软木肟酸
- CAS号:38937-66-5
- 英文名:Suberohydroxamic acid
- 中文名:软木肟酸
- CBNumber:CB6673028
- 分子式:C8H16N2O4
- 分子量:204.22
- MOL File:38937-66-5.mol
- 熔点 :153-155 °C(lit.)
- 密度 :1.219±0.06 g/cm3(Predicted)
- 储存条件 :−20°C
- 溶解度 :H2O: soluble
- 酸度系数(pKa) :9.18±0.20(Predicted)
- 形态 :lyophilized powder
- 颜色 :White to Light Beige
- 稳定性 :Hygroscopic
- 安全说明 :22-24/25
- WGK Germany :3
- 海关编码 :2928009090
软木肟酸性质、用途与生产工艺
- 作用 Suberoylbis-hydroxamic酸(软木肟酸)作为第二代异羟肟酸类组蛋白去乙酰化酶抑制剂，能够抑制组蛋白去乙酰化酶中HDAC1和HDAC3的活性，小剂量、低浓度时可诱导肿瘤分化，并选择性地抑制肿瘤生长而对正常细胞无明显不良反应。通过对乳腺癌的研究发现软木肟酸呈时间、剂量依赖性抑制乳腺癌细胞增殖，使其停滞于G0～G1期。ChemicalBook
- 用途 软木肟酸是一种组蛋白去乙酰化酶抑制剂，它可能具备激活Notch1信号通路的功能。应用Western实验检验Notch1信号通路被激活后所表达的活性蛋白NICD，来判断软木肟酸对Notch1信号通路的作用。
- 生物活性 Suberohydroxamic acid (suberic bishydroxamic acid)是竞争性HDAC抑制剂，对HDAC1和HDAC3的IC50分别为0.25 μM和0.3 μM。
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靶点
Target Value HDAC1
(Cell-free assay)0.25 μM HDAC3
(Cell-free assay)0.3 μM -
体外研究
Suberoyl bis-hydroxamic acid (10, 20 or 50 μM; 24 hours) combination with TRAIL improves apoptosis extent, and when TRAIL is combined with 20 μM SBHA (itself causing only 10–15% apoptosis), resulting in 45–50% cell death.Suberoyl bis-hydroxamic acid (20-50 μM; 10-20 hours) alone has little effect on the expression of the proteins Bcl-xL, Mcl-1, and has albeit mildeffect on Bax. When it combines with TRAIL,which increases the ratio of relative protein expression of Bcl-xL and Bax in early periods, while the change in the ratio of Mcl-1 and Bax increases later in MM-BI and Ist-Mes2 cells.Suberoyl bis-hydroxamic acid (30 μM; 6 hours) causes accumulation of acetylated histone H4 in MEL cells.
Apoptosis Analysis
Cell Line: MM-BI and Ist-Mes2 cells Concentration: 10 μM, 20 μM or 50 μM Incubation Time: 24 hours Result: Showed a cooperative effect in cell apoptosis. -
体内研究
Suberoyl bis-hydroxamic acid (intraperitoneal injection; 200 mg/kg; every 2 days; 12 days) reveals a marked increase in the active form of Notch1 (NICD) with a concomitant decrease in ASCL1. It reduces the MTC tumor growth.
Animal Model: Nude mice injected with human MTC cells Dosage: 200 mg/kg Administration: Intraperitoneal injection; every 2 days; 12 days Result: Resulted in an average 55% inhibition of tumor growth in SBHA treatment group.
- 更新日期：2024/11/11
- 产品编号：XW3893766501
- 产品名称：软木肟酸
- CAS编号：38937-66-5
- 包装：1G
- 价格：143元
- 更新日期：2024/11/08
- 产品编号：HY-W009776
- 产品名称：软木肟酸 Suberoyl bis-hydroxamic acid
- CAS编号：38937-66-5
- 包装：50mg
- 价格：100元
- 公司名称：EPSILON
- 联系电话：--
- 电子邮件：pierre.cornec@epsilon-chimie.com
- 国家：法国
- 产品数：538
- 优势度：61
