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GF 109203X

现货
Catalog No.
A8342
Protein kinase C、MLCK、PKG和PKA 的抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,000.00
Ship with 10-15 days
5mg
¥ 600.00
Ship with 10-15 days
10mg
¥ 1,200.00
Ship with 10-15 days

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Background

GF 109203X is a potent and selective inhibitor of protein kinase C [1].

Protein kinase C (PKC) is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of serine and threonine amino acid residues on target proteins. PKC enzymes are activated by increases in the concentration of Ca2+ or diacylglycerol (DAG).

GF 109203X is a competitive inhibitor with Ki value of 14 nM. It inhibited PKC with IC50 values of 0.020, 0.017, 0.016, 0.020 μM for α, βI, βII and γ, respectively. In human platelets and Swiss 3T3 fibroblasts, GF 109203X significantly inhibited PKC-mediated phosphorylations with Mr of 47000 and 80000 in platelets and Swiss 3T3 cells, respectively. Also, GF 109203X inhibited collagen-triggered ATP secretion as well as α- thrombin- and collagen- induced platelet aggregation [1]. GF 109203X selectively inhibited PKC activity extracted from either fibroblasts or keratinocytes with IC50 values of 0.01 μM and 0.4 μM, respectively. Also, GF 109203X inhibited the expression of c-fos and c-jun, which involved in the cellular differentiation process [2].

References:
[1].  Toullec D, Pianetti P, Coste H, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem, 1991, 266(24): 15771-15781.
[2].  Le Panse R, Coulomb B, Mitev V, et al. Differential modulation of human fibroblast and keratinocyte growth by the protein kinase C inhibitor GF 109203X. Mol Pharmacol, 1994, 46(3): 445-451.

文献引用

1. Liu MF, Xue Y, et al. "Orexin-A Exerts Neuroprotective Effects via OX1R in Parkinson's Disease." Front Neurosci. 2018 Nov 15;12:835. PMID:30524223

Chemical Properties

Physical AppearanceA solid
StorageStore at RT
M.Wt412.49
Cas No.133052-90-1
FormulaC25H24N4O2
SynonymsGö 6850;Bisindolylmaleimide I
Solubility≥20.6mg/mL in DMSO
Chemical Name3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione
SDFDownload SDF
Canonical SMILESCN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

s细胞系

人类血小板,Swiss 3T3成纤维细胞

溶解方法

在DMSO中的溶解度﹥20.6mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

人类血小板:500 nM, 1min

应用

GF 109203X在人类血小板中抑制了diC8刺激诱导的P47磷酸化。在人类血小板中,对于PKC(蛋白激酶C)的IC50为190nM (1 min)。GF 109203X可以抑制胶原蛋白引起的ATP分泌以及α-凝血酶和胶原蛋白诱导的血小板聚集。在Swiss 3T3细胞中,GF109203X可以抑制EGF受体的转化,也可以完全逆转PDBu(phorbol 12,13-dibutyrate二丁酸佛波醇酯)的抑制效果,IC50为0.9μm。

动物实验 [2]:

动物模型

Wistar大鼠

剂量

10 μg溶解于含有10% DMSO的生理盐水,足底注射

应用

GF109203X可以消除由BK(缓激肽)引起的机械异常性疼痛。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Toullec D, Pianetti P, Coste H, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem, 1991, 266(24): 15771-15781.

[2] Souza AL, Moreira FA, et al. In vivo evidence for a role of protein kinase C in peripheral nociceptive processing. Br J Pharmacol. 2002, 135(1), 239-247.

生物活性

描述 GF109203X是PKC的抑制剂,对PKCα、PKCβI、PKCβII和PKCγ的IC50值分别为20 nM、17 nM、16 nM和20 nM。
靶点 PKCα PKCβI PKCβII PKCγ    
IC50 20 nM 17 nM 16 nM 20 nM    

质量控制

化学结构

GF 109203X

相关生物数据

GF 109203X

相关生物数据

GF 109203X

相关生物数据

GF 109203X