NU-7026
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406408

CAS#: 154447-35-5

Description: NU-7026 is a potent DNA-PK inhibitor with potential anticancer activity.


Chemical Structure

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NU-7026
CAS# 154447-35-5

Theoretical Analysis

MedKoo Cat#: 406408
Name: NU-7026
CAS#: 154447-35-5
Chemical Formula: C17H15NO3
Exact Mass: 281.11
Molecular Weight: 281.306
Elemental Analysis: C, 72.58; H, 5.37; N, 4.98; O, 17.06

Price and Availability

Size Price Availability Quantity
5mg USD 270
25mg USD 540
50mg USD 970
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Synonym: NU7026; NU-7026; NU 7026.

IUPAC/Chemical Name: 2-morpholino-4H-benzo[h]chromen-4-one

InChi Key: KKTZALUTXUZPSN-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H15NO3/c19-15-11-16(18-7-9-20-10-8-18)21-17-13-4-2-1-3-12(13)5-6-14(15)17/h1-6,11H,7-10H2

SMILES Code: O=C1C=C(N2CCOCC2)OC3=C1C=CC4=CC=CC=C43

Appearance: yellow solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:         

Product Data:
Biological target: NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.
In vitro activity: NU7026 (10 micro M) potentiated IR cytotoxicity [potentiation factor at 90% cell kill (PF(90)) = 1.51 +/- 0.04] in exponentially growing DNA-PK proficient but not deficient cells. When NU7026 and AG14361 were used in combination, their potentiating effects were additive (e.g., PF(90) = 2.81 +/- 0.19 in PARP-1(+/+) cells). Reference: Cancer Res. 2003 Sep 15;63(18):6008-15. https://pubmed.ncbi.nlm.nih.gov/14522929/
In vivo activity: In mice, the local application of the specific DNA-PK inhibitor NU7026 via thermosensitive Pluronic F-127 gel around dilated arteries significantly reduced the phosphorylation of YB-1. Reference: Arterioscler Thromb Vasc Biol. 2023 Feb;43(2):300-311. https://pubmed.ncbi.nlm.nih.gov/36475703/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 2.1 7.48

Preparing Stock Solutions

The following data is based on the product molecular weight 281.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Liu YY, Zhang WY, Zhang ML, Wang YJ, Ma XY, Jiang JH, Wang R, Zeng DX. DNA-PKcs participated in hypoxic pulmonary hypertension. Respir Res. 2022 Sep 16;23(1):246. doi: 10.1186/s12931-022-02171-x. PMID: 36114572; PMCID: PMC9479248. 2. Veuger SJ, Curtin NJ, Richardson CJ, Smith GC, Durkacz BW. Radiosensitization and DNA repair inhibition by the combined use of novel inhibitors of DNA-dependent protein kinase and poly(ADP-ribose) polymerase-1. Cancer Res. 2003 Sep 15;63(18):6008-15. PMID: 14522929. 3. Nöthen T, Sarabi MA, Weinert S, Zuschratter W, Morgenroth R, Mertens PR, Braun-Dullaeus RC, Medunjanin S. DNA-Dependent Protein Kinase Mediates YB-1 (Y-Box Binding Protein)-Induced Double Strand Break Repair. Arterioscler Thromb Vasc Biol. 2023 Feb;43(2):300-311. doi: 10.1161/ATVBAHA.122.317922. Epub 2022 Dec 8. PMID: 36475703.
In vitro protocol: 1. Liu YY, Zhang WY, Zhang ML, Wang YJ, Ma XY, Jiang JH, Wang R, Zeng DX. DNA-PKcs participated in hypoxic pulmonary hypertension. Respir Res. 2022 Sep 16;23(1):246. doi: 10.1186/s12931-022-02171-x. PMID: 36114572; PMCID: PMC9479248. 2. Veuger SJ, Curtin NJ, Richardson CJ, Smith GC, Durkacz BW. Radiosensitization and DNA repair inhibition by the combined use of novel inhibitors of DNA-dependent protein kinase and poly(ADP-ribose) polymerase-1. Cancer Res. 2003 Sep 15;63(18):6008-15. PMID: 14522929.
In vivo protocol: 1. Nöthen T, Sarabi MA, Weinert S, Zuschratter W, Morgenroth R, Mertens PR, Braun-Dullaeus RC, Medunjanin S. DNA-Dependent Protein Kinase Mediates YB-1 (Y-Box Binding Protein)-Induced Double Strand Break Repair. Arterioscler Thromb Vasc Biol. 2023 Feb;43(2):300-311. doi: 10.1161/ATVBAHA.122.317922. Epub 2022 Dec 8. PMID: 36475703.

