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TETi76 ester | TET inhibitor

CAS:
 1451750-73-4
Catalog Number:
 10-4041

TETi76 ester (1451750-73-4) is a cell permeable inhibitor of TET dioxygenases  (IC50s: TET1 = 1.5 µM; TET2 = 9.4 µM; TET3 = 8.8 µM), indirect (via cytosine hydroxymethylation) erasers of DNA methylation.1,2 TET2 is frequently mutated in myeloid neoplasms – TET2 inhibition with TETi76 restricted clonal outgrowth and induced apoptosis of TET2 mutants but not normal hematopoietic precursor cells in vitro and in vivo.

References/Citations:

  1. Guan et al. (2021), A Therapeutic Strategy for Preferential Targeting of TET2-Mutant and TET Dioxygenase-Deficient Cells in Myeloid Neoplasms; Blood Cancer Discov., 146
  2. Guan et al. (2021), Therapeutic Targeting of TET-Dioxygenase Deficiency in Myeloid Malignancies; Blood, 138 3985
TETi76 ester | TET inhibitor is also available in the Cellular Metabolism Library.
CAS:
1451750-73-4
Catalog Number:
10-4041
Activity:
TET inhibitor
Chemical Names:
Diethyl 2-hydroxy-4-methylenepentanedioate
Molecular Weight:
216.23
Molecular Formula:

C10H16O5

Solubility:
Soluble in DMSO (>100 mg/ml)
Physical Properties:
Colorless oil
Purity:

>98% TLC
NMR (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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