Laduviglusib
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.
For research use only. We do not sell to patients.
- Purity: 99.46%
- CAS No.: 252917-06-9
- Formula: C22H18Cl2N8
- Molecular Weight:465.34
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) Laduviglusib
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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WB
-
IF
-
WB
Biological Activity
|
GSK-3β 6.7 nM (IC50) |
GSK-3α 10 nM (IC50) |
cdc2 8800 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.13 μM
Compound: 1
|
Inhibition of GSK3 in CHO cells expressing insulin receptor assessed as activation of glycogen synthase measured after 30 mins in presence of glucose-6-phosphate by filter paper assay
Inhibition of GSK3 in CHO cells expressing insulin receptor assessed as activation of glycogen synthase measured after 30 mins in presence of glucose-6-phosphate by filter paper assay
|
[PMID: 31926786] |
| HepG2 | EC50 |
1.5 μM
Compound: 1, CHIR-99021
|
Inhibition of GSK3-beta in human HepG2 cells assessed as incorporation of [3H]glucose into glycogen after 3 hrs by liquid scintillation counting
Inhibition of GSK3-beta in human HepG2 cells assessed as incorporation of [3H]glucose into glycogen after 3 hrs by liquid scintillation counting
|
[PMID: 22261023] |
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.
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Cell Line:ES-D3 cells
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Concentration:1-10 μM
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Incubation Time:3 days
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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
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.
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Animal Model:ZDF rats[1]
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Dosage:30 mg/kg
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Administration:Oral administration
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Result:Lowered plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration.
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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.
Chemical Information
-
CAS No. 252917-06-9
-
Appearance Solid
-
Molecular Weight 465.34
-
Formula C22H18Cl2N8
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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
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Synonyms
CHIR-99021; CT99021
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (298)
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Journal Impact Factor
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Most Recent
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Nat Med
Human induced pluripotent stem cell-derived cardiomyocytes recapitulate the predilection of breast cancer patients to doxorubicin-induced cardiotoxicity. [Abstract]2016 May;22(5):547-56. PMID: 27089514 -
Cell
2024 Nov 14;187(23):6566-6583.e22. PMID: 39332412 -
Mol Cancer
Organoids derived from patients provide a new opportunity for research and individualized treatment of malignant peritoneal mesothelioma. [Abstract]2024 Jan 10;23(1):12. PMID: 38200517 -
Cell Metab
Nicotinamide metabolism face-off between macrophages and fibroblasts manipulates the microenvironment in gastric cancer. [Abstract]2024 Jun 18:S1550-4131(24)00189-X. PMID: 38897198 -
Nat Genet
Single-nucleus multi-omic profiling of human placental syncytiotrophoblasts identifies cellular trajectories during pregnancy. [Abstract]2024 Feb;56(2):294-305. PMID: 38267607
Laduviglusib 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).
