HPOB

製品コードS7278 バッチS727801

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H18N2O4
分子量 314.34 CAS No. 1429651-50-2
Solubility (25°C)* 体外 DMSO 62 mg/mL (197.23 mM)
Ethanol 38 mg/mL warmed with 50ºC water bath (120.88 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 HPOB is a potent, selective HDAC6 inhibitor with IC50 of 56 nM, >30-fold selectivity over other HDACs.
in vitro In normal (HFS) and transformed (LNCaP, A549, and U87) cells, HPOB induces acetylation of α-tubulin, however, not histones, and inhibits cell growth, however, not viability. In HFS cells, HPOB enhances transformed cell death induced by etoposide, doxorubicin, or SAHA. HPOB also enhancing etoposide-induced transformed cell death via the apoptotic pathway in transformed cells. [1]
in vivo In mice bearing CWR22 human prostate cancer xenografts, HPOB (300 mg/kg/d i.p.), when in combination with SAHA, causes suppression of the growth of established tumors, while produces no significant suppression when used alone. [1]

プロトコル(参考用のみ)

キナーゼアッセイ In Vitro Enzymatic Assay for Histone Deacetylases
In vitro activities of the 11 recombinant human zinc-dependent HDAC enzymes are detected by fluorigenic release of 7-amino-4-methylcoumarin from substrate upon deacetylase enzymatic activity. A series of dilutions of the unique HDAC6 compound, tubacin, and SAHA are prepared with 10% DMSO in HDAC assay buffer, and 5 μL of the dilution was added to a 50-μL reaction so that the final concentration of DMSO is 1% in all of the reactions. The enzymatic reactions are conducted in duplicate at 37 °C for 30 min in a 50-μL mixture containing HDAC assay buffer, 5 μg BSA, an HDAC substrate, an HDAC enzyme, and a test compound. After enzymatic reactions, 50 μL of 2× HDAC developer is added to each well, and the plate is incubated at room temperature for an additional 15 min. Fluorescence intensity is measured at an excitation of 360 nm and an emission of 460 nm using a Synergy microplate reader. Negative (no enzyme, no inhibitor, a drug with no HDAC inhibition activity) and positive controls (known HDAC inhibitor SAHA) are included in the assays. IC50 is determined at the drug concentration that results in 50% reduction of HDAC activity compared with the control.
細胞アッセイ 細胞株 HFS, A549, LNCaP, and U87 cells
濃度 ~32 μM
反応時間 72 hours
実験の流れ Normal (HFS) and transformed (LNCaP, A549, and U87) cells are cultured with indicated doses of HPOB for 72 h. Five micromolars SAHA is a positive control.Graphs were constructed using Prism 5.
動物実験 動物モデル Mice bearing CWR22 human prostate cancer xenografts
投薬量 300 mg/kg daily
投与方法 i.p.

カスタマーフィードバック

Data from [Data independently produced by , , Neurochem Int, 2016, 99:239-51.]

Data from [Data independently produced by , , Molecules, 2018, 23(5)]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

HDAC3 inhibitor RGFP966 controls bacterial growth and modulates macrophage signaling during Mycobacterium tuberculosis infection [ Tuberculosis (Edinb), 2021, 127:102062] PubMed: 33639591
Anti-Proliferative Activity of HPOB against Multiple Myeloma Cells via p21 Transcriptional Activation [Liu L Molecules, 2018, 23(5)] PubMed: 29710846
HPOB, an HDAC6 inhibitor, attenuates corticosterone-induced injury in rat adrenal pheochromocytoma PC12 cells by inhibiting mitochondrial GR translocation and the intrinsic apoptosis pathway [Li ZY, et al. Neurochem Int, 2016, 99:239-51] PubMed: 27522966

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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