Product Description: Laduviglusib (CHIR-99021) monohydrochloride is a potent and selective GSK-3α/β inhibitor with IC50s of 10 nM and 6.7 nM. Laduviglusib monohydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib monohydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib monohydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib monohydrochloride induces autophagy[1][2][3].
Applications: Cancer-Kinase/protease
Formula: C22H19Cl3N8
Citations: Poult Sci. 8 March 2022, 101825./ Biochemistry and Cell Biology. Rice University. 2019 May./ACS Chem Neurosci. 2018 Dec 19;9(12):3175-3185. /ACS Nano. 2025 Jan 1./Acta Pharm Sin B. 2024 Apr 24./Acta Pharmacol Sin. 2024 Jun 18./Adv Sci (Weinh). 2022 Sep;9(26):e2202505./Adv Sci (Weinh). 2024 Dec 4:e2408852./Adv Sci (Weinh). 2024 Jan 9:e2305992./Am J Physiol Cell Physiol. 2023 May 1./Animals (Basel). 2024 May 4;14(9):1382./Ann Hematol. 2023 Sep 9./Antioxidants (Basel). 2022 Jan 29;11(2):274./Antiviral Res. 2024 Apr 20:226:105891./Biochem Biophys Res Commun. 2018 Sep 5;503(2):1123-1129./Biochem Biophys Res Commun. 2020 Apr 2;524(2):280-287./Biochem Biophys Res Commun. 29 December 2021./Bioengineering (Basel). 2023 Jun 9, 10(6), 702./Biomaterials. 2018 Oct;180:12-23./Biomaterials. 2024 Jul 1:311:122691./Biomaterials. 2018 Dec 6;193:30-46./Biomedicines. 2022 Apr 18;10(4):928. /bioRxiv. 2023 Aug 14./bioRxiv. 2023 Jun 28./bioRxiv. 2024 Dec 6:2024.12.06.627179./bioRxiv. 2024 Feb 2./bioRxiv. 2024 June 27./bioRxiv. 2024 Mar 1./bioRxiv. 2024 Mar 12./bioRxiv. 2024 Mar 14./bioRxiv. 2024 November 15./BMC Oral Health. 2024 Nov 21;24(1):1421./Cancer Biol Med. 2020 Aug 15;17(3):707-725./Cancer Lett. 2024 Jul 31:217147./Cancer Lett. 2024 Jun./Cancers (Basel). 2021 Mar 3;13(5):1079./Cell Biochem Funct. 2024 Sep;42(7):e4120./Cell Biol Int. 2022 Sep 18./Cell Death Differ. 2020 Jul;27(7):2158-2175. /Cell Death Dis. 2020 Mar 30;11(3):206./Cell Death Dis. 2022 Mar 30;13(3):284./Cell Death Discov. 2021 Oct 2;7(1):271./Cell Death Discov. 2024 Mar 9;10(1):123./Cell Discov. 2023 Jun 6;9(1):53./Cell Metab. 2024 Jun 18:S1550-4131(24)00189-X./Cell Prolif. 2021 Jan;54(1):e12932./Cell Prolif. 2022 Mar 11;e13209./Cell Prolif. 2023 May 5;e13498./Cell Prolif. 2024 Jan 12:e13599./Cell Regen. 2020 Sep 3;9(1):15./Cell Rep Med. 2020 Dec 22;1(9):100161./Cell Rep Med. 2024 Apr 16:101520./Cell Rep. 2021 Nov 2;37(5):109949./Cell Rep. 2022 Mar 29;38(13):110570./Cell Reprogram. 2017 Dec;19(6):363-371./Cell Signal. 2016 Mar;28(3):148-56. /Cell Signal. 2022 Nov 17;110526./Cell Stem Cell. 2022 Jul 7;29(7):1102-1118.e8./Cell Stem Cell. 2022 Sep 1;29(9):1366-1381.e9./Cell. 2024 Nov 14;187(23):6566-6583.e22./Cells & Development. 