RGFP966 - 10mM in DMSO , Inhibitor of histone deacetylase 3, CAS No.1396841-57-8, Inhibitor of histone deacetylase 3

CAS: 1396841-57-8 Cat. No.: R409147 Fórmula: C₂₁H₁₉FN₄O Peso molecular: 362.4 PubChem CID: 56650312

CALIDAD & PUREZA 10mM in DMSO

Synonyms

2-Propenamide, N-(2-amino-4-fluorophenyl)-3-[1-[(2E)-3-phenyl-2-propen-1-yl]-1H-pyrazol-4-yl]-, (2E)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

RGFP966 is anHDAC3inhibitor withIC50of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.
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.
Cell Data

cell lines：

Concentrations：~10μM

Incubation Time：24 to 72 h

Powder Purity:≥99%

Especificaciones

Sinónimos

2-Propenamide, N-(2-amino-4-fluorophenyl)-3-[1-[(2E)-3-phenyl-2-propen-1-yl]-1H-pyrazol-4-yl]-, (2E)-

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of histone deacetylase 3

Nombres e identificadores

Isómeros SMILES

C1=CC=C(C=C1)/C=C/CN2C=C(C=N2)/C=C/C(=O)NC3=C(C=C(C=C3)F)N

CAS alternativo

1357389-11-7

PubChem CID

56650312

Términos de entrada MeSH

RGFP966

Peso molecular

362.4

Objetivos asociados (humanos)

HDAC3 Tclin Histone deacetylase 3 (0 Activities)

Discover Target: HDAC3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 69 mg/mL (202.09 mM); Water: Insoluble; Ethanol: Insoluble