(-)-Indolactam V
Based on 2 publication(s) in Google Scholar
(-)-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.
For research use only. We do not sell to patients.
- Purity: 98.42%
- CAS No.: 90365-57-4
- Formula: C17H23N3O2
- Molecular Weight:301.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) (-)-Indolactam V
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Biological Activity
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PKCη-CRD2 3.36 nM (Ki) |
PKCη-C1B 5.5 nM (Kd) |
PKCε-C1B 7.7 nM (Kd) |
PKCδ-C1B 8.3 nM (Kd) |
PKCθ-C1B 8.7 nM (Kd) |
PKCβ-C1A-long 18.9 nM (Kd) |
PKCα-C1A-long 20.8 nM (Kd) |
PKCβ-C1B 137 nM (Kd) |
PKCγ-C1A 138 nM (Kd) |
PKCγ-C1B 213 nM (Kd) |
PKCγ-CRD2 1030 nM (Ki) |
PKCδ-C1A 1900 nM (Kd) |
PKCη-C1A 3770 nM (Kd) |
PKCα-C1B-long 4000 nM (Kd) |
PKCε-C1A 4110 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | EC50 |
5 nM
Compound: 3 (Indolactam V)
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Effective concentration against monocytes of HL-60 cells growth inhibition
Effective concentration against monocytes of HL-60 cells growth inhibition
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[PMID: 9554881] |
| PBMC | CC50 |
>100 μM
Compound: Indolactam-V
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Toxicity in human PBMC assessed as reduction in cell viability after 5 days by WST8 assay
Toxicity in human PBMC assessed as reduction in cell viability after 5 days by WST8 assay
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[PMID: 30413535] |
| U-937 | CC50 |
>100 μM
Compound: Indolactam-V
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Toxicity in human U-937 cells assessed as reduction in cell viability after 48 hrs by WST8 assay
Toxicity in human U-937 cells assessed as reduction in cell viability after 48 hrs by WST8 assay
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[PMID: 30413535] |
(-)-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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 90365-57-4
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Appearance Solid
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Molecular Weight 301.38
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Formula C17H23N3O2
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Color White to light yellow
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SMILES
CC(C)[C@@H](C1=O)N(C)C2=C3C(NC=C3C[C@H](N1)CO)=CC=C2
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Synonyms
Indolactam V
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Automated, High-Throughput Phenotypic Screening and Analysis Platform to Study Pre- and Post-Implantation Morphogenesis in Stem Cell-Derived Embryo-Like Structures. [Abstract]2024 Jan;11(4):e2304987. PMID: 37991133 -
Viruses
Identification of Combinations of Protein Kinase C Activators and Histone Deacetylase Inhibitors That Potently Reactivate Latent HIV. [Abstract]2020 Jun 3;12(6):609. PMID: 32503121
Solvent & Solubility
DMSO : 50 mg/mL (165.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3181 mL | 16.5904 mL | 33.1807 mL | 82.9518 mL |
| 5 mM | 0.6636 mL | 3.3181 mL | 6.6361 mL | 16.5904 mL | |
| 10 mM | 0.3318 mL | 1.6590 mL | 3.3181 mL | 8.2952 mL | |
| 15 mM | 0.2212 mL | 1.1060 mL | 2.2120 mL | 5.5301 mL | |
| 20 mM | 0.1659 mL | 0.8295 mL | 1.6590 mL | 4.1476 mL | |
| 25 mM | 0.1327 mL | 0.6636 mL | 1.3272 mL | 3.3181 mL | |
| 30 mM | 0.1106 mL | 0.5530 mL | 1.1060 mL | 2.7651 mL | |
| 40 mM | 0.0830 mL | 0.4148 mL | 0.8295 mL | 2.0738 mL | |
| 50 mM | 0.0664 mL | 0.3318 mL | 0.6636 mL | 1.6590 mL | |
| 60 mM | 0.0553 mL | 0.2765 mL | 0.5530 mL | 1.3825 mL | |
| 80 mM | 0.0415 mL | 0.2074 mL | 0.4148 mL | 1.0369 mL | |
| 100 mM | 0.0332 mL | 0.1659 mL | 0.3318 mL | 0.8295 mL |
(-)-Indolactam V Related Classifications
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