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Pluripotin (SC1) ERK inhibitor

Name: Pluripotin (SC1)
Brand: Selleck Chemicals
SKU: S7752
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S7752

Pluripotin (SC1) is a dual inhibitor of extracellular signal-regulated kinase 1 (ERK1, MAPK3) and RasGAP that maintains embryonic stem cell (ESC) self-renewal. It also inhibits RSK1, RSK2, RSK3 and RSK4 with IC50 of 0.5 µM, 2.5 µM, 3.3 µM and 10.0 µM, respectively.

Chemical Structure

Molecular Weight: 550.53

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Quality Control

Batch: S775201 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.07%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.07

Related Targets	p38 MAPK K-Ras Raf JNK MEK Ras S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Other ERK Products	SCH772984 Ravoxertinib (GDC-0994) Ulixertinib (BVD-523) Temuterkib (LY3214996) FR 180204 XMD8-92 VX-11e AZD0364 (ATG-017) ERK5-IN-1 MK-8353 (SCH900353)

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (181.64 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.500mg/ml (4.54mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.830mg/ml (1.51mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	550.53	Formula	C₂₇H₂₅F₃N₈O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	839707-37-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)C(F)(F)F)N3CC4=CN=C(N=C4N(C3=O)C)NC5=CC(=NN5C)C

Mechanism of Action

Targets/IC₅₀/Ki	RSK1 ERK1 (Cell-free assay) 98 nM(Kd) RasGAP (Cell-free assay) 212 nM(Kd) RSK1 (Cell-free assay) 0.5 μM RSK2 (Cell-free assay) 2.5 μM RSK3 (Cell-free assay) 3.3 μM RSK4 (Cell-free assay) 10.0 μM
In vitro	Pluripotin (SC1) is a dual function small molecule inhibitor of both ERK1 and RasGAP and that simultaneous inhibition of both protein activities is required and sufficient for its effects on mES cells. This compound activates Ras by inhibition of RasGAP function. It improved the derivation efficiency and pluripotency of ES cells from C57BL/6. Three types of pluripotent stem cells (fES, ntES, and iPS cells) of the C57BL/6 background could generate full-term pups with high efficiency when cultured with SC1.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17088537/ [2] https://pubmed.ncbi.nlm.nih.gov/25211343/ [3] https://pubmed.ncbi.nlm.nih.gov/23437320/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04521231	Recruiting	B Cell Precursor Acute Lymphoblastic Leukemia	Amgen	January 4 2021	Phase 1\|Phase 2

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