AA147 | ATF6 activator

CAS:
393121-74-9
Catalog Number:
10-3973
Activity:
Activator of ER stress sensing protein ATF6
Chemical Names:
N-(2-Hydroxy-5-methylphenyl)-3-phenylpropanamide; Compound 147
Molecular Weight:
255.32
Molecular Formula:
C16H17NO2
Solubility:
Soluble in DMSO (>25 mg/ml); ethanol (>25 mg/mL)
Physical Properties:
Beige to pale orange solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
10 mg$45.00
50 mg$195.00

AA147 (393121-74-9) is a preferential activator of the ER stress sensing protein ATF6.1 It was able to selectively reduce secretion and extracellular aggregation of destabilized amyloidogenic variants of TTR and LC proteins. AA147-dependent ATF6 activation proceeds via metabolic activation to a reactive electrophile that selectively modifies ER proteins including multiple protein disulfide isomerases.2  AA147 suppressed pluripotency and promoted human stem cell differentiation toward a mesodermal lineage via ER expansion.3  It protected the heart against ischemia/reperfusion (I/R) injury in a mouse model of acute myocardial infarction in an ATF6-dependent manner.4 Brain, kidney, and liver tissue was also protected from I/R damage and impaired proteostasis. AA147 reduced infection of multiple strains of dengue and Zika viruses in an ATF6-independent manner.5 Protects against glutamate-induced cell death is a neuronal-derived cell culture model.6 See companion inhibitor 10-3974.

References:

  1. Plate et al. (2016), Small molecule proteostasis regulators that reprogram the ER to reduce extracellular protein aggregation; Elife 5 e15550
  2. Paxman et al. (2018), Pharmacologic ATF6 activating compounds are metabolically activated to selectively modify endoplasmic reticulum, proteins; Elife 7 e37168
  3. Kroeger et al. (2018), The unfolded protein response regulator ATF6 promotes mesodermal differentiation; Sci. Signal. 11 eaan5785
  4. Blackwood et al. (2019), Pharmacological ATF6 activation confers global protection in widespread disease models by reprogramming cellular proteostasis; Nat. Commun. 10 187
  5. Almasy et al. (2021), Small molecule endoplasmic reticulum proteostasis regulator acts as a broad-spectrum inhibitor of dengue and Zika virus infections; Proc. Natl. Acad. Sci. USA 118 e2012209118
  6. Rosardo et al. (2021), Metabolically Activated Proteostasis Regulators against Glutamate Toxicity by Activating NRF2; ACS Chem. Biol. 16 2852
CAS:
393121-74-9
Catalog Number:
10-3973
Activity:
Activator of ER stress sensing protein ATF6
Chemical Names:
N-(2-Hydroxy-5-methylphenyl)-3-phenylpropanamide; Compound 147
Molecular Weight:
255.32
Molecular Formula:
C16H17NO2
Solubility:
Soluble in DMSO (>25 mg/ml); ethanol (>25 mg/mL)
Physical Properties:
Beige to pale orange solid
Purity:
98% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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