1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE5-MethoxyflavoneCat. No.: HY-107790CAS No.: 42079-78-7分式: CHO分量: 252.26作靶點(diǎn): DNA/RNA Synthesis作通路: Cell Cycle/DNA Damage儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg/mL (495.52 mM;

2、Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.9642 mL 19.8208 mL 39.6416 mL5 mM 0.7928 mL 3.9642 mL 7.9283 mL10 mM 0.3964 mL 1.9821 mL 3.9642 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以

3、根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (8.25 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (8.25 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (8

4、.25 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 5-Methoxyflavone，種類 酮， DNA聚合酶 (DNA polymerase-beta) 的抑制劑和 -淀粉樣蛋毒性的神經(jīng)保護(hù)劑。擁有中樞神經(jīng)系統(tǒng)鎮(zhèn)靜劑的作,通過調(diào)控嗜離 GABAA 受體來實(shí)現(xiàn)。IC50 & Target DNA polymerase-beta 1.體外研究 5-Methoxyflavone (compound 1) is identified as a candidate

5、compound endowed with the ability to inhibitDNA pol- in multiple and to prevent cell-cycle initiation and subsequent neuronal apoptosis in A-challengedprimary neuronal cultures. 5-methoxyflavone (10-30 M) is able to significantly enhance toxicity of MMS on92TAg cells. 5-Methoxyflavone (1 or 10 M) si

6、gnificantly reduces polymerase activity on a gapped substrate1.5-Methoxyflavone (5-MF, 0-100 g/mL) results in a time dependent reduction in the levels of antiapoptoticproteins cFLIP, Mcl-1 and an increase in the proapoptotic protein BAX. 5-MF induces both TRAIL-R1(DR4)and TRAIL-R2 (DR5) in a time-de

7、pendent manner 2.體內(nèi)研究 5-Methoxyflavone (100, 150 mg/kg, i.p) significantly decreases the latency time to loss of righting reflex. 5-Methoxyflavone (50, 100 and 150 mg/kg, i.p) exhibits a significant and dose-dependent reduction in thespontaneous locomotor activity. 5-Methoxyflavone (50, 100 mg/kg, i

8、.p) reduces the rearing response. 5-Methoxyflavone (100, 125 and 150 mg/kg, i.p) completely abolishesed the grooming response similar todiazepam treated animals 3.REFERENCES1. Merlo S, et al. Identification of 5-Methoxyflavone as a Novel DNA Polymerase-Beta Inhibitor and Neuroprotective Agent agains

9、t Beta-Amyloid Toxicity. J Nat Prod. 2015 Nov 25;78(11):2704-11.2. Shanmugasundaram J, et al. Sedative-hypnotic like effect of 5-methoxyflavone in mice and investigation on possible mechanisms by invivo and in silico methods. Biomed Pharmacother. 2018 Dec;108:85-94.3. Wudtiwai B, et al. Methoxyflavone derivatives modulate the effect of TRAIL-induced apoptosis in human leukemic cell lines. J HematolOncol. 2011 Dec 21;4:52.McePdfHeightCaution: Product has not been fully validated for