APS-2-79 HCl

Catalog No.S8355 Batch:S835501

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Technical Data

Formula

C23H21N3O3.HCl
Molecular Weight 423.89 CAS No. 2002381-31-7
Solubility (25°C)* In vitro DMSO 97 mg/mL (228.83 mM)
Ethanol 32 mg/mL (75.49 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 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].

Protocol (from reference)

Cell Assay:[1]
  • 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

Customer Product Validation

Data from [Data independently produced by , , Experimental and therapeutic medicine, 2018, https://doi.org/10.3892/etm.2018.6081]

Selleck's APS-2-79 HCl has been cited by 2 publications

Evolutionarily conserved regulation of sleep by epidermal growth factor receptor signaling. [ Sci Adv, 2019, 5(11):eaax4249] PubMed: 31763451
Effect of aromatase inhibitor letrozole on the proliferation of spermatogonia by regulating the MAPK pathway [Wang S, et al. Exp Ther Med, 2018, 15(6):5269-5274] PubMed: 29805545

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.