[CAS NO. 1221186-53-3] TEPP-46 (ML265)

Name: TEPP-46 (ML265)
Brand: Arctom Scientific
SKU: SLK-S7302

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PRODUCTS SPECIFICATIONS [1221186-53-3]

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Catalog

SLK-S7302

Brand

Selleck

CAS

1221186-53-3

DESCRIPTION [1221186-53-3]

Overview

MDL	-
Molecular Weight	372.46
Molecular Formula	C17H16N4O2S2
SMILES	CN1C2=C(C3=C1C(=O)N(CC4=CC(N)=CC=C4)N=C3)SC(S(C)=O)=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.6849 mL	13.4243 mL	26.8485 mL
5 mM	0.5370 mL	2.6849 mL	5.3697 mL
10 mM	0.2685 mL	1.3424 mL	2.6849 mL
50 mM	0.0537 mL	0.2685 mL	0.5370 mL

Description

TEPP-46 (ML265, CID-44246499, NCGC00186528) is a potent activator of 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.

References

[1] Martin J, et al. ML265: A potent PKM2 activator induces tetramerization and reduces tumor formation and size in a mouse xenograft model. 2012 Mar 16 [Updated 2013 May 8]. In: Probe Reports from the NIH Molecular Libraries Program [Internet].

Synonyms

5H-Thieno[2′,3′:4,5]pyrrolo[2,3-d]pyridazin-5-one, 6-[(3-aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-

6-[(3-Aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-5H-thieno[2′,3′:4,5]pyrrolo[2,3-d]pyridazin-5-one

TEPP-46