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S6 kinase&PKD-1

CHIR-99021 (CT99021) (252917-06-9)

CHIR-99021 HCl (CT99021) is hydrochloride of CHIR-99021, which is a GSK-3α/β inhibitor with IC50 of 10 nM/6.7 nM; CHIR-99021 shows greater than 500-fold selectivity for GSK-3 versus its closest homologs Cdc2 and ERK2.

Not Intended for Therapeutic Use. For research use only.

CAS: 252917-06-9 Category

CHIR-99021 (CT99021) (252917-06-9) Description

CHIR 99021 is a member of the class of aminopyrimidines that is 2-aminopyrimidine substituted at positions N2, 5 and 6 by (5-cyanopyridin-2-yl)ethyl, 4-methylimidazol-2-yl and 2,4-dichlorophenyl groups respectively. It has a role as an EC 2.7.11.26 (tau-protein kinase) inhibitor. It is a member of imidazoles, a dichlorobenzene, an aminopyrimidine, an aminopyridine, a cyanopyridine, a secondary amino compound and a diamine.

CHIR-99021 (CT99021) (252917-06-9) Specifications

Product Name CHIR-99021 (CT99021) 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;
Chemical Name C6-[2-[[4-(2,4-dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)pyrimidin-2-yl]amino]ethylamino]pyridine-3-carbonitrile
Drug Class Inhibitor
Purity ≥98% by HPLC
CAS Number 252917-06-9
Molecular Formula C22H18Cl2N8
Molecular Weight 465.35
Monoisotopic Mass 465.35 g/mol
MDL number MFCD11846251
InChIKey AQGNHMOJWBZFQQ-UHFFFAOYSA-N
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)
SMILES N#CC1=CN=C(NCCNC2=NC=C(C3=NC(C)=CN3)C(C4=CC=C(Cl)C=C4Cl)=N2)C=C1
Form Solid powder
Color white to light brown
Solubility  ≥25.1mg/mL in DMSO
Storage Temp.  Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Shelf life  >5 years if stored properly
Handling Protect from air and moisture
Application A GSK-3α/β inhibitor

 


RIDADR NONH for all modes of transport

References:

[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]. 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.

[3]. 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.

[4].  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.

[5]. 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.