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Chemical Structure : STK17A/B inhibitor 9
Catalog No.: PC-22555Not For Human Use, Lab Use Only.
STK17A/B inhibitor 9 is a potent and selective, orally active STK17A/B inhibitor with IC50 of 23 nM (STK17A/DRAK1).
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STK17A/B inhibitor 9 is a potent and selective, orally active STK17A/B inhibitor with IC50 of 23 nM (STK17A/DRAK1).
STK17A/B inhibitor 9 shows high potency against STK17B (DRAK2) with 98.5% inhibition at 1 uM concentration.
STK17A/B inhibitor 9 shows moderate off-target inhibition only for AAK1, MYLK4, and NEK3/5, very low inhibitory potency against CLK4 (IC50 > 10,000 nM).
STK17A/B inhibitor 9 (1-10 uM) dose-dependently decreases STK17A, decreases levels of phosphorylated-p53 Serine-20 and phosphorylated-ILK Serine-246 on HEK293 cells overexpressing STK17A.
STK17A/B inhibitor 9 has EC50 values around or below 1 μM in several AML cell lines.
STK17A/B inhibitor 9 shows good oral bioavailability for in vivo efficacy studies in several AML PDX mouse models.
| M.Wt | 453.55 | |
| Formula | C26H27N7O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Sana Chaudhry, et al. ACS Med Chem Lett. 2024 May 20;15(6):945-949.
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