General description
A structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-α convertase; ADAM17). However, TAPI-1 is more stable in serum than TAPI-0. TAPI-1 Blocks the shedding of several cell surface proteins such as TNF-α, IL-6 receptor, and p60 and p80 TNF receptors. Inhibits constitutive (IC50 = 8.09 μM) and muscarinic receptor-stimulated (IC50 = 3.61 μM) sAPPa release in HEK-293 cells expressing muscarinic receptors. Also blocks the TACE-dependent constitutive release of co-transfected APP(695) (IC50 = 920 nM).
Biochem/physiol Actions
Cell permeable: no
Primary Target
MMPs and TACE
Product does not compete with ATP.
Reversible: no
Target IC50: 8.09 µM, 3.61 µM in blocking constitutive and muscarinic receptor-stimulated sAAPα release in HEK 293 cells expressing M3 muscarinic receptors
Packaging
Packaged under inert gas
Physical form
A 10 mM (500 µg/100 µl) solution of TAPI-1 (Cat. No. 579051) in DMSO.
Preparation Note
Following initial thaw, aliquot and freeze (-20°C).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
| Quality Segment | 100 |
| assay | ≥97% (HPLC) |
| form | liquid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,desiccated (hygroscopic),protect from light |
| shipped in | wet ice |
| storage temp. | −20°C |
