YOK-1304
Based on 1 Customer Validation
YOK-1304 is a p62/Sequestosome-1/SQSTM1 ligand that binds to the p62-ZZ domain. YOK-1304 promotes p62 self-oligomerization and LC3 interaction to facilitate autophagic targeting and p62-dependent selective autophagy. YOK-1304 enhances autophagic flux, induces LC3 puncta formation and p62-LC3 colocalization, and serves as an autophagy-targeting ligand (ATL) that can be linked to target-binding ligands to generate AUTOTAC degraders. YOK-1304 is used in research on cervical cancer and pancreatic cancer.
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- Purity : 98.60%
- CAS No.: 2409960-03-6
- 화학식: C28H35NO4
- 분자량:449.58
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| ACHN | IC50 |
>20 μM
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Cytotoxicity against human ACHN cells assessed as reduction in cell viability by water-soluble tetrazolium salt-based assay.
Cytotoxicity against human ACHN cells assessed as reduction in cell viability by water-soluble tetrazolium salt-based assay.
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35173167 |
In Vitro
YOK-1304 (1 mM; 2 h) acts as an autophagy-targeting ligand that induces p62 self-oligomerization in HEK293T cells[1].
YOK-1304 (2.5 μM; 24 h) activates and targets p62 to autophagic membranes in HeLa cells, and enhances autophagic flux in HeLa cells[1].
YOK-1304 increases LC3 II accumulation but fails to degrade mutant KRAS in PANC-1, MIA PaCa-2, and SK-CO-1 cells, indicating that YOK-1304 alone is insufficient for KRAS degradation[2].
YOK-1304 (1 μM; 24 h) does not induce significant degradation of ERβ in MCF7 cells[1].
YOK-1304 shows low cytotoxicity in ACHN cells with an IC50 of >20 μM[1].
YOK-1304 alone does not alter the secondary structure of KRASG12D, indicating that mutant KRAS recognition is mediated by the KRB moiety[2].
YOK-1304 (20 µM; 12 h) induces p62-dependent selective autophagy in PANC-1 cells, as evidenced by increased LC3 puncta formation and p62-LC3 co-localization[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HeLa
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Concentration:2.5 μM
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Incubation Time:24 h
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Result:Induced the formation and co-localization of p62 and LC3 punctate structures.
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Cell Line:HeLa
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Concentration:2.5 μM
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Incubation Time:24 h
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Result:Enhanced the autophagic turnover of p62 and LC3, with a normalized p62 autophagic flux index of 2.8 and a normalized LC3 II/I autophagic flux index of 4.2.
Chemical Information
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CAS No. 2409960-03-6
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Appearance Solid
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분자량 449.58
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화학식 C28H35NO4
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Color White to off-white
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SMILES
CC(C)NC[C@@H](O)COC1=CC(OCCCC2=CC=CC=C2)=C(OCC3=CC=CC=C3)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (222.43 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
순도&문서
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Data Sheet (273 KB)
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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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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 | 2.2243 mL | 11.1215 mL | 22.2430 mL | 55.6075 mL |
| 5 mM | 0.4449 mL | 2.2243 mL | 4.4486 mL | 11.1215 mL | |
| 10 mM | 0.2224 mL | 1.1121 mL | 2.2243 mL | 5.5607 mL | |
| 15 mM | 0.1483 mL | 0.7414 mL | 1.4829 mL | 3.7072 mL | |
| 20 mM | 0.1112 mL | 0.5561 mL | 1.1121 mL | 2.7804 mL | |
| 25 mM | 0.0890 mL | 0.4449 mL | 0.8897 mL | 2.2243 mL | |
| 30 mM | 0.0741 mL | 0.3707 mL | 0.7414 mL | 1.8536 mL | |
| 40 mM | 0.0556 mL | 0.2780 mL | 0.5561 mL | 1.3902 mL | |
| 50 mM | 0.0445 mL | 0.2224 mL | 0.4449 mL | 1.1121 mL | |
| 60 mM | 0.0371 mL | 0.1854 mL | 0.3707 mL | 0.9268 mL | |
| 80 mM | 0.0278 mL | 0.1390 mL | 0.2780 mL | 0.6951 mL | |
| 100 mM | 0.0222 mL | 0.1112 mL | 0.2224 mL | 0.5561 mL |
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