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。

KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC 50 s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.

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CXXC5-DVL 19 nM (IC50) GSK3β 10 nM (IC

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. 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]. Choi S, et, al. CXXC5 mediates growth plate senescence and is a target for enhancement of longitudinal bone growth. Life Sci Alliance. 2019 Apr 10; 2(2): e201800254.
[2]. Choi KY, et, al. Compositions and methods for suppressing and/or treating metabolic diseases and/or a clinical condition thereof. WO2020079569.

In Vitro: DMSO : 5 mg/mL (13.88 mM; Need ultrasonic)配制储备液