minus-Indolactam-V-Indolactam-V-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE(-)-Indolactam VCat. No.: HY-12307CAS No.: 90365-57-4Synonyms: Indolactam V分式: CHNO分量: 301.38作靶點: PKC作通路: Epigenetics; TGF-beta/Smad儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL

2、(165.90 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 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備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當

3、天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；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 solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (8.30 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Sm

4、all Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (8.30 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 (-)-Indolactam V是PKC 的激活劑，對 -CRD2 (PKC 代替肽)，-CRD2 (PKC 代替肽) 的 Ki 值分別為 3.36nM 和 1.03 M，對 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)，

5、137 nM (-C1B)，138 nM (-C1A) 和 213 nM (-C1B)，具有抗腫瘤活性。IC50 & 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 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

6、(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), -CRD2 (PKC surrogate peptide), and has antitumor activity 1. (-)-Indolactam V shows Kds of 5.5 nM (-C1B), 7.7 nM

7、 (-C1B), 8.3 nM (-C1B), 18.9 nM (-C1A-long), 20.8 nM (-C1A-long), 137 nM (-C1B), 138nM (-C1A), 213 nM (-C1B), respectively 2. (-)-Indolactam V (20 nM-5 M) dose-dependently affectsmultiple hESC lines, such as HUES 2, 4 and 8. (-)-Indolactam V also increases the mRNA levels of Pdx1,HNF6, PTF1A, SOX9,

8、HB9 and PROX1. In addition, (-)-Indolactam V (300 nM) functions in both mouse andhuman cells and confirms that some signals for pancreatic development 3.PROTOCOLCell Assay 3 For induced differentiation to endocrine or exocrine cells, the (-)-Indolactam V (300 nM)-treated populationsare cultured in D

9、MEM/F12 supplemented with 1 N2, 2 mg/mL albumin fraction V and 10 ng/mL bovine FGFfor the first 4 d. 10 mM nicotinamide is then added and maintained for an additional 8 d, changing themedium every 3 d 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.RE

10、FERENCES1. Nakagawa Y, et al. Synthesis and biological activities of indolactone-V, the lactone analogue of the tumor promoter (-)-indolactam-V.Biosci Biotechnol Biochem. 1997 Aug;61(8):1415-7.2. Masuda A, et al. Binding selectivity of conformationally restricted analogues of (-)-indolactam-V to the

11、 C1 domains of protein kinase C2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEisozymes. Biosci Biotechnol 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. 2009Apr;5(4):258-65.McePdfHeightCaution: Product has not b