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Nat Immunol
Delaying pyroptosis with an AI-screened gasdermin D pore blocker mitigates inflammatory response. [Abstract]2025 Oct;26(10):1660-1672. PMID: 40954252 -
Immunity
The transcription factor MEF2C restrains microglial overactivation by inhibiting kinase CDK2. [Abstract]2025 Mar 21:S1074-7613(25)00093-7. PMID: 40139186 -
Mil Med Res
Efficient and rapid conversion of human astrocytes and ALS mouse model spinal cord astrocytes into motor neuron-like cells by defined small molecules. [Abstract]2020 Sep 6;7(1):42. PMID: 32892745 -
Nat Metab
2023 Jun;5(6):1014-1028. PMID: 37337125 -
Cell Stem Cell
An inducible model of human post-implantation development derived from primed and naive stem cells. [Abstract]2025 Oct 2;32(10):1509-1527.e9. PMID: 40885193 -
Cell Stem Cell
Establishing dorsal-ventral patterning in human neural tube organoids with synthetic organizers. [Abstract]2025 Jul 3;32(7):1071-1086.e8. PMID: 40373768 -
Cell Stem Cell
Hepatic cytochrome P450 8B1 and cholic acid potentiate intestinal epithelial injury in colitis by suppressing intestinal stem cell renewal. [Abstract]2022 Sep 1;29(9):1366-1381.e9. PMID: 36055192 -
Cell Stem Cell
Epiblast inducers capture mouse trophectoderm stem cells in vitro and pattern blastoids for implantation in utero. [Abstract]2022 Jul 7;29(7):1102-1118.e8. PMID: 35803228 -
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Cancer Res
CLK2 Regulates the KEAP1/NRF2 and p53 Pathways to Suppress Ferroptosis in Colorectal Cancer. [Abstract]2025 Aug 29. PMID: 40882016 -
Mol Cell
AKT constitutes a signal-promoted alternative exon-junction complex that regulates nonsense-mediated mRNA decay. [Abstract]2022 Aug 4;82(15):2779-2796.e10. PMID: 35675814 -
Mol Cell
Gene Resistance to Transcriptional Reprogramming following Nuclear Transfer Is Directly Mediated by Multiple Chromatin-Repressive Pathways. [Abstract]2017 Mar 2;65(5):873-884.e8. PMID: 28257702 -
ACS Nano
Hybrid Exosome-Liposome Nanoparticles for Dual Modulation of Neuroinflammation and Lipid Metabolism in Ischemic Stroke. [Abstract]2025 Sep 23;19(37):33567-33586. PMID: 40948043 -
ACS Nano
Protein Coronation-Induced Cancer Staging-Dependent Multilevel Cytotoxicity: An All-Humanized Study in Blood Vessel Organoids. [Abstract]2025 Jan 14;19(1):345-368. PMID: 39743836 -
Hepatology
ATP7B gene therapy of autologous reprogrammed hepatocytes alleviates copper accumulation in a mouse model of Wilson's disease. [Abstract]2022 Oct;76(4):1046-1057. PMID: 35340061 -
Nat Commun
Geometrically-engineered human motor assembloids-on-a-chip for neuromuscular interaction readout and hypoxia-driven disease modeling. [Abstract]2025 Sep 30;16(1):8693. PMID: 41028715 -
Nat Commun
Helicobacter hepaticus promotes hepatic steatosis through CdtB-induced mitochondrial stress and lipid metabolism reprogramming. [Abstract]2025 Aug 26;16(1):7954. PMID: 40858606 -
Nat Commun
Klf5-adjacent super-enhancer functions as a 3D genome structure-dependent transcriptional driver to safeguard ESC identity. [Abstract]2025 Jul 1;16(1):5540. PMID: 40592854 -
Nat Commun
2025 Jul 1;16(1):6016. PMID: 40593722 -
Nat Commun
Attenuated growth factor signaling during cell death initiation sensitizes membranes towards peroxidation. [Abstract]2025 Feb 25;16(1):1774. PMID: 40000627
Laduviglusib 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.
