RGFP966_1357389-11-7_DataSheet_MedChemExpress

Product Name:

RGFP966CAS No.:

1357389-11-7

Product Data Sheet

Cat. No.:

HY-13909MWt:

362.40Formula:

C21H19FN4O Purity :

>98%

Solubility:Mechanisms:Biological Activity:

Pathways:Cell Cycle/DNA Damage; Target:HDAC

Pathways:NF-KB; Target:HDAC 25°C: DMSO

g y

Description:

IC50 Value: 80 nM [1]RGFP966 is specific for HDAC3, with an IC50 of 0.08 μM and no effective inhibition of any other

HDAC at concentrations up to 15 μM. in vitro: A titration of RGFP966 showed that at 5-10 ?M there was only a modest affect on H3K56ac,which was approximately 15-fold less than found with Depsipeptide. Treatment of two CTCL cell lines, HH and Hut78, with the HDAC3-selective inhibitors 966 and 136, for 24 hours prior to western blot analysis resulted in increased acetylation at H3K9/K14, H3K27, and H4K5, but not H3K56ac 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 Fe

b 12;110(7):2647-52.[2]. Wells CE, et al. Inhibition of histone deacetylase 3 causes replication stress in cutaneous T cell lymphoma. PLoS One. 2013 Jul 22;8(7):e68915.y y

(even at 10?M) [2].in vivo: To investigate the concentration of RGFP966 in the brain, we treated mice with 10 mg/kg RGFP966administered s c then collected plasma and brain tissue at 153060and 120min after y p ()

Caution: Not fully tested. For research purposes only

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