TEPP-46 (ML265) - Pyruvate Kinase M2 (PKM2) Activator. CAS# 1221186-53-3 60123 resulting in accumulation of ubiquitinated

resulting in accumulation of ubiquitinated substrates

EMCS Crosslinker

CX-5461 was administered orally at 50 mg/kg either once daily or every 3 days

InChi: InChI=1S/C23H33N5O2/c1-2-14-27-15-17-28(18-16-27)20-8-6-19(7-9-20)21(29)26-23(10-4-3-5-11-23)22(30)25-13-12-24/h6-9H

Epub 2019 Jan 23

TEPP-46 (ML265) - Pyruvate Kinase M2 (PKM2) Activator. CAS# 1221186-53-3 60123 resulting in accumulation of ubiquitinatedTEPP 46 (ML265), CAS No. 1221186 53 3, 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