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當(dāng)前位置:杭州昊鑫生物科技股份有限公司>>MCE>> HY-15224PCI-34051
HY-15224
MCE
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杭州市
5mg 617元 10000支可售
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更新時(shí)間:2024-06-24 16:24:24瀏覽次數(shù):129次
聯(lián)系我時(shí),請(qǐng)告知來(lái)自 制藥網(wǎng)CAS號(hào) | 950762-95-5 | 產(chǎn)地 | 國(guó)產(chǎn) |
---|---|---|---|
規(guī)格 | 5mg | 級(jí)別 | 化工級(jí) |
證書(shū) | ISO系列證書(shū) |
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(nèi)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(hào):950762-95-5
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲(chǔ)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(zhì)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(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶
請(qǐng)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
請(qǐng)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
請(qǐng)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(xiàn)
[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]
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