Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
TAS-301 Chemical Structure
|Product name: TAS-301|
|Cat. No.: HY-18965|
TAS-301 is an inhibitor of smooth muscle cell migration and proliferation, inhibits intimal thickening after balloon injury to rat carotid arteries
in vitro: TAS-301 displays a much more potent effect on neointimal formation than tranilast in the rat balloon injury model in terms of dosage and maximum efficiency and propose a possible mechanism of TAS-301 action based on the results of experiments on the migration and proliferation of vascular SMCs. TAS-301 inhibits the migration of smooth muscle cells (SMCs) stimulated by platelet-derived growth factor-BB, insulin-like growth factor-1 or heparin-binding epidermal growth factor-like growth factor. TAS-301 reduces the proliferation of medial and intimal SMCs at 4 and 8 days, respectively, after the injury. TAS-301 inhibits basic fibroblast growth factor-induced proliferation of SMCs dose dependently. TAS-301 shows a higher inhibitory potency on intimal formation than tranilast due to inhibition of both migration of medial SMCs and proliferation of medial and intimal SMCs.
in vivo: TAS-301 is known to block intimal thickening post balloon injury in rat carotid arteries. It inhibits intimal thickening by blocking Ca2+/calmodulin-dependent protein kinase II (CaM kinase II) and cytoskeletal depolymerization. TAS 301 can also inhibit receptor-regulated influx of calcium in rat vascular smooth muscle cells (VSMCs). Inhibitor of smooth muscle cell migration and proliferation. Blocks voltage-independent calcium influx and downstream PKC signaling. Inhibits neointimal thickening after balloon catheter injury to the rat common carotid artery.
|M.Wt||357.4||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
|1 mg||5 mg||10 mg|
|1 mM||2.7980 mL||13.9899 mL||27.9799 mL|
|5 mM||0.5596 mL||2.7980 mL||5.5960 mL|
|10 mM||0.2798 mL||1.3990 mL||2.7980 mL|
(-)-Indolactam V (ILV) is a protein kinase C activator, which strongly directs human ES cell-derived definitive endoderm into pancreatic endoderm.
CGP60474 is a promising inhibitor of PKC with a high degree of selectivity versus other serine/threonine and tyrosine kinases and show competitive kinetics relative to ATP.
Chelerythrine is potent, cell-permeable inhibitor of protein kinase C (IC50 = 660 nM); competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.
Enzastaurin (LY317615) is a potent PKC(beta) selective inhibitor with IC50 of 6 nM, 6- to 20-fold selectivity against PKC(alpha), PKC(gamma) and PKC(epsilon).
Go 6983 is a pan-PKC inhibitor against for PKC(alpha), PKC(beta), PKC(gamma) and PKC(delta) with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKC(zeta) and inactive to PKC(mu).
PKC-IN-1 is a poent PKC beta II inhibitor with Ki of 14.9 nM; compound example H6 from patent WO 2008096260 A1.
PKC412(Midostaurin; CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor; inhibits conventional PKC isoforms ((alpha), (beta), (gamma)), PDFR(beta), VEGFR2, Syk, PKC(eta), Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR.
Sotrastaurin(AEB-071) is a potent and selective pan-PKC inhibitor, mostly for PKC(theta) with Ki of 0.22 nM; inactive to PKC(zeta).
Staurosporine is a prototypical potent ATP-competitive kinase inhibitor with IC50 of 0.7, 7, 8.5, 6, 20 nM for PKC, PKA,PKG, p60v-src tyrosine protein kinase, CaM kinase II, respectively.