TET-IN-C35

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Overview

First-in-class specific inhibitor of Ten-eleven translocation (TET) catalytic domain, reducing 5hmC marks genomewide and promoting somatic cell reprogramming by inducing the BMP-SMAD-ID downstream pathway


Mechanism of Action

TET-IN-C35 specifically targets the catalytic domain of TET enzymes, inhibiting their activity. This inhibition leads to a reduction in 5hmC levels across the genome, effectively blocking the DNA demethylation pathway. The compound demonstrates potent activity against all three TET enzymes, with reported IC₅₀ values of approximately 1.2 µM for TET2, 3.48 µM for TET1, and 2.31 µM for TET3. PMC

Functional Applications

  • Epigenetic Research: By inhibiting TET enzymes, TET-IN-C35 serves as a valuable tool for studying the role of DNA hydroxymethylation in gene expression and epigenetic regulation.

  • Somatic Cell Reprogramming: The compound has been shown to promote somatic cell reprogramming, potentially by modulating the expression of genes involved in pluripotency. PMC+2PMC+2

  • Cancer Research: Given the involvement of TET enzymes in tumor suppressor gene regulation, TET-IN-C35 may aid in understanding cancer epigenetics and developing therapeutic strategies.

Chemical Properties

Molecular FormulaC26H26O10
Molecular Weight498.48
CAS Numbers98570-83-3
SolubilityDMSO
Purity98% by HPLC
IUPAC/Chemical Name (2R,3S)-2-(3,4-Dihydroxyphenyl)-5,7-dihydroxychroman-3-yl (S)-5-(3,4-dihydroxyphenyl)-3-hydroxypentanoate
InChl KeyFKDRTLFRRHQTGU-TYFWRAIDSA-N
InChl CodeInChI=1S/C26H26O10/c27-15(4-1-13-2-5-18(29)21(32)7-13)11-25(34)35-24-12-17-20(31)9-16(28)10-23(17)36-26(24)14-3-6-19(30)22(33)8-14/h2-3,5-10,15,24,26-33H,1,4,11-12H2/t15-,24-,26+/m0/s1
SMILES CodeC1C(C(OC2=CC(=CC(=C21)O)O)C3=CC(=C(C=C3)O)O)OC(=O)CC(CCC4=CC(=C(C=C4)O)O)O

Storage and Handling

0°C (short term), -20°C (long term), desiccated

Synonyms

TETINC35; TETIN-C35; TET-INC35; Phylloflavan; NSC 607319

References

1) Anup Kumar Singh et al., Selective targeting of TET catalytic domain promotes somatic cell reprogramming, PNAS February 18, 2020 117 (7) 3621-3626