2021, 203665./Cells Dev. 2024 Sep 5:203970./Chem Eng J. 1 January 2023, 138737./Chemosphere. 2018 Oct 23;216:372-378. /Commun Biol. 2024 Apr 29;7(1):510./Curr Biol. 2020 Nov 2;30(21):4128-4141.e5./Curr Protoc Cell Biol. 2018 Dec;81(1):e62./Curr Res Neurobiol. 2023 Jun 17, 100095./Discov Oncol. 2025 Jan 20;16(1):63./EMBO Rep. 2023 Jul 4;e57499./Environ Toxicol. 2017 Oct;32(10):2316-2322./Eur J Pharm Sci. 2021 Sep 10;106003./Exp Cell Res. 2022 Nov 11;422(1):113416./Exp Ther Med. 2020 Mar;19(3):1701-1710./FASEB J. 2021 Jun;35(6):e21664./FASEB J. 2024 Jul 15;38(13):e23781./Free Radic Biol Med. 2022 Jun 22;S0891-5849(22)00463-4./Front Cell Dev Biol. 2021 Jun 21;9:671704./Front Cell Dev Biol. 2021 Sep 20;9:712224./Front Cell Dev Biol. 2023 May 10./Front Genet. 22 July 2022./Front Med. 2021 Sep 23;8:746298./Fundamental Research. 3 June 2022./Genes (Basel). 2024 Oct 30;15(11):1400./Genes. 2024 Sep 13./Harvard Medical School LINCS LIBRARY/Hepatology. 2022 Mar 27./Int J Biol Sci. 2024 Sep 16;20(12):4999-5026./Int J Biol Sci. 2021 Jun 26;17(11):2683-2702./Int J Biol Sci. 2023; 19(1): 204-224./Int J Mol Sci. 2022 Aug 12;23(16):9049./Int J Mol Sci. 2022, 23(14), 7586./Int J Mol Sci. 2022, 23(20), 12249./Int J Mol Sci. 2023 Mar 22;24(6):6008./Int J Mol Sci. 2023 Oct 31, 24(21), 15804./Int J Mol Sci. 2024 Jul 27./Int J Stem Cells. 2023 May 30;16(2):156-167./iScience. 2023 Jul 21./iScience. 6 October 2022, 105293./J Appl Polym Sci. 2024 Sep 25./J Biol Chem. 2022: 102703./J Biol Chem. 2023 Dec 12:105556./J Biol Eng. 2024 Jan 16;18(1):7./J Cell Mol Med. 2019 Jul;23(7):4627-4639./J Cell Mol Med. 2021 Nov;25(22):10684-10697./J Cereb Blood Flow Metab. 2021 Dec 8;271678X211065391./J Exp Med. 2022 Nov 7;219(11):e20212405./J Hazard Mater. 2023 Oct 5, 459, 132225./J Int Med Res. 2021 Nov;49(11):3000605211055378./JCI Insight. 2022 Jun 14;e158428./Lab Invest. 2021 May 18./Life Sci Alliance. 2022 Apr 19;5(8):e202201421./Life Sci. 2020 Sep 1;256:117983./Materials Today Chemistry 12 (2019) 78e84/Methods Mol Biol. 2022 Dec 15./Mil Med Res. 2020 Sep 6;7(1):42. /Mol Cancer. 2024 Jan 10;23(1):12./Mol Carcinog. 2024 Jul 9./Mol Cell. 2017 Mar 2;65(5):873-884.e8./Mol Cell. 2022 Jun 3;S1097-2765(22)00480-4./Mol Med. 2024 Dec 20;30(1):260./Mol Ther-Nucl Acids. 2021 May 28./Molecules. 2020 Apr 23;25(8):1980./Nat Chem Biol. 2020 Dec;16(12):1411-1419./Nat Commun. 2022 Sep 6;13(1):5237./Nat Genet. 2024 Feb;56(2):294-305./Nat Med. 2016 May;22(5):547-56. /Nat Metab. 2023 Jun;5(6):1014-1028./Nucleic Acids Res. 2021 Nov 18;49(20):11575-11595./Nucleic Acids Res. 2022 Jul 1;gkac542./Oncol Lett. 2023 Aug 30./Oxid Med Cell Longev. 