SML3121

TETi76 diethyl ester

≥95% (HPLC)

• Synonym(e): 2-Hydroxy-4-methylene-pentanedioic acid, 1,5-diethyl ester, AD145, Diethyl 2-hydroxy-4-methylenepentanedioate, TETi76 ester
• Empirische Formel (Hill-System): C₁₀H₁₆O₅
• CAS-Nummer: 1451750-73-4
• Molekulargewicht: 216.23
• NACRES: NA.77
• UNSPSC Code: 12352108
• Assay: ≥95% (HPLC)
• Form: oil

Eigenschaften

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: oil
• color: colorless to yellow
• storage temp.: 2-8°C

Beschreibung

Biochem/physiol Actions

Cell-permeant, α-KG-competitive and hightly selective TET1/2/3 inhibitor with preferential cytotoxicity against TET-deficient cells in vitro and in vivo.

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.).

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable