Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Purity: ≥98%
GSK503 (GSK-503) is a novel, potent and specific inhibitor of Enhancer of zeste homolog 2 (EZH2) methyltransferase inhibitor with potential antitumor activity. It inhibits EZH2 with Kiapp of 3 to 27 nM. GSK503 demostrates excellent antiproliferative activity and high in vivo antitumor efficacy in a melanoma mouse model.
ln Vitro |
GSK503, which shares structural similarities with GSK126 and GSK343, inhibits the methyltransferase activity of both wild type and mutant EZH2 with a similar potency (Kiapp=3-27 nM). GSK503 exhibits a selectivity of over 2000 fold over other histone methyltransferases and over 200 fold over EZH1 (Kiapp=636 nM)[1].
|
||
---|---|---|---|
ln Vivo |
Conditional EZH2 ablation and GSK503 therapy nearly eliminate the production of metastases in a melanoma mouse model while stabilizing the illness through growth inhibition[2]. Normal melanocyte biology is not affected. In mice, GSK503 has good pharmacokinetics. After SRBC or NP-KLH immunization, GSK503 but not the vehicle suppresses the development of the germinal center, phenotyping the Ezh2 null phenotype. GC B-cell counts are decreased by flow cytometry, GC volume and quantity are decreased by immunohistochemistry, and the production of high affinity antibodies is hindered by GSK503 therapy [1].
|
||
Animal Protocol |
|
||
References |
[1]. Béguelin W, et al. EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation. Cancer Cell. 2013 May 13;23(5):677-92.
[2]. Zingg D, et al. The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors. Nat Commun. 2015 Jan 22;6:6051 |
Molecular Formula |
C31H38N6O2
|
---|---|
Molecular Weight |
526.67
|
CAS # |
1346572-63-1
|
SMILES |
O=C(C1=CC(C2=CC=C(N3CCN(C)CC3)N=C2)=CC4=C1C(C)=CN4C(C)C)NCC5=C(C)C=C(C)NC5=O
|
InChi Key |
HRDQQHUKUIKFHT-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C31H38N6O2/c1-19(2)37-18-21(4)29-25(30(38)33-17-26-20(3)13-22(5)34-31(26)39)14-24(15-27(29)37)23-7-8-28(32-16-23)36-11-9-35(6)10-12-36/h7-8,13-16,18-19H,9-12,17H2,1-6H3,(H,33,38)(H,34,39)
|
Chemical Name |
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
|
Synonyms |
GSK 503; GSK503; GSK-503
|
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) |
|
---|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8987 mL | 9.4936 mL | 18.9872 mL | |
5 mM | 0.3797 mL | 1.8987 mL | 3.7974 mL | |
10 mM | 0.1899 mL | 0.9494 mL | 1.8987 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.