貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S80754-5mg	99.9%	￥320.00 S80754-5mg ￥320.00 現(xiàn)貨	2 2	-	-	-
S80754-10mg	99.9%	￥520.00 S80754-10mg ￥520.00 現(xiàn)貨	6 6	-	-	-
S80754-50mg	≥98%	￥1440.00 S80754-50mg ￥1440.00 2-3天	0 貨期：2-3天	-	-	-

產(chǎn)品介紹

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

產(chǎn)品描述：

靶點(diǎn)：

DNA-PK:14 nM (IC50);mTOR:1.7 μM (IC50);PI3K:5.0 μM (IC50);CRISPR/Cas9 ;DNA-PK;CRISPR/Cas9

體內(nèi)研究：

KU-57788 (0.5 to 10 μM) inhibits the growth of liver cancer HepG2 cells dose- and time-dependently. KU-57788 reduces pDNA-PKcs (S2056) protein expression in liver cancer cells. Furthermore, double treatment of KU-57788 and 60Coγ IR affects DNA damage repair. KU-57788 weakly inhibits BRD4 and BRDT with IC50s of 1 μM and 3.5 μM, respectively. KU-57788 is solvent-exposed in BRD4, this inhibitor can be classified as a Type I BRD inhibitor. KU-57788 reduces the frequency of NHEJ while increasing the rate of HDR following Cas9-mediated DNA cleavage

參考文獻(xiàn)：

1. Justin J J Leahy, et al. Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6083-7. 2. Yang C, et al. NU7441 Enhances the Radiosensitivity of Liver Cancer Cells. Cell Physiol Biochem. 2016;38(5):1897-905 3. Hardcastle IR, et al. Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach. J Med Chem. 2005 Dec 1;48(24):7829-46 4. Ember SW, et al. The acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors. ACS Chem Biol. 2014 Feb 25. 5. Robert F, et al. Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 2015 Aug 27;7:93

溶解性：

DMSO : 14.29 mg/mL (34.56 mM; Need ultrasonic)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.418 ml	12.092 ml	24.184 ml
5 mM	0.484 ml	2.418 ml	4.837 ml
10 mM	0.242 ml	1.209 ml	2.418 ml
50 mM	0.048 ml	0.242 ml	0.484 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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批號(hào)：JS298415 貨號(hào)：S20001-25g
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NU7441 (KU-57788)