الصفحة الرئيسية>>Signaling Pathways>> TGF-β / Smad Signaling>> PKC>>(-)-Indolactam V

(-)-Indolactam V

رقم الكتالوجGC14012

(-) - Indolactam V هو منشط PKC ، مع Kis من 3.36 نانومتر ، 1.03 ميكرومتر لـ η-CRD2 (ببتيد بديل PKCη) ، γ-CRD2 (ببتيد بديل PKCγ) ، و Kds من 5.5 نانومتر (η-C1B) ، 7.7 نانومتر (ε-C1B) ، 8.3 نانومتر (δ-C1B) ، 18.9 نانومتر (β-C1A طويل) ، 20.8 نانومتر (α-C1A طويل) ، 137 نانومتر (β-C1B) ، 138 نانومتر (γ-C1A) ، 213 نانومتر (γ-C1B) ، ولها نشاط مضاد للأورام

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(-)-Indolactam V التركيب الكيميائي

Cas No.: 90365-57-4

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
394٫00
متوفر
5mg
594٫00
متوفر
1mg
162٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of (-)-Indolactam V

(-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.

(-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and has antitumor activity[1]. (-)-Indolactam V shows Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), respectively[2]. (-)-Indolactam V (20 nM-5 μM) dose-dependently affects multiple hESC 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 pancreatic development[3].

References:
[1]. 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 C1 domains of protein kinase C isozymes. 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. 2009 Apr;5(4):258-65.

Protocol of (-)-Indolactam V

Cell experiment:

For induced differentiation to endocrine or exocrine cells, the (-)-Indolactam V (300 nM)-treated populations are cultured in DMEM/F12 supplemented with 1 N2, 2 mg/mL albumin fraction V and 10 ng/mL bovine FGF for the first 4 d. 10 mM nicotinamide is then added and maintained for an additional 8 d, changing the medium every 3 d[3].

References:

[1]. 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 C1 domains of protein kinase C isozymes. 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. 2009 Apr;5(4):258-65.

Chemical Properties of (-)-Indolactam V

Cas No. 90365-57-4 SDF
Chemical Name (2S,5S)-5-(hydroxymethyl)-2-isopropyl-1-methyl-4,5,6,8-tetrahydro-1H-[1,4]diazonino[7,6,5-cd]indol-3(2H)-one
Canonical SMILES O=C1N[C@H](CO)CC2=CNC3=C2C(N(C)[C@H]1C(C)C)=CC=C3
Formula C17H23N3O2 M.Wt 301.38
الذوبان Soluble to 10 mM in DMSO Storage Desiccate at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of (-)-Indolactam V

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.3181 mL 16.5904 mL 33.1807 mL
5 mM 0.6636 mL 3.3181 mL 6.6361 mL
10 mM 0.3318 mL 1.659 mL 3.3181 mL
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