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Nat Commun
Semi-automated IT-scATAC-seq profiles cell-specific chromatin accessibility in differentiation and peripheral blood populations. [Abstract]2025 Mar 17;16(1):2635. PMID: 40097444 -
Nat Commun
PIM1 promotes hepatic conversion by suppressing reprogramming-induced ferroptosis and cell cycle arrest. [Abstract]2022 Sep 6;13(1):5237. PMID: 36068222 -
Cell Death Differ
2020 Jul;27(7):2158-2175. PMID: 31969690 -
Acta Pharm Sin B
2025 Dec;15(12):6382-6398. PMID: 41477334 -
Acta Pharm Sin B
2024 Jul;14(7):3049-3067. PMID: 39027246 -
Adv Sci (Weinh)
Dynamics of the Mammalian Placental Metabolome in Placentogenesis and Embryonic Development. [Abstract]2026 Jan 28:e07928. PMID: 41603190 -
Adv Sci (Weinh)
Quantifying the Single-Cell Morphological Landscape of Cellular Transdifferentiation through Force Field Reconstruction. [Abstract]2025 Nov 7:e12325. PMID: 41203584 -
Adv Sci (Weinh)
Depletion of Sorcs3 Activates Totipotency in Mouse Embryonic Stem Cells by Modulating Key Signaling Pathways. [Abstract]2025 Nov 3:e09151. PMID: 41178446 -
Adv Sci (Weinh)
Preservation of ALYREF Phase Separation Mitigates Doxorubicin-Induced Cardiomyocyte DNA Damage and Cardiotoxicity. [Abstract]2025 Sep 3:e05270. PMID: 40899520 -
Adv Sci (Weinh)
Targeting Fibrotic Scarring by Mechanoregulation of Il11ra1+/Itga11+ Fibroblast Patterning Promotes Axon Growth after Spinal Cord Injury. [Abstract]2025 Sep 9:e13476. PMID: 40923460 -
Adv Sci (Weinh)
2024 Dec 4:e2408852. PMID: 39630006 -
Adv Sci (Weinh)
Cfp1 Controls Cardiomyocyte Maturation by Modifying Histone H3K4me3 of Structural, Metabolic, and Contractile Related Genes. [Abstract]2024 Mar;11(11):e2305992. PMID: 38196272 -
Adv Sci (Weinh)
Near-Infrared-Responded High Sensitivity Nanoprobe for Steady and Visualized Detection of Albumin in Hepatic Organoids and Mouse Liver. [Abstract]2022 Sep;9(26):e2202505. PMID: 35853243 -
Nat Chem Biol
2020 Dec;16(12):1411-1419. PMID: 32778844 -
Theranostics
Inhibition of HSP90β Improves Lipid Disorders by Promoting Mature SREBPs Degradation via the Ubiquitin-proteasome System. [Abstract]2019 Aug 12;9(20):5769-5783. PMID: 31534518 -
Theranostics
Jujuboside A promotes Aβ clearance and ameliorates cognitive deficiency in Alzheimer's disease through activating Axl/HSP90/PPARγ pathway. [Abstract]2018 Jul 30;8(15):4262-4278. PMID: 30128052 -
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Nucleic Acids Res
The kinase GSK-3 alters the RNA-binding protein landscape of lipid metabolism transcripts leading to altered expression in the C. elegans nervous system. [Abstract]2025 Aug 11;53(15):gkaf785. PMID: 40829802 -
Nucleic Acids Res
2022 Jul 22;50(13):7310-7325. PMID: 35776114 -
Nucleic Acids Res
Enhancer architecture-dependent multilayered transcriptional regulation orchestrates RA signaling-induced early lineage differentiation of ESCs. [Abstract]2021 Nov 18;49(20):11575-11595. PMID: 34723340 -
Exp Mol Med
Switching off CK2-mediated activation of survivin offers new therapeutic opportunities in neuroblastoma. [Abstract]2026 Feb;58(1):227-242. PMID: 41571889 -
Biomaterials
2024 Jul 1:311:122691. PMID: 38996673 -
Biomaterials
Chemical induced conversion of mouse fibroblasts and human adipose-derived stem cells into skeletal muscle-like cells. [Abstract]2018 Dec 6;193:30-46. PMID: 30554025 -
Biomaterials
A fluorescent chemical probe CDy9 selectively stains and enables the isolation of live naïve mouse embryonic stem cells. [Abstract]2018 Oct;180:12-23. PMID: 30014963 -
Sci Adv
