RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits > 200-fold selectivity over other HDAC. Systemic treatment with RGFP966 facilitates extinction in mice in a manner resistant to reinstatement. A single treatment of RGFP966 enhances extinction of a previously established cocaine-conditioned place preference, while simultaneously enhancing long-term object-location memory within subjects. HDAC3 inhibition using a first in class selective inhibitor, RGFP966, resulted in decreased cell growth in CTCL cell lines due to increased apoptosis that was associated with DNA damage and impaired S phase progression. Selective inhibition of HDAC3 could be useful in treatment of CTCL by disrupting DNA replication of the rapidly cycling tumor cells, ultimately leading to cell death.
Another CAS# 1396841-57-8
|Source||EMBO Mol Med (2018). Figure 2. RGFP966|
|Cell Lines||C4-2 cells|
|Incubation Time||24 h|
|Results||The HDAC3 inhibitor RGFP966 also undermined AKT ubiquitination|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL|
Inhibition of histone deacetylase 3 causes replication stress in cutaneous T cell lymphoma.
Wells CE, et al. PLoS One. 2013 Jul 22;8(7):e68915. PMID: 23894374.
HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner.
Malvaez M, et al. Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2647-52. PMID: 23297220.
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