1. PI3K/Akt/mTOR Stem Cell/Wnt
  2. GSK-3 Wnt β-catenin
  3. KY19382

KY19382  (Synonyms: A3051)

目录号: HY-131447 纯度: ≥98.0%
COA 产品使用指南

KY19382 是一种有效的和具有口服活性的 CXXC5-DVLGSK3β 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。

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KY19382 Chemical Structure

KY19382 Chemical Structure

CAS No. : 2226664-93-1

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规格 价格 是否有货 数量
1 mg ¥1047
In-stock
5 mg ¥2475
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10 mg ¥4475
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25 mg ¥6800
In-stock
50 mg ¥9500
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100 mg
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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

查看 GSK-3 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s 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[1][2].

IC50 & Target[1]

CXXC5-DVL

19 nM (IC50)

GSK3β

10 nM (IC50)

体外研究
(In Vitro)

KY19382 (0.01 and 0.1 μM; 48 h) promotes ATDC5 cells proliferation[1].
KY19382 (0.1 μM; 3 d) up-regulates the mRNA levels of chondrogenic differentiation markers in ATDC5 and C28/I2 cells[1].
KY19382 (0.01 and 0.1 μM; 24 h) inactivates GSK3α/β in ATDC5 cells[1].
KY19382 (0.1 μM; 4 h) interrupts the CXXC5-DVL interaction in ATDC5 cells[1].
KY19382 (0.001-10 μM; 18 h) enhances the TOPFlash activity in HEK293 reporter cells[1].
KY19382 (0.1 μM; 48 h) elevates nuclear translocation of β-catenin in ATDC5 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: ATDC5 cells
Concentration: 0, 0.01, 0.1 μM
Incubation Time: 48 hours
Result: Enhanced the number of BrdU-positive ATDC5 cells.

Cell Proliferation Assay[1]

Cell Line: ATDC5 cells
Concentration: 0, 0.01, 0.1 μM
Incubation Time: 24 hours
Result: Increased the level of β-catenin in a dose-dependent manner.
体内研究
(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[1].
KY19382 (0.1 mg/kg; i.p. once daily for 10 weeks) significantly increases the length of tibiae in mice[1].
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[1].
KY19382 (A3051) (25 mg/kg; p.o. once daily for 16 weeks) shows reduction in adipocyte size and anti-inflammatory effects[2].
A3051 (25 mg/kg; p.o. once daily for 5 days) reduces fasting glucose in mice[2].
A3051 (25 mg/kg; p.o. once daily for 3 weeks) reduces the hepatosteatosis in mice[2].

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

Animal Model: C57BL/6 male mice (7-weeks-old or 3-weeks-old)[1]
Dosage: 0.1 mg/kg
Administration: I.p. once daily for 2 weeks
Result: Increased nuclear β-catenin in the growth plate chondrocytes dramatically.
Elevated the height of each growth plate zone and BrdU-positive cells.
Did not affect the cartilage resorption of rapidly growing young mice.
Animal Model: SD male rats[1]
Dosage: 1 mg/kg for i.v. and 5 mg/kg for i.p. (Pharmacokinetic Analysis)
Administration: I.v. and i.p. administration
Result: I.v.: t1/2=3.33 h; AUC=7832.81 ng∙h/mL; CL=0.12 L/h/kg.
I.p.: t1/2=16.20 h; F=16.74%; Cmax=463.37 ng/mL.
分子量

360.19

Formula

C17H11Cl2N3O2

CAS 号
性状

固体

颜色

Brown to reddish brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 4.17 mg/mL (11.58 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7763 mL 13.8816 mL 27.7631 mL
5 mM 0.5553 mL 2.7763 mL 5.5526 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥98.0%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7763 mL 13.8816 mL 27.7631 mL 69.4078 mL
5 mM 0.5553 mL 2.7763 mL 5.5526 mL 13.8816 mL
10 mM 0.2776 mL 1.3882 mL 2.7763 mL 6.9408 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
KY19382
目录号:
HY-131447
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