A small-molecule stabilizer of the calpastatin-calpain-2 complex restores mitochondrial function and mitigates neurodegeneration. [Abstract]2026 Mar 27;12(13):eaeb1174. PMID: 41894510 -
Sci Adv
Generation of vascularized retinal organoids containing microglia based on a PDMS microwell platform. [Abstract]2025 Oct 10;11(41):eady6410. PMID: 41071880 -
Sci Adv
Haploid-genetic screening of trophectoderm specification identifies Dyrk1a as a repressor of totipotent-like status. [Abstract]2023 Dec 22;9(51):eadi5683. PMID: 38117886 -
Cell Discov
A live-cell image-based machine learning strategy for reducing variability in PSC differentiation systems. [Abstract]2023 Jun 6;9(1):53. PMID: 37280224 -
Sci Adv
Chemical conversion of human epidermal stem cells into intestinal goblet cells for modeling mucus-microbe interaction and therapy. [Abstract]2021 Apr 14;7(16):eabb2213. PMID: 33853767 -
Small
2020 Jun;16(22):e2001371. PMID: 32338439 -
Redox Biol
The protective role of GPX4 in naïve ESCs is highlighted by induced ferroptosis resistance through GPX4 expression. [Abstract]2025 Apr:81:103539. PMID: 40010136 -
J Hazard Mater
Triazole fungicides exert neural differentiation alteration through H3K27me3 modifications: In vitro and in silico study. [Abstract]2023 Oct 5:459:132225. PMID: 37557044 -
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MedComm (2020)
Gene Therapy Targeting Pkp2 Deficiency Attenuates Cardiac Fibrosis: Insights From Single-Cell Transcriptomics in Pkp2-Knockout Rats. [Abstract]2025 Sep 18;6(10):e70392. PMID: 40979216 -
Cell Rep Med
A human patient-derived organoid biobank to model tumor heterogeneity and therapeutic vulnerability for oral squamous cell carcinoma. [Abstract]2026 Feb 17;7(2):102622. PMID: 41707653 -
Cell Rep Med
Myosin inhibitor reverses hypertrophic cardiomyopathy in genotypically diverse pediatric iPSC-cardiomyocytes to mirror variant correction. [Abstract]2024 May 21;5(5):101520. PMID: 38642550 -
J Exp Med
Transit-amplifying cells control R-spondins in the mouse crypt to modulate intestinal stem cell proliferation. [Abstract]2022 Nov 7;219(11):e20212405. PMID: 36098959 -
Cell Rep Med
An Automated Organoid Platform with Inter-organoid Homogeneity and Inter-patient Heterogeneity. [Abstract]2020 Dec 22;1(9):100161. PMID: 33377132 -
Mater Today Bio
Establishing stable and highly osteogenic hiPSC-derived MSCs for 3D-printed bone graft through microenvironment modulation by CHIR99021-treated osteocytes. [Abstract]2024 Jun 1:26:101111. PMID: 38933413 -
Int J Surg
Unveiling macrophage-fibroblast-driven inflammatory networks mediated pan-cancer immune features by integrated single-cell and bulk RNA sequencing. [Abstract]2025 Nov 20. PMID: 41263399 -
Nat Struct Mol Biol
2025 Sep 1. PMID: 40890525 -
Cancer Lett
Forkhead box protein FOXK1 disrupts the circadian rhythm to promote breast tumorigenesis in response to insulin resistance. [Abstract]2024 Jul 31:217147. PMID: 39094826 -
Int J Biol Sci
RUNX1-MUC13 Interaction Activates Wnt/β-Catenin Signaling Implications for Colorectal Cancer Metastasis. [Abstract]2024 Sep 16;20(12):4999-5026. PMID: 39309442 -
Int J Biol Sci
TGFβ Governs the Pleiotropic Activity of NDRG1 in Triple-Negative Breast Cancer Progression. [Abstract]2023 Jan 1;19(1):204-224. PMID: 36594086 -
Int J Biol Sci
TNF-α augments CXCL10/CXCR3 axis activity to induce Epithelial-Mesenchymal Transition in colon cancer cell. [Abstract]2021 Jun 26;17(11):2683-2702. PMID: 34345201 -
Cell Death Dis
Generation of proliferative hESC-derived grape-clustered hepatocyte organoids with multipolar architecture as regenerative counterpart via synergy of YAP and IGF2 pathways. [Abstract]2026 Mar 26;17(1):381. PMID: 41888105 -
Biomater Res
Distinct Roles of Matrigel Enabled the Production of Expandable Hepatoblast and Polarized Hepatocyte Organoids from Human Embryonic Stem Cells under 3-Dimensional Suspension Conditions. [Abstract]2025 Nov 7:29:0280. PMID: 41209312 -
Cell Death Dis
Both direct and indirect suppression of MCL1 synergizes with BCLXL inhibition in preclinical models of gastric cancer. [Abstract]2025 Mar 12;16(1):170. PMID: 40075071 -
Cell Death Dis
Genome-wide screening in the haploid system reveals Slc25a43 as a target gene of oxidative toxicity. [Abstract]2022 Mar 30;13(3):284. PMID: 35354792 -
Cell Death Dis
PCDHGA9 represses epithelial-mesenchymal transition and metastatic potential in gastric cancer cells by reducing β-catenin transcriptional activity. [Abstract]2020 Mar 30;11(3):206. PMID: 32231199 -
Sci China Life Sci
2018 Oct;61(10):1151-1167. PMID: 30159682 -
Genome Biol
IT-scC&T-seq streamlines scalable, parallel profiling of protein-DNA interactions in single cells. [Abstract]2025 Jul 7;26(1):196. PMID: 40624534 -
Proc Natl Acad Sci U S A
Synergy with TGFβ ligands switches WNT pathway dynamics from transient to sustained during human pluripotent cell differentiation. [Abstract]2019 Mar 12;116(11):4989-4998. PMID: 30819898 -
Cell Commun Signal
2025 Jul 1;23(1):312. PMID: 40598158 -
Dev Cell
Identifying cross-lineage dependencies of cell-type-specific regulators in mouse gastruloids. [Abstract]2025 Jul 21;60(14):2007-2022.e7. PMID: 40101716 -
Int J Biol Macromol
Downregulation of the biological macromolecule Spondin-2 disrupts maternal-fetal immune tolerance and trophoblast invasion, driving unexplained recurrent pregnancy loss. [Abstract]2025 Dec 12;338(Pt 1):149672. PMID: 41391791 -
Acta Pharmacol Sin
PLN-L31A/I40A for the treatment of inherited heart disease caused by PLN-R14del mutations. [Abstract]2026 Jan 16. PMID: 41545752 -
Acta Pharmacol Sin
Galangin 3-methyl ether alleviates mouse hypertrophic cardiomyopathy via targeting HDAC2 and subsequently inactivating the PI3K-AKT signaling pathway. [Abstract]2025 Nov 1. PMID: 41176539 -
Acta Pharmacol Sin
In situ reprogramming of cardiac fibroblasts into cardiomyocytes in mouse heart with chemicals. [Abstract]2024 Nov;45(11):2290-2299. PMID: 38890526
Laduviglusib purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]
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 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]
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 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]
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 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Nov;45(11):2290-2299. [Abstract]
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).
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Cancer Biol Med
SHP2 promotes proliferation of breast cancer cells through regulating Cyclin D1 stability via the PI3K/AKT/GSK3β signaling pathway. [Abstract]2020 Aug 15;17(3):707-725. PMID: 32944401 -
EMBO Mol Med
2022 Dec 7;14(12):e16194. PMID: 36321561 -
Free Radic Biol Med
Canonical Wnt signaling works downstream of iron overload to prevent ferroptosis from damaging osteoblast differentiation. [Abstract]2022 Aug 1:188:337-350. PMID: 35752374 -
Chemosphere
Aryl hydrocarbon receptor mediates the cardiac developmental toxicity of EOM from PM2.5 in P19 embryonic carcinoma cells. [Abstract]2019 Feb:216:372-378. PMID: 30384306
Laduviglusib 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 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 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 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.
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J Transl Med
CENPA promotes clear cell renal cell carcinoma progression and metastasis via Wnt/β-catenin signaling pathway. [Abstract]2021 Oct 9;19(1):417. PMID: 34627268 -
Curr Biol
Synaptic Protein Degradation Controls Sexually Dimorphic Circuits through Regulation of DCC/UNC-40. [Abstract]2020 Nov 2;30(21):4128-4141.e5. PMID: 32857970 -
Stem Cell Res Ther
Beclin1 deficiency unlocks cardiac lineage commitment through convergent Wnt and BMP signaling activation. [Abstract]2025 Nov 13;16(1):636. PMID: 41233909 -
Stem Cell Res Ther
Generation of equine induced pluripotent stem cells from cells of embryonic, perinatal and adult tissues. [Abstract]2025 Oct 8;16(1):547. PMID: 41063189 -
Stem Cell Res Ther
Mesenchymal stem cells derived from hPSC via neural crest attenuate chemotherapy-induced premature ovarian insufficiency by ameliorating apoptosis and oxidative stress in granulosa cells. [Abstract]2025 May 13;16(1):239. PMID: 40361250 -
Stem Cell Res Ther
Dynamic three dimensional environment for efficient and large scale generation of smooth muscle cells from hiPSCs. [Abstract]2024 Dec 3;15(1):463. PMID: 39627821 -
Stem Cell Res Ther
SMYD1 modulates the proliferation of multipotent cardiac progenitor cells derived from human pluripotent stem cells during myocardial differentiation through GSK3β/β-catenin&ERK signaling. [Abstract]2024 Oct 8;15(1):350. PMID: 39380045 -
Stem Cell Res Ther
CDK8/19 inhibition plays an important role in pancreatic β-cell induction from human iPSCs. [Abstract]2023 Jan 5;14(1):1. PMID: 36600289 -
Stem Cell Res Ther
Generation of individualized immunocompatible endothelial cells from HLA-I-matched human pluripotent stem cells. [Abstract]2022 Feb 2;13(1):48. PMID: 35109922 -
Stem Cell Res Ther
Transplantation of human induced pluripotent stem cell-derived neural crest cells for corneal endothelial regeneration. [Abstract]2021 Mar 29;12(1):214. PMID: 33781330 -
Stem Cell Res Ther
Characterisation of extraembryonic endoderm-like cells from mouse embryonic fibroblasts induced using chemicals alone. [Abstract]2020 Apr 16;11(1):157. PMID: 32299508 -
PLoS Biol
2026 Mar 4;24(3):e3003700. PMID: 41779769 -
PLoS Biol
Aging-related peroxisomal dysregulation disrupts intestinal stem cell differentiation through alterations of very long-chain fatty acid oxidation. [Abstract]2025 Dec 19;23(12):e3003552. PMID: 41417787 -
PLoS Biol
Selective suppression of oligodendrocyte-derived amyloid beta rescues neuronal dysfunction in Alzheimer's disease. [Abstract]2024 Jul 23;22(7):e3002727. PMID: 39042667 -
PLoS Biol
Dissecting the dynamics of signaling events in the BMP, WNT, and NODAL cascade during self-organized fate patterning in human gastruloids. [Abstract]2019 Oct 15;17(10):e3000498. PMID: 31613879 -
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Cell Death Discov
2024 Mar 9;10(1):123. PMID: 38461207 -
Cell Death Discov
Gadd45g initiates embryonic stem cell differentiation and inhibits breast cell carcinogenesis. [Abstract]2021 Oct 2;7(1):271. PMID: 34601500 -
Cell Rep
2022 Mar 29;38(13):110570. PMID: 35354046 -
Cell Rep
MK2 promotes Tfcp2l1 degradation via β-TrCP ubiquitin ligase to regulate mouse embryonic stem cell self-renewal. [Abstract]2021 Nov 2;37(5):109949. PMID: 34731635 -
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Antioxidants (Basel)
