TH-257 |
| Catalog No.GC38860 |
TH-257 est un puissant inhibiteur de LIMK1 et LIMK2 avec des valeurs IC50 de 84 nM et 39 nM pour LIMK1 et LIMK2, respectivement, et il peut être utilisé comme sonde chimique pour LIMK1 et LIMK2. Le TH-257 est un inhibiteur allostérique ciblant une poche de liaison induite par une conformation αC et DFG-out. TH257 est extrêmement sélectif et aucune activité significative contre le kinome plus large n'a été observée dans le test KINOMEscan À 1 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2244678-29-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM[1].
[1]. Manetti F. Recent advances in the rational design and development of LIM kinase inhibitors are not enough to enter clinical trials. Eur J Med Chem. 2018 Jul 15;155:445-458.
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *