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

KY19382 (Synonyms: A3051)

Cat. No.: HY-131447
Handling Instructions

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.

For research use only. We do not sell to patients.

KY19382 Chemical Structure

KY19382 Chemical Structure

CAS No. : 2226664-93-1

Size Price Stock
5 mg USD 400 Ask For Quote & Lead Time
10 mg USD 680 Ask For Quote & Lead Time
50 mg USD 1900 Ask For Quote & Lead Time
100 mg USD 2900 Ask For Quote & Lead Time

* Please select Quantity before adding items.

Top Publications Citing Use of Products

View All GSK-3 Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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.
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.
Molecular Weight

360.19

Formula

C₁₇H₁₁Cl₂N₃O₂

CAS No.

2226664-93-1

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (13.88 mM; Need ultrasonic)

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
10 mM 0.2776 mL 1.3882 mL 2.7763 mL
*Please refer to the solubility information to select the appropriate solvent.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

KY19382A3051KY 19382KY-19382A 3051A-3051GSK-3Glycogen synthase kinase-3Glycogen synthase kinase 3Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
KY19382
Cat. No.:
HY-131447
Quantity:
MCE Japan Authorized Agent: