PIK5-12d
Based on 1 publication(s) in Google Scholar
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).
For research use only. We do not sell to patients.
- Purity: 99.15%
- CAS No.: 3036457-38-9
- Formula: C52H64N10O7S
- Molecular Weight:973.19
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PIK5-12d
MoreAll PROTACs Isoforms
More
Biological Activity
|
VHL |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| VCaP | IC50 |
1200 nM
Compound: 12d; PIK5-12d
|
Antiproliferative activity against human VCaP cells assessed as inhibition of cell proliferation incubated for 4 hrs followed by culturing in compound-free medium for 2 weeks by crystal violet staining based analysis
Antiproliferative activity against human VCaP cells assessed as inhibition of cell proliferation incubated for 4 hrs followed by culturing in compound-free medium for 2 weeks by crystal violet staining based analysis
|
[PMID: 37605297] |
| VCaP | IC50 |
522.3 nM
Compound: 12d; PIK5-12d
|
Antiproliferative activity against human VCaP cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by culturing in compound-free medium for 2 weeks by crystal violet staining based analysis
Antiproliferative activity against human VCaP cells assessed as inhibition of cell proliferation incubated for 24 hrs followed by culturing in compound-free medium for 2 weeks by crystal violet staining based analysis
|
[PMID: 37605297] |
| VCaP | IC50 |
55.89 nM
Compound: 12d; PIK5-12d
|
Antiproliferative activity against human VCaP cells assessed as inhibition of cell proliferation incubated for 2 weeks by crystal violet staining based analysis
Antiproliferative activity against human VCaP cells assessed as inhibition of cell proliferation incubated for 2 weeks by crystal violet staining based analysis
|
[PMID: 37605297] |
PIK5-12d (1-10000 nM, 24 h) induces degradation of PIKfyve in VCaP cells, with a DC50 of 1.48 nM and a Dmax of 97.9% for PIKfyve degradation[1].
PIK5-12d (0-3000 nM, 24 h) effectively reduces PIKfyve protein levels in multiple prostate cancer cell lines, including PC3, LNCaP, and 22RV1 cells[1].
PIK5-12d (0-3000 nM, 24 h) induces massive cytoplasmic vacuolization in RFP-labeled DU145 cells and increases autophagy markers LC3A/B and p62 in PC3, LNCaP, and 22RV1 cells[1].
PIK5-12d (24 h) inhibits proliferation of VCaP cells with an IC50 of 522.3 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:PC3, LNCaP, and 22RV1 cells
-
Concentration:0, 10, 100, 300, 1000, 3000 nM
-
Incubation Time:24 h
-
Result:Induced degradation of PIKfyve.
Increased autophagy markers LC3A/B and p62.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:LTL-331R human prostate cancer xenograft tumor tissues were subcutaneously implanted into both sides of the dorsal flanks of male CB17 severe combined immunodeficiency (SCID) mice to construct the in vivo tumor model [1]
-
Dosage:4, 10, 15 mg/kg
-
Administration:i.p., once daily, 3 days or 5 days on and 2 days off, 17 days
-
Result:Depleted PIKfyve protein in LTL-331R human prostate cancer PDX tumor tissues.
Induced tumor cell death.
Suppressed tumor proliferation.
Triggered the increase of autophagy marker LC3A/B in LTL-331R PDX tumor tissues.
Chemical Information
-
CAS No. 3036457-38-9
-
Appearance Solid
-
Molecular Weight 973.19
-
Formula C52H64N10O7S
-
Color Off-white to light yellow
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Cancers (Basel)
Autophagy Blockage Up-Regulates HLA-Class-I Molecule Expression in Lung Cancer and Enhances Anti-PD-L1 Immunotherapy Efficacy. [Abstract]2024 Sep 26;16(19):3272. PMID: 39409895
Solvent & Solubility
DMSO : 200 mg/mL (205.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (274 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0275 mL | 5.1377 mL | 10.2755 mL | 25.6887 mL |
| 5 mM | 0.2055 mL | 1.0275 mL | 2.0551 mL | 5.1377 mL | |
| 10 mM | 0.1028 mL | 0.5138 mL | 1.0275 mL | 2.5689 mL | |
| 15 mM | 0.0685 mL | 0.3425 mL | 0.6850 mL | 1.7126 mL | |
| 20 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2844 mL | |
| 25 mM | 0.0411 mL | 0.2055 mL | 0.4110 mL | 1.0275 mL | |
| 30 mM | 0.0343 mL | 0.1713 mL | 0.3425 mL | 0.8563 mL | |
| 40 mM | 0.0257 mL | 0.1284 mL | 0.2569 mL | 0.6422 mL | |
| 50 mM | 0.0206 mL | 0.1028 mL | 0.2055 mL | 0.5138 mL | |
| 60 mM | 0.0171 mL | 0.0856 mL | 0.1713 mL | 0.4281 mL | |
| 80 mM | 0.0128 mL | 0.0642 mL | 0.1284 mL | 0.3211 mL | |
| 100 mM | 0.0103 mL | 0.0514 mL | 0.1028 mL | 0.2569 mL |
Powered by Bioz