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product name
曲古抑菌素A，来源于链霉菌属, A potent and reversible, cell-permeable inhibitor of histone deacetylase.
质量水平
检测方案
≥98% (HPLC)
形式
lyophilized solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
off-white
溶解性
ethanol: 1 mg/mL
DMSO: 20 mg/mL
methanol: soluble
运输
ambient
储存温度
−20°C
InChI
1S/C17H22N2O3/c1-12(5-10-16(20)18-22)11-13(2)17(21)14-6-8-15(9-7-14)19(3)4/h5-11,13,22H,1-4H3,(H,18,20)/b10-5+,12-11+
InChI key
RTKIYFITIVXBLE-WKWSCTOISA-N
一般描述
一种有效的、可逆的、细胞可渗透性的组蛋白脱乙酰酶抑制剂。阻断HeLa细胞G1期的细胞周期进程，并诱导细胞内凝胶蛋白水平增加12倍。诱导致癌ras-转化NIH/3T3细胞恢复正常形态。抑制Jurkat细胞中IL-2基因的表达（IC50 = 73 nM），并在小鼠模型中显示免疫抑制活性。下调Hep 3B细胞中的p57kip2 。对于HDAC1，IC50 = 6 nM；对于HDAC4为38 nM，对于HDAC6A为8.6 nM。也可提供在DMSO中的10 mM (500 µg/165 µl)曲古抑菌素A、链霉菌属（目录号647926）溶液。
一种有效的、可逆的组蛋白脱乙酰酶抑制剂。阻断HeLa细胞G1期的细胞周期进程，并诱导细胞内凝胶蛋白水平增加12倍。诱导致癌ras转化的NIH 3T3细胞恢复正常形态。抑制Jurkat细胞中IL-2基因的表达（IC50 = 73 nM），并在小鼠模型中显示免疫抑制活性。对于HDAC1，IC50 = 6 nM；对于HDAC4为38 nM，对于HDAC6A为8.6 nM。
生化/生理作用
主靶
组蛋白脱乙酰基酶
组蛋白脱乙酰基酶
产物不与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：73 nM，抑制Jurkat细胞IL-2基因表达
警告
毒性：有害（C）
重悬
在DMSO中复溶后，等分并冷冻保存（-20°C）。在乙醇中复溶后，冷藏保存（4°C）。DMSO贮备溶液可在-20°C最长稳定6个月。乙醇贮备溶液在4°C下可稳定保存至多3个月。
其他说明
Furumai, R., et al. 2001.Proc.Natl.Acad.Sci. USA98, 87.
Gray, S.G. and Ekstrom, T.J.1998.Biochem.Biophys.Res. Commun.245, 423.
Takahashi, I., et al. 1996.J. Antibiot.49, 453.
Taunton, J., et al. 1996.Science 272, 408.
Futamura, M., et al. 1995.Oncogene 10, 1119.
Hoshikawa, Y., et al. 1994.Exp.Cell Res. 214, 189.
Gray, S.G. and Ekstrom, T.J.1998.Biochem.Biophys.Res. Commun.245, 423.
Takahashi, I., et al. 1996.J. Antibiot.49, 453.
Taunton, J., et al. 1996.Science 272, 408.
Futamura, M., et al. 1995.Oncogene 10, 1119.
Hoshikawa, Y., et al. 1994.Exp.Cell Res. 214, 189.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
Gilles Flouriot et al.
Journal of molecular biology, 432(7), 2253-2270 (2020-02-28)
The baseline level of transcription, which is variable and difficult to quantify, seriously complicates the normalization of comparative transcriptomic data, but its biological importance remains unappreciated. We show that this currently neglected ingredient is essential for controlling gene network multistability
Zhenzhen Wei et al.
Cell & bioscience, 12(1), 107-107 (2022-07-14)
Histone deacetylation is one of the most important epigenetic modifications and plays diverse roles in plant development. However, the detailed functions and mechanisms of histone deacetylation in fiber development of cotton are still unclear. HDAC inhibitors (HDACi) have been commonly
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Exogenous molecules derived from catabolic states (e.g., fatty acids, β-hydroxybutyrate) during periods of stress such as the periparturient period or pathogen challenges [e.g., lipopolysaccharide (LPS)] can trigger an inflammatory response in tissues such as the liver and the mammary gland.
Aileen S W Li et al.
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Teratogenic potential has been linked to various industrial compounds. Methoxyacetic acid (MAA) is a primary metabolite of the widely used organic solvent and plasticizer, methoxyethanol and dimethoxyethyl phthalate, respectively. Studies using model animals have shown that MAA acts as the
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The Journal of biological chemistry, 298(3), 101711-101711 (2022-02-13)
Acute and chronic inflammations are key homeostatic events in health and disease. Sirtuins (SIRTs), a family of NAD-dependent protein deacylases, play a pivotal role in the regulation of these inflammatory responses. Indeed, SIRTs have anti-inflammatory effects through a myriad of
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