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Products are for research use only. Not for human use. We do not sell to patients.
(KU 57788; NU-7441; KU57788; NU7441; NU 7441)
KU-57788 Chemical Structure
|Product name: KU-57788|
|Cat. No.: HY-11006|
KU-57788(NU7441) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor with IC50 value of are 14 nM; 1700, 5000, >100000 and >100000 nM for mTOR, PI 3K, ATM and ATR respectively; also is a modest inhibitor of BRD4 and BRDT with IC50s of 1 and 3.5 uM respectively.
IC50 value: 14 nM (DNA-PK); 1/3.5 uM(BRD4/BRDT) 
Target: DNA-PK; BRD4/BRDT
in vitro: NU7441 increased the cytotoxicity of ionizing radiation and etoposide in SW620, LoVo, and V3-YAC cells but not in V3 cells, confirming that potentiation was due to DNA-PK inhibition. NU7441 substantially retarded the repair of ionizing radiation-induced and etoposide-induced DSB. NU7441 appreciably increased G(2)-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells . NU7441 strongly inhibited DNA-PK in cell lines (IC(50) = 0.3 μM) but only weakly inhibited PI3 K (IC(50) = 7 μM). NU7441 caused doxorubicin- and IR-induced DNA DSBs (measured by γ-H2AX foci) to persist and also slightly decreased homologous recombination activity, as assessed by Rad51 foci . NU7441 is a modest inhibitor of BRD4 and BRDT (IC50 = 1 and 3.5 SM, respectively), which establishes a single hydrogen bond in the KAc site through the chromenone oxygen with Asn140 .
in vivo: In mice bearing SW620 xenografts, NU7441 concentrations in the tumor necessary for chemopotentiation in vitro were maintained for at least 4 hours at nontoxic doses. NU7441 increased etoposide-induced tumor growth delay 2-fold without exacerbating etoposide toxicity to unacceptable levels .
|M.Wt||413.49||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥4.8mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
|1 mg||5 mg||10 mg|
|1 mM||2.4184 mL||12.0922 mL||24.1844 mL|
|5 mM||0.4837 mL||2.4184 mL||4.8369 mL|
|10 mM||0.2418 mL||1.2092 mL||2.4184 mL|
. Leahy JJ, 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.
. Tavecchio M, et al. Further characterisation of the cellular activity of the DNA-PK inhibitor, NU7441, reveals potential cross-talk with homologous recombination. Cancer Chemother Pharmacol. 2012 Jan;69(1):155-64.
BMS-509744 is a cell-permeable aminothioaryl-thiazolo compound that potently inhibits ITK kinase activity (IC50 = 19 nM; [ATP] = 1 (mu)M) in an ATP-competitive manner by stabilizing ITK activation loop in a substrate-blocking, inactive conformation, inhibiti
ITK inhibitor is a potent ITK inhibitor.