DNA-PK

Cat. No.

A11098

CAS No.

503468-95-9

NU-7441 (KU-57788)

Synonyms: KU57788

NU-7441 (KU-57788) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor. The IC50 values are 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively.

Cat. No.

A10726

CAS No.

371935-74-9

PI-103

PI-103 is a potent, cell-permeable, ATP-competitive inhibitor of phosphatidylinositol 3-kinase (PI3K) family members with selectivity toward DNA-PK, PI3K (p110α), and mTOR.

Cat. No.

A12752

CAS No.

154447-35-5

NU7026

NU7026 is a novel DNA-dependent protein kinase inhibitor that potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia.

Cat. No.

A10729

CAS No.

372196-77-5

PIK-75 hydrochloride

PIK-75 is an imidazopyridine that selectively inhibits p110α with an IC50 value of 5.8 nM.2 It inhibits p110γ and p110β considerably less effectively with IC50 values of 0.076 μM and 1.3 μM, respectively.

Cat. No.

A13328

CAS No.

1345675-02-6

ETP-46464

ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.

Cat. No.

A11778

CAS No.

168425-64-7

Compound 401

Compound 401 is a cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (IC50 = 5.3 μM).

Cat. No.

A13224

CAS No.

881375-00-4

KU 0060648

KU0060648 is a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases. KU-0060648 enhances HDR efficiency and attenuates NHEJ frequency.

Cat. No.

A14136

CAS No.

220036-08-8

NU6027

NU6027 is a potent inhibitor of cellular ATR activity (IC(50)=6.7 μM) and enhanced hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.

Cat. No.

A15779

CAS No.

1228013-15-7

CC-115

CC-115 is a inhibitor of mTOR/DNA-PK (IC50= 21/ 13 nM).

Cat. No.

A17055

CAS No.

1637542-33-6

Nedisertib

Synonyms: MSC2490484A; M3814

Nedisertib, also known as M-3814, MSC2490484A, is an orally available inhibitor of DNA-dependent protein kinase (DNA-PK), with potential antineoplastic and chemo/radiosensitizing activities.

Cat. No.

A18410

CAS No.

1326852-06-5

STL127705

STL127705 is a Ku 70/80 heterodimer protein inhibitor, inhibits Ku70/80-DNA interaction, with an IC50 of 3.5 μM.

Cat. No.

A19994

CAS No.

1879887-96-3

LTURM34

LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines.

Cat. No.

A20049

CAS No.

2230820-11-6

AZD-7648

AZD-7648 is a potent and selective DNA-PK inhibitor. Anti-tumor activity.

Cat. No.

A20614

CAS No.

1943733-16-1

YU238259

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

Cat. No.

A21383

CAS No.

1637542-34-7

(Rac)-Nedisertib

Synonyms: (Rac)-M3814; M 3814

(Rac)-Nedisertib ((Rac)-M3814) is a racemate of Nedisertib, a potent DNA-PK inhibitor, with an IC50 of

Cat. No.

A30438

CAS No.

372196-67-3

PIK-75

PIK-75 is a selective inhibitor of DNA-PK and p110α, exhibiting IC50 values of 2 nM and 5.8 nM, respectively, while demonstrating over 200-fold greater potency against p110α compared to p110β (IC50 = 1.3 μM). This compound effectively induces apoptosis, making it a valuable tool for research in cancer biology and therapies targeting DNA repair pathways. Its specificity for these kinases facilitates investigations into their roles in cellular processes and potential therapeutic interventions.

Cat. No.

A31120

CAS No.

404009-40-1

IC 86621

IC 86621 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 of 120 nM, acting as a selective and reversible ATP-competitive inhibitor. This compound impedes DNA-PK mediated repair of DNA double-strand breaks (DSB), displaying an EC50 of 68 µM. IC 86621 enhances antitumor activity in the presence of DSBs without inducing cytotoxicity and provides protection against apoptosis in T cells from rheumatoid arthritis. Its applications extend to cancer research and the study of immune responses in autoimmune disorders.

Cat. No.

A54076

CAS No.

2595308-10-2

XRD-0394

XRD-0394 is a highly potent and orally active inhibitor of ATM and DNA-PKcs, exhibiting IC50 values of 0.39 nM and 0.89 nM, respectively. This compound demonstrates selectivity for its target enzymes over other members of the PIKK and PI3K families. In preclinical studies, XRD-0394 has been shown to significantly enhance the cytotoxic effects of ionizing radiation on tumor cells both in vitro and in vivo. Additionally, it can synergize with PARP and topoisomerase I inhibitors, making it a valuable tool for research in cancer treatment and DNA repair mechanisms.

Cat. No.

A54584

CAS No.

79105-88-7

NU-7031

NU-7031 is a coumarin derivative that selectively inhibits DNA-PK with an IC50 of 1.7 μM. This compound is utilized in cancer research to investigate DNA repair mechanisms and therapeutic strategies targeting DNA damage response pathways. Its role as a DNA-PK inhibitor makes it a valuable tool for understanding the implications of DNA repair in tumor biology.

Cat. No.

A54585

CAS No.

1300118-55-1

CC-115 hydrochloride

CC-115 hydrochloride is a potent dual inhibitor of DNA-PK and mTOR, exhibiting IC50 values of 13 nM and 21 nM, respectively. It effectively disrupts signaling pathways associated with both mTORC1 and mTORC2. This compound is valuable for research focused on cancer therapeutics and the modulation of DNA damage response mechanisms.

Cat. No.

A54586

CAS No.

1476074-39-1

VX-984

Synonyms: M9831

VX-984 is a potent and selective DNA-PK inhibitor that effectively penetrates the blood-brain barrier. It disrupts the non-homologous end joining (NHEJ) repair pathway, leading to an increase in DNA double-strand breaks (DSBs). This compound has significant research applications in the study of glioblastomas (GBM) and non-small cell lung cancer (NSCLC). Ideal for investigations into cancer therapy and DNA damage response mechanisms.

Cat. No.

A54587

CAS No.

2763602-59-9

BAY-8400

BAY-8400 is a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), with an IC50 of 81 nM. This orally active compound is primarily employed in cancer research, where it can help elucidate DNA repair mechanisms and investigate therapeutic strategies targeting DNA damage response pathways.

Cat. No.

A54589

CAS No.

2792146-91-7

DNA-PK-IN-12

DNA-PK-IN-12 is a potent DNA-PK inhibitor, displaying an IC50 of 0.1 nM. This compound effectively inhibits cell growth and Hct116 cell colony formation with an IC50 of 33.28 μM. Additionally, DNA-PK-IN-12 demonstrates significant antitumor activity in vivo, making it a valuable reagent for cancer research and therapeutic studies.

Cat. No.

A54590

CAS No.

404009-46-7

AMA-37

AMA-37 is an ATP-competitive inhibitor of DNA-dependent protein kinase (DNA-PK), demonstrating an IC50 value of 0.27 μM for this target. In addition, it shows moderate inhibitory activity against phosphoinositide 3-kinase isoforms with IC50 values of 32 μM for p110α, 3.7 μM for p110β, and 22 μM for p110γ. This compound is suitable for research applications focusing on DNA repair mechanisms and cancer therapeutics, where modulation of DNA-PK activity may be beneficial.

Cat. No.

A54592

CAS No.

2865115-39-3

ZL-2201

ZL-2201 is a potent inhibitor of DNA-dependent protein kinase (DNA-PK) with an IC50 value of 1 nM. This compound plays a critical role in the study of DNA repair mechanisms and cellular responses to DNA damage. It is valuable for researchers investigating cancer biology, therapeutic resistance, and the modulation of DNA repair pathways.