蛋白磷酸酯酶抑制剂
| 中文名称 | 蛋白磷酸酯酶抑制剂 |
|---|---|
| 中文同义词 | 蛋白磷酸酯酶抑制剂;PP2A催化亚基抑制剂(CALYCULIN A);花萼海绵诱癌素;花萼海绵体诱癌素A |
| 英文名称 | CALYCULIN A |
| 英文同义词 | C05370;N-[(3S)-[4-(1E)-3-[(2R,3R,4R,7S,8S,9R)-2-[(1S,3S,4S,5R,7E,9E,11E,13Z)-14-Cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyl-7,9,11,13-tetradecatetraenyl]-9-hydroxy-4,4,8-trimethyl-3-(phosphonooxy)-1,6-dioxaspiro[4.5]dec-7-yl]-1-propenyl]-2-oxazoly]butyl]-4-deoxy-4-(dimethylamino)-5-O-methyl-L-ribonamide;CALYCULIN A, DISCODERMIA CALYX;calyculin A from discodermia calyx;CALYCULIN A FROM DISCODERMIA CALYX, 10 U G;N-[(3S)-[4-(1E)-3-[(2R,3R,4R,7S,8S,9R)-2-[(1S,3S,4S,5R,7E,9E,11E,13Z)-14-Cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentam;N-[(3S)-[4-(1E)-3-[(2R,3R,4R,7S,8S,9R)-2-[(1S,3S,4S,5R,7E,9E,11E,13Z)-14-Cyano-3,5-dihydroxy-1-Methoxy-4,6,8,9,13-pentaMethyl-7,9,11,13-tetradecatetraenyl]-9-hydroxy-4,4,8-triMethyl-3-(phosphonooxy)-1,6-dioxaspiro[4.5]dec-7-yl]-1-propenyl]-2-o;L-Ribonamide, N-(3S)-3-4-(1E)-3-(2R,3R,5R,7S,8S,9R)-2-(1S,3S,4S,5R,6R,7E,9E,11E,13Z)-14-cyano-3,5-dihydroxy-1-methoxy-4,6,8,9,13-pentamethyl-7,9,11,13-tetradecatetraenyl-9-hydroxy-4,4,8-trimethyl-3-(phosphonooxy)-1,6-dioxaspiro4.5dec-7-yl-1-propenyl-2-oxa |
| CAS号 | 101932-71-2 |
| 分子式 | C50H81N4O15P |
| 分子量 | 1009.17 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂;Kinase/Phosphatase Biology;Serine/Threonine Kinase Biology;Protein phosphatase-1, Catalytic SubunitCancer Research;Tumor Promotors;Cell Signaling and Neuroscience;P to;Phosphatase InhibitorsSerine/Threonine Kinase Biology;Serine/Threonine Phosphatase Substrates;Protein Phosphatase 1 (PP1)Enzyme Inhibitors by Enzyme;Serine/Threonine Phosphatase Inhibitors;Tumor Growth Regulation;Inhibitor |
| Mol文件 | 101932-71-2.mol |
| 结构式 |  |
蛋白磷酸酯酶抑制剂 性质
| 熔点 | 247-249° |
|---|---|
| 比旋光度 | D -60° (c = 0.1 in ethanol) |
| 密度 | 1.25±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | 可溶于DMSO |
| 酸度系数(pKa) | 1.81±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色 |
| 水溶解性 | Soluble in DMSO (50 mM), ethanol (1 mg/ml), methanol, acetone, acetonitrile, chloroform, methylene chloride, and benzene. Insoluble in water. |
| Merck | 13,1731 |
| BRN | 4903216 |
Calyculin A ((-)-Calyculin A) 是有效，可渗透细胞的蛋白磷酸酶 1 (PP1) 和蛋白磷酸酶 2A (PP2A) 抑制剂，其 IC50 值分别为 2 nM 和 0.5-1 nM。
IC50: 2 nM (PP1); 0.5-1 nM (PP2A)
Calyculin A (1-10 nM; 24 hours) induces cytotoxicity in MG63 cells in a dose-dependent manner up to 10 nM in MG63 cells.
Cell Cytotoxicity Assay
| Cell Line: | Human osteosarcoma MG63 cells |
| Concentration: | 0, 1, 2, 5, 10 nM |
| Incubation Time: | 24 hours |
| Result: | Treatment with 0.1 nM for 24 h had a minimal effect on MG63 cell survival. Cell rounding and shrinking were obvious in the cultures treated for 24 h with 5 nM. The level of the cell viability treated with 10 nM was 27% that of the control cultures. |
安全信息
| 危险品标志 | T |
|---|---|
| 危险类别码 | 23/24/25-38 |
| 安全说明 | 36/37/39-45 |
| 危险品运输编号 | UN 3462 6.1/PG 3 |
| WGK Germany | 3 |
| F | 8-10 |
| 危险等级 | 6.1(a) |
| 包装类别 | II |
| 海关编码 | 2934999090 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-18983 | 蛋白磷酸酯酶抑制剂 Calyculin A | 101932-71-2 | 10μg(0.5mM * 20μL in DMSO) | 1200元 |
| 2024/01/25 | HY-18983 | 蛋白磷酸酯酶抑制剂 Calyculin A | 101932-71-2 | 25μg(0.5mM * 50μL in DMSO) | 2050元 |