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BI 4394

Cat. No. 8842 Submit a Review Datasheet / COA / SDS
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Description: Highly potent and selective MMP-13 inhibitor
Chemical Name: 2-Ethyl 5-[3-[[[(4-carboxyphenyl)methyl]amino]carbonyl]-1-methyl-1H-pyrazol-5-yl]-1H-indole-2-carboxylate
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for BI 4394

BI 4394 is a highly potent and selective MMP-13 inhibitor (IC50 = 1 nM). BI 4394 inhibits the degradation of isolated bovine nasal cartilage explants (IC50 = 31 nM). It shows high selectivity (>1000 fold) for MMP-13 over other MMPs. In vivo, BI 4394 decreases the mean arthritic score vs control in a murine model of rheumatoid arthritis, when administered at a dose of 100 mg/kg over a 14-day period. BI 4394 is orally bioavailable.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the BI 4394 page on the SGC website.

Technical Data for BI 4394

M. Wt 446.46
Formula C24H22N4O5
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1222173-37-6
PubChem ID 45376872
InChI Key MMJPVSDTLGFIQW-UHFFFAOYSA-N
Smiles O=C(O)C1=CC=C(C=C1)CNC(=O)C2=NN(C(=C2)C=3C=CC=4NC(=CC4C3)C(=O)OCC)C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for BI 4394

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.65 100

Preparing Stock Solutions for BI 4394

The following data is based on the product molecular weight 446.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.24 mL 11.2 mL 22.4 mL
5 mM 0.45 mL 2.24 mL 4.48 mL
10 mM 0.22 mL 1.12 mL 2.24 mL
50 mM 0.04 mL 0.22 mL 0.45 mL

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References for BI 4394

References are publications that support the biological activity of the product.

Taylor et al (2011) Fragment-based discovery of indole inhibitors of matrix metalloproteinase-13. J.Med.Chem. 54 8174 PMID: 22017539

Taylor et al (2021) Indole inhibitors of MMP-13 for arthritic disorders. ACS Omega 6 18635 PMID: 34337203

If you know of a relevant reference for BI 4394, please let us know.

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Keywords: BI 4394, BI 4394 supplier, BI4394, potent, selective, inhibitors, inhibits, MMP13, Matrixins, Matrix, Metalloproteinase, MMP, Metalloprotease, proteinases, Proteases, orally, bioavailable, in, vivo, 8842, Tocris Bioscience

Citations for BI 4394

Citations are publications that use Tocris products.

Currently there are no citations for BI 4394. Do you know of a great paper that uses BI 4394 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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