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| | 4-[4-(5-ニトロフラン-2-イルメチレン)-3,5-ジオキソピラゾリジン-1-イル]安息香酸エチル 製品概要 |
| 化学名: | 4-[4-(5-ニトロフラン-2-イルメチレン)-3,5-ジオキソピラゾリジン-1-イル]安息香酸エチル | | 英語化学名: | PYR 41 | | 别名: | PYR 41;4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester;Benzoic acid, 4-[4-[(5-nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]-, ethyl ester;4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester PYR 41;PYR 41 4-[4-[(5-Nitro-2-furanyl)methylene]-3,5-dioxo-1-pyrazolidinyl]benzoic acid ethyl ester;4[4-(5-Nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester;PYR 41, >=98%;PYR 41 USP/EP/BP | | CAS番号: | 418805-02-4 | | 分子式: | C17H13N3O7 | | 分子量: | 371.3 | | EINECS: | | | カテゴリ情報: | Inhibitors | | Mol File: | 418805-02-4.mol | ![4-[4-(5-ニトロフラン-2-イルメチレン)-3,5-ジオキソピラゾリジン-1-イル]安息香酸エチル](CAS/20150408/GIF/418805-02-4.gif) |
| | 4-[4-(5-ニトロフラン-2-イルメチレン)-3,5-ジオキソピラゾリジン-1-イル]安息香酸エチル 物理性質 |
| 融点 | 228 - 235°C | | 比重(密度) | 1.486±0.06 g/cm3(Predicted) | | 貯蔵温度 | -20°C | | 溶解性 | Soluble in DMSO at 5mg/ml with warming | | 外見 | powder | | 酸解離定数(Pka) | 7.43±0.20(Predicted) | | 色 | red to brown | | Sensitive | Light Sensitive | | 安定性： | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 week. | | InChIKey | ARGIPZKQJGFSGQ-LCYFTJDESA-N |
| | 4-[4-(5-ニトロフラン-2-イルメチレン)-3,5-ジオキソピラゾリジン-1-イル]安息香酸エチル Usage And Synthesis |
| 説明 | Pyr41 (418805-02-4) inhibits ubiquitin activating enzyme E1 (>60% inhibition at 10 μM) with little or no activity against E2 or E3. Cell permeable | | 使用 | PYR 41 is an irreversible and cell-permeable UBE1 inhibitor. | | 定義 | ChEBI: PYR-41 is an ethyl ester resulting from the formal condensation of the carboxy group of 4-{4-[(5-nitrofuran-2-yl)methylidene]-3,5-dioxopyrazolidin-1-yl}benzoic acid with ethanol. It is an irreversible and cell-permeable inhibitor of ubiquitin-activating enzyme E1. It has a role as an EC 6.2.1.45 (E1 ubiquitin-activating enzyme) inhibitor and an antineoplastic agent. It is an ethyl ester, a member of furans, a C-nitro compound, a member of pyrazolidines and a benzoate ester. | | Biochem/physiol Actions | PYR-41 is a cell permeable inhibitor of Ubiquitin activating enzyme (E1) with little or no activity against E3, E2, or caspase enzymatic activity. | | in vitro | in addition to blocking ubiquitylation, pyr-41 was found to increase total sumoylation in cells. pyr-41 could attenuate cytokine-mediated nuclear factor-kbactivation. this correlated with inhibition of nonproteasomal ubiquitylation of traf6, which is important to ikbkinase activation. pyr-41 also prevented the downstream ubiquitylation and proteasomal degradation of ikba. moreover, pyr-41 has demonstrated effective uae e1 inhibition as well as some off-target inhibition of the other ubiquitin regulatory enzymes and signal-transducing proteins, suggesting it is a nonspecific inhibitor [1]. | | 貯蔵 | Store at -20°C | | 参考文献 | 1) Yang et al. (2007), Inhibitors of Ubiquitin-Activating Enzyme (E1), a New Class of Potential Cancer Therapeutics; Cancer Res., 67 9472
2) Mi et al. (2009), Cancer Preventive isothiocyanates induce selective degradation of cellular alpha- and beta-tubulins by proteasomes; J. Biol. Chem., 284 17039
3) Maehama et al. (2014), Nucleolar Stress Induces Ubiquitination-independent Proteasomal Degradation of PICT1 Protein PYR41; J. Biol. Chem., 289 20802 [Focus Citation] |
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