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NU7441(KU-57788),DNA-PK抑制剂, 蛋白激酶抑制剂；DNA 激活；催化亚基

强效选择性DNA-PK抑制剂
1篇引用文献
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货号 (SKU) 包装规格 是否现货 价格 数量
K126842-5mg
 5mg 现货 Stock Image
K126842-25mg
 25mg 现货 Stock Image
K126842-100mg
 100mg 现货 Stock Image
大包装询价 添加到收藏夹 比较  SDS中文版  DATASHEET
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Cell Cycle/DNA Damage (2603) CRISPR/Cas9 (10) DNA-PK (29) PI3K/Akt/mTOR (764) protein kinase，DNA-activated，catalytic subunit Inhibitor (15)
main product photo

基本描述

英文别名 SCHEMBL8246439 | A6548 | NU7441 | NU-7441 | SMR004702957 | MLS006011188 | NU-7441 (KU-57788) | NU7441 (KU-57788) | 8-(Dibenzo[b,D]thiophen-4-Yl)-2-(Morpholin-4-Yl)-4h-Chromen-4-One | GTPL8010 | 8-dibenzothiophene-4-yl-2-morpholin-4-yl-chromen-4-on | FT-06
规格或纯度 Moligand™, ≥98%
英文名称 NU7441 (KU-57788)
生化机理 高效的选择性DNA-PK抑制剂（IC50 = 14 nM）。对包括mTOR，PI 3-K，ATM和ATR在内的多种激酶具有选择性的DNA-PK。增强了阿霉素和依托泊苷的体外和体内依托泊苷的作用。还可以将CRISPR-Cas9介导的同源性定向修复（HDR）效率提高2至3倍，并降低非同源末端连接（NHEJ）频率〜40％。
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 蛋白激酶抑制剂；DNA 激活；催化亚基
产品介绍

KU-57788(NU7441)是DNA-PK选择性抑制剂，IC50为14 nM，对mTOR，PI3K，ATM和ATR的抑制性较弱。A DNA-PK inhibitor, and antitumor agent in vitro.

NU7441 (KU-57788) is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 μM in cell-free assays.
A DNA-PK inhibitor, and antitumor agent in vitro.

关联靶点（人）

BRD4 Tchem 含溴结构域蛋白 4(Bromodomain-containing protein 4) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
PRKDC Tchem DNA依赖性蛋白激酶催化亚基(DNA-dependent protein kinase catalytic subunit) (9 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
PIK3CB Tchem 磷脂酰肌醇 4,5-双磷酸 3-激酶催化亚基 β 异构体(Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KCNH2 Tclin HERG (29587 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKDC Tchem DNA-dependent protein kinase (1929 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PKN2 Tchem Protein kinase N2 (1991 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RAF1 Tclin Serine/threonine-protein kinase RAF (4169 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SYK Tclin Tyrosine-protein kinase SYK (7372 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPKAPK2 Tchem MAP kinase-activated protein kinase 2 (4814 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPKAPK5 Tchem MAP kinase-activated protein kinase 5 (2831 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ROCK2 Tclin Rho-associated protein kinase 2 (6206 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CD Tclin PI3-kinase p110-delta subunit (6699 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MTOR Tclin Serine/threonine-protein kinase mTOR (13850 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 (4127 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BLK Tchem Tyrosine-protein kinase BLK (2498 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FYN Tclin Tyrosine-protein kinase FYN (5308 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LYN Tclin Tyrosine-protein kinase Lyn (4251 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA2 Tchem Ribosomal protein S6 kinase alpha 2 (2184 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CG Tclin PI3-kinase p110-gamma subunit (5411 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ZAP70 Tchem Tyrosine-protein kinase ZAP-70 (2189 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CB Tchem PI3-kinase p110-beta subunit (4044 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SGK1 Tchem Serine/threonine-protein kinase Sgk1 (2343 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
YES1 Tclin Tyrosine-protein kinase YES (2781 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ATM Tchem Serine-protein kinase ATM (4198 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ATR Tchem Serine-protein kinase ATR (986 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
5637 (630 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A 172 (535 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A204 (242 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A2058 (690 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A-375 (9258 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A-427 (643 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A498 (42825 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A673 (619 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ACHN (49357 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AGS (1999 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BT-20 (503 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BT-474 (2113 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BXPC-3 (2997 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
C8166 (1658 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CAKI-1 (44928 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Calu-3 (339 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Calu-6 (398 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CAPAN-1 (772 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

PIK3CA PI3-kinase p110-alpha subunit (51 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
H4 (48 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hsf1 Heat shock factor protein 1 (5445 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasma (328 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Vero C1008 (1716 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

