BG45 是一种有效的HDAC3抑制剂，抑制 HDAC3、HDAC1、HDAC2 和 HDAC6 的IC50值分别为 0.289、2、2.2 和 >20 μM。BG45 选择性靶向多发性骨髓瘤 (MM) 细胞，诱导 caspase 依赖性凋亡 (apoptosis)。
| 生物活性 | BG45 is a potentHDAC3inhibitor withIC50values of 0.289, 2, 2.2 and ﹥20 μM forHDAC3,HDAC1,HDAC2andHDAC6, respectively. BG45 selectively targets multiple myeloma (MM) cells and induces caspase-dependentapoptosis[1][2]. |
| IC50& Target[2] | HDAC3 0.289 μM (IC50) | HDAC1 2.0 μM (IC50) | HDAC2 2.2 μM (IC50) | HDAC6 >20 μM (IC50) |
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体外研究
(In Vitro) | BG45 (1.875-30 μM; 48 and 72 h) targets multiple myeloma (MM) cells and inhibits cell growth in a dose-dependent manner[1].
BG45 (15 μM; 0-48 h; MM.1S cells) induces apoptosis via caspase-3/PARP cleavage[1].
BG45 (10 and 20 μM; 12 h; MM.1S cells) induces acetylation of histone H2A, H3, and H4 in a dose-dependent manner[1].
BG45 (10 and 20 μM; 10 h; MM.1S cells) induces multiple myeloma (MM) cells toxicity is associated with hyperacetylation of histones and STAT3 and downregulation of p-STAT3[1].
Cell Viability Assay[1] | Cell Line: | MM.1S, RPMI8226, U266, OPM1, and H929 cells | | Concentration: | 1.875, 3.75, 7.5, 15, and 30 μM | | Incubation Time: | 48 and 72 hours | | Result: | Inhibited multiple myeloma (MM) cells growth in a dose-dependent manner. |
Western Blot Analysis[1] | Cell Line: | MM.1S cells | | Concentration: | 15 μM | | Incubation Time: | 0, 6, 12, 24, and 48 hours | | Result: | Induced caspase-dependent apoptosis in multiple myeloma (MM) cells. |
Western Blot Analysis[1] | Cell Line: | MM.1S cells | | Concentration: | 10 and 20 μM | | Incubation Time: | 12 hours | | Result: | Increased acetylation of histone in a dose-dependent manner. |
Western Blot Analysis[1] | Cell Line: | MM.1S cells | | Concentration: | 10 and 20 μM | | Incubation Time: | 10 hours | | Result: | Downregulated p-STAT3 in a dose-dependent manner.
Increased acetylation of STAT3 in MM.1S cells. |
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体内研究
(In Vivo) | BG45 (15-50 mg/kg; i.p.; 5 days a week for 3 weeks; CB17 SCID mice with MM.1S xenograft model) inhibits human multiple myeloma (MM) cells growth and enhancesbortezomib(HY-10227) induced cytotoxicity in vivo[1].
| Animal Model: | CB17 SCID mice (48-54 days old) with MM.1S xenograft model[1] | | Dosage: | 15 and 50 mg/kg | | Administration: | Intraperitoneal injection; 5 days a week for 3 weeks | | Result: | Inhibited MM tumor growth in a dose-dependent fashion.
Enhanced either single agent activity in combination withbortezomib(HY-10227). |
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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 : ≥ 48 mg/mL(224.07 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 4.6681 mL | 23.3405 mL | 46.6810 mL | | 5 mM | 0.9336 mL | 4.6681 mL | 9.3362 mL | | 10 mM | 0.4668 mL | 2.3340 mL | 4.6681 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 (11.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.67 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 (11.67 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (11.67 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。 *以上所有助溶剂都可在本网站选购。
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