For research use only. Not for therapeutic Use.
GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin[1].
GSK2646264 (0.01-10 μM; 1 h) significantly inhibits anti‐IgE (but not C5a)‐induced histamine release from skin mast cells in a concentration‐dependent manner. The IC50 is 0.7 μM and the IC90 is 6.8 μM[2].
GSK2646264 cream (0.5, 1, and 3% [wt/wt]; 1 cm2; 4 and 24 h) inhibits anti‐IgE‐induced histamine release from mast cells in ex vivo human skin[2].
| Catalog Number | I028351 |
| CAS Number | 1398695-47-0 |
| Synonyms | 7-[2-methoxy-6-[(4-methylpyridin-2-yl)methoxy]phenyl]-2,3,4,5-tetrahydro-1H-3-benzazepine |
| Molecular Formula | C24H26N2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H26N2O2/c1-17-8-13-26-21(14-17)16-28-23-5-3-4-22(27-2)24(23)20-7-6-18-9-11-25-12-10-19(18)15-20/h3-8,13-15,25H,9-12,16H2,1-2H3 |
| InChIKey | KYANYGKXMNYFBX-UHFFFAOYSA-N |
| SMILES | CC1=CC(=NC=C1)COC2=CC=CC(=C2C3=CC4=C(CCNCC4)C=C3)OC |
| Reference | [1]. Barker MD, et al. Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease. Bioorg Med Chem Lett. 2018 Nov 15;28(21):3458-3462. [2]. Ramirez Molina C, et al. GSK2646264, a spleen tyrosine kinase inhibitor, attenuates the release of histamine in ex vivo human skin. Br J Pharmacol. 2019 Apr;176(8):1135-1142. |
