PT 1

AMPK activator, selective CAS# 331002-70-1

PT 1

Catalog No. BCC7846----Order now to get a substantial discount!

Product Name & Size Price Stock
PT 1: 5mg $115 In Stock
PT 1: 10mg Please Inquire In Stock
PT 1: 20mg Please Inquire Please Inquire
PT 1: 50mg Please Inquire Please Inquire
PT 1: 100mg Please Inquire Please Inquire
PT 1: 200mg Please Inquire Please Inquire
PT 1: 500mg Please Inquire Please Inquire
PT 1: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of PT 1

Number of papers citing our products

Chemical structure

PT 1

3D structure

Chemical Properties of PT 1

Cas No. 331002-70-1 SDF Download SDF
PubChem ID 5753734 Appearance Powder
Formula C23H16ClN3O6S M.Wt 497.91
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 100 mM in 1.1eq. NaOH
Chemical Name 2-chloro-5-[[(5Z)-5-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-4-oxo-1,3-thiazol-2-yl]amino]benzoic acid
SMILES CC1=C(C=C(C(=C1)C2=CC=C(O2)C=C3C(=O)N=C(S3)NC4=CC(=C(C=C4)Cl)C(=O)O)[N+](=O)[O-])C
Standard InChIKey RTHRCOIONCZINZ-JMIUGGIZSA-N
Standard InChI InChI=1S/C23H16ClN3O6S/c1-11-7-16(18(27(31)32)8-12(11)2)19-6-4-14(33-19)10-20-21(28)26-23(34-20)25-13-3-5-17(24)15(9-13)22(29)30/h3-10H,1-2H3,(H,29,30)(H,25,26,28)/b20-10-
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PT 1

DescriptionAMP-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.

PT 1 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

PT 1 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of PT 1

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.0084 mL 10.042 mL 20.084 mL 40.1679 mL 50.2099 mL
5 mM 0.4017 mL 2.0084 mL 4.0168 mL 8.0336 mL 10.042 mL
10 mM 0.2008 mL 1.0042 mL 2.0084 mL 4.0168 mL 5.021 mL
50 mM 0.0402 mL 0.2008 mL 0.4017 mL 0.8034 mL 1.0042 mL
100 mM 0.0201 mL 0.1004 mL 0.2008 mL 0.4017 mL 0.5021 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on PT 1

PT 1 is a selective activator of AMPK with EC50 value of 0.3 μM for AMPK α1β1γ1 [1].

AMP-activated protein kinase (AMPK) is serine/threonine protein kinase that involved in cellular energy homeostasis and acts as an energy sensor. AMPK is a heterotrimer and increases ATP generation [1].

PT 1 is a selective AMPK activator. PT1 activated human AMPK α1394, AMPK α2398 and AMPK(α1β1γ1) with EC50 values of 8, 12 and 0.3 μM, respectively. PT1 exhibited maximum activity against AMPK(α1β1γ1) at concentration up to 5 μM. PT1 exhibited high selectivity for AMPK α catalytic subunit. PT1 activated truncated AMPK α1 subunit proteins including 313-335 aa with EC50 values of 8 μM, which was autoinhibitory domain. In HeLa cells without LKB1, PT1 induced AMPK and ACC phosphorylation, which were independent of LKB1. In human hepatoma HepG2 cells, PT1 dose-dependently reduced triacylglycerol and cholesterol content and induced AMPK and ACC phosphorylation [1]. In incubated mouse muscle, PT-1 increased γ1-containing AMPK activity and increased the AMPK-dependent phosphorylation of ULK1 on Ser555. However, in HEK293 cells expressing human γ1-, γ2- or γ3-AMPK, PT-1 activated them equally [2].

References:
[1].  Pang T, Zhang ZS, Gu M, et al. Small molecule antagonizes autoinhibition and activates AMP-activated protein kinase in cells. J Biol Chem, 2008, 283(23): 16051-16060.
[2].  Jensen TE, Ross FA, Kleinert M, et al. 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, 2015, 467(3): 461-472.

