[CAS NO. 1396841-57-8] RGFP966
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PRODUCTS SPECIFICATIONS [1396841-57-8]
Store
Catalog
SLK-S7229
Brand
Selleck
CAS
1396841-57-8
DESCRIPTION [1396841-57-8]
Overview
| MDL | MFCD26960954 |
|---|---|
| Molecular Weight | 362.4 |
| Molecular Formula | C21H19FN4O |
| SMILES | O=C(NC1=CC=C(F)C=C1N)/C=C/C2=CN(C/C=C/C3=CC=CC=C3)N=C2 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7594 mL | 13.7969 mL | 27.5938 mL |
| 5 mM | 0.5519 mL | 2.7594 mL | 5.5188 mL |
| 10 mM | 0.2759 mL | 1.3797 mL | 2.7594 mL |
| 50 mM | 0.0552 mL | 0.2759 mL | 0.5519 mL |
Description
RGFP966 is an inhibitor with of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
Targets
| HDAC3 [1] (Cell-free assay) |
| 80 nM |
In vitro
RGFP966 is a slow-on/slow-off, competitive tight-binding HDAC inhibitor, with an IC50 of 0.08μM for HDAC3 and no effective inhibition of any other HDAC at concentrations up to 15μM. RGFP966 treatment on two CTCL cell lines for 24 hours prior to western blot analysis resulted in increased acetylation at H3K9/K14, H3K27, and H4K5, but not H3K56ac. RGFP966 decreases cell growth in CTCL (cutaneous T cell lymphoma) cell lines due to increased apoptosis that is associated with DNA damage and impaired S phase progression. RGFP966 causes a significant reduction in DNA replication fork velocity within the first hour of drug treatment.
In vivo
RGFP966 treatment (10 mg/kg) enhances long-term memory for object memory. RGFP966 (3 or 10 mg/kg, s.c.) facilitates extinction and prevents reinstatement of cocaine- conditioned place preference.
References
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