吲哚內(nèi)酰胺 V作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data Sheet(-)-Indolactam VCat. No.: HY-12307CAS No.: 90365-57-4分式: CHNO分量: 301.38作靶點(diǎn): PKC作通路: 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 : 50 mg/mL (165.90 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM

2、 3.3181 mL 16.5904 mL 33.1807 mL5 mM 0.6636 mL 3.3181 mL 6.6361 mL10 mM 0.3318 mL 1.6590 mL 3.3181 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)物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊?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

3、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 (8.30 mM); Clear solution此案可獲得 2.5 mg/mL (8.30 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

4、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 (8.30 mM); Clear solution此案可獲得 2.5 mg/mL (8.30 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 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

5、添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.30 mM); Clear solution此案可獲得 2.5 mg/mL (8.30 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。BIOLOGICAL ACTIVITY物活性 (-)-Indolactam V是PKC 的激活劑，對(duì) -CRD2 (PKC 代替肽)，-CRD2 (PKC 代替肽) 的 Ki 值分別為 3.36 nM 和 1.03

6、M，對(duì) PKC C1A 和 C1B 結(jié)構(gòu)域的 Kd 值分別為 5.5 nM (-C1B)，7.7 nM (-C1B)，8.3 nM (-C1B)，18.9 nM (-C1A-long)，20.8 nM (-C1A-long)，137 nM (-C1B)，138 nM (-C1A) 和 213 nM (-C1B)，具有抗腫瘤活性。IC & Target PKC-CRD2 PKC-C1B PKC-C1B PKC-C1B3.36 nM (Ki) 5.5 nM (Kd) 7.7 nM (Kd) 8.3 nM (Kd)PKC-C1B PKC-C1A-long PKC-C1A-long PKC-C1B8.

7、7 nM (Kd) 18.9 nM (Kd) 20.8 nM (Kd) 137 nM (Kd)PKC-C1A PKC-C1B PKC-CRD2 PKC-C1A138 nM (Kd) 213 nM (Kd) 1030 nM (Ki) 1900 nM (Kd)PKC-C1A PKC-C1B-long PKC-C1A3770 nM (Kd) 4000 nM (Kd) 4110 nM (Kd)體外研究 (-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 M for -CRD2 (PKC surrogate peptide), -

8、CRD2 (PKCsurrogate peptide), and has antitumor activity1. (-)-Indolactam V shows Kds of 5.5 nM (-C1B), 7.7 nM (-C1B), 8.3nM (-C1B), 18.9 nM (-C1A-long), 20.8 nM (-C1A-long), 137 nM (-C1B), 138 nM (-C1A), 213 nM (-C1B),respectively2. (-)-Indolactam V (20 nM-5 M) dose-dependently affects multiple hESC

9、 lines, such as HUES 2, 4 and 8.(-)-Indolactam V also increases the mRNA levels of Pdx1, HNF6, PTF1A, SOX9, HB9 and PROX1. In addition, (-)-Indolactam V (300 nM) functions in both mouse and human cells and confirms that some signals for pancreaticdevelopment3.PROTOCOLCell Assay 3 For induced differe

10、ntiation to endocrine or exocrine cells, the (-)-Indolactam V (300 nM)-treated populations arecultured in DMEM/F12 supplemented with 1 N2, 2 mg/mL albumin fraction V and 10 ng/mL bovine FGF for the first 4d. 10 mM nicotinamide is then added and maintained for an additional 8 d, changing the medium e

11、very 3 d3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Nakagawa Y, et al. Synthesis and biological activities of indolactone-V, the lactone analogue of the tumor promoter (-)-indolactam-V. Biosci BiotechnolBiochem. 1997 Aug;61(8):1415-7.

12、2. Masuda A, et al. Binding selectivity of conformationally restricted analogues of (-)-indolactam-V to the C1 domains of protein kinase C isozymes. BiosciPage 2 of 3 www.MedChemEBiotechnol Biochem. 2002 Jul;66(7):1615-7.3. Chen S, et al. A small molecule that directs differentiation of human ESCs into the pancreatic lineage. Nat Chem Biol. 2009 Apr;5(4):258-65.McePdfHeightCaution: Product has not be