2020 Nov 26;2020:4830418./Patent. US20180263995A1./Patent. US20210002607A1./Pigment Cell Melanoma Res. 2023 Aug 9./PLoS Biol. 2019 Oct 15;17(10):e3000498./PLoS Biol. 2024 Jul 23;22(7):e3002727./Proc Natl Acad Sci U S A. 2019 Mar 12;116(11):4989-4998./Programa de Doctorado en Biomedicina. 2020 Sep./Res Sq. 2024 Jun 03./Res Sq. 2024 May 20./Research Square Preprint. 2021 Feb./Research Square Preprint. 2021 Nov./Respir Res. 2022 Mar 25;23(1):70./Rice University, Department of Biological Sciences. 2020 Apr./Ruperto Carola University Heidelberg. Faculty of Natural Sciences and Mathematics. 03 Mar 2022./Sci Adv. 2021 Apr 14;7(16):eabb2213./Sci Adv. 2023 Dec 22;9(51):eadi5683./Sci China Life Sci. 2018 Oct;61(10):1151-1167./Sci Rep. 2019 Dec 10;9(1):18731. /SLAS Discov. 2024 Nov 5;29(8):100191./Small. 2020 Jun;16(22):e2001371./SSRN. 2023 Sep 1./STAR Protoc. 17 June 2022, 101426./STAR Protoc. 2021 Nov 5;2(4):100881./STAR Protoc. 2023 Feb 3;4(1):102092./STAR Protoc. 2023 Mar 16;4(2):102151./Stem Cell Res Ther. 2021 Mar 29;12(1):214./Stem Cell Res Ther. 2022 Feb 2;13(1):48./Stem Cell Res Ther. 2023 Jan 5;14(1):1./Stem Cell Res Ther. 2024 Dec 3;15(1):463./Stem Cell Res Ther. 2024 Oct 8;15(1):350./Stem Cell Res Ther. 2020 Apr 16;11(1):157./Stem Cells Int. 2018 Dec 25;2018:5965727./Stem Cells Int. 2020 Feb 3;2020:8483035./Stem Cells Transl Med. 2021 May;10(5):743-755./Stem Cells. 2019 Apr;37(4):489-503./Stem Cells. 2022 Jul 28;sxac050./Theranostics. 2018 Jul 30;8(15):4262-4278./Theranostics. 2019 Aug 12;9(20):5769-5783./Tissue Eng Regen Med. 2025 Jan 17./Toxicol Appl Pharmacol. 2020 Jan 1;386:114813./Toxicol Appl Pharmacol. 2024 Nov 26:494:117175./Toxicology. 2016 May 20;355-356:31-38. /Toxicology. 2020 Apr 15;435:152422./Toxins. 2021 Aug 22;13(8):585./University of Otago. Biomedical Sciences. 2021 Nov./UNIVERSITY OF PAVIA. 2023 Jul 9./Zool Res. 2021 May 18;42(3):377-388./EMBO Mol Med. 2022 Nov 2;e16194./J Transl Med. 2021 Oct 9;19(1):417./Transl Oncol. 2024 Jul 5:47:102054.
References: [1]Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95./[2]Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004./[3]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./[4]Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566./[5]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.
CAS Number: 1797989-42-4
Molecular Weight: 501.80
Compound Purity: 99.93
Research Area: Cancer
Solubility: DMSO : 60 mg/mL (ultrasonic)/H2O : 7.14 mg/mL (ultrasonic)
Target: Autophagy;GSK-3;Organoid;Wnt;β-catenin
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