  • MW: 407.43
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VX-984

VX-984 (M9831) is a selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 of 88±64 nM for A549 lung cancer cells.

  • CAS Number: 1562396-65-9
  • MF: C22H19D2N7O
  • MW: 401.46
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PIK-75 HCl

PIK-75 is a DNA-PK and PI3K inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM).

  • CAS Number: 372196-77-5
  • MF: C16H15BrClN5O4S
  • MW: 488.74
  • Catalog: DNA-PK
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Torin 2

Torin 2 is an mTOR inhibitor with EC50 of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC50: 200 nM). Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.

  • CAS Number: 1223001-51-1
  • MF: C24H15F3N4O
  • MW: 432.397
  • Catalog: Autophagy
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 623.7±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 331.0±31.5 °C

DNA-PK-IN-2

DNA-PK-IN-2 is a potent inhibitor of DNA-PK. DNA-dependent protein kinase (DNA-PK) is a DNA-PK enzyme complex composed of Ku70/Ku80 heterodimer and DNA-dependent protein kinase catalytic subunit (DNA-PKcs). DNA-PK-IN-2 has the potential for the research of cancer diseases (extracted from patent WO2021136462A1, compound 1)[1].

  • CAS Number: 2665720-22-7
  • MF: C20H23N5O3
  • MW: 381.43
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PIK-90

PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.

  • CAS Number: 677338-12-4
  • MF: C18H17N5O3
  • MW: 351.36
  • Catalog: DNA-PK
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 817.3±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 448.1±34.3 °C

CC-115 hydrochloride

CC-115 hydrochloride is a potent and dual DNA-PK and mTOR kinase inhibitor with IC50s of 13 nM and 21 nM, respectively. CC-115 blocks both mTORC1 and mTORC2 signaling.

  • CAS Number: 1300118-55-1
  • MF: C16H17ClN8O
  • MW: 372.812
  • Catalog: DNA-PK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KU-0060648

KU-0060648 is a dual inhibitor of PI3K and DNA-PK with IC50s of 4 nM, 0.5 nM, 0.1 nM, 0.594 nM and 8.6 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and DNA-PK, respectively[1].

  • CAS Number: 881375-00-4
  • MF: C33H34N4O4S
  • MW: 582.713
  • Catalog: DNA-PK
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 819.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 449.7±34.3 °C