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SynKinase
GSK-J1
CHF 0.00
In stock
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| Product Details | |
|---|---|
| Synonyms | N-[2-(2-Pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alanine |
| Product Type | Chemical |
| Properties | |
| Formula | C22H23N5O2 |
| MW | 389.5 |
| CAS | 1373422-53-7 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data | Target: JMJD3 - UTX | Kinase Group: N/A | Substrate: N/A |
| InChi Key | AVZCPICCWKMZDT-UHFFFAOYSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS | Inquire |
| Product Specification Sheet | |
| Datasheet |
 Download PDF |
Description
GSK-J1 is a potent inhibitor of the H3K27 histone demethylases JMJD3 (KDM6B) and UTX (KDM6A), with IC50 values of 28nM and 53nM, respectively. GSK-J1 also has less potent inhibitory activity against KDM5B, KDM5C and KDM5A, with IC50 values of 170, 550 and 6,800nM, respectively. It shows no activity against other histone demethylases (IC50 >20μM), and displays no significant inhibitory activity against 100 protein kinases at a concentration of 30μM.
Product References
- A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response: J. Kruidenier, et al.; Nature 488, 404 (2012)
- Inhibition of demethylases by GSK-J1/J4: B. Heinemann, et al.; Nature 514, E1 (2014)
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