| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
ERK1 (MAPK3) and RasGAP. Pluripotin is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP. It also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 μM, respectively. The compound sustains mES self-renewal through simultaneous inhibition of both ERK1 and RasGAP activities.
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| ln Vitro |
Pluripotin (SC-1) has IC50s of 0.005, 1.4, 2.2, 0.5, 2.5, 3.3, and 10.0 µM, respectively, and inhibits Abl1, p70S6K, PLK2, RSK1, RSK2, RSK3, and RSK4. Pluripotin (SC-1) inhibits the development of seven cell lines used in colon tumors. Following a five-day exposure to 0.1 µM SC-1, the vitality and quantity of cells in each of the seven colon tumor lines are assessed. The number of cells has decreased statistically significantly, but the viability is still around 95%[2].
Pluripotin inhibits ERK1 with a KD of 98 nM and RasGAP with a KD of 212 nM. It also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 μM, respectively. Simultaneous inhibition of both ERK1 and RasGAP is required and sufficient for Pluripotin's effects on mES cells. The compound sustains mES self-renewal and maintains pluripotency. |
| ln Vivo |
Six
week old female NOD.SCID mice were randomly assigned to each of 20
treatment arms (n = 5/group). Treated and control colon tumor lines were
enzymatically harvested and counted prior to dilution in RPMI 1640 (at
10, 100, 1,000, 10,000 cells/inoculum) for subcutaneous injection into
the axillary region using a volume of 1 ml/mouse. Positive control
groups were established such that tumor formation occurred in all mice
in approximately one week thus confirming that all tumor lines studied
were tumorigenic. Cell inocula for the positive control groups ranged
from 1×106 to 2.5×106. Cell viability of the cell stocks was assessed by
trypan blue exclusion prior to dilution for injection and was routinely
found to be >95%. Tumor formation was monitored weekly using caliper
measurements and the tumor mass was calculated as weight in mg
= 1/2×(tumor length)×(tumor width)2. All experiments were terminated at
120 days or when tumor weight exceeded 2000 mg for any individual
mouse. In selected studies, tumor cells were resuspended in Matrigel
(50% concentration, BD Biosciences) prior to injection. |
| Enzyme Assay |
In vitro enzyme assays for Pluripotin involve measuring the inhibition of ERK1 and RasGAP activities. Kinase activity is measured using appropriate substrates and various concentrations of Pluripotin. IC50 and KD values are determined from concentration-response curves. Pluripotin inhibits ERK1 with a KD of 98 nM and RasGAP with a KD of 212 nM.
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| Cell Assay |
In vitro cellular assays for Pluripotin involve treating murine embryonic stem (mES) cells with the compound and assessing self-renewal, pluripotency marker expression, and differentiation. Cells are treated with various concentrations of Pluripotin, and markers such as Oct4, Nanog, and SSEA-1 are measured by immunofluorescence or flow cytometry. Pluripotin sustains mES self-renewal and maintains pluripotency.
|
| Animal Protocol |
NA | Female NOD.SCID mice
| ADME/Pharmacokinetics |
Pharmacokinetic data for Pluripotin HCl is limited. The compound has a molecular formula of C27H25F3N8O2 and a molecular weight of 550.53. It is a white to off-white solid powder. The compound is soluble in DMSO and is typically stored at -20°C. Further pharmacokinetic studies are needed to support its development as a therapeutic agent.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of Pluripotin HCl are limited. The compound is primarily used as a research tool for stem cell applications. Comprehensive toxicological evaluation is needed before clinical development. The compound's mechanism of action—dual inhibition of ERK1 and RasGAP—suggests potential for targeted effects on cell proliferation and differentiation.
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| References | |
| Additional Infomation |
Pluripotin HCl (SC1) is a novel and potent activator of murine embryonic stem cells and a dual inhibitor of ERK1 (MAPK3) and RasGAP. It inhibits ERK1 with a KD of 98 nM and RasGAP with a KD of 212 nM. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s ranging from 0.5 to 10.0 μM. Simultaneous inhibition of both protein activities is required for Pluripotin's effects on mES cells. The compound is widely used in stem cell research.
|
| Molecular Formula |
C27H25F3N8O2
|
|---|---|
| Molecular Weight |
550.53
|
| Exact Mass |
550.205
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| Elemental Analysis |
C, 58.90; H, 4.58; F, 10.35; N, 20.35; O, 5.81
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| CAS # |
839707-37-8
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| PubChem CID |
12003241
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.662
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| LogP |
2.37
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
40
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| Complexity |
925
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| Defined Atom Stereocenter Count |
0
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| SMILES |
0
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| Synonyms |
SC-1; SC 1; SC1; Pluripotin
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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)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~45.41 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.54 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 (4.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8164 mL | 9.0822 mL | 18.1643 mL | |
| 5 mM | 0.3633 mL | 1.8164 mL | 3.6329 mL | |
| 10 mM | 0.1816 mL | 0.9082 mL | 1.8164 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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