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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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K126842-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $67.90 | |
K126842-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $306.90 | |
K126842-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $525.90 |
Potent and selective DNA-PK inhibitor
Synonyms | 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 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Potent and selective DNA-PK inhibitor (IC50= 14 nM). Selective for DNA-PK over a range of kinases including mTOR, PI 3-K, ATM and ATR. Potentiates the effects ofdoxorubicin andetoposide in vitroand etoposidein vivo. Also enhances CRISPR-Cas9-mediated homo |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of protein kinase; DNA-activated; catalytic subunit |
Note | 卖完停产,不再备货 |
Product Description | 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. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 8-dibenzothiophen-4-yl-2-morpholin-4-ylchromen-4-one |
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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 |
Molecular Weight | 413.49 |
PubChem CID | 11327430 |
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CAS Registry No. | 503468-95-9 |
ChEMBL Ligand | CHEMBL188678 |
RCSB PDB Ligand | 2R4 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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E1708069 | Certificate of Analysis | Dec 08, 2022 | K126842 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 2.07, Max Conc. mM: 5 with gentle warming |
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Refractive Index | 1.73 |
Boil Point(°C) | ~646.9° C at 760 mmHg |
Melt Point(°C) | 246.28°C |
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] |
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] |