| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R409147-1ml |
1ml |
现货  |
|
| 英文别名 | 2-Propenamide, N-(2-amino-4-fluorophenyl)-3-[1-[(2E)-3-phenyl-2-propen-1-yl]-1H-pyrazol-4-yl]-, (2E)- |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | RGFP966 |
| 生化机理 | RGFP966 是一种 HDAC3 抑制剂，在无细胞实验中的 IC50 值为 0.08 μM，与其他 HDAC 相比，具有 > 200 倍的选择性。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 组蛋白去乙酰化酶 3 抑制剂 |
| 产品介绍 |
RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC. Information RGFP966 is anHDAC3inhibitor withIC50of 0.08 μM in cell-free assay, exhibits > 200-fold selectivity over other HDAC. 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 lines： Concentrations：~10μM Incubation Time：24 to 72 h Powder Purity:≥99% |
| IC50 | HDAC3, IC50: 80 nM |
|---|
| Canonical SMILES | NC1=CC(=CC=C1NC(=O)\C=C\C2=C[N](C\C=C\C3=CC=CC=C3)N=C2)F |
|---|---|
| 分子量 | 362.4 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 69 mg/mL (202.09 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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