WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 200774

CAS#: 252917-06-9 (free base)

Description: CHIR-99021, also known as CT99021, is a glycogen synthase kinase 3β (GSK3β) inhibitor that has antiproliferative activity in vitro and in vivo. CHIR-99021 inhibits GSK-3 with IC50 at 7 nM. In a series of carcinoma cell lines, the IC50 of CHIR99021 for proliferation is about 10μM.

Chemical Structure

CAS# 252917-06-9 (free base)

Theoretical Analysis

MedKoo Cat#: 200774
Name: CHIR-99021
CAS#: 252917-06-9 (free base)
Chemical Formula: C22H18Cl2N8
Exact Mass: 464.10315
Molecular Weight: 465.34
Elemental Analysis: C, 56.78; H, 3.90; Cl, 15.24; N, 24.08

Size Price Shipping out time Quantity
50mg USD 150 Same day
100mg USD 250 Same day
200mg USD 450 Same day
500mg USD 850 Same day
1g USD 1350 Same day
2g USD 2450 Same day
Inquire bulk and customized quantity

Pricing updated 2021-02-28. Prices are subject to change without notice.

CHIR-99021 free base, purity > 98%, is in stock. The same day shipping out after order is received.

Related CAS #: 252917-06-9 (free base)   1782235-14-6 (3HCl)   2109414-84-6 (2HCl)   1797989-42-4 (HCl)    

Synonym: CHIR-911; CHIR911; CHIR 911; CT-99021; CT99021; CT 99021; CHIR-73911; CHIR73911; CHIR 73911; GSK 3 inhibitor XVI; GSK 3IXV; CHIR99021; CHIR 99021; Laduviglusib

IUPAC/Chemical Name: 6-((2-((4-(2,4-dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-yl)amino)ethyl)amino)nicotinonitrile


InChi Code: 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)


Solid powder

>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO, not in water

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:

Preparing Stock Solutions

The following data is based on the product molecular weight 465.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.


Dilution Calculator

Calculate the dilution required to prepare a stock solution.

1: Wu Y, Liu F, Liu Y, Liu X, Ai Z, Guo Z, Zhang Y. GSK3 inhibitors CHIR99021 and 6-bromoindirubin-3'-oxime inhibit microRNA maturation in mouse embryonic stem cells. Sci Rep. 2015 Mar 2;5:8666. doi: 10.1038/srep08666. PubMed PMID: 25727520; PubMed Central PMCID: PMC4345320.

2: Bock AS, Leigh ND, Bryda EC. Effect of Gsk3 inhibitor CHIR99021 on aneuploidy levels in rat embryonic stem cells. In Vitro Cell Dev Biol Anim. 2014 Jun;50(6):572-9. doi: 10.1007/s11626-014-9734-5. Epub 2014 Feb 12. PubMed PMID: 24519175; PubMed Central PMCID: PMC4062835.

3: Li C, Zhang S, Lu Y, Zhang Y, Wang E, Cui Z. The roles of Notch3 on the cell proliferation and apoptosis induced by CHIR99021 in NSCLC cell lines: a functional link between Wnt and Notch signaling pathways. PLoS One. 2013 Dec 18;8(12):e84659. doi: 10.1371/journal.pone.0084659. eCollection 2013. PubMed PMID: 24367688; PubMed Central PMCID: PMC3867546.

4: Wu Y, Ai Z, Yao K, Cao L, Du J, Shi X, Guo Z, Zhang Y. CHIR99021 promotes self-renewal of mouse embryonic stem cells by modulation of protein-encoding gene and long intergenic non-coding RNA expression. Exp Cell Res. 2013 Oct 15;319(17):2684-99. doi: 10.1016/j.yexcr.2013.08.027. Epub 2013 Sep 7. PubMed PMID: 24021571.

5: Petkov S, Hyttel P, Niemann H. The small molecule inhibitors PD0325091 and CHIR99021 reduce expression of pluripotency-related genes in putative porcine induced pluripotent stem cells. Cell Reprogram. 2014 Aug;16(4):235-40. doi: 10.1089/cell.2014.0010. Epub 2014 Jun 24. PubMed PMID: 24960205.

6: Ai Z, Shao J, Wu Y, Yu M, Du J, Shi X, Shi X, Zhang Y, Guo Z. CHIR99021 enhances Klf4 Expression through β-Catenin Signaling and miR-7a Regulation in J1 Mouse Embryonic Stem Cells. PLoS One. 2016 Mar 3;11(3):e0150936. doi: 10.1371/journal.pone.0150936. eCollection 2016. PubMed PMID: 26938105; PubMed Central PMCID: PMC4777400.

7: Yin X, Farin HF, van Es JH, Clevers H, Langer R, Karp JM. Niche-independent high-purity cultures of Lgr5+ intestinal stem cells and their progeny. Nat Methods. 2014 Jan;11(1):106-12. doi: 10.1038/nmeth.2737. Epub 2013 Dec 1. PubMed PMID: 24292484; PubMed Central PMCID: PMC3951815.

8: Ye S, Tan L, Yang R, Fang B, Qu S, Schulze EN, Song H, Ying Q, Li P. 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. doi: 10.1371/journal.pone.0035892. Epub 2012 Apr 23. PubMed PMID: 22540008; PubMed Central PMCID: PMC3335080.

9: Wang X, Wei L, Cramer JM, Leibowitz BJ, Judge C, Epperly M, Greenberger J, Wang F, Li L, Stelzner MG, Dunn JC, Martin MG, Lagasse E, Zhang L, Yu J. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566. doi: 10.1038/srep08566. PubMed PMID: 25858503; PubMed Central PMCID: PMC4392360.

