| 中文名称: | KY19382 | ||||
|---|---|---|---|---|---|
| 英文名称: | KY19382 | ||||
| 别名: | 2H-Indol-2-one,5,6-dichloro-3-[1,3-dihydro-3-(methoxyimino)-2H-indol-2-ylidene]-1,3-dihydro- | ||||
| CAS No: | 2226664-93-1 | 分子式: | C17H11Cl2N3O2 | 分子量: | 360.19 |
| CAS No: | 2226664-93-1 | ||||
| 分子式: | C17H11Cl2N3O2 | ||||
| 分子量: | 360.19 | ||||
包装规格：
1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：
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。
溶解性：
溶于DMSO （5 mg/mL）
储备液保存：
-80°C, 6 months
-20°C, 1 month
-20°C, 1 month
靶点：
CXXC5-DVL：19 nM (IC50)
GSK3β：10 nM (IC50)
GSK3β：10 nM (IC50)
体外研究：
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.
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.
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) 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.
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.
保存条件：
-20°C
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
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参考文献 & 客户发表文献
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质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
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开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
