产品名称
胡桃醌, A highly selective cell-permeable, irreversible inhibitor of PPlases (peptidyl-prolyl cis/trans isomerases of the parvulin family).
SMILES string
Oc1c2c(ccc1)C(=O)C=CC2=O
InChI
1S/C10H6O3/c11-7-4-5-9(13)10-6(7)2-1-3-8(10)12/h1-5,12H
InChI key
KQPYUDDGWXQXHS-UHFFFAOYSA-N
description
Merck USA index - 14, 5269
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
orange
solubility
DMSO: 10 mg/mL
ethanol: 10 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
主要靶标
PPIases（细小蛋白家族的肽基-脯氨酰顺式/反式异构酶）
PPIases（细小蛋白家族的肽基-脯氨酰顺式/反式异构酶）
产物不与ATP竞争。
可逆：否
细胞可渗透性：是
Disclaimer
毒性：有毒（F）
General description
PPlases（细小蛋白家族的肽基-脯氨酰顺式/反式异构酶）的高选择性细胞渗透性，不可逆抑制剂。尚未报道其他已知的PPlase抑制剂（例如环孢菌素A，FK506和雷帕霉素）可抑制PPlases的细小蛋白家族。灭活显示是通过向胡桃酮中添加硫醇基团而不是通过任何氧化还原过程发生的。表现出抑菌和抑真菌作用。据报道对真核细胞具有细胞毒性，并通过RNA聚合酶II阻断转录。
胡桃酮最初是从核桃树的果壳和叶子中分离出来的，是肽基-脯氨酰顺/反异构酶（PPIase）的细小蛋白家族的高度选择性、细胞可渗透且不可逆的抑制剂。通过共价修饰目标酶中的巯基起作用。在真核细胞中表现出抑菌和抑真菌特性以及细胞毒性。还报道了通过核径流确定的RNA聚合酶I、II和III直接阻断真核细胞中的转录（IC50分别为7 µM，7 µM和2 µM）。通过修饰巯基破坏功能性预起始复合物的形成，但不会显著影响起始或延伸。不抑制限制性核酸内切酶或T7 RNA聚合酶。
Other Notes
Chao, S.H., et al. 2001.Nucleic Acids Res.29, 767.
Hennig, L., et al. 1998.Biochemistry37, 5953.
Hennig, L., et al. 1998.Biochemistry37, 5953.
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Packaging
用惰性气体包装
Preparation Note
复溶后，等分并冷冻（-20°C）。储备溶液在-20°C下可稳定保存至多6个月。
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
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