10: Lam AQ, Freedman BS, Morizane R, Lerou PH, Valerius MT, Bonventre JV. Rapid and efficient differentiation of human pluripotent stem cells into intermediate mesoderm that forms tubules expressing kidney proximal tubular markers. J Am Soc Nephrol. 2014 Jun;25(6):1211-25. doi: 10.1681/ASN.2013080831. Epub 2013 Dec 19. PubMed PMID: 24357672; PubMed Central PMCID: PMC4033376.

11: Qin H, Hejna M, Liu Y, Percharde M, Wossidlo M, Blouin L, Durruthy-Durruthy J, Wong P, Qi Z, Yu J, Qi LS, Sebastiano V, Song JS, Ramalho-Santos M. YAP Induces Human Naive Pluripotency. Cell Rep. 2016 Mar 15;14(10):2301-12. doi: 10.1016/j.celrep.2016.02.036. Epub 2016 Mar 3. PubMed PMID: 26947063; PubMed Central PMCID: PMC4807727.

12: Fu Y, Huang C, Xu X, Gu H, Ye Y, Jiang C, Qiu Z, Xie X. Direct reprogramming of mouse fibroblasts into cardiomyocytes with chemical cocktails. Cell Res. 2015 Sep;25(9):1013-24. doi: 10.1038/cr.2015.99. Epub 2015 Aug 21. PubMed PMID: 26292833; PubMed Central PMCID: PMC4559819.

13: Ninomiya H, Mizuno K, Terada R, Miura T, Ohnuma K, Takahashi S, Asashima M, Michiue T. Improved efficiency of definitive endoderm induction from human induced pluripotent stem cells in feeder and serum-free culture system. In Vitro Cell Dev Biol Anim. 2015 Jan;51(1):1-8. doi: 10.1007/s11626-014-9801-y. Epub 2014 Aug 15. PubMed PMID: 25124871.

14: Cheng T, Zhai K, Chang Y, Yao G, He J, Wang F, Kong H, Xin H, Wang H, Jin M, Gong B, Gu L, Yang Z, Wu Y, Ji G, Sun Y. CHIR99021 combined with retinoic acid promotes the differentiation of primordial germ cells from human embryonic stem cells. Oncotarget. 2017 Jan 31;8(5):7814-7826. doi: 10.18632/oncotarget.13958. PubMed PMID: 27999196; PubMed Central PMCID: PMC5352363.

15: Cheng L, Hu W, Qiu B, Zhao J, Yu Y, Guan W, Wang M, Yang W, Pei G. Generation of neural progenitor cells by chemical cocktails and hypoxia. Cell Res. 2014 Jun;24(6):665-79. doi: 10.1038/cr.2014.32. Epub 2014 Mar 18. Erratum in: Cell Res. 2015 May;25(5):645-6. PubMed PMID: 24638034; PubMed Central PMCID: PMC4042166.

16: Besing RC, Paul JR, Hablitz LM, Rogers CO, Johnson RL, Young ME, Gamble KL. Circadian rhythmicity of active GSK3 isoforms modulates molecular clock gene rhythms in the suprachiasmatic nucleus. J Biol Rhythms. 2015 Apr;30(2):155-60. doi: 10.1177/0748730415573167. Epub 2015 Feb 27. PubMed PMID: 25724980; PubMed Central PMCID: PMC4586074.

17: Roccio M, Hahnewald S, Perny M, Senn P. Cell cycle reactivation of cochlear progenitor cells in neonatal FUCCI mice by a GSK3 small molecule inhibitor. Sci Rep. 2015 Dec 8;5:17886. doi: 10.1038/srep17886. PubMed PMID: 26643939; PubMed Central PMCID: PMC4672274.

18: van den Berg CW, Elliott DA, Braam SR, Mummery CL, Davis RP. Differentiation of Human Pluripotent Stem Cells to Cardiomyocytes Under Defined Conditions. Methods Mol Biol. 2016;1353:163-80. doi: 10.1007/7651_2014_178. PubMed PMID: 25626427.

19: Briolotti P, Chaloin L, Balaguer P, Da Silva F, Tománková V, Pascussi JM, Duret C, Fabre JM, Ramos J, Klieber S, Maurel P, Daujat-Chavanieu M, Gerbal-Chaloin S. Analysis of Glycogen Synthase Kinase Inhibitors That Regulate Cytochrome P450 Expression in Primary Human Hepatocytes by Activation of β-Catenin, Aryl Hydrocarbon Receptor and Pregnane X Receptor Signaling. Toxicol Sci. 2015 Nov;148(1):261-75. doi: 10.1093/toxsci/kfv177. Epub 2015 Aug 10. PubMed PMID: 26259606.

20: Preston GC, Sinclair LV, Kaskar A, Hukelmann JL, Navarro MN, Ferrero I, MacDonald HR, Cowling VH, Cantrell DA. Single cell tuning of Myc expression by antigen receptor signal strength and interleukin-2 in T lymphocytes. EMBO J. 2015 Aug 4;34(15):2008-24. doi: 10.15252/embj.201490252. Epub 2015 Jul 1. PubMed PMID: 26136212; PubMed Central PMCID: PMC4551349.

Additional Information

CHIR99021 inhibits GSK-3 with IC50 at 7 nM. In a series of carcinoma cell lines, the IC50 of CHIR99021 for proliferation is about 10uM.
Current developer:   Chiron (Originator)