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

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.

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KY19382 Chemical Structure

KY19382 Chemical Structure

CAS No. : 2226664-93-1

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5 mg USD 275 En stock
10 mg USD 495 En stock
25 mg USD 935 En stock
50 mg USD 1485 En stock
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Based on 1 publication(s) in Google Scholar

KY19382 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE KY19382

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Description

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)

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].

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

KY19382 Related Antibodies

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.
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].

MedChemExpress (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.
Masse moléculaire

360.19

Formule

C17H11Cl2N3O2
CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C1NC2=C(C=C(Cl)C(Cl)=C2)/C1=C3NC4=C(C=CC=C4)C/3=N/OC
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : 4.17 mg/mL (11.58 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Pureté et documentation

Purity: ≥98.0%

COA (261 KB) HNMR (256 KB)

Instruction de manipulation (2659 KB)
Références

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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KY19382 Related Classifications

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.

Keywords:

KY193822226664-93-1A3051KY 19382KY-19382A 3051A-3051GSK-3Wntβ-cateninGlycogen synthase kinase-3Glycogen synthase kinase 3Beta cateninInhibitorinhibitorinhibit

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