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RGFP966

Cat. No. M2977

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RGFP966 Structure
Synonym:

CAS# 1396841-57-8

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
1mg USD 30  USD30 In stock
2mg USD 45  USD45 In stock
5mg USD 70  USD70 In stock
10mg USD 115  USD115 In stock
25mg USD 200  USD200 In stock
50mg USD 310  USD310 In stock
100mg USD 510  USD510 In stock
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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

Product Citations
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
Chemical Information
Molecular Weight 362.4
Formula C21H19FN4O
CAS Number 1357389-11-7
Solubility (25°C) DMSO 55 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Wells CE, et al. PLoS One. Inhibition of histone deacetylase 3 causes replication stress in cutaneous T cell lymphoma.

[2] Malvaez M, et al. Proc Natl Acad Sci U S A. HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner.

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

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