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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G129390-1mg | 1mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $18.90 | |
G129390-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $75.90 | |
G129390-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $129.90 | |
G129390-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $489.90 |
Potent, selective PKC inhibitor. Potent GSK-3 inhibitor. Potent 5-HT3 antagonist.
Synonyms | NCGC00024760-07 | Go 6850 | KBio2_003068 | Bio2_000900 | Bisindolylmaleimide I (GF 109203X) | MFCD00236428 | AKOS024458625 | SCHEMBL338086 | 3-{1-[3-(DIMETHYLAMINO)PROPYL]-1H-INDOL-3-YL}-4-(1H-INDOL-3-YL)-1H-PYRROLE-2,5-DIONE | IDI1_002175 | 1H-Pyrrole-2, |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | Bisindolylmaleimide I (GF 109203X) is a staurosporine inspired molecule, which has been shown to display equally potent inhibition, but with vastly superior selectivity, for all of the known isoforms of PKC (IC50 = 8-20 nM). Inhibition is competitive with |
Storage Temp | Store at 2-8°C |
Shipped In | Wet ice |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of protein kinase C alpha;Inhibitor of protein kinase C beta;Inhibitor of protein kinase C gamma |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | GF109203X is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione |
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INCHI | InChI=1S/C25H24N4O2/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31) |
InChi Key | QMGUOJYZJKLOLH-UHFFFAOYSA-N |
Canonical SMILES | CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54 |
Isomeric SMILES | CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54 |
WGK Germany | 3 |
RTECS | UX9590000 |
PubChem CID | 2396 |
Molecular Weight | 412.48 |
CAS Registry No. | 133052-90-1 |
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PubChem CID | 2396 |
ChEMBL Ligand | CHEMBL7463 |
Wikipedia | BIM-1 |
RCSB PDB Ligand | BI1 |
Enter Lot Number to search for COA:
Solubility | Soluble in DMSO (~1 mg/ml), DMF (10 mg/ml; warm to 40°C & vortex well), and 1:10 DMSO:PBS (pH 7.2) (~0.1 mg/ml). Insoluble in water. |
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Sensitivity | Heat Sensitive |
Melt Point(°C) | 270 °C |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H302:Harmful if swallowed |
Precautionary Statements | P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P301+P317:IF SWALLOWED: Get medical help. |
WGK Germany | 3 |
RTECS | UX9590000 |
1. Li M et al.. (2017) Protein Kinase C Mediates the Corticosterone-induced Sensitization of Dorsal Root Ganglion Neurons Innervating the Rat Stomach.. J Neurogastroenterol Motil, 23 (3): (464-476). [PMID:28343377] |
1. Toullec D, Pianetti P, Coste H, Bellevergue P, Grand-Perret T, Ajakane M, Baudet V, Boissin P, Boursier E, Loriolle F et al.. (1991) The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.. J Biol Chem, 266 (24): (15771-81). [PMID:1874734] [10.1021/op500134e] |
2. Wu K et al.. (2021) Activity- and sleep-dependent regulation of tonic inhibition by Shisa7.. Cell Rep, 34 (12): (108899). [PMID:33761345] |
3. Sutherland-Deveen ME et al.. (2019) Differential Regulation of Human Ether-à-Go-Go-Related Gene (hERG) Current and Expression by Activation of Protein Kinase C.. Mol Pharmacol, 96 (1-12). [PMID:31015282] |
4. Du Y et al.. (2021) Kv1.5 channels are regulated by PKC-mediated endocytic degradation.. J Biol Chem, 296 (100514). [PMID:33676894] |
5. Li M et al.. (2017) Protein Kinase C Mediates the Corticosterone-induced Sensitization of Dorsal Root Ganglion Neurons Innervating the Rat Stomach.. J Neurogastroenterol Motil, 23 (3): (464-476). [PMID:28343377] |