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Chemical Structure : PERK inhibitor 28
Catalog No.: PC-49644Not For Human Use, Lab Use Only.
PERK inhibitor 28 is a potent, selective, and orally bioavailable PERK inhibitor with biochemical IC50 of 2 nM, and cellular IC50 of 9 nM in p-eIF2α cellular TR-FRET assays.
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PERK inhibitor 28 is a potent, selective, and orally bioavailable PERK inhibitor with biochemical IC50 of 2 nM, and cellular IC50 of 9 nM in p-eIF2α cellular TR-FRET assays.
PERK inhibitor 28 shows a very clean kinase selectivity profile with S(35), S(10), and S(1) selectivity scores of 0.007, 0, and 0, respectively at a concentration of 1 μM in the 468-kinase scanMAXSM panel.
PERK inhibitor 28 (10 mg/kg BID) showed statistically significant tumor growth inhibition in the clear cell renal cell carcinoma (ccRCC)xenograft model 786-O.
| M.Wt | 468.50 | |
| Formula | C25H26F2N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Veronica Calvo, et al. Bioorg Med Chem Lett. 2021 Jul 1;43:128058.
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