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1: Tu Y, Yang B, Ji C, Yang Z, Gu H, Lu CC, Wang R, Su ZL, Chen B, Sun WL, Xia JP, Bi ZG, He L. DNA-dependent protein kinase catalytic subunit (DNA-PKcs)-SIN1 association mediates ultraviolet B (UVB)-induced Akt Ser-473 phosphorylation and skin cell survival. Mol Cancer. 2013 Dec 24;12(1):172. [Epub ahead of print] PubMed PMID: 24365180.

2: Tichy A, Durisova K, Salovska B, Pejchal J, Zarybnicka L, Vavrova J, Dye NA, Sinkorova Z. Radio-sensitization of human leukaemic MOLT-4 cells by DNA-dependent protein kinase inhibitor, NU7441. Radiat Environ Biophys. 2013 Oct 8. [Epub ahead of print] PubMed PMID: 24100951.

3: Chiang JH, Yang JS, Lu CC, Hour MJ, Liu KC, Lin JH, Lee TH, Chung JG. Effect of DNA damage response by quinazolinone analogue HMJ-38 on human umbilical vein endothelial cells: Evidence for γH2A.X and DNA-PK-dependent pathway. Hum Exp Toxicol. 2013 Sep 23. [Epub ahead of print] PubMed PMID: 24064905.

4: Zhou X, Zhang X, Xie Y, Tanaka K, Wang B, Zhang H. DNA-PKcs inhibition sensitizes cancer cells to carbon-ion irradiation via telomere capping disruption. PLoS One. 2013 Aug 27;8(8):e72641. doi: 10.1371/journal.pone.0072641. PubMed PMID: 24013362; PubMed Central PMCID: PMC3754927.

5: Bee L, Fabris S, Cherubini R, Mognato M, Celotti L. The efficiency of homologous recombination and non-homologous end joining systems in repairing double-strand breaks during cell cycle progression. PLoS One. 2013 Jul 11;8(7):e69061. doi: 10.1371/journal.pone.0069061. Print 2013. PubMed PMID: 23874869; PubMed Central PMCID: PMC3708908.

6: Li Y, Wang X, Yue P, Tao H, Ramalingam SS, Owonikoko TK, Deng X, Wang Y, Fu H, Khuri FR, Sun SY. Protein phosphatase 2A and DNA-dependent protein kinase are involved in mediating rapamycin-induced Akt phosphorylation. J Biol Chem. 2013 May 10;288(19):13215-24. doi: 10.1074/jbc.M113.463679. Epub 2013 Mar 27. PubMed PMID: 23536185; PubMed Central PMCID: PMC3650361.

7: Okazawa S, Furusawa Y, Kariya A, Hassan MA, Arai M, Hayashi R, Tabuchi Y, Kondo T, Tobe K. Inactivation of DNA-dependent protein kinase promotes heat-induced apoptosis independently of heat-shock protein induction in human cancer cell lines. PLoS One. 2013;8(3):e58325. doi: 10.1371/journal.pone.0058325. Epub 2013 Mar 11. PubMed PMID: 23505488; PubMed Central PMCID: PMC3594312.

8: Weingeist DM, Ge J, Wood DK, Mutamba JT, Huang Q, Rowland EA, Yaffe MB, Floyd S, Engelward BP. Single-cell microarray enables high-throughput evaluation of DNA double-strand breaks and DNA repair inhibitors. Cell Cycle. 2013 Mar 15;12(6):907-15. doi: 10.4161/cc.23880. Epub 2013 Feb 19. PubMed PMID: 23422001; PubMed Central PMCID: PMC3637349.

9: You H, Kong MM, Wang LP, Xiao X, Liao HL, Bi ZY, Yan H, Wang H, Wang CH, Ma Q, Liu YQ, Bi YY. Inhibition of DNA-dependent protein kinase catalytic subunit by small molecule inhibitor NU7026 sensitizes human leukemic K562 cells to benzene metabolite-induced apoptosis. J Huazhong Univ Sci Technolog Med Sci. 2013 Feb;33(1):43-50. doi: 10.1007/s11596-013-1069-z. Epub 2013 Feb 8. PubMed PMID: 23392706.

10: Urushihara Y, Kobayashi J, Matsumoto Y, Komatsu K, Oda S, Mitani H. DNA-PK inhibition causes a low level of H2AX phosphorylation and homologous recombination repair in Medaka (Oryzias latipes) cells. Biochem Biophys Res Commun. 2012 Dec 14;429(3-4):131-6. doi: 10.1016/j.bbrc.2012.10.128. Epub 2012 Nov 7. PubMed PMID: 23142596.