PCI-34051
PCI-34051 是一種有效的選擇性的 HDAC8 抑制劑，IC50 為 10 nM。
生物活性
PCI-34051 is a potent and selective HDAC8 inhibitor with IC50 of 10 nM, with >200-fold selectivity over the other HDAC isoforms.
體外研究(In Vitro)
PCI-34051 inhibits pure recombinant HDAC8 with Ki of 10 nM with >200-fold selectivity over the other HDACs tested, including HDACs 1, 2, 3, 6 and 10. PCI-34051 is derived from a low molecular weight hydroxamic acid scaffold that possessed promising potency (HDAC8; Ki=2 μM) and selectivity (approximately fivefold) for HDAC8 relative to the other class I HDACs. PCI-34051 is found to induce apoptosis at low micromolar concentrations in cell lines derived from T-cell lymphomas, including Jurkat and HuT78, whereas doses as high as 20 μM has no effect on B-cell- or myeloid-derived lymphomas or solid tumor lines[1].
體內研究(In Vivo)
Administration of PCI-34051 and Dexamethasone reduces the eosinophilic inflammation and airway hyperresponsiveness in asthma to reduce the airway remodeling[2].
分子量：296.32
性狀：Solid
Formula：C17H16N2O3
CAS 號：950762-95-5
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : ≥ 30 mg/mL (101.24 mM)
* "≥" means soluble, but saturation unknown.
| 濃度溶劑體積質量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.3747 mL | 16.8736 mL | 33.7473 mL |
| 5 mM | 0.6749 mL | 3.3747 mL | 6.7495 mL |
| 10 mM | 0.3375 mL | 1.6874 mL | 3.3747 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.44 mM); Clear solution
- 2.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.44 mM); Clear solution
- 3.
請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.44 mM); Clear solution
參考文獻
[1]. Balasubramanian S, et al. A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas. Leukemia. 2008 May;22(5):1026-34. [Content Brief]
[2]. Ren Y, et al. Therapeutic effects of histone deacetylase inhibitors in a murine asthma model. Inflamm Res. 2016 Dec;65(12):995-1008. [Content Brief]
注：產(chǎn)品僅用于科研
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