Home MAPK MEK antagonist APS-2-79 HCl For research use only.

APS-2-79 HCl

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 Chemical Structure

APS-2-79 HCl Chemical Structure

CAS No. 2002381-31-7

Purity & Quality Control

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

APS-2-79 HCl Related Products

Signaling Pathway

MEK Signaling Pathways

MEK Signaling Pathway

Biological Activity

Description 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.
Targets
MEK [1] KSR2 [1]
(Cell-free assay)
120 nM
In vitro
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[1].
Cell Research Cell lines HCT-116, A549, SK-MEL-239 and A375 cell lines
Concentrations 1 μM
Incubation Time 72 h
Method Cell viability assays are performed in 96 well plates. Optimal cell densities for 96 well plate assays are determined to obtain linear growth over the timecourse of assays. Specifically, A549, HCT-116, A375, SK-MEL-239, COLO-205, LOVO, SK-MEL-2, CALU-6, MEWO, SW620 and SW1417 cells are plated at 500 cells per well and treated with inhibitors for 72hrs before measuring viability. H2087 and HEPG2 cells are plated at 2000 cells per well, and treated with inhibitors for 72hrs. Cell viability is measured using resazurin, and the percent cell viability is determined by normalizing inhibitor-treated samples to DMSO controls

Chemical Information & Solubility

Molecular Weight 423.89 Formula

C23H21N3O3.HCl
CAS No. 2002381-31-7 SDF Download APS-2-79 HCl SDF
Smiles CC1=C(C=CC(=C1)OC2=CC=CC=C2)NC3=NC=NC4=CC(=C(C=C43)OC)OC.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 97 mg/mL ( (228.83 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 32 mg/mL

Water : Insoluble


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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.

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