Home MAPK ERK inhibitor - S6 Kinase inhibitor Pluripotin (SC1)

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Pluripotin (SC1) ERK inhibitor

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.

Pluripotin (SC1) ERK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 550.53

Purity & Quality Control

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

Related Products

Signaling Pathway

ERK Signaling Pathways

ERK Signaling Pathway

Mechanism of Action

Targets
RSK1 [3] ERK1 [1]
(Cell-free assay)		 RasGAP [1]
(Cell-free assay)		 RSK1 [3]
(Cell-free assay)		 RSK2 [3]
(Cell-free assay)		 Click to View More Targets
98 nM(Kd) 212 nM(Kd) 0.5 μM 2.5 μM

In vitro
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. It activates Ras by inhibition of RasGAP function[1]. This compound 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 it[1].
Cell Research Cell lines Mouse ES cells
Concentrations 300 nM, 1 μM, 3 μM
Incubation Time --
Method

Pluripotin (SC1) is used to maintain mES cells seeded in gelatin-coated six-well plates at 1.6×104 cells/cm2 at concentrations of 3 μM in ESC-SR media, 1 μM in ESC-N2B27 media, or 300 nM in ESC-N2 media without LIF or feeder cells. mES cells maintained with 103 units/ml LIF plus 10 ng/ml BMP4 in ESC-N2B27 media are used as a positive control. mES cells treated with DMSO in ESC-SR media, ESC-N2B27 media, or ESC-N2 media for two passages are used as negative controls. Cells are split every 3 days and seeded at same density (1.6×104 cells/cm2). mES cells at passage 11 are analyzed with FACS, immunocytochemistry, histocytochemistry, and RT-PCR.
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

References
  • https://pubmed.ncbi.nlm.nih.gov/17088537/
  • https://pubmed.ncbi.nlm.nih.gov/25211343/
  • https://pubmed.ncbi.nlm.nih.gov/23437320/

Chemical Information

Molecular Weight 550.53 Formula

C27H25F3N8O2
CAS No. 839707-37-8 SDF Download SDF
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

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (181.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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