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KY19382

CAS No. : 2226664-93-1

MCE 站：KY19382

产品活性：KY19382 是一种有效的和具有口服活性的 CXXC5-DVL 和 GSK3β 的双重抑制剂，IC₅₀ 值分别为 19 和 10 nM。KY19382 通过对 CXXC5-DVL 相互作用和 GSK3β 活性的抑制作用激活 Wnt/β-catenin 信号传导。KY19382 可用于高脂饮食 (HFD) 诱发的代谢性疾病的研究。

研究领域：PI3K/Akt/mTOR  |  Stem Cell/Wnt

作用靶点：GSK-3

In Vitro: KY19382 (0.01 and 0.1 μM; 48 h) promotes ATDC5 cells proliferation.
KY19382 (0.1 μM; 3 d) up-regulates the mRNA levels of chondrogenic differentiation markers in ATDC5 and C28/I2 cells.
KY19382 (0.01 and 0.1 μM; 24 h) inactivates GSK3α/β in ATDC5 cells.
KY19382 (0.1 μM; 4 h) interrupts the CXXC5-DVL interaction in ATDC5 cells.
KY19382 (0.001-10 μM; 18 h) enhances the TOPFlash activity in HEK293 reporter cells.
KY19382 (0.1 μM; 48 h) elevates nuclear translocation of β-catenin in ATDC5 cells.

In Vivo: 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) significantly increases the length of tibiae in mice.
KY19382 (5 mg/kg; i.p.) displays a relatively favorable bioavailability (F=16.74%), showing half-life of 16.20 h and an exposure level of 6,555.79 ng?h/ml.
KY19382 (A3051) (25 mg/kg; p.o. once daily for 16 weeks) shows reduction in adipocyte size and anti-inflammatory effects.
A3051 (25 mg/kg; p.o. once daily for 5 days) reduces fasting glucose in mice.
A3051 (25 mg/kg; p.o. once daily for 3 weeks) reduces the hepatosteatosis in mice.

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