CHIR-99021 NEW
| Price | $36 | $58 | $88 |
| Package | 2mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: CHIR-99021 | CAS No.: 252917-06-9 |
| Purity: ≥95% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | CHIR-99021 |
| Description | CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells. |
| Cell Research | The Wnt/beta-catenin reporter assay was performed with the M50 Super 8× TOPFlash and M51 Super 8× FOPFlash vector containing the firefly luciferase gene under the control of TCF/LEF binding sites or mutated bindings sites. 12,500 cells were seeded overnight on gelatine-coated 96-well plates in LIF-containing ES cell medium. On the next day, the cells were transfected using Lipofectamine with one of the aforementioned vectors plus pGL4.75 [hRluc/CMV] encoding the renilla luciferase reporter gene hRluc as a transfection control. Six hours after transfection the medium was changed to medium devoid of LIF, with reduced serum, and supplemented with 5 μM CHIR-99021. The Dual-Luciferase? reporter assay system was employed 48 and 72 h after the medium change to follow the luminescence reaction using a GloMax?-multi detection system [4]. |
| Kinase Assay | Kinases were purified from SF9 cells through the use of their His or Glu tag. Glu-tagged proteins were purified as described, and His-tagged proteins were purified according to the manufacturer's instructions. Kinase assays were performed in 96-well plates with appropriate peptide substrates in a 300-μl reaction buffer (variations on 50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, 1 mM dithiothreitol, 25 mMβ-glycerophosphate, 1 mM NaF, and 0.01% bovine serum albumin). Peptides had Km values from 1 to 100 μM. CHIR 99021 or CHIR GSKIA was added in 3.5 μl of Me2SO, followed by ATP to a final concentration of 1 μM. After incubation, triplicate 100-μl aliquots were transferred to Combiplate 8 plates containing 100 μl/well of 50 μM ATP and 20 mM EDTA. After 1 hour, the wells were rinsed five times with phosphate-buffered saline, filled with 200 μl of scintillation fluid, sealed, and counted in a scintillation counter 30 min later. All of the steps were at room temperature. The percentage of inhibition was calculated as 100 × (inhibitor ? no enzyme control)/(Me2SO control ? no enzyme control) [4]. |
| Animal Research | Blood was obtained by shallow tail snipping at lidocaine-anesthetized tips. Blood glucose was measured directly or heparinized plasma was collected for measurement of glucose or insulin. Animals were pre-bled and randomized to vehicle control or GSK-3 inhibitor treatment groups. For glucose tolerance tests (GTTs), animals fasted throughout the procedure with food removal early in the morning, 3 h before the first prebleed (db/db mice), or the previous night, 16 h before the bleed (ZDF rats). When the time course of plasma glucose and insulin changes in fasting ZDF rats was measured, food was removed ～16 h before test agent administration. The glucose challenges in the GTT were 1.35 g/kg i.p. (ipGTT) or 2 g/kg via oral gavage (oGTT). CHIR-99021 were formulated as solutions in 20 mmol/l citrate-buffered 15% Captisol or as fine suspensions in 0.5% carboxymethylcellulose [1]. |
| In vitro | METHODS: Mouse stem cells ES-D3 were treated with CHIR-99021 (1-10 μM) for 72 h. Cell growth inhibition was detected using MTT. RESULTS: CHIR-99021 dose-dependently inhibited ES-D3 cell growth with an IC50 of 4.9 μM.[1] METHODS: Mouse embryonic stem cells J1 mESCs and mouse embryoma cells F9 mEC were treated with CHIR-99021 (3 μM) for 24 h. The expression levels of target proteins were detected by immunofluorescence. RESULTS: After CHIR-99021 treatment, β-linker proteins were increased in the cytoplasm and nucleus of J1-mESCs and F9-mEC cells. [2] METHODS: Human Tenon fibroblast HTFs were treated with CHIR-99021 (5 μM) for 48 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: The production of the active form of GSK-3β (p-GSK-3β (Y216)) was significantly reduced by CHIR-99021 treatment. [3] |
| In vivo | METHODS: To test the antitumor activity in vivo, CHIR-99021 (37.5 mg/kg/twice daily on days 0-3, 6-10, 13-17, and 20) was orally administered and paclitaxel (10 mg/kg/one dose on day 0) was intraperitoneally injected into Balb/c nude mice harboring human non-small cell lung cancer tumor H1975. RESULTS: CHIR-99021 and paclitaxel synergistically inhibited NSCLC tumor growth in vivo. [4] METHODS: To investigate whether direct pharmacological inhibition of GSK-3 alters the positive potentiation of alcohol in mice, CHIR-99021 (1-10 mg/kg) was administered by single intraperitoneal injection to C57BL/6J mice with a history of alcohol or sucrose self-administration. RESULTS: CHIR-99021 dose-dependently increased alcohol-enhanced responses with no effect on sucrose self-administration or locomotor activity. ChIR-99021 significantly decreased pGSK-3β expression in all brain regions tested, decreased PICK1 and increased total GluA2 expression only in NAcb. [5] |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.93 mg/mL (2 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. DMSO : 50 mg/mL (107.45 mM) |
| Keywords | GSK-3 | Glycogen synthase kinase 3 | CHIR99021 | β-catenin | inhibit | Autophagy | Beta catenin | CT-99021 | CHIR 99021 | Wnt | Inhibitor | Glycogen synthase kinase-3 | CT 99021 |
| Inhibitors Related | Stavudine | Xylitol | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Salicylic acid | Gefitinib |
| Related Compound Libraries | Highly Selective Inhibitor Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Kinase Inhibitor Library | Neuroprotective Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
You may like
Recommended supplier
| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
| $0.00/1bottle |
VIP4Y
|
Wuhan Nutra Biotechnology Co.,Ltd
|
2022-06-24 | |
| $0.00/1kg |
Nanjing Fred Technology Co., Ltd
|
2023-12-28 | ||
| $3.00/1KG |
VIP6Y
|
Career Henan Chemical Co
|
2020-02-20 | |
| $30.00/1kg |
Anhui Ruihan Technology Co., Ltd
|
2023-09-08 | ||
| $2.00/1kg |
VIP7Y
|
Career Henan Chemical Co
|
2018-12-23 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
INQUIRY