互变霉素
基本信息
| 产品名称 | 互变霉素 |
|---|---|
| 英文名称 | Tautomycin |
| 规格或纯度 | ≥85% |
| 运输条件 | 超低温冰袋运输 |
一般描述
互变霉素是一种有效且特异性的蛋白磷酸酶抑制剂，可作为抗真菌抗生素。互变霉素比蛋白磷酸酶2A（K | app | = 0.4 nM）（PP2）更有效地抑制蛋白磷酸酶-1（K | app | = 0.16 nM）（PP1）。研究表明，在存在互变霉素的情况下，转移受体（TFR）的表达水平增加，并且还阻断了PDBu诱导的CD4下调。用互变霉素和互变霉素（也是一种抗真菌抗生素）治疗的甲状腺髓样癌（MTC）细胞显示出抑制的激素分泌水平，减少的神经内分泌标志物以及通过细胞凋亡抑制生长。互变异构酶和互变霉素都可以通过阻断
Tautomycin is a potent and specific protein phosphatase inhibitor that functions as an antifungal antibiotic. Protein phosphatase-1 (K|iapp|= 0.16 nM) (PP1) is more potently inhibited by tautomycin than protein phosphatase 2A (K|iapp|= 0.4 nM) (PP2). Studies show that in the presence of tautomycin the expression levels of transferring receptor (TFR) increase and it also blocks PDBu-induced down regulation of CD4. Medullary thyroid cancer (MTC) cells treated with tautomycin and tautomycetin, also an antifungal antibiotic, showed suppressed levels of hormonal secretion, decreased neuroendocrine markers, and inhibition of growth through apoptosis. Both compounds, tautomycin and tautomycetin, can inhibit the growth of MTC cells by blocking glycogen synthase kinase-3β. Tautomycin can also activate the Raf-1 pathway, prevent neuroendocrine (NE) production, and decrease carcinoid cell development.
相关属性
| CAS编号 | 109946-35-2 |
|---|---|
| 折光率 | n20D1.53 (Predicted) |
| 沸点 | 854.28° C at 760 mmHg (Predicted) |
| pKa值 | pKₐ: 12.33 (Predicted) |
| 溶解性 | Soluble in 100% ethanol, methanol, ethyl acetate, DMSO, acetone, water (slightly soluble), and chloroform. |
| 储存温度 | -20°C储存 |
| RTECS | WX1000000 |
| 密度 | 1.19 g/cm3(Predicted) |
| 分子量 | 766.95 |
| 分子式 | C₄₁H₆₆O₁₃ |
| 品牌 | Jinpan |
| 备注 | Stable for up to 1 year after receipt when stored at -20°C. Stock solutions should be aliquoted and stored at -20°C for up to 1 month. Hygroscopic, protect form light and moisture sensitive. |
| Smiles | C[C@@H]1CC[C@@]2(CC[C@@H]([C@@H](O2)[C@H](C)CC[C@@H]([C@H](C)C(=O)C[C@H]([C@H]([C@ |
| IC50 | Serine/threonine protein phosphatase PP1-gamma catalytIC₅₀ubunit: IC₅₀= 0.7 nM (human); Serine-threonine protein phosphatase 2A regulatory subunit: IC₅₀= 0.7 nM (Gallus gallus); Protein-tyrosine phosphatase 1B: IC₅₀= 0.67 nM (human); Serine/threonine prot |
| PubChem CID | 440646 |