KU-57788 NEW
| Price | $34 | $54 | $90 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-12 |
Product Details
| Product Name: KU-57788 | CAS No.: 503468-95-9 |
| Purity: 99.87% | Supply Ability: 10g |
| Release date: 2024/11/12 |
Product Introduction
Bioactivity
| 名稱 | KU-57788 |
| 描述 | NU7441 (KU-57788 (NU7441)) is a highly effective and specific DNA-PK inhibitor (IC50: 14 nM). |
| 細(xì)胞實驗 | Cells were irradiated with 290 MeV/n carbon ions (LET: 50 keV/μm) at the Heavy Ion Medical Accelerator in Chiba. The dose rate for carbon ions was 1 Gy/min. X‐ray irradiation was performed using a TITAN‐320 (200 kV, 20 mA) at a dose rate of 1 Gy/min. NU7441 was dissolved in DMSO and stored at ?20°C in a freezer. Cells were pretreated with NU7441 1 h before irradiation, and the drug was kept throughout the experiment [1]. |
| 動物實驗 | All in vivo experiments were reviewed and approved by the relevant institutional animal welfare committees and done according to national law. We determined the plasma pharmacokinetics after administering NU7441 i.v. at 5 mg/kg in 10% DMSO/10% cyclodextrin in saline or i.p. or orally at 10 mg/kg (dissolved at 1 mg/mL in 40% PEG400/saline) to female BALB/c mice. These were the maximum administrable doses by the route used due to the limit of solubility of NU7441. Mice were killed at intervals up to 360 minutes after NU7441 administration; blood was taken and immediately centrifuged, and the plasma fraction was removed and stored at ?20°C [5]. |
| 體外活性 | 0.3 μM of KU-57788 (NU7441), nontoxic to both normal and tumor cells, caused a significant radio-sensitization in tumor cells exposed to X-rays and carbon ions. This concentration did not seem to cause inhibition of DNA DSB repair but induced a significant G2/M arrest [1]. The addition of NU7441 to cells following introduction of the Cas9/sgGFP editing system and the ΔGFP repair template caused a decrease of approximately 40 % in NHEJ events which was accompanied by an approximately two-fold stimulation in HDR. This effect was dose-dependent and reached a maximum at approximately 2.0 μM for NU7441 [2]. NU7441 reduced the CCK-8 counts in the HepG2 culture, further enhanced 60Cox03B3; radiation injury to HepG2 cells, which was manifested by decreasing the DNA-PKcs (S2056) protein expression, increasing x03B3 [3]. Even though RPA p34 is still localized into foci following UV-irradiation and inhibitor treatment, treatment of cells with NU7441 eliminates staining for hyperphosphorylated RPA p34 [4]. |
| 體內(nèi)活性 | Tumors in control mice reached four times their starting volume (RTV4) at a median time of 5.6 days. Treatment with etoposide phosphate alone caused a tumor growth delay of 2.7 days, which was extended to 5.4 days by coadministration of NU7441 [5]. |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 1 mg/ml, Sonication is recommended. |
| 關(guān)鍵字 | inhibit | DNA-dependent protein kinase | NU-7441 | Inhibitor | NU 7441 | KU-57788 | CRISPR/Cas9 | KU 57788 | DNA-PK | KU57788 |
| 相關(guān)產(chǎn)品 | PI-3065 | Compound 401 | STL127705 | YU238259 | PI3K-IN-1 | Samotolisib | Torin 1 | NU6027 | PI-103 | Nocodazole | Onatasertib | LY294002 |
| 相關(guān)庫 | PI3K/Akt/mTOR 化合物庫 | 神經(jīng)再生化合物庫 | 表型篩選靶點鑒定庫 | 抗胰腺癌化合物庫 | 經(jīng)典已知活性庫 | 抗抑郁癥化合物庫 | 激酶抑制劑庫 | 抑制劑庫 | 抗衰老化合物庫 | 已知活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
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