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TEPP-46 (ML265), Pyruvate Kinase M2 (PKM2) Activator

Overview
Catalog # bs-60304c-2-mg-solid
Product Name TEPP-46 (ML265), Pyruvate Kinase M2 (PKM2) Activator
Specifications
Storage Buffer Powder
Storage Condition Store in dry, dark place at -20C for 1 year.
Target
Product Information Molecular Weight: 372.46

Formula: C17 H16 N4 O2 S2

CAS Number: 1221186-53-3

InChi Key: ZWKJWVSEDISQIS-UHFFFAOYSA-N

InChi: InChI=1S/C17H16N4O2S2/c1-20-13-7-14(25(2)23)24-16(13)12-8-19-21(17(22)15(12)20)9-10-4-3-5-11(18)6-10/h3-8H,9,18H2,1-2H3

Smiles: CN1C2=C(C=NN(CC3=CC(N)=CC=C3)C2=O)C2SC(=CC1=2)S(C)=O

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years
Description TEPP-46 (ML265) is a potent and selective Pyruvate kinase M2 (PKM2) activator with EC50 ~92 nM. It demonstrates >100-fold selectivity for PKM2 over the related PKM1, PKR, and PKL isoforms. It can stabilize pyruvate kinase subunit interactions, promote PKM2 tetramer formation and prevent inhibition by phosphotyrosine signaling. It can alter metabolism in cultured cells, and inhibit xenograft tumor growth in vivo. TEPP-46 inhibits LPS-induced Hif-1α and IL-1β, as well as the expression of a range of other Hif-1α-dependent genes.