133052-90-1
GF109203X
CAS: 133052-90-1
Molecular Formula: C25H24N4O2
133052-90-1 - Names and Identifiers
| Name | GF109203X |
| Synonyms | GO 6850 GF109203X GF 109203X GO 6850 HCL GF-109203X HCL BISINDOLYLMALEIMIDE GF109203X HYDROCHLORIDE InSolution? Bisindolylmaleimide I Bisindolylmaleimide I (GF 109203X) |
| CAS | 133052-90-1 |
133052-90-1 - Physico-chemical Properties
| Molecular Formula | C25H24N4O2 |
| Molar Mass | 412.48 |
| Density | 1.30±0.1 g/cm3(Predicted) |
| Melting Point | 280℃ (decomposition) |
| Boling Point | 685.6±55.0 °C(Predicted) |
| Water Solubility | Insoluble in water. |
| Solubility | Soluble in DMSO (~1 mg/ml), DMF (10 mg/ml; warm to 40°C & vortex well), and 1:10 DMS |
| Appearance | Orange to crimson powder |
| Color | Orange |
| pKa | 8.13±0.60(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 6 months. |
| MDL | MFCD00236428 |
| Use | A highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3 |
| In vitro study | GF109203X, as an ATP competitive PKC inhibitor, inhibits platelet aggregation induced by activated protein kinase C and can be used as a potential tool to study the role of PKC in signal transduction pathways. GF109203X produced reversal activity against P-glycoprotein and MRP-mediated multidrug resistance. GF109203X significantly reduced Carbachol-stimulated ERK1/2 activation and SNU-407 subsequent spread of colon cancer cells by inhibiting PKC. |
| In vivo study | GF109203X (10 μg/mouse, I. pl.) dose-dependently inhibits BK-induced mechanical hyperalgesia in Wistar rats. |
133052-90-1 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R40 - Limited evidence of a carcinogenic effect R22 - Harmful if swallowed |
| Safety Description | 36/37 - Wear suitable protective clothing and gloves. |
| WGK Germany | 3 |
| RTECS | UX9590000 |
133052-90-1 - Introduction
GF109203X is a potent PKC inhibitor, inhibiting PKCα, PKCβI, PKCβII and PKCγ,IC50 is 20 nM, 17 nM, 16nM and 20 nM, respectively, and the selectivity of PKC is more than 3000 times higher than that of EGFR, PDGFR and insulin receptor.
Last Update：2022-10-16 17:41:25
133052-90-1 - Reference Information
| biological activity | GF109203X is an effective PKC inhibitor, inhibiting PKCα, PKCβI, PKCβII and PKCγ,IC50 are 20 nM, 17 nM, 16nM and 20 nM respectively, and the selectivity of PKC is more than 3000 times higher than that of EGFR, PDGFR and insulin receptor. Bisindolylmaleimide I (GF109203X, GO 6850) is an effective PKC inhibitor, which acts on PKCα,PKCβI,PKCβII and PKCγ. in cell-free test, IC50 is 20 nM, 17 nM, 16nM and 20 nM respectively. the selectivity of PKC is more than 3000 times higher than that of EGFR,PDGFR and insulin receptor. |
| Features | staurosporine greater selectivity than PKC inhibitors. GF109203X is a chemical probe for studying protein kinase C signal transduction pathway. Potential use in a variety of cancers. |
| Target | Value |
| PKCβ2 (Cell-free assay) | 16 nM |
| PKCβ1 (Cell-free assay) | 17 nM |
| PKCα (Cell-free assay) | 20 nM |
| PKCγ (Cell-free assay) | 20 nM |
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: GF109203X Visit Supplier Webpage Request for quotationCAS: 133052-90-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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