TEPP-46 (ML265, CID-44246499, NCGC00186528)

Catalog No.S7302

TEPP-46 (ML265, CID-44246499, NCGC00186528) Chemical Structure

Molecular Weight(MW): 372.46

ML265 is a potent activator of PKM2 in both biochemical (AC50 = 92 nM) and cell-based assays with high selectivity over PKM1, PKR and PKL.

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Biological Activity

Description ML265 is a potent activator of PKM2 in both biochemical (AC50 = 92 nM) and cell-based assays with high selectivity over PKM1, PKR and PKL.
Targets
PKM2 [1]
()
In vitro

ML265 potently activates PKM2 in vitro with an AC50 = 92 nM and shows a high degree of selectivity over the other 3 pyruvate kinase isoforms. ML265 binds at the dimer-dimer interface of the PKM2 homotetramer. It is capable of activating PKM2 in cell lysate of pervanadate treated cells, which is a condition known to inhibit PKM2 activity through accumulation of phosphotyrosine peptides. ML265 significantly increased the doubling time of H1299 cells under hypoxic conditions, but interestingly showed no effect under normoxia[1].

In vivo

ML265 gave superior plasma concentrations that persisted at higher levels over the 24 hour study. ML265 also displayed good oral bioavailability, low clearance, a long half-life and good volume of distrubtion. The 7-week mouse xenograft model (H1299 mouse xenograft) showed that the activation of PKM2 with ML265 was able to significantly reduce tumor size and occurrence without showing signs of acute toxicity. [1].

Protocol

Kinase Assay:

[1]

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PKM2 activity assay:

Pyruvate kinase activity is measured by monitoring pyruvate-dependent conversion of NADH to NAD+ by lactate dehydrogenase (LDH). Briefly, for cell line experiments, the medium is replaced with fresh medium 1 hr prior to the start of treatment with DMSO or activator. Also, where indicated, 100 μM pervanadate is added 10 min prior to cell lysis. Cells are lysed on ice with RIPA buffer containing 2 mM DTT and protease inhibitors and clarified by centrifugation at 21,000 × g. 5 μL of the supernatant is used to assess pyruvate kinase activity. Pyruvate kinase activity was subsequently normalized for total protein content.
Cell Research:

[1]

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  • Cell lines: H1299 cells
  • Concentrations: 50 μM
  • Incubation Time: 1 h
  • Method:

    H1299 cells incubated with 50 μM ML265 for 1 hour, lysed followed by 2-D electrophoresis, Western blot and PGAM1 antibody staining.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Male Balb/c mice
  • Formulation: IV: 40% w/v beta hydroxy cylcodextrin in water; IP: 40% w/v beta hydroxy cylcodextrin in water; PO: 0.5% w/v carboxy methyl cellulose (400–1000 cps) with 0.1 % v/v Tween 80
  • Dosages: IV: 1 mg/kg, PO: 10 mg/kg; IP: 10 and 50 mg/kg
  • Administration: IV, IP and PO
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (198.67 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 372.46
Formula

C17H16N4O2S2

CAS No. 1221186-53-3
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID