GF 109203X (Bisindolylmaleimide I)
(Synonyms: Gö 6850;Bisindolylmaleimide I) 目录号 : GC15431
A PKC inhibitor
Cas No.:133052-90-1
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
human platelets, Swiss 3T3 fibroblasts |
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Preparation method |
The solubility of this compound in DMSO﹥20.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
human platelets: 500 nM, 1min |
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Applications |
GF 109203X inhibited diC8-stimulated P47 phosphorylation in human platelets. Half-maximal inhibition (IC50) for protein kinase C (PKC) is obtained at 190nM (1 min) in human platelets. GF 109203X inhibited collagen-triggered ATP secretion as well as α- thrombin- and collagen- induced platelet aggregation. GF109203X could inhibit EGF receptor transmodulation in Swiss 3T3 Cells. GF 109203X completely reversed the inhibitory effect of PDBu with a half-maxima effect at 0.9μm in Swiss 3T3 fibroblasts. |
| Animal experiment [2]: | |
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Animal models |
Wistar rats |
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Dosage form |
10 μg in 10% DMSO in saline by intraplantar (i.pl.) injection. |
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Application |
GF109203X abolished the mechanical allodynia induced by BK (bradykinin). |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. | |
| Cas No. | 133052-90-1 | SDF | |
| 别名 | Gö 6850;Bisindolylmaleimide I | ||
| 化学名 | 3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione | ||
| Canonical SMILES | CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54 | ||
| 分子式 | C25H24N4O2 | 分子量 | 412.49 |
| 溶解度 | ≥ 20.6mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4243 mL | 12.1215 mL | 24.243 mL |
| 5 mM | 0.4849 mL | 2.4243 mL | 4.8486 mL |
| 10 mM | 0.2424 mL | 1.2122 mL | 2.4243 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet