| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
CHIR-98024 targets glycogen synthase kinase 3 (GSK3), a serine/threonine protein kinase that plays a critical role in multiple cellular processes, including glycogen synthesis, cell proliferation, and apoptosis. It is a potent inhibitor of both the α and β isoforms of GSK3. In cell-free assays, it exhibits IC50 values of 0.65 nM for GSK3α and 0.58 nM for GSK3β. It demonstrates selectivity by distinguishing GSK-3 from its close homologs Cdc2 and ERK2.
|
|---|---|
| ln Vitro |
In vitro, CHIR-98024 is a highly potent GSK3 inhibitor. It has an EC50 of 0.2566 μM. In cell-free assays, it shows IC50 values of 0.65 nM for GSK3α and 0.58 nM for GSK3β. The compound's potency is also reported with an IC50 of approximately 0.57 nM for GSK3-beta. These values indicate its high efficacy in inhibiting GSK3 enzymatic activity.
|
| ln Vivo |
Specific in vivo activity data for CHIR-98024 are not detailed in the available sources. As a potent GSK3 inhibitor, it would be expected to have effects in animal models of conditions where GSK3 is implicated, such as diabetes, neurodegenerative diseases, and cancer. However, specific in vivo studies, dosing regimens, or efficacy data are not provided in the references cited.
|
| Enzyme Assay |
Cell-free assays for CHIR-98024 typically involve measuring its inhibition of GSK3 enzymatic activity. In these assays, recombinant GSK3α or GSK3β is incubated with a peptide substrate and ATP in the presence of varying concentrations of the compound. The incorporation of phosphate into the substrate is measured, and IC50 values are calculated. For CHIR-98024, IC50 values of 0.65 nM (GSK3α) and 0.58 nM (GSK3β) have been reported in such assays.
|
| Cell Assay |
Cellular assays for CHIR-98024 typically involve assessing its effects on GSK3-dependent signaling pathways in cultured cells. Cells are treated with the compound, and downstream targets of GSK3, such as β-catenin or glycogen synthase, are measured. The compound's ability to inhibit GSK3 in cells is reflected by changes in the phosphorylation status of these targets. The compound is cell-permeable, enabling its use in cell-based studies.
|
| Animal Protocol |
Specific in vivo animal实验 protocols for CHIR-98024 are not described in the available sources. As a research compound with potent GSK3 inhibitory activity, it could be evaluated in animal models of diabetes, neurodegenerative diseases, or cancer. In such studies, the compound would be administered via various routes, and its effects on disease progression and biomarkers would be assessed. However, no specific protocols are provided.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of CHIR-98024 are not reported in the available sources. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) profiles have not been characterized in the accessible literature. Information concerning product stability, particularly in solution, is rarely reported. The compound is soluble in DMSO.
|
| Toxicity/Toxicokinetics |
Toxicity data for CHIR-98024 are not provided in the available sources. As with many research compounds, detailed toxicological profiles are typically established during later stages of drug development. The compound is intended for research use only and is not for human consumption. Standard laboratory safety precautions should be observed when handling this compound.
|
| References | |
| Additional Infomation |
CHIR-98024 (CAS: 556813-39-9) is a potent, reversible, and cell-permeable inhibitor of GSK3α and GSK3β. It is also known as CT-98024 and Compound L. The compound demonstrates high potency in cell-free assays with IC50 values of 0.65 nM for GSK3α and 0.58 nM for GSK3β, and an EC50 of 0.2566 μM. It shows selectivity for GSK-3 over its close homologs Cdc2 and ERK2. CHIR-98024 is a valuable tool for studying GSK3 biology and the therapeutic potential of GSK3 inhibition. It is not an approved drug and is strictly for research purposes.
|
| Molecular Formula |
C20H17CL2N9O2
|
|---|---|
| Molecular Weight |
486.3141
|
| Exact Mass |
485.088
|
| CAS # |
556813-39-9
|
| Related CAS # |
556813-39-9 (CHIR98024);252935-94-7 (CHIR98014);CHIR98014 HCl;
|
| PubChem CID |
9957049
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.6±0.1 g/cm3
|
| Boiling Point |
839.0±75.0 °C at 760 mmHg
|
| Flash Point |
461.2±37.1 °C
|
| Vapour Pressure |
0.0±3.1 mmHg at 25°C
|
| Index of Refraction |
1.753
|
| LogP |
3.76
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
33
|
| Complexity |
645
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
NDFXSHIIGXVOKT-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H17Cl2N9O2/c21-11-1-2-12(14(22)9-11)17-13(19-25-6-7-26-19)10-28-20(30-17)27-8-5-24-16-4-3-15(31(32)33)18(23)29-16/h1-4,6-7,9-10H,5,8H2,(H,25,26)(H3,23,24,29)(H,27,28,30)
|
| Chemical Name |
6-N-[2-[[4-(2,4-dichlorophenyl)-5-(1H-imidazol-2-yl)pyrimidin-2-yl]amino]ethyl]-3-nitropyridine-2,6-diamine
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~257.04 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0563 mL | 10.2815 mL | 20.5630 mL | |
| 5 mM | 0.4113 mL | 2.0563 mL | 4.1126 mL | |
| 10 mM | 0.2056 mL | 1.0282 mL | 2.0563 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
