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BCI
- NSC 150117
- Soluble in DMSO
- MF: C22H23NO
- MW: 317.42
Description
BCI (NSC150117) is an allosteric inhibitor of dual-specificity phosphatases (DUSPs) that selectively inhibits DUSP6 and DUSP1 with IC50 values of 12.3 μM and 11.5 μM, respectively, while showing no significant inhibition of DUSP5. BCI suppresses DUSP-mediated dephosphorylation of ERK1/2, resulting in sustained MAPK/ERK pathway activation.
DUSP6 is a key negative feedback regulator of fibroblast growth factor (FGF)-mediated ERK signaling and plays an important role in development, cell proliferation, differentiation, and tissue regeneration. BCI-mediated DUSP6 inhibition promotes expansion of myocardial progenitor cells and increases heart size in zebrafish embryos. BCI has also demonstrated activity against lung cancer and uveal melanoma cells, making it a valuable tool for studying ERK signaling, regenerative biology, developmental processes, and cancer biology.
The salt form, BCI hydrochloride (Axon 2852) is available as a more hydrophilic alternative. Researchers seeking enhanced potency and optimized DUSP inhibition may also consider BCI-215 (Axon 4452), a second-generation,refined, analogue of BCI.
Key Features
- Allosteric inhibitor of DUSP6 and DUSP1
- IC50: 12.3 μM for DUSP6 and 11.5 μM for DUSP1
- No significant inhibition of DUSP5
- Enhances ERK1/2 signaling through DUSP inhibition
- Promotes myocardial progenitor expansion in vivo
Applications
- DUSP and phosphatase biology research
- MAPK/ERK signaling studies
- FGF signaling investigations
- Cardiac regeneration and developmental biology research
- Cancer biology and target validation studies
More Information
| Parent CAS No. | 1245792-51-1 |
|---|---|
| Chemical Name | 2-Benzylidene-3-(cyclohexylamino)-2,3-dihydro-1H-inden-1-one |
| SMILES | C1(=O)C2=C(C=CC=C2)C(NC2CCCCC2)/C/1=CC1=CC=CC=C1 |
| MFCD | MFCD20232928 |
| InChi | InChI=1S/C22H23NO/c24-22-19-14-8-7-13-18(19)21(23-17-11-5-2-6-12-17)20(22)15-16-9-3-1-4-10-16/h1,3-4,7-10,13-15,17,21,23H,2,5-6,11-12H2/b20-15+ |
| InChiKey | XJDKPLZUXCIMIS-HMMYKYKNSA-N |
| CID | 6419844 |
| Short Description | DUSP inhibitor |
References
- G. Molina et al. Zebrafish chemical screening reveals an inhibitor of Dusp6 that expands cardiac cell lineages. Nat. Chem. Biol. 2009, 5, 680-687.
- A.M. Best et al. Identification of four potential epigenetic modulators from the NCI structural diversity library using a cell-based assay. J. Biomed. Biotechnol. 2011, 868095.
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