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Results for "

DNA-PK inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	DNA-PK (43) DNA/RNA Synthesis (1) Apoptosis (10) ATM/ATR (7) Autophagy (6) Bcr-Abl (1) c-Met/HGFR (1) Casein Kinase (1) CRISPR/Cas9 (1) EGFR (1) Epigenetic Reader Domain (1) mTOR (13) PDGFR (1) PI3K (16) Src (1) VEGFR (1)
By Research Areas:	Cancer (50) Infection (1) Inflammation/Immunology (2)

Inhibitors & Agonists

Screening Libraries

Isotope-Labeled Compounds

Targets Recommended: DNA-PK DNA Methyltransferase DNA Stain DNA Alkylator/Crosslinker DNA/RNA Synthesis

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12030

PIK-90 3 Publications Verification	PI3K DNA-PK	Cancer
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.

HY-101667

LTURM34 4 Publications Verification	DNA-PK	Cancer
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 .

HY-100706

AMA-37	DNA-PK	Cancer
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 .

HY-163134

DNA-PK-IN-12	DNA-PK	Cancer
DNA-PK-IN-12 (compound 31t) is an oral active *DNA-PK* inhibitor with the IC₅₀ of 0.1 nM. DNA-PK-IN-12 inhibits cell growth and Hct116 cell colony formation with the IC₅₀ of 33.28 μM, and shows antitumor activity in vivo .

HY-142943

DNA-PK-IN-1	DNA-PK	Cancer
DNA-PK-IN-1 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-1 has the potential for the research of cancer diseases (extracted from patent WO2021136463A1, compound 1) .

HY-142944

DNA-PK-IN-2	DNA-PK	Cancer
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) .

HY-153943

DNA-PK-IN-10	DNA-PK	Cancer
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 .

HY-146566

DNA-PK-IN-9	DNA-PK	Cancer
DNA-PK-IN-9 (compound YK6) is a potent DNA-dependent protein kinase (DNA-PK) inhibitor with an IC₅₀ value of 10.47 nM. DNA-PK-IN-9 can be used for researching anticancer .

HY-162692

DNA-PK-IN-14	DNA-PK	Cancer
DNA-PK-IN-14 (compound 78) is a potent, selective *DNA-PK* inhibitor with an IC₅₀ value of 7.95 nM. DNA-PK-IN-14 has oral activity and has the potential to be a radiosensitizer for cancer treatment .

HY-144036

DNA-PK-IN-3	DNA-PK	Cancer
DNA-PK-IN-3 is a potent inhibitor of *DNA-PK. DNA-PK-IN-3 synergistically enhances the effect of radiotherapy and chemotherapy and effectively inhibits* tumor growth. DNA-PK-IN-3 also effectively reduces the damage to normal cells and reducing side effects. DNA-PK-IN-3 has the potential for the research of cancer disease (extracted from patent WO2021213460A1, compound 4) .

HY-144037

DNA-PK-IN-4	DNA-PK	Cancer
DNA-PK-IN-4 is a potent inhibitor of *DNA-PK. DNA-PK-IN-4 is a imidazolinone derivative compound. DNA-PK-IN-4 inhibits* DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-4 has the potential for the research of cancer disease (extracted from patent WO2021209055A1, compound 27) .

HY-19939S2

(R)-VX-984 (R)-M9831	DNA-PK	Others
(R)-VX-984 is the (R)-enantiomer of VX-984. VX-984 is a potent DNA-PK inhibitor.

HY-142471A

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

HY-158166

DNA-PK-IN-13	DNA-PK	Inflammation/Immunology Cancer
DNA-PK-IN-13 (Compound SK10) is a *DNA-PK* inhibitor that exhibits potent inhibitory activity (IC₅₀= 0.11 nM). DNA-PK-IN-13 regulates tumor cell proliferation by decreasing the expression level of γH2A.X and enhancing the sensitivity of tumor cells to chemotherapeutic agents. DNA-PK-IN-13 is suitable for oncology studies .

HY-142471

ZL-2201 free base	DNA-PK	Cancer
ZL-2201 free base is a potent *DNA-PK* inhibitor with an IC₅₀ of 1 nM (WO2021104277A1, compound 5) .

HY-13431

KU-0060648 2 Publications Verification	DNA-PK PI3K mTOR	Cancer
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 .

