3-吲哚甲醇作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetIndole-3-carbinolCat. No.: HY-N0170CAS No.: 700-06-1分式: CHNO分量: 147.17作靶點(diǎn): NF-B; Aryl Hydrocarbon Receptor; E1/E2/E3 Enzyme; Endogenous Metabolite作通路: NF-B; Immunology/Inflammation; Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)

2、體外實(shí)驗(yàn) DMSO : 25 mg/mL (169.87 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 6.7949 mL 33.9743 mL 67.9486 mL5 mM 1.3590 mL 6.7949 mL 13.5897 mL10 mM 0.6795 mL 3.3974 mL 6.7949 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)

3、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: 2.5 mg/mL (16.99 mM); Clea

4、r solution此案可獲得 2.5 mg/mL (16.99 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 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: 2.5 mg/mL (16.99 mM); Clear solution此案可獲得 2.5 mg/mL (16.99 mM，飽和度未知) 的澄清溶液。Pa

5、ge 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 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: 2.5 mg/mL (16.99 mM); Clear solution此案可獲得 2.5 mg/mL (16.99 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 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOL

6、OGICAL ACTIVITY物活性 Indole-3-carbinol (I3C)是芳烴受體 (AhR) 的激動(dòng)劑，為 NF-B 和 WWP1 (含有 WW 結(jié)構(gòu)域的 E3 連接酶 1) 的抑制劑。IC & Target NF-B Human Endogenous AhRMetabolite(批量添加)體外研究 It is found that Indole-3-carbinol (I3C) inhibits the proliferation of THP-1 cells in a dose- and time dependent mannerwith minimal toxicity o

7、ver normal monocytes. The AhR target genes (CYP1A1, IL1) are overexpressed upon Indole-3-carbinol treatment (p0.05 to p0.001). The antiproliferative effects of Indole-3-carbinol are in association withprograming cell death. Indole-3-carbinol downregulates BCL2 and upregulates FasR in THP-1 cells (p0

8、.05 top0.001). G1 cell cycle arrest is also observed using flow cytometry. G1-acting cell cycle genes (P21, P27 and P53) areoverexpressed (p0.05 to p0.001), while CDK2 is downregulated upon Indole-3-carbinol treatment (p0.01 top0.001)1.Indole-3-carbinol suppresses NF-B activity and stimulates the p5

9、3 pathway in pre-B acute lymphoblasticleukemia cells2.PROTOCOLCell Assay 1 THP-1 cells are cultured in RPMI 1640 supplemented with 10% FBS, 100 U/mL penicillin, 100 mg/mL streptomycinand 2 mM Glutamax in a fully humidified atmosphere with 5% CO2. Cells (2-5105 mL-1) are seeded in six well platesfoll

10、owed by resuspension in complete growth media. THP-1 monocyte cells are then treated with 10 ng/mL phorbol12-myristate 13-acetate as a tumor promoter to induce stable differentiation into attaching macrophage-like cellsand overexpression of AhR. The cells are then treated with varying concentrations

11、 of Indole-3-carbinol (1, 10 and 100M, and 1 mM). THP-1 cells and enriching normal monocytes are seeded at 5104 cells/well in 24-well plate withdifferent concentrations of Indole-3-carbinol and observed for 24 and 48 h followed by MTT assay. The cells areincubated in triplicates in a final volume of

12、 200 mL of Phenol Red free RPMI 1640 for 20 h . An aliquot of 20 mL ofMTT solution (5 mg/mL) is added to each well and incubated for 4 h. Formazan crystals are formed. An amount of300 mL DMSO is then added to each well as a cell lysis solution. Percentage of cell viability is assessed byspectrophoto

13、metry at 570 nm1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) Molecules. 2018 Oct 11;23(10). pii: E2600.See more customer validations on HYPERLINK www.MedChemE www.MedChemEPage 2 of 3 www.MedChemEREFERENCES1. Mohammadi S, et al. Indole-3-

14、carbinol induces G1 cell cycle arrest and apoptosis through aryl hydrocarbon receptor in THP-1 monocytic cell line.JRecept Signal Transduct Res. 2017 Oct;37(5):506-514.2. Safa M, et al. Indole-3-carbinol suppresses NF-B activity and stimulates the p53 pathway in pre-B acute lymphoblastic leukemia cells. Tumour Biol. 2015May;36(5):3919-30.3. Lee YR, et al. Reactivation of PTEN tumor suppressor for cancer treatment through inhibition of a MYC-WWP1 inhibitory pathway. Science. 2019 May17;364(6441). pii: eaau0159.M