货号 | 3712/50 |
别名 | 8-(4-Dibenzothienyl)-2-(4-morpholin |
供应商 | Tocris |
生物活性 | 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 of doxorubicin (Cat. No. 2252) and etoposide (Cat. No. 1226) in vitro and etoposide in vivo. Also enhances CRISPR-Cas9-mediated homology-directed repair (HDR) efficiency 2 to 3-fold, and decreases nonhomologous end-joining (NHEJ) frequency ~40%. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >99 % |
计算分子量 | 413.49 |
分子式 | C25H19NO3S |
可溶性/溶解性 | Soluble to 5 mM in DMSO with gentle warming |
CAS号 | 503468-95-9 |
参考文献 | Robertet al (2015) Pharmacological inhibition of DNA-PK stimulates Cas9-mediated genome editing. Genome Med. 7 93. PMID: 26307031. Willmoreet al (2008) DNA-dependent protein kinase is a therapeutic target and an indicator of poor prognosis in B-cell chronic lymphocytic leukemia. Clin.Cancer Res. 14 3984. PMID: 18559621. Zhaoet al (2006) Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441. Cancer Res. 66 5354. PMID: 16707462. Leahyet al (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 6083. PMID: 15546735. |