HY-19341

Compound 401 1 Publications Verification	DNA-PK	Cancer
Compound 401 is a synthetic inhibitor of *DNA-PK* (IC₅₀ = 0.28 μM) that also targets mTOR but not PI3K in vitro.

HY-101570

Nedisertib 15+ Cited Publications Peposertib; M3814	DNA-PK	Cancer
Nedisertib (M3814) is a potent, orally available and selective inhibitor of *DNA-PK, with an IC₅₀* of <3 nM. Anti-tumor activity .

HY-146565

DNA-PK-IN-8	DNA-PK	Cancer
DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC₅₀ value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin .

HY-144039

DNA-PK-IN-6	DNA-PK	Cancer
DNA-PK-IN-6 is a potent inhibitor of *DNA-PK. DNA-PK-IN-6 inhibits* DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-6 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021197159A1, compound 6) .

HY-144038

DNA-PK-IN-5	DNA-PK	Cancer
DNA-PK-IN-5 is a potent inhibitor of *DNA-PK. DNA-PK-IN-5 inhibits* DNA-PKcs activity, thus greatly reducing tumor DNA repair and inducing cells to enter the apoptotic program. DNA-PK-IN-5 enhances the sensitivity of tumor tissues to radiotherapy, overcomes the problem of agent resistance, and enhances the inhibitory effect on a variety of solid tumors and hematological tumors (extracted from patent WO2021204111A1, compound 2) .

HY-114923

SU-11752	DNA-PK PI3K	Cancer
SU-11752 is an inhibitor for DNA-dependent protein kinase (DNA-PK) with an IC₅₀ of 0.13 μM. SU-11752 inhibits PI3K p110γ kinase with IC₅₀ of 1.1 μM. SU-11752 binds competitively for ATP-site in DNA-PK, results in inhibition of intracellular DNA double-strand break repair and increases the sensitivity of cells to radiotherapy .

HY-100707

IC 86621	DNA-PK Apoptosis	Inflammation/Immunology Cancer
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 .

HY-15719

NU 7026 10+ Cited Publications LY293646	DNA-PK Apoptosis	Cancer
NU 7026 (LY293646) is a novel specific *DNA-PK* inhibitor with IC₅₀ of 0.23 μM, also inhibits PI3K with IC₅₀ of 13 μM.

HY-18650

KU 59403	ATM/ATR	Cancer
KU 59403 is a potent ATM inhibitor, with IC₅₀ values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively .

HY-111783

AZD-7648 15+ Cited Publications	DNA-PK ATM/ATR PI3K Apoptosis	Cancer
AZD-7648 is a potent, orally active, selective *DNA-PK* inhibitor with an IC₅₀ of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity .

HY-13281

PIK-75 hydrochloride 4 Publications Verification	DNA-PK PI3K Apoptosis	Cancer
PIK-75 hydrochloride 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 hydrochloride inhibits p110α >200-fold more potently than p110β (IC₅₀=1.3 μM) . PIK-75 hydrochloride induces apoptosis .

HY-107834

PIK-75 4 Publications Verification	DNA-PK PI3K Apoptosis	Cancer
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) . PIK-75 induces apoptosis .

HY-10108

LY294002 Maximum Cited Publications 769 Publications Verification	PI3K Casein Kinase DNA-PK Apoptosis Autophagy	Infection Cancer
LY294002 is a broad-spectrum inhibitor of PI3K with IC₅₀s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively . LY294002 also inhibits CK2 with an IC₅₀ of 98 nM . LY294002 is a competitive *DNA-PK* inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC₅₀ of 1.4?μM. LY294002 is an apoptosis activator .

HY-16962

CC-115 2 Publications Verification	DNA-PK mTOR	Cancer
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.

HY-16962A

CC-115 hydrochloride 2 Publications Verification	DNA-PK mTOR	Cancer
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.

HY-132293

BAY-8400 2 Publications Verification	DNA-PK	Cancer
BAY-8400 is an orally active, potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (IC₅₀=81 nM). BAY-8400 can be used for the research of cancer .

HY-12513

Samotolisib 5+ Cited Publications LY3023414	PI3K DNA-PK mTOR Autophagy	Cancer
Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, *DNA-PK, and mTORC1/2* with IC₅₀s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations .

HY-12016

KU-55933 35+ Cited Publications	ATM/ATR Autophagy	Cancer
KU-55933 is a potent ATM inhibitor with an IC₅₀ and K_i of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.