Featured Products
  • IQ 1

    Catalog No.:BCC7965
    CAS No.:331001-62-8
  • Caffeic acid

    Catalog No.:BCN5979
    CAS No.:331-39-5
  • AS 1269574

    Catalog No.:BCC7878
    CAS No.:330981-72-1
  • Betrixaban

    Catalog No.:BCC5118
    CAS No.:330942-05-7
  • Amitraz

    Catalog No.:BCC8816
    CAS No.:33089-61-1
  • MRT 10

    Catalog No.:BCC7950
    CAS No.:330829-30-6
  • PCI 29732

    Catalog No.:BCC4100
    CAS No.:330786-25-9
  • Avanafil

    Catalog No.:BCC2288
    CAS No.:330784-47-9
  • Paclitaxel

    Catalog No.:BCN4650
    CAS No.:33069-62-4
  • KH 7

    Catalog No.:BCC7787
    CAS No.:330676-02-3
  • HCTU

    Catalog No.:BCC2818
    CAS No.:330645-87-9
  • TCTU

    Catalog No.:BCC2689
    CAS No.:330641-16-2
New Products
 

References on PT 1

An in vivo active 1,2,5-oxadiazole Pt(II) complex: A promising anticancer agent endowed with STAT3 inhibitory properties.[Pubmed:28324784]

Eur J Med Chem. 2017 May 5;131:196-206.

New Pt(II) complexes (Pt-1-3) bearing 1,2,5-oxadiazole ligands (1-3) were synthesized, characterized and evaluated for their ability to disrupt STAT3 dimerization. Ligand 3.HCl showed cytotoxic effects on HCT-116 cells (IC50 = 95.2 muM) and a selective ability to interact with STAT3 (IC50 = 8.2 muM) versus STAT1 (IC50 > 30 muM). Its corresponding platinum complex Pt-3 exhibited an increased cytotoxicity (IC50 = 18.4 muM) and a stronger interaction with STAT3 (IC50 = 1.4 muM), leading to inhibition of its signaling pathway. Pt-3 was also evaluated in cell-based assays for its action on p53 expression and on STAT3 phosphorylation. In syngeneic murine Lewis lung carcinoma (LLC) implanted in C57BL/6 mice, Pt-3 showed a higher antitumor activity with fewer side effects than cisplatin.

Pt nanoparticles immobilized in mesostructured silica: a non-leaching catalyst for 1-octene hydrosilylation.[Pubmed:28229136]

Chem Commun (Camb). 2017 Mar 7;53(20):2962-2965.

A catalyst containing small (ca. 2.5 nm) and crystalline Pt nanoparticles embedded into the walls of a mesostructured silica framework was found to be highly active in alkene hydrosilylation reaching TONs of ca. 10(5). More importantly, no Pt leaching was detected. This result is remarkable because Pt leaching is a recurrent problem in alkene hydrosilylation, which often prevents heterogeneous catalysts from being used industrially. This result is in contrast to the significant Pt leaching observed for other Pt/SiO2 catalysts.

Probing the Interactions of Cytotoxic [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)] and Its Pt(IV) Derivatives with Human Serum.[Pubmed:28206707]

ChemMedChem. 2017 Apr 6;12(7):510-519.

The discrepancy between the in vitro cytotoxic results and the in vivo performance of Pt56MeSS prompted us to look into its interactions and those of its Pt(IV) derivatives with human serum (HS), human serum albumin (HSA), lipoproteins, and serum-supplemented cell culture media. The Pt(II) complex, Pt56MeSS, binds noncovalently and reversibly to slow-tumbling proteins in HS and in cell culture media and interacts through the phenanthroline group with HSA, with a Kd value of approximately 1.5x10(-6) m. All Pt(IV) complexes were found to be stable toward reduction in HS, but those with axial carboxylate ligands, cct-[Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenantroline)(acetato)2 ](TFA)2 (Pt56MeSS(OAc)2 ) and cct-[Pt(1S,2S-DACH)(5,6-dimehtyl-1,10-phenantroline)(phenylbutyrato)2 ](TFA)2 (Pt56MeSS(PhB)2 ), were spontaneously reduced at pH 7 or higher in phosphate buffer, but not in Tris buffer (pH 8). HS also decreased the rate of reduction by ascorbate of the Pt(IV) complexes relative to the reduction rates in phosphate buffer, suggesting that for this compound class, phosphate buffer is not a good model for HS.

