Home MAPK MEK antagonist APS-2-79 HCl

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APS-2-79 HCl MEK antagonist

Cat.No.S8355

APS-2-79 is a MAPK antagonist that modulating KSR-dependent MAPK signalling by antagonizing RAF heterodimerization as well as the conformational changes required for phosphorylation and activation of KSR-bound MEK. IC50=120 ± 23 nM.
APS-2-79 HCl MEK antagonist Chemical Structure

Chemical Structure

Molecular Weight: 423.89

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Quality Control

Batch: S835501 DMSO]97 mg/mL]false]Ethanol]32 mg/mL]false]Water]Insoluble]false Purity: 99.26%
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99.26

Solubility

In vitro
Batch:

DMSO : 97 mg/mL (228.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 32 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 423.89 Formula

C23H21N3O3.HCl

 Storage (From the date of receipt)
CAS No. 2002381-31-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C=CC(=C1)OC2=CC=CC=C2)NC3=NC=NC4=CC(=C(C=C43)OC)OC.Cl

Mechanism of Action

Targets/IC50/Ki
MEK
KSR2
(Cell-free assay)
120 nM
In vitro
APS-2-79 functions as an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site. APS-2-79 is inactive when KSR was absent or when the KSR2(A690F) mutant was used for in vitro assays. APS-2-79 increases the potency of several MEK inhibitors specifically within Ras-mutant cell lines by antagonizing release of negative feedback signalling.
References

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