| Identification | Back Directory | [Name]
CHIR-99021 (monohydrochloride) | [CAS]
1797989-42-4 | [Synonyms]
CHIR-99012 HCl
CHIR99021; CHIR 99021
CT-99021 monohydrochloride)
SCQDMKUZHIGAIB-UHFFFAOYSA-O
CHIR-99021 (monohydrochloride)
CHIR-99021 monohydrochloride
(CT99021 monohydrochloride | [Molecular Formula]
C22H18Cl2N8.HCl | [MDL Number]
MFCD30489757 | [MOL File]
1797989-42-4.mol | [Molecular Weight]
501.8 |
| Chemical Properties | Back Directory | [storage temp. ]
Keep in dark place,Inert atmosphere,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 Information | Back Directory | [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]. | [in vivo]
In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) monohydrochloride rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration[1]. Laduviglusib (2 mg/kg) monohydrochloride given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib monohydrochloride treatment significantly blocks crypt apoptosis and accumulation of p-H2AX+ cells, and improves crypt regeneration and villus height. Laduviglusib monohydrochloride treatment increases Lgr5+ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h[5]. | [IC 50]
GSK-3β: 6.7 nM (IC50); GSK-3α: 10 nM (IC50); cdc2: 8800 nM (IC50) | [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. |
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