双辛基马来酰亚胺是有效的,选择性的蛋白激酶C(PKC)抑制剂。它们在结构上与天然存在的分子星形孢菌素相似,但相对于其他蛋白激酶,它们对PKC的选择性更高。双辛基马来酰亚胺用于选择性探测PKC介导的激素,细胞因子和生长因子信号的转导途径。双辛基马来酰亚胺通过与催化亚基相互作用抑制PKC。抑制作用与ATP竞争。对类似物的结构-活性关系的研究表明,吲哚氮上的阳离子取代基增加了其作为PKC抑制剂的能力。 Bisindolylmaleimides are potent, selective inhibitors of protein kinase C (PKC). They are structurally similar to the naturally occurring molecule, staurosporine, but they are more selective for PKC over other protein kinases. Bisindolylmaleimides are used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals. Bisindolylmaleimides inhibit PKC by interacting with the catalytic subunit. Inhibition is competitive with ATP. Studies of structure-activity relationships of analogs indicate that cationic substituents at the indole nitrogen increase the potency as an inhibitor of PKC.
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3-(1H-indol-3-yl)-4-[1-(3-piperazin-1-ylpropyl)indol-3-yl]pyrrole-2,5-dione
Dangerous GoodsCAS number:137592-47-3 molecular formula:C27H27N5O2
overview
compound introduction
Specs
| Chinese alias | 3-(1H-吲哚-3-基)-4-{1-[3-(1-哌嗪基)丙基]-1H-吲哚-3-基}-1H-吡咯-2,5-二酮 | ||
| English alias | 3-(1H-indol-3-yl)-4-[1-(3-piperazin-1-ylpropyl)indol-3-yl]pyrrole-2,5-dione | DTXSID40274364 | SCHEMBL7978092 | Bisindolylmaleimide VII, 96% (TLC), solid | BDBM2686 | Bisindolyl deriv. 24 | bisindolylmaleimide vii | 3-(1H-indol-3-yl)-4-(1-(3-(piperazin-1- | ||
| CAS number | 137592-47-3 | molecular formula | C27H27N5O2 |
| molecular weight | 453.5 | Exact mass | ≥96% |
| PSA | 82.2 | logp | 2.4 |
numbering system
| CAS | 137592-47-3 |
| Wikidata | Q82003731 |
| ChEMBL ID | CHEMBL446199 |
| PubChem CID | 2402 |
| Nikkaji Number | J1.479.496D |
| DSSTox Substance ID | DTXSID40274364 |
physicochemical properties
| XLogP3 | XLogP3-AA: 2.4 |
| 复杂性 | 822 |
| Exact Mass | 453.21647512 |
| 形式电荷 | 0 |
| 重原子计数 | 34 |
| Molecular Weight | 453.5 |
| Monoisotopic Mass | 453.21647512 |
| 可旋转键计数 | 6 |
| 氢键供体计数 | 3 |
| 氢键受体计数 | 4 |
| 共价键单元计数 | 1 |
| 同位素原子计数 | 0 |
| 拓扑极性表面积 | 82.2 Ų |
| 定义键立体中心计数 | 0 |
| 定义原子立体中心计数 | 0 |
| 未定义键立体中心计数 | 0 |
| 未定义原子手性中心计数 | 0 |
Safety information
WGK Germany:
3
Personal protective equipment:
Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter
Production methods and uses
purpose
工业应用参考:
工业分类参考:电气机械和器材制造业。
应用场景参考:常见于生产制造场景,可作为主料、辅料、添加剂或工艺辅助材料参与配方与加工流程 。
作用参考:可作为基础工业材料参与合成、提纯或改性过程,为后续产品制造和工艺放大提供支撑 。
选型提示:不同品牌和不同标准体系下的技术参数可能存在差异,应用前应优先核对规格、检测方法和质量要求 。
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