ITSA-1 是HDAC的激活剂，可抵消曲古抑菌素 A (trichostatin A, TSA) 诱导的细胞周期停滞，组蛋白乙酰化和转录水平的激活。
| 生物活性 | ITSA-1 is an activator ofhistone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | ITSA1 (50 μM; A549 cells) treatment serves to revert the TSA-arrested population to a normal cell cycle distribution. ITSA1 is also able to effect cell cycle rescue over longer duration[1].
ITSA1 (50 μM; 5 hours; A549 cells) treatment reduces the number of apoptosis in TSA-treated cells[1].
ITSA1 (50 μM; 2 hours; A549 and murine ES cells cells) treatment suppresses TSA-induced histone acetylation. Importantly, suppression of acetylation levels is only observable when ITSA1 is added concurrent with or post TSA treatment[1].
ITSA1 (50 μM; 30 minutes; murine ES cells cells) suppresses TSA-activated transcription in murine ES cells[1].
Cell Cycle Analysis[1] | Cell Line: | Murine ES cells | | Concentration: | 50 μM | | Incubation Time: | | | Result: | Served to revert the TSA-arrested population to a normal cell cycle distribution. |
Apoptosis Analysis[1] | Cell Line: | A549 cells | | Concentration: | 50 μM | | Incubation Time: | 5 hours | | Result: | Reduced the number of apoptosis. |
Western Blot Analysis[1] | Cell Line: | A549 and murine ES cells | | Concentration: | 50 μM | | Incubation Time: | 2 hours | | Result: | Reduced histone acetylation to the baseline level. |
RT-PCR[1] | Cell Line: | Murine ES cells | | Concentration: | 50 μM | | Incubation Time: | 30 minutes | | Result: | Suppressed TSA-activated transcription. |
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体内研究
(In Vivo) | ITSA-1 (0.5 mg/kg; intraperitoneal injection; 3 times/week; for 8 weeks; CBS+/–mice) treatment balances deacetylation activity and suppresses IL-6 and TNF-α expression and thereby attenuated histone acetylationdependent infammatory signaling[2].
| Animal Model: | CBS+/–mice[2] | | Dosage: | 0.5 mg/kg | | Administration: | Intraperitoneal injection; 3 times/week; for 8 weeks | | Result: | Balanced deacetylation activity and suppressed IL-6 and TNF-α expression. |
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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 : ≥ 32 mg/mL(109.54 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 3.4233 mL | 17.1163 mL | 34.2325 mL | | 5 mM | 0.6847 mL | 3.4233 mL | 6.8465 mL | | 10 mM | 0.3423 mL | 1.7116 mL | 3.4233 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 (8.56 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.56 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 (8.56 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (8.56 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 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 (8.56 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.56 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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