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Laduviglusib

(Synonyms: CHIR-99021; CT99021)
298 Cited Publications
고객리뷰

Based on 298 publication(s) in Google Scholar

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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  • Purity: 99.46%
  • CAS No.: 252917-06-9
  • 화학식: C22H18Cl2N8
  • 분자량:465.34
  • 보관:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 1 year , -20°C, 6 months
  • Laduviglusib Chemical Structure
    Laduviglusib Chemical Structure
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
  • Experimental Validation Results for Laduviglusib
CAS No.: 252917-06-9
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  • Laduviglusib Chemical Structure
    Laduviglusib Chemical Structure
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  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

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

  • 1/16

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

    Customer Validation
     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).

  • 1/16

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

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

  • 1/16

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

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

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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).

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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).

  • 1/16

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

    Customer Validation
     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).

  • 1/16

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

    Customer Validation
     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).

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

    Laduviglusib purchased from MedChemExpress. Usage Cited in: Chemosphere. 2019 Feb:216:372-378. [Abstract]

    Customer Validation
     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.

  • 1/16

    Laduviglusib purchased from MedChemExpress. Usage Cited in: Chemosphere. 2019 Feb:216:372-378. [Abstract]

    Customer Validation
     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.

  • 1/16

    Laduviglusib purchased from MedChemExpress. Usage Cited in: Chemosphere. 2019 Feb:216:372-378. [Abstract]

    Customer Validation
     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.

  • 1/16

    Laduviglusib purchased from MedChemExpress. Usage Cited in: Chemosphere. 2019 Feb:216:372-378. [Abstract]

    Customer Validation
     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.

  • 1/16

    Laduviglusib purchased from MedChemExpress. Usage Cited in: Toxicology. 2016 Apr 29:355-356:31-8. [Abstract]

    Customer Validation
     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.

  • Laduviglusib