CHIR-99021 (monohydrochloride) Property

storage temp. 

under inert gas (nitrogen or Argon) at 2–8 °C

solubility 

≥25.1 mg/mL in DMSO; ≥4.23 mg/mL in H2O; ≥4.83 mg/mL in EtOH

form 

solid

color 

White to yellow

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

CHIR-99021 (monohydrochloride) Chemical Properties,Usage,Production

Uses

CHIR-99021 is a potent and highly selective inhibitor of glycogen synthase kinase 3 (GSK-3). CHIR-99021 activates glycogen synthesis in CHO-IR cells and in isolated type 1 diabetic rat skeletal muscle. CHIR-99021 has also been shown to induce the reprogramming of murine and human somatic cells into stem cells. GSK-3α/β inhibitor

Biological Activity

chir-99021 is a highly specific glycogen synthase kinase-3 (gsk-3) inhibitor which can inhibit both isoforms with ic50 of 10 nm (gsk-3α) and 6.7 nm (gsk-3β).chir-99021 was proved to promote self-renewal and maintain pluripotency of both b6 and balb/c es cells via stabilizing the downstream effectors like c-myc and β -catenin[1]. in j1 mesc cells, chir-99021 played an important role in maintaining the colony morphology as well as the self-renewal when combined with leukemia inhibitory factor (lif). chir-99021 has shown to regulate multiple signaling pathways which involve wnt/β-catenin, tgf-β, nodal and mapk, and the expression of epigenetic regulatory genes like dnmt3l[2].chir-99021 has been demonstrated to promote dn3 thymocytes proliferation and differentiation in the absence of pre-tcr signaling, notch1 signaling or cxcl12[3]. however, study has also found that higher concentration (10 μm but not 1 μm or 3 μm) of chir99021 might selectively inhibit differentiation by activating il-7 signaling pathway[3].

References

1. ye s1, 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):e35892.2. wu y1, 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. 20133. plos one. 2013;8(3):e58501. doi: 10.1371/journal.pone.0058501. epub 2013 mar 20. schroeder jh1, bell ls, janas ml, turner m. pharmacological inhibition of glycogen synthase kinase 3 regulates t cell development in vitro. plos one. 2013;8(3):e58501.