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Chemical Structure : PIK5-12d
CAS No.:
Catalog No.: PC-21468Not For Human Use, Lab Use Only.
PIK5-12d is a highly potent, selective, first-in-class PIKfyve PROTAC degrader, potently degrades PIKfyve protein with DC50 value of 1.48 nM and Dmax value of 97.7% in prostate cancer VCaP cells.
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PIK5-12d is a highly potent, selective, first-in-class PIKfyve PROTAC degrader, potently degrades PIKfyve protein with DC50 value of 1.48 nM and Dmax value of 97.7% in prostate cancer VCaP cells.
PIK5-12d (100 nM) causes fast degradation of PIKfyve protein with a t1/2 value of 1.5 h in VCaP cells, also effectively reduces PIKfyve in other prostate cancer PC3, LNCaP, and 22RV1 cells.
PIK5-12d is a highly specific PIKfyve degrader with only 3 proteins significantly downregulated including PIKfyve, which accounts for the off-target rate at 2 out of 7573 detectable proteins.
PIK5-12d is selective for PIKfyve over other lipid kinases.
PIK5-12d mediated-PIKfyve degradation is VHL and proteasome-dependent.
PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagy in prostate cancer cells.
PIK5-12d inhibits VCaP cell proliferation with an IC50 of 522.3 nM, exerts prolonged suppression of PIKfyve downstream signaling.
PIK5-12d (10 mg/kg) almost completely depleted PIKfyve protein in LTL-331R human prostate cancer patient-derived xenograft (PDX) model, significantly suppressed tumor proliferation in vivo.
| M.Wt | 973.21 | |
| Formula | C52H64N10O7S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N1-((S)-1-((2S,4R)-4-Hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-N6-(4-(2-((4-(2-((E)-3-methylbenzylidene)hydrazineyl)-6-morpholinopyrimidin-2-yl)oxy)ethyl)phenyl)adipamide |
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1. Chungen Li, et al. J Med Chem. 2023 Sep 14;66(17):12432-12445.
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