GF109203X
- CAS No.
- 133052-90-1
- Chemical Name:
- GF109203X
- Synonyms
- BIM 1;GO 6850;G 6850];CS-1080;Estorra;GF 109203X;GO 6850 HCL;GF-109203X HCL;RBT205 INHIBITOR;GF109203X Go-6850
- CBNumber:
- CB2103079
- Molecular Formula:
- C25H24N4O2
- Molecular Weight:
- 412.48
- MDL Number:
- MFCD00236428
- MOL File:
- 133052-90-1.mol
- MSDS File:
- SDS
| Melting point | 280℃ (decomposition) |
|---|---|
| Boiling point | 685.6±55.0 °C(Predicted) |
| Density | 1.30±0.1 g/cm3(Predicted) |
| storage temp. | 2-8°C |
| solubility | DMSO: ~1 mg/mlsoluble |
| form | Liquid |
| pka | 8.13±0.60(Predicted) |
| color | Orange |
| Water Solubility | Insoluble in water. |
| 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. |
| FDA UNII | L79H6N0V6C |
GF109203X price More Price(50)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | 203290 | Bisindolylmaleimide I - CAS 133052-90-1 - Calbiochem A highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor (IC?? = 10 nM) that is structurally similar to staurosporine. | 133052-90-1 | 250μg | $56.2 | 2024-03-01 | Buy |
| Sigma-Aldrich | 203290 | Bisindolylmaleimide I | 133052-90-1 | 1mg | $187 | 2024-03-01 | Buy |
| TCI Chemical | B5781 | Bisindolylmaleimide I | 133052-90-1 | 5MG | $95 | 2024-03-01 | Buy |
| TCI Chemical | B5781 | Bisindolylmaleimide I | 133052-90-1 | 25MG | $330 | 2024-03-01 | Buy |
| Alfa Aesar | J63401 | Bisindolylmaleimide 1 | 133052-90-1 | 5mg | $153.65 | 2024-03-01 | Buy |
GF109203X Chemical Properties,Uses,Production
Description
GF-109203X (133052-90-1) is a potent and selective protein kinase C inhibitor (IC50 = 10 nM; cAMP-dependent protein kinase IC50 = 2 μM and phosphorylase kinase IC50 = 0.7 μM). Inactive against the tyrosine kinases EGFR, PGDFR and Insulin receptor. Potent inhibitor of GSK-3β in cell lysates (IC50 = 360nM) and GSK-3β immunoprecipitates (IC50 = 170nM) derived from rat epididymal adipocytes.2 Cell permeable.
Uses
Bisindolylmaleimide is used as a highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3, used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals, very potent and selective inhibitor of protein kinase C.
Biological Activity
Very potent and selective inhibitor of protein kinase C, selective for the α and β 1 isoforms (IC 50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μ M for α , β 1, δ , ε , and ζ isoforms respectively). Selective over MLCK, PKG and PKA (IC 50 values are 0.6, 4.6, and 33 μ M respectively). Potent antagonist at the 5-HT 3 receptor (K i = 29.5 nM). Anti-inflammatory in vivo . Also available as part of the Mixed Kinase Inhibitor Tocriset™ .
Biochem/physiol Actions
A potent and selective competitive inhibitor of protein kinase C (PKC) and of glycogen synthase kinase-3 (GSK-3). Inhibits parathyroid hormone-induced Ca2+ resorption from isolated bone tissue, Staurosporine, another protein kinase inhibitor, actually enhanced Ca2+ resorption elicited by a number of agents, but GF109203X counteracted that enhancement.
storage
Store at RT
References
1) Toullec, et al. (1991), The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C; J. Biol .Chem. 266 15771 2) Hers, et al. (1999) The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity; FEBS Lett. 460 433
GF109203X Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | fandachem@gmail.com | China | 9352 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29474 | 58 |
| Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 | shawn@hirisunpharm.com | CHINA | 9923 | 58 |
| Dayang Chem (Hangzhou) Co.,Ltd. | 571-88938639 +8617705817739 | info@dycnchem.com | CHINA | 52867 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
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