Exposure of Pt(5 5 3) and Rh(1 1 1) to atomic and molecular oxygen: do defects enhance subsurface oxygen formation?[Pubmed:28323632]

J Phys Condens Matter. 2017 Apr 26;29(16):164002.

Subsurface oxygen is known to form in transition metals, and is thought to be an important aspect of their ability to catalyze chemical reactions. The formation of subsurface oxygen is not, however, equivalent across all catalytically relevant metals. As a result, it is difficult to predict the stability and ease of the formation of subsurface oxygen in metals, as well as how the absorbed oxygen affects the chemical and physical properties of the metal. In comparing how a stepped platinum surface, Pt(5 5 3), responds to exposure to gas-phase oxygen atoms under ultra-high vacuum conditions to planar Rh(1 1 1), we are able to determine what role, if any, steps have on the capacity of a metal for subsurface oxygen formation. Despite the presence of regular defects, we found that only surface-bound oxygen formed on Pt(5 5 3). Alternatively, on the Rh(1 1 1) surface, oxygen readily absorbed into the selvedge of the metal. These results suggest that defects alone are insufficient for the formation of subsurface oxygen, and the ability of the metal to absorb oxygen is the primary factor in the formation and stabilization of subsurface oxygen.

PT-1 selectively activates AMPK-gamma1 complexes in mouse skeletal muscle, but activates all three gamma subunit complexes in cultured human cells by inhibiting the respiratory chain.[Pubmed:25695398]

Biochem J. 2015 May 1;467(3):461-72.

AMP-activated protein kinase (AMPK) occurs as heterotrimeric complexes in which a catalytic subunit (alpha1/alpha2) is bound to one of two beta subunits (beta1/beta2) and one of three gamma subunits (gamma1/gamma2/gamma3). The ability to selectively activate specific isoforms would be a useful research tool and a promising strategy to combat diseases such as cancer and Type 2 diabetes. We report that the AMPK activator PT-1 selectively increased the activity of gamma1- but not gamma3-containing complexes in incubated mouse muscle. PT-1 increased the AMPK-dependent phosphorylation of the autophagy-regulating kinase ULK1 (unc-51-like autophagy-activating kinase 1) on Ser555, but not proposed AMPK-gamma3 substrates such as Ser231 on TBC1 (tre-2/USP6, BUB2, cdc16) domain family, member 1 (TBC1D1) or Ser212 on acetyl-CoA carboxylase subunit 2 (ACC2), nor did it stimulate glucose transport. Surprisingly, however, in human embryonic kidney (HEK) 293 cells expressing human gamma1, gamma2 or gamma3, PT-1 activated all three complexes equally. We were unable to reproduce previous findings suggesting that PT-1 activates AMPK by direct binding between the kinase and auto-inhibitory domains (AIDs) of the alpha subunit. We show instead that PT-1 activates AMPK indirectly by inhibiting the respiratory chain and increasing cellular AMP:ATP and/or ADP:ATP ratios. Consistent with this mechanism, PT-1 failed to activate AMPK in HEK293 cells expressing an AMP-insensitive R299G mutant of AMPK-gamma1. We propose that the failure of PT-1 to activate gamma3-containing complexes in muscle is not an intrinsic feature of such complexes, but is because PT-1 does not increase cellular AMP:ATP ratios in the specific subcellular compartment(s) in which gamma3 complexes are located.

Turning enzymes ON with small molecules.[Pubmed:20154666]

Nat Chem Biol. 2010 Mar;6(3):179-188.

Drug discovery and chemical genetic efforts typically focus on the identification and design of inhibitors or loss-of-function probes as a means to perturb enzyme function. These tools are effective in determining the physiological consequence of ablating the activity of a specific enzyme. Remarkably, nearly a dozen examples of non-natural small molecules that activate enzyme catalysis have been identified within the past decade. In aggregate, these studies delineate four unique activation mechanisms that the small molecules exploit. These complementary gain-of-function probes offer a way to address the sufficiency of an enzyme to drive a particular cellular phenotype, and they also provide new opportunities for drug discovery. This review covers the identification and characterization of these unique small-molecule activators.

Description

AMPK activator

Keywords:

PT 1,331002-70-1,Natural Products,AMPK, buy PT 1 , PT 1 supplier , purchase PT 1 , PT 1 cost , PT 1 manufacturer , order PT 1 , high purity PT 1

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: