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LEQ506 (NVP-LEQ506) (Synonyms: NVP-LEQ506)

Katalog-Nr.GC32954

LEQ506 (NVP-LEQ506) ist ein Inhibitor der zweiten Generation von Smoothened (Smo) mit IC50-Werten von 2 bzw. 4 nM bei Mensch und Maus.

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LEQ506 (NVP-LEQ506) Chemische Struktur

Cas No.: 1204975-42-7

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively.

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[1]. 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[2].

[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.

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