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

Laduviglusib dihydrochloride  (Synonyms: CHIR-99021 dihydrochloride; CT99021 dihydrochloride)

Cat. No.: HY-10182C
Handling Instructions Technical Support

Laduviglusib dihydrochloride (CHIR-99021 dihydrochloride; CT99021 dihydrochloride) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib dihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib dihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib dihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib dihydrochloride induces autophagy.

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

CAS No. : 2109414-84-6

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Laduviglusib dihydrochloride Related Antibodies

Top Publications Citing Use of Products

295 Publications Citing Use of MCE Laduviglusib dihydrochloride

IF
Bio/Physico-chemical Assay
WB
In Vivo Efficacy Study
RT-PCR
Histological Imaging/Staining
Cell Proliferation/Viability Assay

    Laduviglusib dihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 25;16(1):1774.  [Abstract]

    Viable cell numbers and PUFA-PC ratio after treatment with LY294002 (iPI3K, 10 µM), picropodophyllin (iRTK, 10 µM), ipatasertib (iAkt, 10 µM), or fatostatin (iSREBP1, 20 µM) for 48 h.

    Laduviglusib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cell Proteomics. 2025 May 12:100991.  [Abstract]

    Laduviglusib monohydrochloride (18 mg/kg; i.p.; every other day) significantly reduced the phosphorylation level of GSK3α in CCl4-induced hepatic fibrosis mice.

    Laduviglusib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cell Proteomics. 2025 May 12:100991.  [Abstract]

    Western blotting assay of collagen I expression in CCl4-induced hepatic fibrosis mice after treatment with GSK3α inhibitor Laduviglusib monohydrochloride (6-18 mg/kg; i.p.; every other day).

    Laduviglusib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cell Proteomics. 2025 May 12:100991.  [Abstract]

    GSK3α inhibitor Laduviglusib monohydrochloride (100 nM) significantly inhibited TGF-β-induced activation of HSCs and reduced COL1A1 production.

    Laduviglusib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cell Proteomics. 2025 May 12:100991.  [Abstract]

    GSK3α inhibitor Laduviglusib monohydrochloride (100 nM) diminished the expression levels of both αSMA and COL1A1 in mouse primary HSCs and LX-2 cell line.

    Laduviglusib dihydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cell Proteomics. 2025 May 12:100991.  [Abstract]

    Liver tissues from vehicle- or Laduviglusib monohydrochloride (6-18 mg/kg; i.p.; every other day) -treated fibrotic mice were stained with H&E, Sirius Red, and α-SMA, and quantitative results of Sirius Red and α-SMA staining were shown.

    Laduviglusib dihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Genet. 2024 Feb;56(2):294-305.  [Abstract]

    Trophoblast organoids constructed from hTSCs-BL. Trophoblast markers: CDH1 and hCG. Briefly, hTSCs were cultured in hTSCs medium (DMEM/F12 supplemented with 0.1 mM 2-mercaptoethanol, 0.2% FBS, 0.5% Penicillin–Streptomycin, 0.3% BSA, 1% ITS-X supplement, 1.5 μg/ml L-ascorbicacid, 50 ng/mL Epidermal Growth Factor (EGF)(MedChemExpress), 2 μM CHIR99021 (MedChemExpress), 0.5 μM A83-01 (MedChemExpress), 1 μM SB431542 (MedChemExpress), 0.8 mM Valproic acid and 5 μM Y27632 (MedChemExpress).

    Laduviglusib dihydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299.

    Schemes of generating Fsp1-Cre:R26R-loxp-tdTomato mice and drug treatment to induce in situ transdifferentiation. Fsp1-Cre mice were crossed with R26Rloxp-tdTomato mice in which the expression of tdTomato is prevented by a loxP-flanked STOP cassette. The F1 mice would have the red fluorescent protein tdTomato expressed specifically in the fibroblasts. CRFVPTM were given once a week for 6 weeks. Immunofluorescence staining of the cryosections of the hearts from Fsp1-Cre:R26R-loxp-tdTomato mice treated with vehicle (b) or CRFVPTM (c) for 6 weeks. C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age.

    Laduviglusib dihydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299.

