AB120890

CHIR99021, GSK3 inhibitor

Name: CHIR99021, GSK3 inhibitor (CAS 252917-06-9) | Abcam
Brand: Abcam Limited
SKU: AB120890
Price: 80 USD
Availability: InStock

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(13 Publications)

CHIR99021 (ab120890) is a potent and highly selective glycogen synthase kinase 3 (GSK3) inhibitor. (IC₅₀ values are 6.7 and 10 nM at GSK3β and GSK3α, respectively). MW 465.3, Purity >98%.

- Exhibits >500-fold selectivity for GSK3 when tested against 20 closely related protein kinases
- Solubility in DMSO: 2.5 mg/mL
- Available in multiple sizes to fit your experimental needs

1 Images

Chemical Structure - CHIR99021, GSK3 inhibitor (AB120890)

Chemical Structure

Lab

Chemical Structure - CHIR99021, GSK3 inhibitor (AB120890)

2D chemical structure image of ab120890, CHIR99021, GSK3 inhibitor

Key facts

CAS number

252917-06-9

Purity

>98%

Form

Solid

form

Molecular weight

465.3 Da

Molecular formula

C22H18Cl2N8

PubChem

9956119

Nature

Synthetic

Biochemical name

6-((2-((4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile

Biological description

Potent, highly selective aminopyrimidine GSK3 inhibitor (IC₅₀ values are 6.7 and 10 nM at GSK3β and GSK3α, respectively). Exhibits >500-fold selectivity for GSK3 against 20 closely related protein kinases and >800-fold selectivity for 23 additional enzymes and 22 receptors. Promotes self-renewal of mouse and human ESC due to β-catenin and c-Myc protein level stabilization. Commonly used in multiple stages of organoid generation.

Canonical smiles

CC1=CN=C(N1)C2=CN=C(N=C2C3=C(C=C(C=C3)Cl)Cl)NCCNC4=NC=C(C=C4)C#N

InChi

InChI=1S/C22H18Cl2N8/c1-13-10-29-21(31-13)17-12-30-22(32-20(17)16-4-3-15(23)8-18(16)24)27-7-6-26-19-5-2-14(9-25)11-28-19/h2-5,8,10-12H,6-7H2,1H3,(H,26,28)(H,29,31)(H,27,30,32)

InChiKey

AQGNHMOJWBZFQQ-UHFFFAOYSA-N

IUPAC Name

6-[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl]amino]ethylamino]pyridine-3-carbonitrile

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Properties and storage information

Shipped at conditions

Blue Ice

Appropriate short-term storage conditions

-20°C

Appropriate long-term storage conditions

-20°C

Storage information

Store under desiccating conditions|The product can be stored for up to 12 months

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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Glycogen synthase kinase 3 beta (GSK3β) and glycogen synthase kinase 3 alpha (GSK3α) are serine/threonine protein kinases involved in various cellular processes. GSK3β weighs approximately 47 kDa while GSK3α is around 51 kDa. These proteins are expressed in various tissues including brain heart and liver. GSK3 isoforms act as key regulators in signaling pathways by phosphorylating target proteins affecting their function and stability. Alternative names for GSK3 include GSK-3β and GSK-3α respectively.

Biological function summary

The kinases play essential roles in cellular functions like glycogen metabolism cell cycle regulation and apoptosis. GSK3 proteins often function as part of larger enzyme complexes influencing cellular responses to external signals. They bind to numerous substrates impacting processes such as glucose homeostasis and neuron function. Dramatic changes in GSK3 activity can disrupt these biological processes highlighting their importance.

Pathways

These kinases are integral components of the Wnt/β-catenin and insulin signaling pathways. In the Wnt pathway GSK3 is involved in β-catenin phosphorylation affecting its degradation and transcriptional activity. In the insulin pathway GSK3 influences glycogen synthesis by phosphorylating and regulating glycogen synthase. Both pathways highlight how GSK3 interacts with other proteins such as adenomatous polyposis coli (APC) and axin to coordinate cellular activities.

GSK3 has links to conditions like Alzheimer's disease and diabetes mellitus. Dysregulation of GSK3 activity is observed in Alzheimer's disease where abnormal GSK3 signaling contributes to tau hyperphosphorylation and neurofibrillary tangle formation. In diabetes altered GSK3 function affects insulin signaling pathways influencing glucose metabolism. GSK3's involvement in these diseases often connects it to proteins like tau in Alzheimer's and insulin receptor substrate 1 (IRS1) in diabetes.

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Product protocols

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Publications (13)

Recent publications for all applications. Explore the full list and refine your search

PLoS genetics 20:e1011510 PubMed39666736

2024

The Tumor-Associated Calcium Signal Transducer 2 (TACSTD2) oncogene is upregulated in cystic epithelial cells revealing a potential new target for polycystic kidney disease.

Applications

Unspecified application

Species

Unspecified reactive species

Abigail O Smith,William Tyler Frantz,Kenley M Preval,Yvonne J K Edwards,Craig J Ceol,Julie A Jonassen,Gregory J Pazour

International journal of molecular sciences 24: PubMed37958655

2023

A Strainer-Based Platform for the Collection and Immunolabeling of Porcine Epidemic Diarrhea Virus-Infected Porcine Intestinal Organoid.

