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AdipoGen Life Sciences
Bisindolylmaleimide I
70
CHF
CHF 70.00
In stock
AG-CR1-0009-M0011 mgCHF 70.00
AG-CR1-0009-M0055 mgCHF 210.00
| Product Details | |
|---|---|
| Synonyms | GF-109203X; Gö 6850; BIM I |
| Product Type | Chemical |
| Properties | |
| Formula |
C25H24N4O2 |
| MW | 412.5 |
| CAS | 133052-90-1 |
| Purity Chemicals | ≥97% (NMR) |
| Appearance | Orange solid. |
| Solubility | Soluble in DMSO. |
| InChi Key | QMGUOJYZJKLOLH-UHFFFAOYSA-N |
| Smiles | CN(C)CCCN1C=C(C2=C1C=CC=C2)C1=C(C(=O)NC1=O)C1=CNC2=C1C=CC=C2 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Cell permeable kinase inhibitor with improved selectivity for protein kinase C (PKC) (Ki = 10 nM) [1].
- Competetive inhibitor for the ATP-binding site of PKC [1].
- Anti-inflammatory [2].
- Binds to P-glycoprotein [3].
- Telomerase activity inhibitor [4].
- Potent glycogen synthase kinase-3 (GSK-3) inhibitor [5].
- Necrosis inhibitor [6].
- Blocks hERG potassium channels [7-9].
- Promotes osteoblastogenesis in human mesenchymal stem cells [10].
Product References
- The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C: D. Toullec, et al.; J. Biol. Chem. 266, 15771 (1991)
- Anti-inflammatory properties of the protein kinase C inhibitor, 3-[1-[3- (dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H- pyrrole-2,5- dione monohydrochloride (GF109203X) in the PMA-mouse ear edema model: S. Kuchera, et al.; Agents Actions 39, C169 (1993)
- Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance: V. Gekeler, et al.; Br. J. Cancer 74, 897 (1996)
- Inhibition of telomerase activity by PKC inhibitors in human nasopharyngeal cancer cells in culture: W.C. Ku, et al.; BBRC 241, 730 (1997)
- The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity: I. Hers, et al. FEBS Lett. 460, 433 (1999)
- Bisindolylmaleimide I and V inhibit necrosis induced by oxidative stress in a variety of cells including neurons: R. Asakai, et al.; Neurosci. Res. 44 297 (2002)
- Direct block of hERG potassium channels by the protein kinase C inhibitor bisindolylmaleimide I (GF109203X): D. Thomas, et al.; Cardiovasc. Res. 64, 467 (2004)
- The protein kinase C inhibitor, bisindolylmaleimide (I), inhibits voltage-dependent K+ channels in coronary arterial smooth muscle cells: W.S. Park, et al.; Life Sci. 77 512 (2005)
- Effects of the PKC inhibitors chelerythrine and bisindolylmaleimide I (GF 109203X) on delayed rectifier K(+) currents: G. Harmati, et al.; Naunyn Schmiedebergs Arch. Pharmacol. 383, 141 (2011)
- Bisindolylmaleimide I enhances osteogenic differentiation: F. Zhou, et al.; Prot. Cell 3, 311 (2012)
- Methylglyoxal augments uridine diphosphate-induced contraction via activation of p38 mitogen-activated protein kinase in rat carotid artery: T. Matsumoto, et al.; Eur. J. Pharmacol. 904, 174155 (2021)
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