價(jià)格 | ¥315 | ¥447 | ¥715 |
包裝 | 1mg | 2mg | 5mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-09-14 |
中文名稱:5-碘代殺結(jié)核菌素 | 英文名稱:5-Iodotubercidin |
CAS:24386-93-4 | 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: 99.98% | 產(chǎn)品類別: 抑制劑 |
貨號(hào): T6745 |
名稱 | 5-Iodotubercidin |
描述 | 5-Iodotubercidin (NSC-113939) is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC. |
細(xì)胞實(shí)驗(yàn) | HeLa cells are grown in DME supplemented with 10% fetal bovine serum (FBS) and 2 mM?l-glutamine. Nocodazole is used at a concentration of 3.3 μM unless differently specified. Thymidine (2.5 mM) is used in the asssay. For transfection, FuGENE 6 Transfection Agent is used at a 3:1 ratio with plasmid DNA. Cells are analyzed 24-48 h after transfection. |
激酶實(shí)驗(yàn) | AK activity is measured in a radiochemical assay. The final reaction volume is 100 μL and contained 70 mM Tris-maleate (pH 7.0), 0.1% (w/v) bovine serum albumin, 1.0 mM MgCl2, 1.0 mM ATP, 1.0 μM [U-14C]adenosine (400-600 mCi/mmol) and various inhibitor concentrations. Inhibitors are prepared as 10 mM stock solutions in DMSO. The final DMSO concentration in the assay is 5% (v/v). Eleven different concentration of the test solutions ranging from 0.001 to 10.0 μM are utilized to determine a dose response curve of the inhibition of the enzyme. Reactions are started by adding the appropriate amount of purified human recombinant AK and incubated for 20 min at 37°C. The reactions are terminated by addition of the potent AKI GP3269. A 30-μL aliquot of each reaction is spotted on DEAE cellulose filter paper (cut in squares of appr 1×1 cm) and air-dried for 30 min. The dry filters are then washed for 3 min in deionized water to remove residual [U-14C]adenosine, rinsed with ethanol and dried at 90°C for 20 min. The filter papers are counted in 5.5 mL of Ready Safe liquid scintillation cocktail using a Beckman LS3801 scintillation counter. Control AK activity is determined from the amount of [14C]AMP formed in the presence of 5% DMSO. The concentration of inhibitor required to inhibit 50% of the AK activity (IC50) is determined graphically from plots of inhibitor concentration versus percent (%) control enzyme activity. |
動(dòng)物實(shí)驗(yàn) | Animal Models: Male Mongolian gerbilsFormulation: salineDosages: 1, 2.5 and 5 mg/kgAdministration: i.p. |
體外活性 | 5-Iodotubercidin(Itu)是一種具有抗腫瘤活性的基因毒性藥物,能夠激活A(yù)tm-p53途徑。與其他核苷類似物相比,Itu獨(dú)特之處在于它以p53依賴的方式誘導(dǎo)G2階段阻滯。此外,在較高劑量下,Itu可能激活p53獨(dú)立途徑,這可能與p53合作,殺死細(xì)胞并抑制腫瘤生長(zhǎng)。Itu代謝產(chǎn)物整合到DNA中會(huì)導(dǎo)致DNA斷裂,從而觸發(fā)DNA損傷響應(yīng)。Itu可能是一種具有獨(dú)特作用機(jī)制的潛在化療化合物[2]。 |
體內(nèi)活性 | 5-Iodotubercidin是一種在大鼠大腦中強(qiáng)效的腺苷激酶抑制劑。該化合物在小鼠中表現(xiàn)出顯著的降血壓、肌肉松弛及降低體溫作用,這些效果可被茶堿(一種腺苷受體拮抗劑)阻斷。盡管已知5-Iodotubercidin (1 mg/kg, i.p.)在缺血發(fā)作前使用可以增強(qiáng)腦片段中的細(xì)胞外腺苷水平,但其在通過運(yùn)動(dòng)或組織病理學(xué)指標(biāo)評(píng)估時(shí),未能提供任何腦保護(hù)作用。 |
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 | DMSO : 19.6 mg/mL (50 mM) |
關(guān)鍵字 | 5-Iodotubercidin | Inhibitor | 5Iodotubercidin | NSC113939 | inhibit | 5 Iodotubercidin | ADK | NSC-113939 | Adenosine Kinase |
相關(guān)產(chǎn)品 | Theophylline | Theobromine | Doxofylline |
相關(guān)庫 | 抑制劑庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 抗病毒庫 | GPCR靶點(diǎn)分子庫 | 神經(jīng)退行性疾病化合物庫 | 膜蛋白靶向化合物庫 | 酪氨酸激酶分子庫 |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.2651萬人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)行業(yè) | 化學(xué)試劑,生物活性小分子 | 經(jīng)營(yíng)模式 | 貿(mào)易,試劑,定制,服務(wù) |
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