Applications

Unspecified application

Species

Unspecified reactive species

Yinju Liu,Jinlong Tan,Nianzhang Zhang,Wenhui Li,Baoquan Fu

Cell reports 40:111136 PubMed35905723

2022

HOTAIR interacts with PRC2 complex regulating the regional preadipocyte transcriptome and human fat distribution.

Applications

Unspecified application

Species

Unspecified reactive species

Feng-Chih Kuo,Matt J Neville,Rugivan Sabaratnam,Agata Wesolowska-Andersen,Daniel Phillips,Laura B L Wittemans,Andrea D van Dam,Nellie Y Loh,Marijana Todorčević,Nathan Denton,Katherine A Kentistou,Peter K Joshi,Constantinos Christodoulides,Claudia Langenberg,Philippe Collas,Fredrik Karpe,Katherine E Pinnick

Nature communications 13:2791 PubMed35589755

2022

RNA splicing is a key mediator of tumour cell plasticity and a therapeutic vulnerability in colorectal cancer.

Applications

Unspecified application

Species

Unspecified reactive species

Adam E Hall,Sebastian Öther-Gee Pohl,Patrizia Cammareri,Stuart Aitken,Nicholas T Younger,Michela Raponi,Caroline V Billard,Alfonso Bolado Carrancio,Aslihan Bastem,Paz Freile,Fiona Haward,Ian R Adams,Javier F Caceres,Paula Preyzner,Alex von Kriegsheim,Malcolm G Dunlop,Farhat V Din,Kevin B Myant

Development (Cambridge, England) 149: PubMed35299237

2022

Epha1 is a cell-surface marker for the neuromesodermal competent population.

Applications

Unspecified application

Species

Unspecified reactive species

Luisa de Lemos,André Dias,Ana Nóvoa,Moisés Mallo

FASEB journal : official publication of the Federation of American Societies for Experimental Biology 35:e21883 PubMed34569659

2021

Mechanosensitive miR-100 coordinates TGFβ and Wnt signaling in osteocytes during fluid shear stress.

Applications

Unspecified application

Species

Unspecified reactive species

Neha S Dole,Jihee Yoon,David A Monteiro,Jason Yang,Courtney M Mazur,Serra Kaya,Cassandra D Belair,Tamara Alliston

Cancer research 80:3631-3648 PubMed32586983

2020

A Pygopus 2-Histone Interaction Is Critical for Cancer Cell Dedifferentiation and Progression in Malignant Breast Cancer.

Applications

Unspecified application

Species

Unspecified reactive species

Meera Saxena,Ravi K R Kalathur,Natalia Rubinstein,Andrea Vettiger,Nami Sugiyama,Melanie Neutzner,Mairene Coto-Llerena,Venkatesh Kancherla,Caner Ercan,Salvatore Piscuoglio,Jonas Fischer,Ernesta Fagiani,Claudio Cantù,Konrad Basler,Gerhard Christofori

Nature protocols 14:1991-2014 PubMed31160788

2019

Derivation and maintenance of mouse haploid embryonic stem cells.

Applications

Unspecified application

Species

Unspecified reactive species

Ulrich Elling,Michael Woods,Josep V Forment,Beiyuan Fu,Fengtang Yang,Bee Ling Ng,Jose R Vicente,David J Adams,Brendan Doe,Stephen P Jackson,Josef M Penninger,Gabriel Balmus

Nature communications 10:87 PubMed30622252

2019

ATM orchestrates the DNA-damage response to counter toxic non-homologous end-joining at broken replication forks.

Applications

Unspecified application

Species

Unspecified reactive species

Gabriel Balmus,Domenic Pilger,Julia Coates,Mukerrem Demir,Matylda Sczaniecka-Clift,Ana C Barros,Michael Woods,Beiyuan Fu,Fengtang Yang,Elisabeth Chen,Matthias Ostermaier,Tatjana Stankovic,Hannes Ponstingl,Mareike Herzog,Kosuke Yusa,Francisco Munoz Martinez,Stephen T Durant,Yaron Galanty,Petra Beli,David J Adams,Allan Bradley,Emmanouil Metzakopian,Josep V Forment,Stephen P Jackson

International journal of molecular sciences 18: PubMed28587156

2017

Differential Sarcomere and Electrophysiological Maturation of Human iPSC-Derived Cardiac Myocytes in Monolayer vs. Aggregation-Based Differentiation Protocols.

Applications

Unspecified application

Species

Unspecified reactive species

Dorota Jeziorowska,Vincent Fontaine,Charlène Jouve,Eric Villard,Sébastien Dussaud,David Akbar,Valérie Letang,Pauline Cervello,Jean-Michiel Itier,Marie-Pierre Pruniaux,Jean-Sébastien Hulot

View all publications

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Product promise

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CHIR99021, GSK3 inhibitor

Chemical Structure - CHIR99021, GSK3 inhibitor (AB120890)

Key facts

CAS number

Purity

Form

Molecular weight

Molecular formula

PubChem

Nature

Biochemical name

Biological description

Canonical smiles

InChi

InChiKey

IUPAC Name

Complementary Products

Secondary Antibodies

Primary Antibodies

Primary Antibodies

Primary Antibodies

Properties and storage information

Shipped at conditions

Appropriate short-term storage conditions

Appropriate long-term storage conditions

Storage information

Supplementary information

Biological function summary

Pathways

Product protocols

Publications (13)

Product promise