Creative Biolabs

A 769662 [AMPK Activator]

[CAT#: MOD2005ZP64]

A highly potent, reversible AMPK activator. Inhibits MSC proliferation.

Datasheet MSDS Request COA

Certificate of Analysis Lookup
To download a Certificate of Analysis, please enter a lot number in the search box below. Note: Certificate of Analysis not available for kit components.
Lot Number

Bulk Quote
Description
Powerful reversible AMP-activated protein kinase (AMPK) activator (EC50 = 0.8 µM). Allosteric activation of AMPK and inhibition of AMPK dephosphorylation. Na +-K +-ATPase inhibitors (IC50 values for rats and humans are 57 and 220 µM, respectively). Stimulates glucose uptake and reduce fatty acid synthase levels. It also shown to inhibit MSC proliferation.
Chemical Name
6,7-Dihydro-4-hydroxy-3-(2'-hydroxy[1,1'-biphenyl]-4-yl)-6-oxo-thieno[2,3-b]pyridine-5-carbonitrile
Modulator Type
Activator
Relevant Disease
Neurological Disorders
Assay Description
A-769662 also effectively activated the α1, β1, and γ1 recombinant isoforms of AMPK expressed by baculovirus (EC50 = 0.7 μM). A-769662 and A-592107 activated AMPK purified from multiple tissues and species in a dose-responsive manner, with slight changes in EC50 observed. The EC50 of A-769662 measured using partially purified AMPK extracts from rat heart, rat muscle or human embryonic kidney cells (HEK) was 2.2 μM, 1.9 μM or 1.1 μM, respectively [1]. A-769662 activates endogenous AMPK in LKB1-expressing (HEK293) and LKB1-deficient (CCL13) cells. A-769662 allosterically activates the AMPK complex containing γ1, which has arginine residue 298 instead of glycine (R298G). A-769662 can inhibit the dephosphorylation of Thr-172 in the mutant γ1-containing complex, and its degree of inhibition is similar to that of the wild-type complex [2]. A769662 (300μM) has a toxic effect on MEF cells. A769662 reversibly inhibits proteasome activity [3].
Reference
[1]. Cool B, et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab, 2006, 3(6), 403-416.

[2]. Sanders MJ, et al. Defining the mechanism of activation of AMP-activated protein kinase by the small molecule A-769662, a member of the thienopyridone family. J Biol Chem, 2007, 282(45), 32539-32548.

[3]. Moreno D, et al, A769662, a novel activator of AMP-activated protein kinase, inhibits non-proteolytic components of the 26S proteasome by an AMPK-independent mechanism. FEBS Lett, 2008, 583(17), 2650-2654.
Assay Description
A-769662 (30 mg/kg, i.p.) significantly reduced the respiratory exchange rate (RER) of SD rats. The levels of malonyl-CoA in the livers of animals treated with 30 mg/kg A-769662 (0.905 nmol/g) or 500 mg/kg metformin (0.574 nmol/g) were reduced by 33% and 58%, respectively. A-769662 (30 mg/kg, bid) will significantly reduce the plasma glucose consumed (30%-40% reduction), while lower doses (3 and 10 mg/kg) of A-769662 have a diabetic/ ob mice [1].
References
[1]. Cool B, et al. Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome. Cell Metab, 2006, 3(6), 403-416.
Molecular Weight
360.39
Form
Powder
Chemical Formula
C20H12N2O3S
Source
Synthetic
SMILES
C1=CC=C(C(=C1)C2=CC=C(C=C2)C3=CSC4=C3C(=C(C(=O)N4)C#N)O)O
Solubility
Soluble in DMSO (100 mM)
EC50
0.8 μM
CAS NO.
844499-71-4
PubChem Substance ID
54708532
Purity
>98%
Storage
Store at +4°C
Shipping
Room Temperature
Handling Advice
For obtaining a higher solubility, please warm the tube at 37 °C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -21°C for several months.
Research Use Only
For research use only

For Research Use Only. Not For Clinical Use.
Send Inquiry Send Inquiry
Inquiry Basket
compare

Go to compare