SML3121

TETi76 diethyl ester

≥95% (HPLC)

• Synonyme(s) : 2-Hydroxy-4-methylene-pentanedioic acid, 1,5-diethyl ester, AD145, Diethyl 2-hydroxy-4-methylenepentanedioate, TETi76 ester
• Formule empirique (notation de Hill): C₁₀H₁₆O₅
• Numéro CAS: 1451750-73-4
• Poids moléculaire : 216.23
• Code UNSPSC : 12352108

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: oil
• Couleur: colorless to yellow
• Température de stockage: 2-8°C

Description

Actions biochimiques/physiologiques

TETi76 diethyl ester is a cell-permeant diester form of the α-KG-competitive and hightly selective TET1/2/3 dioxygenase inhibitor TETi76 acid (TET2 cat. domain Kd = 0.3 μM; no potency against 16 other αKG/Fe2+-dependent enzymes, including closely related RNA dioxygenase FTO). TETi76 ester downregulates cellular 5-hydroxymethylcytosine (5hmC) levels (IC50 = 20-37 μM; K562, MEG01, SIGM5, OCI-AML5, MOLM13), exerts preferential cytotoxicity in TET-deficient cultures (TET2/3-knockout K562 LD50 ~10 μM vs wt K562 LD50 ~40 μM) and significantly reduces TET2-deficient SIGM5 tumor burden in mice in vivo (50 mg/kg p.o.).

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable