Name | GSK-J1 |
Synonyms | GSK J1 GSK-J1 GCK J1 Histone Lysine Demethylase Inhibitor VII, GSK-J1 N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-beta-alanine 3-((6-(4,5-Dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoic acid |
CAS | 1373422-53-7 |
EINECS | 200-258-5 |
InChIKey | AVZCPICCWKMZDT-UHFFFAOYSA-N |
Molecular Formula | C22H23N5O2 |
Molar Mass | 389.45 |
Density | 1.292±0.06 g/cm3(Predicted) |
Boling Point | 608.9±55.0 °C(Predicted) |
Solubility | DMSO: ≥ 33 mg/mL |
Appearance | powder |
Color | white to beige |
pKa | 4.20±0.10(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 2 years from date of purchase? as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
In vitro study | GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3. GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5-fold increased potency compared with that of KDM5B at 1 mM α-ketoglutarate, with IC 50 of 11 μM and 94 μM, respectively. |
Hazard Symbols | Xi - Irritant |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.568 ml | 12.839 ml | 25.677 ml |
5 mM | 0.514 ml | 2.568 ml | 5.135 ml |
10 mM | 0.257 ml | 1.284 ml | 2.568 ml |
5 mM | 0.051 ml | 0.257 ml | 0.514 ml |
biological activity | GSK-J1 is an inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, and the IC50 value for KDM6B is 60 nM. |
target | IC50: 60 nM (KDM6B) |
in vitro study | GSK-J1 is selective for H3K27 demethylases of the KDM6 subfamily and specifically binds to endogenous JMJD3. GSK-J1 inhibits TNF-α production by human primary macrophages in an H3K27-dependent manner. GSK-J1 inhibits the demethylase activity of KDM5C with 8.5-fold increased potency compared with that of KDM5B at 1 mM α-ketoglutarate, with IC 50 of 11 μM and 94 μM, respectively. |