Cat. No. Name Size Price Add Cart
KI2259RGFP96610 mg$236
RGFP96650 mg$912

Chemical Characteristic

Product NameRGFP966
SynonymsN/A
CAS No.1396841-57-8
Molecular Weight 362.4
FormulaC21H19FN4O
Chemical Name2-Propenamide, N-(2-amino-4-fluorophenyl)-3-[1-[(2E)-3-phenyl-2-propen-1-yl]-1H-pyrazol-4-yl]-, (2E)-
SmilesC(=O)(/C=C/c1cnn(c1)C/C=C/c1ccccc1)Nc1c(cc(cc1)F)N
Chemical Structure

Biological activities

RGFP966 is a potent HDAC3 inhibitor with an IC50 of 80 nM. RGFP966 at concentrations up to 15 μM have no effective inhibition of any other HDAC.[1] In vitro, RGFP966 treatment increases apoptosis that is associated with DNA damage and impaires S phase progression, resulting in decreased cell growth in cutaneous T cell lymphoma (CTCL) cell lines.[2] In vivo in mice, systemic treatment with RGFP966 enhances extinction of cocaine-seeking behavior in a persistent manner.[1]

References

[1] Malvaez M, et al. HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner. Proc Natl Acad Sci U S A. 2013, 110(7): 2647-2652.
[2] Wells CE, et al. Inhibition of histone deacetylase 3 causes replication stress in cutaneous T cell lymphoma. PLoS One. 2013, 8(7): e68915.

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