KY19382 is a potent dual inhibitor of CXXC5-DVL and GSK3β, exhibiting IC50s of 19 and 10 nM, respectively. It activates Wnt/β-catenin signaling by inhibiting both the CXXC5-DVL interaction and GSK3β activity. KY19382 is suitable for investigating high fat diet (HFD)-induced metabolic diseases[1][2].
体内研究
KY19382 (0.1 mg/kg; i.p. once daily for 2 weeks) delays growth plate senescence in older mice and promotes growth plate maturation in rapidly growing young mice.
KY19382 (0.1 mg/kg; i.p. once daily for 10 weeks) induces a significant increase in the length of tibiae in mice[1].
KY19382 (5 mg/kg; i.p.) exhibits a relatively favorable bioavailability (F=16.74%), with a half-life of 16.20 h and an exposure level of 6,555.79 ng•h/ml[1].
KY19382 (A3051) (25 mg/kg; pO. once daily for 16 weeks) demonstrates a decrease in adipocyte size and exhibits anti-inflammatory effects[2].
A3051 (25 mg/kg; pO. once daily for 5 days) lowers fasting glucose levels in mice[2].
A3051 (25 mg/kg; pO. once daily for 3 weeks) decreases hepatosteatosis in mice[2].
体外研究
KY19382 (0.01 and 0.1 μM; 48 h) enhances proliferation of ATDC5 cells[1].
KY19382 (0.1 μM; 3 d) increases mRNA expression of chondrogenic differentiation markers in ATDC5 and C28/I2 cells[1].
KY19382 (0.01 and 0.1 μM; 24 h) inhibits GSK3α/β activity in ATDC5 cells[1].
KY19382 (0.1 μM; 4 h) disrupts the CXXC5-DVL interaction in ATDC5 cells[1].
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