PT 1

Discontinued Product

PT 1 (Cat. No. 4039) has been withdrawn from sale for commercial reasons.
Description: AMPK activator
Chemical Name: 2-Chloro-5-[[5-[[5-(4,5-Dimethyl-2-nitrophenyl)-2-furanyl]methylene]-4,5-dihydro-4-oxo-2-thiazolyl]amino]benzoic acid
Purity: ≥98% (HPLC)
Citations (2)
Pathways (1)

Biological Activity for PT 1

PT 1 is an aMP-activated protein kinase (AMPK) activator. Stimulates AMPK heterotrimer (α1β1γ1) activity (EC50 = 0.3 μM). Selectively increases the activity of γ1- but not γ3-containing complexes. Thought to directly activate AMPK by antagonizing autoinhibition.

Technical Data for PT 1

M. Wt 497.91
Formula C23H16ClN3O6S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 331002-70-1
PubChem ID 5753734
Smiles ClC1=C(C(O)=O)C=C(/N=C3/NC(/C(S3)=C/C2=CC=C(C4=C([N+]([O-])=O)C=C(C)C(C)=C4)O2)=O)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for PT 1

References are publications that support the biological activity of the product.

Zorn and Wells (2010) Turning enzymes ON with small molecules. Nat.Chem.Biol. 6 179 PMID: 20154666

Pang et al (2007) Small molecule antagonizes autoinhibition and activates AMP-activated protein kinase in cells. J.Biol.Chem. 283 16051

Jensen et al (2015) PT-1 selectively activates AMPK-γ1 complexes in mouse skeletal muscle, but activates all three γ subunit complexes in cultured human cells by inhibiting the respiratory chain. Biochem.J. 467 461 PMID: 25695398

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Keywords: PT 1, PT 1 supplier, AMPK, amp-activated, protein, kinase, activators, PT1, Enzyme, Substrates, /, Activators, 4039, Tocris Bioscience

2 Citations for PT 1

Citations are publications that use Tocris products. Selected citations for PT 1 include:

Asiedu et al (2017) The AMPK Activator A769662 Blocks Voltage-Gated Sodium Channels: Discovery of a Novel Pharmacophore with Potential Utility for Analgesic Development. PLoS One 12 e0169882 PMID: 28118359

Huang et al (2016) The AMPK Agonist PT1 and mTOR Inhibitor 3HOI-BA-01 Protect Cardiomyocytes After Ischemia Through Induction of Autophagy. J Cardiovasc Pharmacol Ther 21 70 PMID: 25868658

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Pathways for PT 1

AMPK Signaling Pathway

AMPK Signaling Pathway

AMPK signaling pathway plays an important role in the cellular reponse to low levels of available ATP, often caused by stresses such as heat shock, ischemia or hypoxia.