| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Indolactam V targets protein kinase C (PKC), a family of serine/threonine kinases involved in cell proliferation, differentiation, and apoptosis. It binds to and activates PKC at the phorbol ester binding site, modulating downstream signaling pathways. Indolactam V has a Ki of 3.36 nM for eta-CRD2 (PKCη replacement peptide).
|
|---|---|
| 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].
Indolactam V is a potent and selective PKC activator. It has a Ki of 3.36 nM for eta-CRD2 (PKCη replacement peptide). The compound has antitumor activity and induces changes in muscarinic receptor functions. It directs differentiation of human and mouse ESCs to pancreatic cells. |
| ln Vivo |
Indolactam V has antitumor activity in vivo. It promotes differentiation to human and mouse pancreatic precursors from pluripotent stem cell-derived definitive endoderm. The compound may be used, along with other agents, to differentiate human iPS cells into glucose-responsive insulin-secreting progeny.
|
| Enzyme Assay |
Indolactam V's binding to PKC can be assessed using in vitro binding assays. PKC is incubated with a radiolabeled or fluorescent phorbol ester ligand in the presence of varying concentrations of indolactam V. Competition for the phorbol ester binding site is measured, and Ki values are calculated.
|
| Cell Assay |
The cellular activity of indolactam V is evaluated in cell-based assays. Cells are treated with increasing concentrations of indolactam V, and PKC activation is assessed by measuring phosphorylation of PKC substrates. Cell proliferation, differentiation, and apoptosis are also assessed. The compound is used to direct differentiation of stem cells to pancreatic cells.
|
| Animal Protocol |
Indolactam V is used in vivo to promote differentiation of pluripotent stem cells. In animal models, the compound would be administered to evaluate its effects on cell differentiation and tissue regeneration. Specific protocols are not extensively detailed in standard reference sources.
|
| ADME/Pharmacokinetics |
Indolactam V has a molecular formula of C17H23N3O2 and a molecular weight of 301.38. It is typically supplied as a powder with a purity of ≥95%. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources.
|
| Toxicity/Toxicokinetics |
The toxicity profile of indolactam V is not extensively documented. As a PKC activator, potential adverse effects may include those related to PKC activation in various tissues. Specific LD50 values and organ-specific toxicity data are not readily available.
|
| References |
|
| Additional Infomation |
(-)-Indolinamide V is a 9-membered ring compound and a potent protein kinase C activator. Indolinamide V has been reported in Streptomyces, and relevant data are available for reference.
Indolactam V (CAS# 90365-57-4) is a potent and selective PKC activator that acts at the phorbol ester binding site. It has antitumor activity and directs stem cell differentiation. Indolactam V is a research tool for studying PKC signaling, cell differentiation, and proliferation. |
| Molecular Formula |
C17H23N3O2
|
|---|---|
| Molecular Weight |
301.38342
|
| Exact Mass |
301.179
|
| CAS # |
90365-57-4
|
| PubChem CID |
105000
|
| Appearance |
White to light yellow solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
584.0±50.0 °C at 760 mmHg
|
| Flash Point |
307.0±30.1 °C
|
| Vapour Pressure |
0.0±1.7 mmHg at 25°C
|
| Index of Refraction |
1.590
|
| LogP |
0.75
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
22
|
| Complexity |
415
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC(C)[C@H]1C(=O)N[C@@H](CC2=CNC3=C2C(=CC=C3)N1C)CO
|
| InChi Key |
LUZOFMGZMUZSSK-LRDDRELGSA-N
|
| 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
|
| 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
|
| Synonyms |
Indolactam-V (-)-Indolactam V (-)-ILV
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~165.90 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA