吲哚内酰胺 V作用机制 - Medchemexpress - MCE中国

1、Product Data Sheet(-)-Indolactam VCat. No.: HY-12307CAS No.: 90365-57-4分式: CHNO分量: 301.38作靶点: PKC作通路: Epigenetics; TGF-beta/Smad储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (165.90 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证

3、实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.30 mM); Clear solution此案可获得 2.5 mg/mL (8.30 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L

4、PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.30 mM); Clear solution此案可获得 2.5 mg/mL (8.30 mM，饱和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合3. 请依序

5、添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.30 mM); Clear solution此案可获得 2.5 mg/mL (8.30 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 (-)-Indolactam V是PKC 的激活剂，对 -CRD2 (PKC 代替肽)，-CRD2 (PKC 代替肽) 的 Ki 值分别为 3.36 nM 和 1.03

6、M，对 PKC C1A 和 C1B 结构域的 Kd 值分别为 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)，具有抗肿瘤活性。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)体外研究 (-)-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