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Chemical Structure : SPT inhibitor compound-2
Catalog No.: PC-20274Not For Human Use, Lab Use Only.
SPT inhibitor compound-2 is a potent, orally active serine palmitoyltransferase (SPT) inhibitor with IXC50 of 0.51 nM in cell-free assays.
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SPT inhibitor compound-2 is a potent, orally active serine palmitoyltransferase (SPT) inhibitor with IXC50 of 0.51 nM in cell-free assays.
Compound-2 reduced the intracellular levels of 3-ketosphinganine (3-KDS), C16, C24-Cer, and C16, C24-SM downstream of SPT in a dose-dependent manner in PL-21 cells.
Compound-2 exhibited anti-proliferative effect in PL-21 cells with GI50 of 3.32 nM, reducing the levels of the sphingolipids ceramide and sphingomyelin.
Compound-2 (3 mg/kg, oral) showed potent antitumor activity without causing significant body weight loss in the PL-21 acute myeloid leukemia mouse xenograft model.
| M.Wt | 542.95 | |
| Formula | C26H22ClF3N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Hirata Y, et al. PLoS Pathog. 2012;8(8):e1002860.
2. Katsume A, et al. Gastroenterology. 2013 Oct;145(4):865-73.
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