APS-2-79 hydrochloride

SKU: orb1300491

Description

APS-2-79 HCl is a small molecule MAPK pathway antagonist that disrupts RAF dimerization and the conformational activation of KSR-bound MEK. It is a valuable research tool for studying oncogenic RAS/MAPK signaling in both cellular and animal models of cancer and developmental disorders.

Research Area

Signal Transduction

Key Properties

• CAS Number: 2002381-31-7
• MW: 423.89
• Purity: 97.08%
• Formula: C₂₃H₂₁N₃O₃·HCl
• SMILES: Cl.COc1cc2ncnc(Nc3ccc(Oc4ccccc4)cc3C)c2cc1OC
• Target: MEK,MAPK
• Solubility: DMSO:90 mg/mL (212.32 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:30 mg/mL (70.77 mM)

Bioactivity

• Target IC50:
  KSR2:120 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.
• Cell Research:
  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(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

APS 2 79 hydrochloride, APS-2-79 HCl, APS279 hydrochloride, APS-2-79 Hydrochloride, MAP2K, MAPKK, MEK, KSR2, Mitogen-activated protein kinase kinase

Compound Identifiers

PubChem CID

122177134