[CAS NO. 1373422-53-7] GSK J1
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PRODUCTS SPECIFICATIONS [1373422-53-7]
Catalog
SLK-S7581
Brand
Selleck
CAS
1373422-53-7
DESCRIPTION [1373422-53-7]
Overview
| MDL | MFCD22683851 |
|---|---|
| Molecular Weight | 389.45 |
| Molecular Formula | C22H23N5O2 |
| SMILES | O=C(O)CCNC1=NC(C2=NC=CC=C2)=NC(N3CCC4=CC=CC=C4CC3)=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5677 mL | 12.8386 mL | 25.6772 mL |
| 5 mM | 0.5135 mL | 2.5677 mL | 5.1354 mL |
| 10 mM | 0.2568 mL | 1.2839 mL | 2.5677 mL |
| 50 mM | 0.0514 mL | 0.2568 mL | 0.5135 mL |
Description
GSK-J1 is a highly potent inhibitor of H3K27 JMJD3 (KDM6B) and UTX (KDM6A) with of 60 nM in cell-free assays for JMJD3 (KDM6B) , respectively, >10-fold selectivity over other tested demethylases, with of 0.95μM and 1.76μM towards JARID1B/C.
Targets
| JMJD3 [1] |
| 60 nM |
In vitro
In HEK-293 cells, GSK-J1 inhibits the activities of transiently transfected JMJD3 and UTX. GSK-J1 also inhibits TNF-α production by human primary macrophages by increasing total nuclear H3K27me3 levels. In MC3T3-E1 cells, GSK-J1 suppresses Runx2 and Osterix expressions and ALP activity, and increases the global levels of H3K27me3.
References
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