2. PROTAC PI3K/Akt/mTOR Autophagy
  3. PROTACs PIKfyve Autophagy
  4. 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)).

For research use only. We do not sell to patients.

PIK5-12d

PIK5-12d Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PIK5-12d Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PIK5-12d

View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target[1]

VHL

 

In Vitro

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.

PIK5-12d Related Antibodies

Western Blot Analysis[1]

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.
In Vivo

PIK5-12d (4-10 mg/kg, i.p., once daily, 3 days or 15 mg/kg, i.p., 5 days on and 2 days off, 17 days) significantly suppresses tumor proliferation in male CB17 SCID mice bearing LTL-331R human prostate cancer PDX tumors [1].

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.
Molecular Weight

973.19

Formula

C52H64N10O7S
Appearance

Solid

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
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0275 mL 5.1377 mL 10.2755 mL
5 mM 0.2055 mL 1.0275 mL 2.0551 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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
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PIK5-12d Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PIK5-12dPROTACsPIKfyveAutophagyFYVE domain-containing phosphatidylinositol 3-phosphate 5-kinasePhosphatidylinositol 3-phosphate 5-kinaseFab1PROTACprostate cancerVHLInhibitorinhibitorinhibit

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