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
Warning
Toxicity: Irritant (B)
Physical form
A 10 mM (500 µg/100 µl) solution of TAPI-1 (Cat. No. 579051) in DMSO.
Reconstitution
Following initial thaw, aliquot and freeze (-20°C).
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 499.60. Empirical Formula: C26H37N5O5. Quality Level: 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. Storage Class Code: 10 - Combustible liquids. WGK: WGK 1. Flash Point(F): 188.6 °F - (Dimethylsulfoxide). Flash Point(C): 87 °C - (Dimethylsulfoxide).- UPC:
- 41141713
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 579053-500UG