Bisindolylmaleimide I

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Chemical Structure| 133052-90-1 同义名 : Go 6850;GF109203X;GO6850. BIMI.;bisindolylmaleimide;Gö 6850;BIM I
CAS号 : 133052-90-1
货号 : A439059
分子式 : C25H24N4O2
纯度 : 99%+
分子量 : 412.484
MDL号 : MFCD00236428
存储条件：

Pure form Inert atmosphere,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(72.73 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PKCβ

    PKCβ1, IC50:17 nM

    PKCβ2, IC50:16 nM

  • PKCγ

    PKCγ, IC50:20 nM

  • PKCα

    PKCα, IC50:20 nM
描述 Protein kinase C (PKC) is a Ser/ Thr protein kinase whose activation is one of the earliest events in the cascade of signal transduction pathways leading to a variety of cellular responses such as secretion, gene expression, proliferation, and muscle contraction. Bisindolylmaleimide I, also called GF109203X, is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively[3]. GF109203X (20 nM) significantly increased the response to sciatic nerve stimulation in diabetic rats, producing a dilation not significantly different from controls. The administration of GF109203X was able to reverse the effects of hyperglycemia on NS1619 (10 µM)-mediated dilations[4]. GF109203X significantly decreased mechanical withdrawal threshold (mean ± SEM: 7.75 ± 0.47 g vs 2.74 ± 0.43 g) and cold withdrawal latency (mean ± SEM: 7.66 ± 0.29 seconds vs 3.96 ± 0.79 seconds) in complete Freundʼs adjuvant (CFA)‐induced rheumatoid arthritis[5].
作用机制 Bisindolylmaleimide I inhibits PKC activity exclusively via the ATP-binding site.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO cells Function assay Inhibition of Bacillus anthracis anthrax protective antigen heptamer pre-pore to pore conversion in CMG2-expressing CHO cells 19540764
mouse RAW264.7 cells Function assay 24 h Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay, IC50=0.19055 μM 17485504
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.12mL

2.42mL

1.21mL

24.24mL

4.85mL

2.42mL
参考文献

[1]Vetri F, Qi M, et al. Impairment of neurovascular coupling in Type 1 Diabetes Mellitus in rats is prevented by pancreatic islet transplantation and reversed by a semi-selective PKC inhibitor. Brain Res. 2017 Jan 15;1655:48-54.

[2]Toullec D, Pianetti P, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81.

[3]Toullec D, Pianetti P, Coste H, Bellevergue P, Grand-Perret T, Ajakane M, Baudet V, Boissin P, Boursier E, Loriolle F, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81. PMID: 1874734.

[4]Vetri F, Qi M, Xu H, Oberholzer J, Paisansathan C. Impairment of neurovascular coupling in Type 1 Diabetes Mellitus in rats is prevented by pancreatic islet transplantation and reversed by a semi-selective PKC inhibitor. Brain Res. 2017 Jan 15;1655:48-54. doi: 10.1016/j.brainres.2016.11.012. Epub 2016 Nov 16. PMID: 27865779; PMCID: PMC5195876.

[5]Bai Q, Shao J, Cao J, Ren X, Cai W, Su S, George S, Tan Z, Zang W, Dong T. Protein kinase C-α upregulates sodium channel Nav1.9 in nociceptive dorsal root ganglion neurons in an inflammatory arthritis pain model of rat. J Cell Biochem. 2020 Jan;121(1):768-778. doi: 10.1002/jcb.29322. Epub 2019 Aug 5. PMID: 31385361.