HY-101146

SF2523 2 Publications Verification	PI3K Epigenetic Reader Domain DNA-PK	Cancer
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.

HY-147567

ATR-IN-15	ATM/ATR DNA-PK PI3K	Cancer
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 .

HY-116621

NU-7163	DNA-PK	Cancer
NU-7163 is an ATP-competitive *DNA-PK* inhibitor (IC₅₀=0.19 μM; K_i=24 nM). NU-7163 enhances the cytotoxicity of ionizing radiation against the HeLa human tumor cell line in vitro .

HY-11006

KU-57788 25+ Cited Publications NU7441	DNA-PK CRISPR/Cas9	Cancer
KU-57788 (NU7441) is a highly potent and selective *DNA-PK* inhibitor with an IC₅₀ of 14 nM. KU-57788 is an NHEJ pathway inhibitor. KU-57788 also inhibits PI3K and mTOR with IC₅₀s of 5.0 and 1.7 μM, respectively .

HY-13002

Torin 2 10+ Cited Publications	mTOR DNA-PK Autophagy Apoptosis	Cancer
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.

HY-19939S

VX-984 4 Publications Verification M9831	DNA-PK	Cancer
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .

HY-16124

Canfosfamide TLK-286; TER286	DNA-PK Apoptosis	Cancer
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 .

HY-151915

ATR-IN-20	ATM/ATR mTOR	Cancer
ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC₅₀ of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC₅₀ of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects .

HY-139609

Camonsertib RP-3500; ATR inhibitor 4	ATM/ATR mTOR	Cancer
Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC₅₀ of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC₅₀=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity .

HY-15268

PP487	c-Met/HGFR PI3K DNA-PK mTOR Bcr-Abl Src VEGFR EGFR PDGFR	Cancer
PP487 is a dual inhibitor of tyrosine kinase/PI(3)Ks with IC₅₀ values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against *DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR*, respectively. PP487 can be used for cancer research .

HY-10115

PI-103 20+ Cited Publications	PI3K mTOR DNA-PK Autophagy Apoptosis	Cancer
PI-103 is a potent PI3K and mTOR inhibitor with IC₅₀s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits *DNA-PK* with an IC50 of 2 nM. PI-103 induces autophagy .

HY-10115A

PI-103 Hydrochloride 20+ Cited Publications	PI3K mTOR DNA-PK Autophagy Apoptosis	Cancer
PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC₅₀s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits *DNA-PK* with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy .

HY-150279

PolQi2	DNA/RNA Synthesis	Others
PolQi2 is a PolΘ inhibitor that targets and inhibits alt-EJ (alternative end-joining) repair by inhibiting the helicase domain at the N-terminus of PolΘ. PolQi2 enhances the precision and integration efficiency of gene editing at different loci and in various cell lines. Furthermore, the combined use of PolQi2 with DNA-PK inhibitors reduces the off-target effects of Cas9, significantly improving the fidelity and performance of CRISPR/Cas9 gene editing. PolQi2 can be used in gene editing research .

HY-15900

Voxtalisib 5 Publications Verification XL765; SAR245409	PI3K mTOR	Cancer
Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC₅₀s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC₅₀=150 nM) and mTOR (IC₅₀=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC₅₀s of 160 and 910 nM, respectively.

HY-110109

ETP-45658	PI3K DNA-PK mTOR	Cancer
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 .

HY-10116

PI-540	PI3K mTOR	Cancer
PI-540 is a bicyclic thienopyrimidine derivative and an orally active PI3K inhibitor. PI-540 has anti-cancer cell proliferation properties and high tissue distribution. PI-540 can inhibit different isoforms of PI3K, with IC₅₀s of 10 nM (P110α), 3510 nM (P110β), 410 nM (P110δ), and 33110 nM (P110γ). PI-540 also inhibits mTOR (IC₅₀: 61 nM) and DNA-PK (IC₅₀: 525 nM) .

Cat. No.	Product Name

HY-L015

PI3K/Akt/mTOR Compound Library

616 compounds

The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials.

MCE owns a unique collection of 616 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

Cat. No.	Product Name	Chemical Structure

HY-19939S2

(R)-VX-984
(R)-VX-984 is the (R)-enantiomer of VX-984. VX-984 is a potent DNA-PK inhibitor.

HY-19939S

VX-984 4 Publications Verification
VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .

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