2. PI3K/Akt/mTOR Stem Cell/Wnt Autophagy
  3. Organoid GSK-3 Wnt β-catenin Autophagy
  4. Laduviglusib

Laduviglusib  (Synonyms: CHIR-99021; CT99021)

Cat. No.: HY-10182 Purity: 99.71%
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CHIR-99021 (CT99021) est un inhibiteur puissant et sélectif de GSK-3α/β avec des IC50 de 10 nM et 6,7 nM. CHIR-99021 montre une sélectivité> 500 fois pour GSK-3 sur CDC2, ERK2 et d'autres protéines kinases. CHIR-99021 est également un activateur puissant de la voie de signalisation Wnt/β-caténine. CHIR-99021 améliore l'auto-renouvellement des cellules souches embryonnaires humaines et murines. CHIR-99021 induit l'autophagie.

CHIR-99021 (CT99021) ist ein potenter und selektiver GSK-3α/β-Inhibitor mit IC50s von 10 nM und 6,7 nM. CHIR-99021 zeigt eine >500-fache Selektivität für GSK-3 gegenüber CDC2, ERK2 und anderen Proteinkinasen. CHIR-99021 ist auch ein potenter Aktivator des Wnt/β-Catenin-Signalweges. CHIR-99021 verstärkt die Selbsterneuerung von embryonalen Stammzellen der Maus und des Menschen. CHIR-99021 induziert Autophagie.

Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy.

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

Laduviglusib Chemical Structure

Laduviglusib Chemical Structure

CAS No. : 252917-06-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 79 In-stock
Solution
10 mM * 1 mL in DMSO USD 79 In-stock
Solid
1 mg USD 29 In-stock
5 mg USD 72 In-stock
10 mg USD 108 In-stock
50 mg USD 324 In-stock
100 mg USD 516 In-stock
200 mg USD 880 In-stock
500 mg   Get quote  
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Based on 169 publication(s) in Google Scholar

Other Forms of Laduviglusib:

Laduviglusib Related Antibodies

Top Publications Citing Use of Products

163 Publications Citing Use of MCE Laduviglusib

RT-PCR
IF
WB

    Laduviglusib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287.  [Abstract]

    Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with the indicative different small molecules for 1 h and then treated with CHIR for 24 h.

    Laduviglusib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287.  [Abstract]

    Western blot analysis of Tcf7l1 protein levels in mESCs pre-treated with D4476 or DMAT and then treated with CHIR or PD03 for 24 h.

    Laduviglusib purchased from MedChemExpress. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378.  [Abstract]

    AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. mRNA expression changes of β-catenin by Q-PCR. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

    Laduviglusib purchased from MedChemExpress. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378.  [Abstract]

    AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. Percentage of cTnT positive cells at differentiation day 14. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

    Laduviglusib purchased from MedChemExpress. Usage Cited in: Chemosphere. 2018 Oct 23;216:372-378.  [Abstract]

    AhR mediates EOM-inhibited cardiac differentiation by downregulating β-catenin expression in P19 cells. Percentage of cTnT positive cells at differentiation day 14. The concentrations of CH (CH223191, AhR antagonist) and CHIR (CHIR99021, Wnt activator) are 0.25 and 0.5 μM respectively.

    Laduviglusib purchased from MedChemExpress. Usage Cited in: Toxicology. 2016 May 20;355-356:31-38.  [Abstract]

    Western analysis of β-catenin protein level in zebrafish embryos exposed to EOM in the presence or absence of CH/CHIR (n = 3). Different letters indicate significant differences. Moreover, both CH and CHIR attenuate the EOM-induced changes in the protein level of b-catenin and in EROD activity.

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    GSK-3 GSK-3α GSK-3β

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    Description

    Laduviglusib (CHIR-99021) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib enhances mouse and human embryonic stem cells self-renewal. Laduviglusib induces autophagy[1][2][3].

    IC50 & Target[1]

    GSK-3β

    6.7 nM (IC50)

    GSK-3α

    10 nM (IC50)

    cdc2

    8800 nM (IC50)

    In Vitro

    Laduviglusib (1-10 μM, 3 days) reduces the viability of the ES-D3 cells with an IC50 of 4.9 μM[2].
    Laduviglusib (5 μM, 48 h) activates the canonical Wnt-pathway in ES-D3 cells and ES-CCE cells[2].
    Laduviglusib (3 μM, 4 days) inhibits ES cell differentiation into neural cells[3].
    Laduviglusib (1 μM, 2 weeks) inhibits adipogenesis by blocking induction of C/EBPα and PPARγ in 3T3-L1 preadipocytes[4].
    Laduviglusib (2.5 μM, 24 h) protects Lgr5+ cells against radiation-induced apoptosis[5].

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

    Laduviglusib Related Antibodies

    Cell Viability Assay[2]

    Cell Line: ES-D3 cells
    Concentration: 1-10 μM
    Incubation Time: 3 days
    Result: Reduced the viability of the ES-D3 cells by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM
    In Vivo

    Laduviglusib (30 mg/kg, p.o ) rapidly lowers plasma glucose[1].
    Laduviglusib (2 mg/kg, i.p.) protects mice against radiation-induced lethal GI injury[5].

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

    Animal Model: ZDF rats[1]
    Dosage: 30 mg/kg
    Administration: Oral administration
    Result: Lowered plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration.
    Animal Model: WT C57BL/6 mice[5]
    Dosage: 2 mg/kg
    Administration: Intraperitoneal injection (i.p.)
    Result: Blocked crypt apoptosis and increased Lgr5+ cell survival.
    Molecular Weight

    465.34

    Formula

    C22H18Cl2N8
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light brown

    SMILES

    N#CC1=CC=C(N=C1)NCCNC2=NC=C(C(C3=CC=C(Cl)C=C3Cl)=N2)C4=NC=C(N4)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 16.67 mg/mL (35.82 mM; Need ultrasonic; 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 2.1490 mL 10.7448 mL 21.4897 mL
    5 mM 0.4298 mL 2.1490 mL 4.2979 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 5 mg/mL (10.74 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  20% SBE-β-CD in Saline adjusted to pH 4-4.5 with 1 N Acetic

      Solubility: 5 mg/mL (10.74 mM); Clear solution; Need ultrasonic

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

    Dosage

    mg/kg

    Animal weight
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    g

    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.76%

    COA (248 KB) HNMR (194 KB) LCMS (343 KB) Elemental Analysis Report (105 KB)

    Handling Instructions (2659 KB)
    References

    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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1490 mL 10.7448 mL 21.4897 mL 53.7242 mL
    5 mM 0.4298 mL 2.1490 mL 4.2979 mL 10.7448 mL
    10 mM 0.2149 mL 1.0745 mL 2.1490 mL 5.3724 mL
    15 mM 0.1433 mL 0.7163 mL 1.4326 mL 3.5816 mL
    20 mM 0.1074 mL 0.5372 mL 1.0745 mL 2.6862 mL
    25 mM 0.0860 mL 0.4298 mL 0.8596 mL 2.1490 mL
    30 mM 0.0716 mL 0.3582 mL 0.7163 mL 1.7908 mL
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    Laduviglusib 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:

    Laduviglusib252917-06-9CHIR-99021 CT99021CHIR99021CHIR 99021CT99021CT 99021CT-99021OrganoidGSK-3Wntβ-cateninAutophagyGlycogen synthase kinase-3Glycogen synthase kinase 3Beta cateninGMPWnt/β-cateninES cellES-D3 celladipogenesisGI injuryInhibitorinhibitorinhibit

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