nu7026


Catalog No. size PriceQuantity
M112-2S 2 mg solid $129
M112-10S 10mg solid $516

Description

Product Information
Molecular Weight: 281.31
Formula: C17H15NO3
Purity: >98%
CAS#: 154447-35-5
Solubility: DMSO: 2.8 mg/mL (Need ultrasonic)
Chemical Name: 2-morpholino-4H-benzo[h]chromen-4-one
Storage: Powder -20oC 3 years 4oC 2 years In solvent -80oC 6 months -20oC 1 month

Biological Activity:


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.

How to use:

In Vitro:  NU7026 (10 μM) potentiates ionizing radiation (IR) cytotoxicity [potentiation factor at 90% cell kill (PF90)=1.51±0.04] in exponentially growing DNA-PK proficient but not deficient cells[1]. NU7026 synergistically sensitizes I83 cells to Chlorambucil (CLB) 3.5-fold[2].NU7026, a novel inhibitor of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). At a dose of 10 μM, which is nontoxic to cells per se, a minimum NU7026 exposure of 4 h in combination with 3 Gy radiation is required for a significant radiosensitisation effect in CH1 human ovarian cancer cells[3].

In Vivo: NU7026, a novel inhibitor of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). Following intravenous administration to mice at 5 mg/kg, NU7026 underwent rapid plasma clearance (0.108 L/h) and this is largely attributed to extensive metabolism. Bioavailability following interperitoneal (i.p.) and p.o. administration at 20 mg/kg is 20 and 15%, respectively[3].

Reference:

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.

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