All AbMole products are for research use only, cannot be used for human consumption.
For this product's availability, delivery time and price, please email [email protected] directly or click the "Inquiry Now" button below.
PIK5-12d is a highly active and selective PIKfyve degrader constructed based on the PIKfyve inhibitor Apilimod and VHL ligand. The compound induced PIKfyve degradation with a DC50 value of 1.5 nM and a Dmax of 97.7% could be achieved after treating prostate cancer VCaP cells for 24 h. The PIK5-12d was also found to be highly active and highly selective for PIKfyve degradation. Secondly, PIK5-12d could effectively inhibit the autophagy pathway in a variety of prostate cancer cells by degrading PIKfyve and significantly induced obvious vacuolization of tumor cytoplasm. In terms of VCaP cell proliferation inhibition, the degrader PIK5-12d was more advantageous compared to the inhibitor Apilimod. In addition, PIK5-12d was effective in inducing PIKfyve degradation as well as inhibiting tumor growth in a human-derived tissue xenograft (PDX) model.PIK5-12d, as the first highly active and selective PIKfyve degrader, may serve as a valuable tool molecule to explore the feasibility of targeting PIKfyve as a therapeutic oncology strategy.
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PROTAC Products |
|---|
| MS4322
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. |
| xStAx-VHLL TFA
xStAx-VHLL TFA, a PROTAC, sustains β-catenin degradation and manifested strong inhibition of Wnt signaling. xStAx-VHLL TFA promotes β-catenin ubiquitination. |
| (S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine
(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual target PROTAC that can not only target to the ubiquitination and degradation of Smad3 but also improve the HIF-α protein level. |
| MTX-23
MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis. |
| YD23
YD23 is a SMARCA2 PROTAC. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
