LEQ506 是第二代 smoothened (smo) 抑制剂，在人类和小鼠中的 IC₅₀ 值分别为 2 和 4 nM。

LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC 50 s of 2 and 4 nM in human and mouse, respectively.

Solid

IC50: 2 nM (human smo), 4 nM (mouse smo)

LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively. LEQ506 inhibits Hedgehog (Hh) signaling in a human cell line (HEPM) as measured by the amount of Gli mRNA with an IC50 ~6-fold lower than that of Compound 2. LEQ506 is an efficacious compound by consistently decreasing Gli1 mRNA by about 70 to 80%. LEQ506 shows a tendency to preferentially inhibit Gli1 rather than Ptch1 mRNA. LEQ506 (at 1%) is also an efficacious compound with an inhibition of 80 to 90% for Gli1 and of 60 to 70% for Ptch1. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Peukert S, et al. Discovery of NVP-LEQ506, a second-generation inhibitor of smoothened. ChemMedChem. 2013 Aug;8(8):1261-5.
[2]. Lauressergues E, et al. Pharmacological evaluation of a series of smoothened antagonists in signaling pathways and after topical application in a depilated mouse model. Pharmacol Res Perspect. 2016 Mar 4;4(2):e00214.

In Vitro: DMSO : ≥ 100 mg/mL (231.18 mM)配制储备液