An inhibitor of Ca2+ mobilization and CaM kinase II
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TAS 301

Item No. 14976

Technical Information
Formal Name
3-[bis(4-methoxyphenyl)methylene]-1,3-dihydro-2H-indol-2-one
CAS Number
193620-69-8
Molecular Formula
C23H19NO3
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 20 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: 0.33 mg/ml
λmax
253, 358 nm
SMILES
COC(C=C1)=CC=C1/C(C2=CC=C(OC)C=C2)=C3C(C=CC=C4)=C4NC\3=O
InChi Code
InChI=1S/C23H19NO3/c1-26-17-11-7-15(8-12-17)21(16-9-13-18(27-2)14-10-16)22-19-5-3-4-6-20(19)24-23(22)25/h3-14H,1-2H3,(H,24,25)
InChi Key
KUEYYIJXBRWZIB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    TAS 301 (10 μM) impedes Ca2+ mobilization and Ca2+/calmodulin-dependent protein kinase II (CaM kinase II) activation that inhibits vascular smooth muscle cell (VSMC) proliferation in vitro.1,2 At a concentration of 10 μM, TAS 301 also inhibits platelet-derived growth factor (PDGF)-induced tyrosine phosphorylation of focal adhesion kinase and paxillin and promotes cytoskeletal rearrangment.1 TAS 301 (3-100 mg/kg) inhibits migration and proliferation of VSMCs and prevents arterial intimal thickening in vivo in a model of balloon-injured arteries in rats.3 In a micro pig model, TAS 301 administration (30-100 mg/kg) prevents coronary artery stenosis after balloon overstretch injury.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sasaki, E., Miyoshi, K., Nozawa, Y., et alTas-301, a new synthetic inhibitor of neointimal thickening after balloon injury, inhibits calcium-dependent signal transduction and cytoskeletal reorganization. Pharmacology 63(1), 17-27 (2001).

    2. Sasaki, E., Nozawa, Y., Miyoshi, K., et alTAS-301 blocks receptor-operated calcium influx and inhibits rat vascular smooth muscle cell proliferation induced by basic fibroblast growth factor and platelet-derived growth factor. Jpn. J. Pharmacol. 84(3), 252-258 (2000).

    3. Muranaka, Y., Yamasaki, Y., Nozawa, Y., et alTAS-301, an inhibitor of smooth muscle cell migration and proliferation, inhibits intimal thickening after balloon injury to rat carotid arteries. J. Pharmacol. Exp. Ther. 285(3), 1280-1286 (1998).

    4. Sasaki, E., Tanahashi, Y., Yamasaki, Y., et alInhibitory effect of TAS-301, a new synthesized constrictive remodeling regulator, on renarrowing after balloon overstretch injury of porcine coronary artery. J. Pharmacol. Exp. Ther. 295(3), 1043-1050 (2000).