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> Laduviglusib [252917-06-9]

Laduviglusib [252917-06-9]

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Référence HY-10182-1ml

Conditionnement : 10mM/1mL

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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.

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Laduviglusib Chemical Structure

Laduviglusib Chemical Structure

CAS No. : 252917-06-9

This product is a controlled substance and not for sale in your territory.

Based on 147 publication(s) in Google Scholar

Other Forms of Laduviglusib:

  • Laduviglusib monohydrochloride In-stock
  • Laduviglusib trihydrochloride In-stock
  • Laduviglusib dihydrochloride Obtenir un devis

    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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    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.
    Masse moléculaire

    465.34

    Formule

    C22H18Cl2N8
    CAS No.

    252917-06-9
    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
    Livraison

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

    DMSO : 50 mg/mL (107.45 mM; ultrasonic and warming and heat to 60°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 2.1490 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.

    • Calculateur de molarité

    • Calculateur de dilution

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 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
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    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 +
    %
    Saline
    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.
    Pureté et documentation

    Purity: 99.76%

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

    Instruction de manipulation (2659 KB)
    Références

    • [1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.  [Content Brief]

      [2]. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.BMC Res Notes. 2014 Apr 29;7:273.  [Content Brief]

      [3]. Ye S, et al. Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embryonic stem cells from refractory mouse strains. PLoS One. 2012;7(4):e35892.  [Content Brief]

      [4]. Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004.  [Content Brief]

      [5]. Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566.  [Content Brief]

    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
    40 mM 0.0537 mL 0.2686 mL 0.5372 mL 1.3431 mL
    50 mM 0.0430 mL 0.2149 mL 0.4298 mL 1.0745 mL
    60 mM 0.0358 mL 0.1791 mL 0.3582 mL 0.8954 mL
    80 mM 0.0269 mL 0.1343 mL 0.2686 mL 0.6716 mL
    100 mM 0.0215 mL 0.1074 mL 0.2149 mL 0.5372 mL
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    Laduviglusib Related Classifications

    Help & FAQs

    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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