    Whole-heart imaging with light-sheet fluorescence microscopy after tissue clearing of the hearts from Fsp1-Cre:R26R-loxp-tdTomato mice treated with vehicle (a) or CRFVPTM (b). (C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age).

    Laduviglusib dihydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299.

    a Schemes of obtaining PDGFRα-DreER:R26R-rox-tdTomato mice and drug treatment to induce in situ cardiac reprogramming in PDGFRα-DreER:R26R-roxtdTomato mice. PDGFRα-DreER mice were mated with R26R-rox-tdTomato mice in which the expression of tdTomato is prevented by a roxflanked STOP cassette. The expression of tdTomato in fibroblasts was turned on by tamoxifen treatment. CRFVPTM were given once a week for 6 weeks. b Body weigh change of the mice after chemical treatment. Immunofluorescence staining of the cryosections of the hearts from PDGFRα-DreER:R26R-rox-tdTomato mice treated with vehicle (c) or CRFVPTM (d) for 6 weeks. (C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age).

    Laduviglusib dihydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299.

    Immunofluorescence staining of α-actinin in cryosections of hearts from Fsp1-Cre:R26R-loxp-tdTomato mice treated with 7 C cocktail (CRFVPTM) or cocktails by removing 1 compound from 7 C (7C-X) for 6 weeks in vivo with Fsp1-Cre:R26R-loxp-tdTomato mice. (C: CHIR99021, 14 mg/kg; R: RepSox, 8.6 mg/kg; F: Forskolin, 61.6 mg/kg; V: VPA, 250 mg/kg; T: TTNPB, 1 mg/kg and M: Rolipram, 2.5 mg/kg; P: Parnate, 2.7 mg/kg, CRFTM by oral gavage and VP by intraperitoneal injection once a week for 6 weeks in mice at about 8 weeks of age).

    Laduviglusib dihydrochloride 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 dihydrochloride 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 dihydrochloride purchased from MedChemExpress. Usage Cited in: Chemosphere. 2019 Feb: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 dihydrochloride purchased from MedChemExpress. Usage Cited in: Chemosphere. 2019 Feb: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 dihydrochloride purchased from MedChemExpress. Usage Cited in: Chemosphere. 2019 Feb: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 dihydrochloride purchased from MedChemExpress. Usage Cited in: Chemosphere. 2019 Feb: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 dihydrochloride purchased from MedChemExpress. Usage Cited in: Toxicology. 2016 Apr 29:355-356:31-8.  [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 dihydrochloride (CHIR-99021 dihydrochloride; CT99021 dihydrochloride) is a potent, selective and orally active GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib dihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib dihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib dihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib dihydrochloride induces autophagy[1][2][3].

    IC50 & Target

    IC50: 10 nM/6.7 nM (GSK-3α/β)[1]
    In Vitro

    Laduviglusib dihydrochloride (1-10 μM, 3 days) reduces the viability of the ES-D3 cells with an IC50 of 4.9 μM[2].
    Laduviglusib dihydrochloride (5 μM, 48 h) activates the canonical Wnt-pathway in ES-D3 cells and ES-CCE cells[2].
    Laduviglusib dihydrochloride (3 μM, 4 days) inhibits ES cell differentiation into neural cells[3].
    Laduviglusib dihydrochloride (1 μM, 2 weeks) inhibits adipogenesis by blocking induction of C/EBPα and PPARγ in 3T3-L1 preadipocytes[4].
    Laduviglusib dihydrochloride (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 dihydrochloride 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 dihydrochloride (30 mg/kg, p.o ) rapidly lowers plasma glucose[1].
    Laduviglusib dihydrochloride (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

    538.26

    Formula

    C22H20Cl4N8
    CAS No.
    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    Laduviglusib dihydrochloride Related Classifications

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    • 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:

    Laduviglusib2109414-84-6CHIR-99021CT99021CHIR99021CHIR 99021CT 99021CT-99021WntGSK-3β-cateninAutophagyOrganoidGlycogen synthase kinase-3Glycogen synthase kinase 3Beta cateninGMPWnt/β-cateninES cellES-D3 celladipogenesisGI injuryInhibitorinhibitorinhibit

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