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RGFP966

Cat. No. M2977
RGFP966 Structure
Synonym:

CAS# 1396841-57-8

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Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 110 In stock
50mg USD 440 In stock
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Quality Control
Biological Activity

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

Customer Product Validations & Biological Datas
Source EMBO Mol Med (2018). Figure 2. RGFP966
Method Western blots
Cell Lines C4-2 cells
Concentrations 3 μM
Incubation Time 24 h
Results The HDAC3 inhibitor RGFP966 also undermined AKT ubiquitination
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 362.4
Formula C21H19FN4O
CAS Number 1357389-11-7
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: RGFP966, CAS# 1396841-57-8 supplier, HDAC, inhibitors

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