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Submit ReviewBisindolylmaleimide II
说明： Potent PKC inhibitor; also potent nAChR antagonist
化学名： 3-(1H-Indol-3-yl)-4-[1-[2-(1-methyl-2-pyrrolidinyl)ethyl]-1H-indol-3-yl]-1H-pyrrole-2,5-dione
纯度： ≥97% (HPLC)
生物活性 for Bisindolylmaleimide II
Bisindolylmaleimide II is a potent, ATP-competitive protein kinase C (PKC) inhibitor (IC50 = 0.01 μM). Displays selectivity for PKC over protein kinase A (PKA) and phosphorylase kinase (PK) (IC50 values are 0.75 and 2μM for PK and PKA respectively). Also displays potent, noncompetitive antagonism at nicotinic cholinergic receptors (IC50 ~ 0.03 μM for inhibition of catecholamine secretion in nicotine-stimulated PC-12 cells).
化合物库 for Bisindolylmaleimide II
Bisindolylmaleimide II is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Epigenetics Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Bisindolylmaleimide II
| 分子量 | 438.52 |
| 公式 | C27H26N4O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥97% (HPLC) |
| CAS Number | 137592-45-1 |
| PubChem ID | 2397 |
| InChI Key | LBFDERUQORUFIN-UHFFFAOYSA-N |
| Smiles | O=C(NC3=O)C(C4=CNC5=C4C=CC=C5)=C3C1=CN(CCC6CCCN6C)C2=CC=CC=C12 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Bisindolylmaleimide II
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 43.85 | 100 |
制备储备液 for Bisindolylmaleimide II
以下数据基于产品分子量 438.52。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.28 mL | 11.4 mL | 22.8 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.56 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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产品说明书 for Bisindolylmaleimide II
参考文献 for Bisindolylmaleimide II
参考文献是支持产品生物活性的出版物。
Toullec et al (1991) The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J.Biol.Chem. 266 15771 PMID: 1874734
Mahata et al (2002) Chromaffin cell catecholamine secretion: bisindolylmaleimide compounds exhibit novel and potent antagonist effects at the nicotinic cholinergic receptor in pheochromocytoma cells. Mol.Pharmacol. 61 1340 PMID: 12021395
If you know of a relevant reference for Bisindolylmaleimide II, please let us know.
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关键词: Bisindolylmaleimide II, Bisindolylmaleimide II supplier, protein, kinase, C, PKC, inhibits, inhibitors, nicotinic, cholinergic, acetylcholine, nAChRs, antagonists, antagonism, catecholamines, potent, Protein, Kinase, Nicotinic, Receptors, (Non-selective), 4128, Tocris Bioscience
4 篇 Bisindolylmaleimide II 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Bisindolylmaleimide II 的部分引用包括：
James H et al (2020) Contributing mechanisms underlying desensitization of cholecystokinin-induced activation of primary nodose ganglia neurons. Am J Physiol Cell Physiol 318 C787-C796 PMID: 32073876
John et al (2020) Small Molecule Inhibitor Screen Reveals Calcium Channel Signaling as a Mechanistic Mediator of Clostridium difficile TcdB-Induced Necrosis. ACS Chem Biol 15 1212-1221 PMID: 31909964
O'Neill & Sylantyev (2018) Selective modulation of tonically active GABAA receptor functional subgroups by G-proteins and protein kinase C. Exp Biol Med (Maywood) 243 1046 PMID: 30205722
Jones et al (2004) Regulation of SHP-1 tyrosine phosphatase in human platelets by serine phosphorylation at its C terminus. PLoS One 279 40475 PMID: 15269224
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BII upregulates GABA-dependent affects of GABA-A receptor.
By
Anonymous on 07/21/2019
分析类型： In Vitro
种属： Rat
细胞系/组织： Hippocampus
Bisindolylmaleimide II (BII) was used to block PKC in hippocampal granule cells. Such a block enhances activity of GABA receptors and, as a sequence, increases effect of competitive antagonists of GABA on root mean square noise (RMS) amplitude of holding current in electrophysiological recording. Figure: changes of RMS after application of SR 95531 and SR 95531 + Picrotoxin. BII makes significant an effect of SR 95531 applied alone.
