Skip to Content
MilliporeSigma
All Photos(1)

Key Documents

SML3121

Sigma-Aldrich

TETi76 diethyl ester

≥95% (HPLC)

Synonym(s):

2-Hydroxy-4-methylene-pentanedioic acid, 1,5-diethyl ester, AD145, Diethyl 2-hydroxy-4-methylenepentanedioate, TETi76 ester

Sign Into View Organizational & Contract Pricing


About This Item

Empirical Formula (Hill Notation):
C10H16O5
CAS Number:
Molecular Weight:
216.23
UNSPSC Code:
12352108
NACRES:
NA.77

Quality Level

assay

≥95% (HPLC)

form

oil

color

colorless to yellow

storage temp.

2-8°C

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.).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Choose from one of the most recent versions:

Certificates of Analysis (COA)

Lot/Batch Number

It looks like we've run into a problem, but you can still download Certificates of Analysis from our Documents section.

If you need assistance, please contact Customer Support.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service