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Purity: ≥98%
Indolactam V is a novel, potent and selective activator of protein kinase C (PKc) with antitumor activity. It induces changes in muscarinic receptor functions. Indolactam V has 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)
| ln Vitro |
(-)-Indolactam V is a PKC activator that has anti-tumor activity and has a Kis of 3.36 nM for eta-CRD2 (PKCeta replacement peptide) and 1.03 μM for γ-CRD2 (PKCγ replacement peptide) [1]. Kd values for (-)-Indolactam V are as follows: 5.5 nM for eta-C1B, 7.7 nM for ε-C1B, 8.3 nM for δ-C1B, 18.9 nM for β-C1A-long, 20.8 nM for α-C1A-long, 137 nM for β-C1B, 138 nM for γ-C1A, and 213 nM for γ-C1B, each [2]. (-)-Indolactam V (20 nM-5 μM) affects HUES 2, 4, and 8 hESC lines in a dose-dependent manner. Additionally, Pdx1, HNF6, PTF1A, SOX9, HB9, and PROX1 are increased by (-)-Indolactam V. Furthermore, (-)-Indolactam V (300 nM) acted in both mouse and human cells and demonstrated several signals of pancreatic development [3].
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| References |
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| Additional Infomation |
(-)-indolactam V is a 9-membered ring that is a potent protein kinase C activator
Indolactam V has been reported in Streptomyces blastmyceticus with data available. |
| Molecular Formula |
C17H23N3O2
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|---|---|
| Molecular Weight |
301.38342
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| Exact Mass |
301.179
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| CAS # |
90365-57-4
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| PubChem CID |
105000
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| Appearance |
White to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
584.0±50.0 °C at 760 mmHg
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| Flash Point |
307.0±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.590
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| LogP |
0.75
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
415
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(C)[C@H]1C(=O)N[C@@H](CC2=CNC3=C2C(=CC=C3)N1C)CO
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| InChi Key |
LUZOFMGZMUZSSK-LRDDRELGSA-N
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| InChi Code |
InChI=1S/C17H23N3O2/c1-10(2)16-17(22)19-12(9-21)7-11-8-18-13-5-4-6-14(15(11)13)20(16)3/h4-6,8,10,12,16,18,21H,7,9H2,1-3H3,(H,19,22)/t12-,16-/m0/s1
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| Chemical Name |
(2S,5S)-1,2,4,5,6,8-Hexahydro-5-(hydroxymethyl)-1-methyl-2-(1-methylethyl)-3H-pyrrolo(4,3,2-gh)-1,4-benzodiazonin-3-one
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| Synonyms |
Indolactam-V (-)-Indolactam V (-)-ILV
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~165.90 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 | 1.6590 mL | 3.3181 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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