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DF-A7

Chemical Structure : DF-A7

CAS No.: 105580-96-9

DF-A7 (YTHDF2 inhibitor DF-A7)

Catalog No.: PC-22438Not For Human Use, Lab Use Only.

DF-A7 a specific small-molecule degrader/inhibitor of m6A reader YTHDF2 with IC50 of 50 nM in immunoblotting assays (HEK 293T cells), induces degradation of YTHDF2 without affecting the degradation of YTHDF1 and YTHDF3.

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Biological Activity

DF-A7 a specific small-molecule degrader/inhibitor of m6A reader YTHDF2 with IC50 of 50 nM in immunoblotting assays (HEK 293T cells), induces degradation of YTHDF2 without affecting the degradation of YTHDF1 and YTHDF3.
DF-A7 predictively binds to the YTHDF2 protein at the K416, G463, K521, N518, and R527 sites, forming a total of seven hydrogen bonds.
DF-A7 increases the mRNA expression of Cx3cl1 and PRR5 after degrading YTHDF2.
DF-A7 (12.5 mg/kg) significantly inhibited tumor growth compared with vehicle control in both MC38 and B16-OVA tumor models, significantly prolonged the survival of mice.
DF-A7 inhibits tumor growth and improves antitumor efficacy when in combination with PD-1/PD-L1 blockade therapy.

Physicochemical Properties

M.Wt 446.50
Formula C22H30N4O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5,8-bis((2-((2-hydroxyethyl)amino)ethyl)amino)anthracene-1,4,9,10-tetraol

References

1. Xiao S, et al. Sci Immunol. 2024 May 31;9(95):eadl2171.

2. Durand M, et al. J Exp Clin Cancer Res. 2024 May 22;43(1):148.

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