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CHIR-99021 HCl

Cat. No. M1989

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CHIR-99021 HCl Structure

CHIR-99021 hydrochloride;Laduviglusib hydrochloride

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 80  USD80 In stock
2mg USD 50  USD50 In stock
5mg USD 75  USD75 In stock
10mg USD 100  USD100 In stock
50mg USD 260  USD260 In stock
100mg USD 520  USD520 In stock
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Quality Control & Documentation
Biological Activity

CHIR-99021 exhibits >500-fold selectivity for GSK-3 over closely related kinases. CHIR-99021 also displays >800-fold selectivity against 45 additional enzymes and receptors. CHIR-99021 (3 μM) increases free cytosolic β-catenin by 1.9-fold, mimicking the canonical Wnt signaling pathway in 3T3-L1 preadipocytes. CHIR-99021 promotes primary beta cell replication in isolated rat islets at concentrations as low as 1 μM, with 2-3 fold increase of cell replication at 5 μM of CHIR-99021 treatment. Oral administration of CHIR-99021 at 16 or 48 mg/kg 1 hour before oral glucose challenges in ZDF rats significantly improves glucose tolerance with 14% and 33% reduction in plasma glucose at 16 mg/kg and 48 mg/kg, respectively, and the higher dose of CHIR-99021 also reduces hyperglycemia before the oral glucose challenge.

Product Citations
Customer Product Validations & Biological Datas
Source Sci Rep (2015). Figure 3. CHIR-99021
Method qPCR
Cell Lines J1 mESCs and F9 mEC cells
Concentrations 3 μM
Incubation Time 24 h
Results By contrast, all of the ESCC miRNAs were downregulated by CHIR (Fig. 3a–e). The miR-200b-429 and miR-183-182 clusters, which are highly expressed in pluripotent cells, were downregulated by both BIO and CHIR (Fig. 3f, 3g).
Source Sci Rep (2015). Figure 1. CHIR-99021
Method immunofluorescence staining
Cell Lines J1 mESCs and F9 mEC cells
Concentrations 3 μM
Incubation Time 24 h
Results The relativemRNA expression level of Nanog was determined in response to BIO or CHIR in J1mESCs and F9mEC cells by qPCR. As expected, transcription of Nanog in J1 mESCs and F9 mEC cells was upregulated by both BIO and CHIR
Protocol (for reference only)
Cell Experiment
Cell lines CHO-IR cells
Preparation method GS activity assays.
CHO-IR cells expressing human insulin receptor, (provided by Hans Bos) were grown to 80% confluence in Hamm’s F12 medium with 10% fetal bovine serum and without hypoxanthine (34). Trypsinized cells were seeded in 6-well plates at 1 × 106 cells/well in 2 ml of medium without fetal bovine serum. After 24 h, medium was replaced with 1 ml of serum-free medium containing GSK-3 inhibitor or control (final DMSO concentration <0.1%) for 30 min at 37°C. Cells were lysed by freeze/thaw in 50 mmol/l tris (pH 7.8) containing 1 mmol/l EDTA, 1 mmol/l DTT, 100 mmol/l NaF, 1 mmol/l phenylmethylsulfonyl fluoride, and 25 μg/ml leupeptin (buffer A) and centrifuged 15 min at 4°C/14000g. The activity ratio of GS was calculated as the GS activity in the absence of glucose-6-phosphate divided by the activity in the presence of 5 mmol/l glucose-6-phosphate, using the filter paper assay of Thomas et al.
Concentrations 0~500nM
Incubation time 30min
Animal Experiment
Animal models fasting ZDF rats
Formulation 20 mmol/l citrate-buffered 15% Captisol or suspensions in 0.5% carboxymethylcellulose
Dosages 30 mg/kg
Administration oral gavage
Chemical Information
Molecular Weight 501.8
Formula C22H18Cl2N8.HCl
CAS Number 1797989-42-4
Solubility (25°C) DMSO 60 mg/mL
Water 6 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month

[1] Ring DB, et al. Diabetes. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo.

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Abmole Inhibitor Catalog

Keywords: CHIR-99021 HCl, CHIR-99021 hydrochloride;Laduviglusib hydrochloride supplier, GSK-3, inhibitors, activators

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