Raphin1 acetate

SKU: orb1298863

Description

Raphin1 acetate is an orally active small molecule inhibitor that selectively targets the regulatory phosphatase PPP1R15B (R15B). It is a research tool used to study cellular stress response pathways, including the integrated stress response (ISR), in both in vitro and in vivo models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 2242616-04-0
• MW: 291.13
• Purity: 99.95%
• Formula: C₁₀H₁₂Cl₂N₄O₂
• SMILES: CC(O)=O.NC(=N)N\N=C\c1cccc(Cl)c1Cl
• Target: Phosphatase
• Solubility: DMSO:40 mg/mL (137.4 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.87 mM)

Bioactivity

• Target IC50:
  R15B-PP1c holophosphatase:33 nM(Kd)
• In Vivo:
  Raphin1 was orally bioavailable, crossed the blood-brain barrier, and demonstrated efficacy in a mouse model of Huntington's disease.
• In Vitro:
  Raphin1, a selective inhibitor of R15B. In cells, Raphin1 caused a rapid and transient accumulation of its phosphorylated substrate, resulting in a transient attenuation of protein synthesis. In vitro, Raphin1 inhibits the recombinant R15B-PP1c holoenzyme, but not the closely related R15A-PP1c, by interfering with substrate recruitment.

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

inhibit, Inhibitor, phosphatase PPP1R15B (R15B), Phosphatase, Raphin1 acetate, Raphin1 Acetate, Raphin-1 acetate, Raphin 1, Raphin1, Raphin-1

Compound Identifiers

PubChem CID

139035044