| 名稱 | Pracinostat |
| 描述 | Pracinostat (SB939) is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in Clinicalal trials, allowing oral dosing. Data demonstrate that Pracinostat is a potent and effective anti-tumor drug with potential as an oral therapy for a variety of human hematological and solid tumors. |
| 細胞實驗 | Cells are seeded in 96-well plates in the log growth phase at a predetermined optimal density, and rested for 24 hours (adherent cells) or 2 hours (suspension cells), respectively. They are exposed to different concentrations of SB939 for 96 hours. Cell proliferation assays are done using either the CyQUANT cell proliferation assay kit for adherent cells or the CellTiter96 Aqueous One solution cell proliferation kit for suspension cells.(Only for Reference) |
| 激酶實驗 | HDAC enzyme assay: All recombinant HDAC enzymes, with the exception of SIRT1, are cloned and expressed in S*BIO. The reaction mix containing 2.5 or 5 μL of the HDAC isoenzyme, assay buffer (25 mM Tris-HCl, pH 7.5; 137 mM NaCl; 2.7 mM KCl, 1 mM MgCl2 and 1 mg/mL BSA), different concentrations of SB939, and the fluorogenic deacetylase substrate Flour de LysTM in a total reaction volume of 33 μL is incubated at room temperature for 2 hours. 16 μL of Flour de LysTM developer is added and incubated for an additional 10 minutes. The emitted light is measured at 460 nm in a microplate reader. IC50 values are generated using the XLfit software. |
| 體外活性 | 50 mg/kg SB939選擇性刺激CT-116移植瘤組織生長.SB939對SAHA的腫瘤生長抑制率為94％.SB939作用于裸鼠,比SAHA具有更強的藥物動力學(xué)效果和口服生物有效性.SB939抑制APCmin鼠腺瘤形成和提高血球密度,效果比5-氟尿嘧啶好.SB939作用于腫瘤模型(HCT-116,PC-3,A2780,MV4-11,Ramos),具有抗癌活性和高效性. |
| 體內(nèi)活性 | SB939對HDAC的選擇性比鋅結(jié)合的非HDAC酶、受體和離子通道高100倍。SB939可顯著抑制HDAC II類同工酶,HDAC4,HDAC5,HDAC7,HDAC9和HDAC10,IC50值范圍為40 nM至137 nM,對HDAC6無此作用,其顯示的IC50為1008 nM。它顯著抑制HDAC IV類酶的HDAC11,IC50為93 nM,但對III類HDACs的SIRT1沒有抑制活性。SB939對各種腫瘤細胞系,尤其是白血病細胞和皮膚T細胞淋巴瘤細胞顯示出顯著的抗增殖活性,IC50值范圍從50 nM（H9細胞）至170 nM（HEL92.1.7細胞）。 |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 26 mg/mL (72.5 mM)
DMSO : 75 mg/mL (209.22 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| 關(guān)鍵字 | Apoptosis | Pracinostat | Inhibitor | cancer | inhibit | SB-939 | HDAC | MBLAC2 | SB 939 | Histone deacetylases |
| 相關(guān)產(chǎn)品 | Valproic Acid | L-Glutamic acid | Metronidazole | 5-Fluorouracil | Curcumin | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate |
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