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 分子式: C₂₁H₁₉FN₄O 分子量: 362.4 PubChem CID: 56650312

グレード＆純度 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

概要

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%

仕様

同義語

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

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

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

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

作用メカニズム

Inhibitor of histone deacetylase 3

名前と識別子

異性体SMILES

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

代替CAS番号

1357389-11-7

PubChem CID

56650312

MeSH用語

RGFP966

分子量

362.4

関連ターゲット（人間）

HDAC3 Tclin Histone deacetylase 3 (0 Activities)

Discover Target: HDAC3

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

化学的性質と物理的性質

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