TH-257 |
| Catalog No.GC38860 |
TH-257 es un potente inhibidor de LIMK1 y LIMK2 con valores IC50 de 84 nM y 39 nM para LIMK1 y LIMK2, respectivamente, y puede usarse como sonda quÍmica para LIMK1 y LIMK2. TH-257 es un inhibidor alostérico que se dirige a un bolsillo de uniÓn inducido por una conformaciÓn de salida de αC y DFG. TH257 es exquisitamente selectivo y no se ha observado actividad significativa contra el kinoma mÁs amplio en el ensayo KINOMEscan a 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.
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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.)
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