Blue Light Alters the Composition of the Jejunal Microbiota and Promotes the Development of the Small Intestine by Reducing Oxidative Stress. [Abstract]2022 Jan 29;11(2):274. PMID: 35204158 -
J Biol Eng
Tissue engineering RPE sheet derived from hiPSC-RPE cell spheroids supplemented with Y-27632 and RepSox. [Abstract]2024 Jan 16;18(1):7. PMID: 38229139 -
Mol Med
CGREF1 modulates osteosarcoma proliferation by regulating the cell cycle through the Wnt/β-catenin signaling pathway. [Abstract]2024 Dec 20;30(1):260. PMID: 39707194 -
Fundam Res
Droplet-engineered organoids recapitulate parental tissue transcriptome with inter-organoid homogeneity and inter-tumor cell heterogeneity. [Abstract]2022 Jun 3;4(6):1506-1514. PMID: 39734523 -
Cell Mol Life Sci
Dual phosphorylation of glycogen synthase kinase 3β differentially integrates metabolic programs to determine T cell immunity across vertebrates. [Abstract]2025 May 28;82(1):218. PMID: 40434714 -
Cell Mol Life Sci
Single-cell transcriptomics reveals liver developmental trajectory during lineage reprogramming of human induced hepatocyte-like cells. [Abstract]2025 Apr 6;82(1):139. PMID: 40188417 -
EMBO Rep
ER-mitochondria contacts and cholesterol metabolism are disrupted by disease-associated tau protein. [Abstract]2023 Aug 3;24(8):e57499. PMID: 37401859 -
Mol Ther Nucleic Acids
AAV-mediated GBA1 and GDNF rescue neurological defects in a murine model of neuronopathic Gaucher disease. [Abstract]2025 Mar 7;36(2):102506. PMID: 40206656 -
JCI Insight
CTNND1 variants cause familial exudative vitreoretinopathy through the Wnt/cadherin axis. [Abstract]2022 Jun 14;e158428. PMID: 35700046 -
Mol Ther Nucleic Acids
ALKBH5-mediated m6A mRNA methylation governs human embryonic stem cell cardiac commitment. [Abstract]2021 May 29:26:22-33. PMID: 34513291 -
Cell Biol Toxicol
USP18 promotes ferroptosis in lipopolysaccharide-induced human kidney organoids by stabilizing STING1. [Abstract]2025 Aug 20;41(1):126. PMID: 40833519 -
Acta Neuropathol Commun
Therapeutic potential of NGF-enriched extracellular vesicles in modulating neuroinflammation and enhancing peripheral nerve remyelination. [Abstract]2025 May 27;13(1):118. PMID: 40420167 -
Biochem Pharmacol
Glucocorticoid impairs angiogenesis-dependent osteogenesis by downregulating EphB4 in endothelial cells. [Abstract]2025 Dec 2:244:117586. PMID: 41344513 -
Cell Prolif
ISRIB facilitates the co-culture of human trophoblast stem cells and embryonic stem cells. [Abstract]2024 Jun;57(6):e13599. PMID: 38217296 -
Cell Prolif
2023 Dec;56(12):e13498. PMID: 37144356 -
Cell Prolif
Genome-scale screening in a rat haploid system identifies Thop1 as a modulator of pluripotency exit. [Abstract]2022 Apr;55(4):e13209. PMID: 35274380 -
Cell Prolif
2021 Jan;54(1):e12932. PMID: 33107129 -
Mol Autism
UBE3A stabilization of β-catenin preserves synaptic proteins essential for motor and cognitive functions in Angelman Syndrome. [Abstract]2025 Nov 27;16(1):60. PMID: 41310868 -
Mol Cell Proteomics
Proteomics and Phosphoproteomics Revealed Dysregulated Kinases and Potential Therapy for Liver Fibrosis. [Abstract]2025 May 12:100991. PMID: 40368138
Laduviglusib 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 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 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 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 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.
