PIK5-12d
PIK5-12d is a PROTAC PIKfyve degrader (DC50 = 1.48 nM) . PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagic flux in multiple prostate cancer cells. PIK5-12d inhibits prostate cancer cell proliferation. PIK5-12d significantly suppresses tumor proliferation in mice bearing LTL-331R human prostate cancer PDX tumors. PIK5-12d can be used for the study of prostate cancer. (Pink: PIKfyve ligand (HY-175631), Blue: VHL Ligand (HY-125845), Black: Linker, PIKfyve ligand-linker conjugate (HY-175632) ) [1].
Product Specifications
UNSPSC
12352005
Target
Autophagy; PIKfyve; PROTACs
Type
Reference compound
Related Pathways
Autophagy; PI3K/Akt/mTOR; PROTAC
Applications
COVID-19-immunoregulation
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/pik5-12d.html
Purity
99.90
Solubility
DMSO : 200 mg/mL (ultrasonic)
Smiles
CC1=CC=CC(/C=N/NC2=NC(OCCC3=CC=C(NC(CCCCC(N[C@H](C(N4[C@@H](C[C@H](C4)O)C(NCC5=CC=C(C=C5)C6=C(N=CS6)C)=O)=O)C(C)(C)C)=O)=O)C=C3)=NC(N7CCOCC7)=C2)=C1
Molecular Formula
C52H64N10O7S
Molecular Weight
973.19
References & Citations
[1]Li C, et al. Discovery of a First-in-Class Degrader for the Lipid Kinase PIKfyve. J Med Chem. 2023 Sep 14;66 (17) :12432-12445.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Von Hippel-Lindau (VHL)
Available Sizes
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