1、Product Data SheetDesmethylglyciteinCat. No.: HY-N5072CAS No.: 17817-31-1分式: CHO分量: 270.24作靶點(diǎn): CDK; PI3K; PKC作通路: Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Epigenetics; TGF-beta/Smad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 (462.55 mM; Need ultrason

2、ic)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 3.7004 mL 18.5021 mL 37.0041 mL5 mM 0.7401 mL 3.7004 mL 7.4008 mL10 mM 0.3700 mL 1.8502 mL 3.7004 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；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。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

3、選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(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，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (7.70 mM); Clear solution此案可獲得 2.08 mg/mL (7.70 mM，飽和度未知) 的澄清溶

4、液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (7.70 mM); Clear solution此案可獲得 2.08 mg/mL (7.70 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 20.8

5、mg/mL 的澄均勻。DMSO 儲(chǔ)備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (7.70 mM); Clear solution此案可獲得 2.08 mg/mL (7.70 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Desmethylglycitein (4,6,7-Tr

6、ihydroxyisoflavone)，苷元的代謝產(chǎn)物，來(lái) 于 Glycine max，具有抗氧化性和抗 癌活性。Desmethylglycitein 在體內(nèi)直接結(jié)合 CDK1 和 CDK2，抑制 CDK1 和 CDK2 活性。Desmethylglycitein 蛋激 酶 C (PKC) 的直接抑制劑，抑制正常膚成纖維細(xì)胞中的太陽(yáng)紫外線 (sUV) 誘導(dǎo)的 質(zhì)屬蛋酶1 (MMP1)。Desmethylglycitein 以 ATP 競(jìng)爭(zhēng)式與細(xì)胞質(zhì)中的 PI3K 結(jié)合，抑制 PI3K 和下游信號(hào)級(jí)聯(lián)的活性，從抑制 3T3-L1 前脂肪細(xì)胞中的脂肪形成。IC & Target CDK1 CDK2

7、 PKC體外研究Desmethylglycitein (4,6,7-Trihydroxyisoflavone)(0-100 M; 24-72 hours) suppesses anchorage-dependent growth ofHCT-116 and DLD1 cells in a dose- and time-dependent manner without cytotoxicity 1.Desmethylglycitein (4,6,7-Trihydroxyisoflavone)(0-100 M; 24-72 hours) suppresses CDK1 activity in a

8、dose-dependent manner and inhibits CDK2 activity in HCT-116 cells1.Desmethylglycitein (4,6,7-Trihydroxyisoflavone)(0-100 M; 24-72 hours) induces cell cycle arrest at the S and G2/Mphases, the percentage of cells in S phase is higher in the 100 M 6,7,4-THIF-treated group, and the same pattern isobser

9、ved in G2/M phase (29.5% versus 19.1% ) 1.Cell Viability Assay1Cell Line: HCT-116 cellsConcentration: 0, 12.5, 25, 50 or 100 MIncubation Time: 24, 48 or 72 hoursResult: Inhibited anchorage-dependent and -independent growth of HCT-116 cells.Western Blot Analysis1Cell Line: HCT-116 and DLD1 cellsConce

10、ntration: 0, 25, 50 or 100 MIncubation Time: 48 hoursResult: Inhibited CDK1,CDK2 expression.Cell Cycle Analysis1Cell Line: HCT-116 cellsConcentration: 0, 25, 50 or 100 MIncubation Time: 24, 48 or 72 hoursPage 2 of 3 www.MedChemEResult: Induces cell cycle arrest of HCT-116 cells at S and G2/M phases.

11、體內(nèi)研究 Desmethylglycitein (4,6,7-Trihydroxyisoflavone) (intraperitoneally injection; 5 or 25 mg/kg; once daily; 20 days)suppresses tumor development in mice and serves as an effective anticancer treatment with the potential to inhibit ordelay the tumorigenicity of HCT-116 cells in an in vivo system1.A

12、nimal Model: Female athymic nude mice subcutaneously injected with HCT-116 cells1Dosage: 5 or 25 mg/kgAdministration: Intraperitoneally injection; 5 or 25 mg/kg; once daily; 20 daysResult: Decreased tumor growth, volume and weight of HCT-116 xenografts.REFERENCES1. Lee DE, et al. 6,7,4-trihydroxyiso

13、flavone inhibits HCT-116 human colon cancer cell proliferation by targeting CDK1 and CDK2. Carcinogenesis. 2011Apr;32(4):629-35.2. Lim TG, et al. The daidzein metabolite, 6,7,4-Trihydroxyisoflavone, is a novel inhibitor of PKC in suppressing solar UV-induced matrix metalloproteinase1. Int J Mol Sci. 2014 Nov 19;15(11):21419-323. Seo SG, et al. A metabolite of daidzein, 6,7,4-trihydroxyisoflavone, suppresses adipogenesis in 3T3-L1 preadipocytes via ATP-competitive inhibition ofPI3K.McePdfHeightCautio