價(jià)格 | ¥346 | ¥498 | ¥897 |
包裝 | 1mg | 2mg | 5mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-12 |
中文名稱(chēng):化合物 YU238259 | 英文名稱(chēng):YU238259 |
CAS:1943733-16-1 | 品牌: TargetMol |
產(chǎn)地: 美國(guó) | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.43% | 產(chǎn)品類(lèi)別: 抑制劑 |
貨號(hào): T4339 |
名稱(chēng) | YU238259 |
描述 | YU238259 is a novel inhibitor of homology-dependent DNA repair(HDR), but does not inhibit non-homologous end-joining (NHEJ), in cell-based GFP reporter assays. |
細(xì)胞實(shí)驗(yàn) | U2OS cells were pretreated with 25 μM YU238259 or DMSO vehicle for 1 h and cells were then irradiated with 10 Gy IR. Cells were fixed at 8 h post-IR, stained with antibodies and Hoechst dye, and imaged. Foci were quantified using the InCell Analyzer algorithm developed by YCMD. Cells were scored as foci-positive if they contained ≥15 foci (BRCA1, pDNA-PK) or ≥20 foci (53BP1). |
激酶實(shí)驗(yàn) | The cloning, expression and purification of USP21 from BL21 (DE3) bacteria are performed using standard molecular biology techniques. USP2, USP5, USP7, USP8, USP28, USP47, Ub-PLA2 (Ub-CHOP) and Ub-EKL (Ub-CHOP2) are generated. Caspase 3 and the caspase 3 substrate DEVD-Rh110 are used. Deubiquitylating enzyme, cathepsin B and 20S proteasome chymotrypsin like protease activities are measured. Caspase 3 activity is determined using a similar protocol. Briefly, dose ranges of compound (including USP7/USP47 inhibitor) are incubated with caspase 3 for 30 minutes before the addition of DEVD-Rh110 and reading on a fluorometric plate reader using excitation and emission maxima of 485 nm and 531 nm respectively. The final concentrations of caspase 3 and DEVD-Rh110 are 2 nM and 100 nM respectively |
動(dòng)物實(shí)驗(yàn) | Animal Models: 069(nu)/070(nu/+) athymic nude mice. Formulation: 3:1 DMSO:PBS. Dosages: 3 mg/kg . Administration: i.p |
體外活性 | YU238259通過(guò)增敏腫瘤細(xì)胞對(duì)放射療法和引起雙鏈斷裂(DSB)的化療的反應(yīng)。YU238259的治療不僅與電離輻射(IR)、依托泊苷和PARP抑制劑具有協(xié)同作用,而且這種協(xié)同作用因BRCA2缺陷而得到加強(qiáng)。YU238259在高度重組修復(fù)(HDR)缺陷細(xì)胞中的合成致死作用是由于在抑制殘余HDR途徑活性后,未解決的DSB累積。YU238259對(duì)HDR活性的抑制對(duì)非同源末端連接(NHEJ)途徑幾乎沒(méi)有影響。 |
體內(nèi)活性 | 在裸鼠體內(nèi),YU238259處理可延緩了BRCA2缺陷型人類(lèi)腫瘤異種移植物的生長(zhǎng)。 |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 84 mg/mL (182.6 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) |
關(guān)鍵字 | inhibit | Inhibitor | YU 238259 | DNA-dependent protein kinase | DNA-PK | YU238259 | YU-238259 |
相關(guān)產(chǎn)品 | LY294002 | Onatasertib | Torin 1 | IC 86621 | SF2523 | PIK-90 | PI-103 | NU6027 | PI-3065 | STL127705 | PI3K-IN-1 | Compound 401 |
相關(guān)庫(kù) | 抑制劑庫(kù) | 抗乳腺癌化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | 激酶抑制劑庫(kù) | 抗衰老化合物庫(kù) | 抗肝癌化合物庫(kù) | 抗卵巢癌化合物庫(kù) | 抗抑郁癥化合物庫(kù) | 神經(jīng)元分化化合物庫(kù) |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.265100萬(wàn)人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營(yíng)模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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