research use only
Cat.No.S7155
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| Sf9 insect cells | Function assay | Inhibition of human matrix metalloprotease-2 expressed in Sf9 insect cells, IC50=0.013 μM | 15582436 | |||
| Sf9 insect cells | Function assay | Inhibition of human matrix metalloprotease-9 expressed in Sf9 insect cells, IC50=0.025 μM | 15582436 | |||
| HT1080 | Function assay | In vitro inhibitory activity against matrix metalloprotease 2 isolated from human HT1080 fibrosarcoma cells induced with TNF, IC50=0.0021μM | 9873712 | |||
| white blood cells | Antifibrotic assay | 25 to 150 mg/kg | 13 days | Antifibrotic activity in bleomycin-induced C57B1/6 mouse model assessed as inhibition of white blood cells in bronchoalveolar lavage at 25 to 150 mg/kg, po bid administered 2 hrs prior bleomycin induction for 13 days | 15582436 | |
| RPM18866 | Function assay | Tested for inhibition against CD23 (IgE receptor) proteolysis in membranes derived from RPM18866 cells ( a human B-cell line), IC50=0.1μM | 9871622 | |||
| RPM18866 | Function assay | Inhibition against CD23 (IgE receptor) proteolysis in membranes derived from RPM18866 cells, IC50=0.1μM | 9871623 | |||
| Click to View More Cell Line Experimental Data | ||||||
| Molecular Weight | 477.64 | Formula | C23H31N3O4S2 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 130370-60-4 | Download SDF | Storage of Stock Solutions |
|
|
| Synonyms | N/A | Smiles | CC(C)CC(C(CSC1=CC=CS1)C(=O)NO)C(=O)NC(CC2=CC=CC=C2)C(=O)NC | ||
|
In vitro |
DMSO
: 96 mg/mL
(200.98 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
| Targets/IC50/Ki |
MMP-1
3 nM
MMP-2
4 nM
MMP-9
4 nM
MMP-7
6 nM
MMP-3
20 nM
|
|---|---|
| In vitro |
Batimastat (BB-94) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3 with IC50 of 3 nM, 4 nM, 4 nM, 6 nM and 20 nM, respectively. This compound exhibits an unexpected binding geometry, with the thiophene ring deeply inserted into the primary specificity site. |
| Kinase Assay |
Enzyme assays
|
|
In enzyme assays, IC50s are determined for Batimastat (BB-94) in vitro against different metalloproteinases.
|
|
| In vivo |
Batimastat (BB-94) can inhibit metastatic spread and growth of B16-BL6 murine melanoma. In an orthotopic colon tumor model in mice, treatment with this compound results in inhibition of primary tumor growth (by 50%), local/regional spread (from 67% to 35%), and distant metastasis (from 30% to 10%). It reduces in vivo growth of experimental hemangiomas, most probably by blocking endothelial cell recruitment by the transformed cells or by interfering with cell organization in vascular structures. |
References |
|
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.