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Chem Biol Interact
Modeling diabetic cardiomyopathy using human cardiac organoids: Effects of high glucose and lipid conditions. [Abstract]2025 Apr 25:411:111421. PMID: 39984109 -
Commun Biol
Mapk7 enhances osteogenesis and suppresses adipogenesis by activating Lrp6/β-catenin signaling axis in mesenchymal stem cells. [Abstract]2025 Feb 26;8(1):310. PMID: 40000807 -
Stem Cell Reports
An acidic residue within the OCT4 dimerization interface of SOX17 is necessary and sufficient to overcome its pluripotency-inducing activity. [Abstract]2025 Jan 23:102398. PMID: 39919754 -
Commun Biol
Wnt/β-catenin signaling regulates amino acid metabolism through the suppression of CEBPA and FOXA1 in liver cancer cells. [Abstract]2024 Apr 29;7(1):510. PMID: 38684876 -
Life Sci
Arctigenin inhibits proliferation of ER-positive breast cancer cells through cell cycle arrest mediated by GSK3-dependent cyclin D1 degradation. [Abstract]2020 Sep 1;256:117983. PMID: 32565252 -
Respir Res
CRISPR/Cas9-mediated B2m knockout paves the way for allogeneic basal cell transplantation. [Abstract]2026 Feb 28;27(1):109. PMID: 41764471 -
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Int J Mol Sci
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Int J Mol Sci
2024 Jul 27;25(15):8209. PMID: 39125777 -
Int J Mol Sci
2023 Oct 31;24(21):15804. PMID: 37958789 -
Int J Mol Sci
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Toxicology
Crosstalk between AhR and wnt/β-catenin signal pathways in the cardiac developmental toxicity of PM2.5 in zebrafish embryos. [Abstract]2016 Apr 29:355-356:31-8. PMID: 27216425
Laduviglusib 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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Sci Rep
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ACS Chem Neurosci
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Stem Cells
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Exp Cell Res
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Front Med
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2025 Jul 11:2025:5105796. PMID: 40689086 -
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Mol Carcinog
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Environ Toxicol
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Cell Biol Int
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Biol Reprod
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Life Sci Alliance
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Front Genet
2022 Jul 22:13:905395. PMID: 35937980 -
Animals (Basel)
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SLAS Discov
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Cell Biochem Funct
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Animals (Basel)
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APMIS
Mesalazine Suppresses Colorectal Cancer Liver Metastasis via the HDAC3/Wnt/β-Catenin Axis Through Downregulating Bacteroides fragilis Abundance. [Abstract]2025 Nov;133(11):e70078. PMID: 41199687 -
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Reprod Sci
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Ann Hematol
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Exp Ther Med
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Biochem Biophys Res Commun
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Biochem Biophys Res Commun
β-catenin stimulates Tcf7l1 degradation through recruitment of casein kinase 2 in mouse embryonic stem cells. [Abstract]2020 Apr 2;524(2):280-287. PMID: 31987502
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.
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Biochem Biophys Res Commun
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Naturwissenschaften
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Cell Reprogram
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STAR Protoc
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STAR Protoc
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STAR Protoc
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bioRxiv
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2025 May 14:2025.05.11.653328. PMID: 40462978 -
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Endogenous Nodal switches Wnt interpretation from posteriorization to germ layer differentiation in geometrically constrained human pluripotent cells. [Abstract]2024 Mar 14:2024.03.13.584912. PMID: 38559061 -
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Methods Mol Biol
Workflow for Performing Genetic Manipulation in Human Trophoblast Stem Cells Using CRISPR/Cas9 Technology. [Abstract]2024:2767:53-62. PMID: 36515893 -
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (279 KB)
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SDS (483 KB)
- English - EN (483 KB)
- Français - FR (483 KB)
- Deutsch - DE (483 KB)
- Norwegian - NO (483 KB)
- Español - ES (483 KB)
- Swedish - SV (483 KB)
- Italian - IT (483 KB)
- Portuguese - PT (483 KB)
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Handling Instructions (2659 KB)
References
[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 |