Nexturastat A 是一种有效的选择性HDAC6抑制剂。Nexturastat A 对 HDAC6 具有抑制作用,IC50为 5 nM。Nexturastat A 可用于多发性骨髓瘤 (MM) 的研究。
生物活性 | Nexturastat A is a potent, selectiveHDAC6inhibitor. Nexturastat A has inhibitory forHDAC6with anIC50of 5 nM. Nexturastat A can be used for the research of multiple myeloma (MM)[1][2]. |
IC50& Target[1] | HDAC6 5.02 nM (IC50) | HDAC8 0.954 μM (IC50) | HDAC1 3.02 μM (IC50) | HDAC7 4.46 μM (IC50) | HDAC11 5.14 μM (IC50) | HDAC3 6.68 μM (IC50) | HDAC9 6.72 μM (IC50) | HDAC2 6.92 μM (IC50) | HDAC10 7.57 μM (IC50) | HDAC4 9.39 μM (IC50) | HDAC5 11.7 μM (IC50) |
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体外研究 (In Vitro) | Nexturastat A (5 g) has inhibitory for HDAC6 with IC50values of 0.005 μM[1]. Nexturastat A (0-10 μM; 24 h) has substrate selectivity for HDAC62[1]. Nexturastat A has antiproliferative activity against B16 murine melanoma cells with IC50values of 14.3 μM[1]. Nexturastat A (NexA) (0-40 μM; 48 h) suppresses viability and induced G1 phase arrest of human MM cells[2]. Nexturastat A (0, 30, 40 μM; 48 h) promotes apoptosis of MM cells via transcriptional activation of the p21 promoter[2].
Western Blot Analysis[1] Cell Line: | B16 murine melanoma cells | Concentration: | 0-10 μM | Incubation Time: | 24 h | Result: | Increased the level of acetyl α-tubulin levels in a dose-dependent. |
Cell Viability Assay[2] Cell Line: | RPMI-8226 and U266 cells | Concentration: | 0-40 μM | Incubation Time: | 48 h | Result: | Impaired multiple myeloma (MM) cells viability in a dose- and time-dependent manner. |
Apoptosis Analysis[2] Cell Line: | RPMI-8226 and U266 cells | Concentration: | 0, 30, 40 μM | Incubation Time: | 48 h | Result: | Induced cell apoptosis in human MM cells. |
RT-PCR[2] Cell Line: | RPMI-8226 and U266 cells | Concentration: | 30 μM | Incubation Time: | 48 h | Result: | Increased the levels of p21 mRNA in RPMI-8226 and U266 cells. |
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体内研究 (In Vivo) | Nexturastat A (NexA) (every two days, 20 days) inhibits tumor growth in murine xenograft models of MM[2].
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : ≥ 56 mg/mL(164.03 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.9291 mL | 14.6456 mL | 29.2912 mL | 5 mM | 0.5858 mL | 2.9291 mL | 5.8582 mL | 10 mM | 0.2929 mL | 1.4646 mL | 2.9291 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.32 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.32 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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