分子类型 小分子
IUPAC Name 8-dibenzothiophen-4-yl-2-morpholin-4-ylchromen-4-one
INCHI InChI=1S/C25H19NO3S/c27-21-15-23(26-11-13-28-14-12-26)29-24-17(6-3-9-20(21)24)19-8-4-7-18-16-5-1-2-10-22(16)30-25(18)19/h1-10,15H,11-14H2
InChi Key JAMULYFATHSZJM-UHFFFAOYSA-N
Canonical SMILES C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC5=C4SC6=CC=CC=C56
Isomeric SMILES C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC5=C4SC6=CC=CC=C56
PubChem CID 11327430
分子量 413.49

化学和物理性质

溶解性 溶于DMSO, 最高浓度 (mg/mL): 2.07, 最高浓度(mM): 5 温和加热
密度 1.4
折光率 1.73
沸点 ~646.9° C at 760 mmHg
熔点 246.28°C
分子量 413.500 g/mol
XLogP3 5.500
氢键供体数Hydrogen Bond Donor Count 0
氢键受体数Hydrogen Bond Acceptor Count 5
可旋转键计数Rotatable Bond Count 2
精确质量Exact Mass 413.109 Da
单同位素质量Monoisotopic Mass 413.109 Da
拓扑极表面积Topological Polar Surface Area 67.000 Ų
重原子数Heavy Atom Count 30
形式电荷Formal Charge 0
复杂度Complexity 690.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性（GHS）

 SDS英文版

技术规格说明书

Purity(HPLC) 98-100（%）
Appearance（K126842) White to off-white solid
NMR spectrum Conforms to Structure

 技术规格说明书

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批号(Lot Number) 证书类型 日期 货号
E1708069 分析证书 22-12-08 K126842

此产品的引用文献

如何在您的发表作品中引用阿拉丁的产品和网站?
1. Zhao Mengjie, Li Yanhui, Lu Chenfei, Ding Fangshu, Xu Miao, Ge Xin, Li Mengdie, Wang Zhen, Yin Jianxing, Zhang Junxia, Wang Xiefeng, Ge Zehe, Xiao Hong, Xiao Yong, Liu Hongyi, Liu Wentao, Cao Yuandong, Wang Qianghu, You Yongping, Wang Xiuxing, Yang Kun, Shi Zhumei, Qian Xu.  (2023)  PGC1α Degradation Suppresses Mitochondrial Biogenesis to Confer Radiation Resistance in Glioma.  CANCER RESEARCH,  83  (7): (1094-1110).  [PMID:36696363] [10.1158/0008-5472.CAN-22-3083]

参考文献

1. Leahy JJ, Golding BT, Griffin RJ, Hardcastle IR, Richardson C, Rigoreau L, Smith GC.  (2004)  Identification of a highly potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor (NU7441) by screening of chromenone libraries..  Bioorg Med Chem Lett,  14  (24): (6083-7).  [PMID:15546735] [10.1021/op500134e]
2. Zhao Y, Thomas HD, Batey MA, Cowell IG, Richardson CJ, Griffin RJ, Calvert AH, Newell DR, Smith GC, Curtin NJ.  (2006)  Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441..  Cancer Res,  66  (10): (5354-62).  [PMID:16707462] [10.1021/op500134e]
3. Smith GC, Jackson SP.  (1999)  The DNA-dependent protein kinase..  Genes Dev,  13  (8): (916-34).  [PMID:10215620] [10.1021/op500134e]
4. Kodama M, Murakami M, Kodama T.  (1997)  Differential implications of the oncogene-tumor suppressor gene complex in the geneses of 19 human neoplasias. Evidence in support of the steroid carcinogenesis hypothesis..  Anticancer Res,  17  (3C): (2285-92).  [PMID:9216703] [10.1021/op500134e]
5. Rosenzweig KE, Youmell MB, Palayoor ST, Price BD.  (1997)  Radiosensitization of human tumor cells by the phosphatidylinositol3-kinase inhibitors wortmannin and LY294002 correlates with inhibition of DNA-dependent protein kinase and prolonged G2-M delay..  Clin Cancer Res,  3  (7): (1149-56).  [PMID:9815794] [10.1021/op500134e]
6. Zhao Mengjie, Li Yanhui, Lu Chenfei, Ding Fangshu, Xu Miao, Ge Xin, Li Mengdie, Wang Zhen, Yin Jianxing, Zhang Junxia, Wang Xiefeng, Ge Zehe, Xiao Hong, Xiao Yong, Liu Hongyi, Liu Wentao, Cao Yuandong, Wang Qianghu, You Yongping, Wang Xiuxing, Yang Kun, Shi Zhumei, Qian Xu.  (2023)  PGC1α Degradation Suppresses Mitochondrial Biogenesis to Confer Radiation Resistance in Glioma.  CANCER RESEARCH,  83  (7): (1094-1110).  [PMID:36696363] [10.1158/0008-5472.CAN-22-3083]

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