WZS0347
Based on 1 Customer Validation
WZS0347 is a MITF PROTAC degrader. WZS0347 effectively reduces MITF protein levels in various melanoma cell lines. WZS0347 induces MITF degradation via the cereblon-dependent ubiquitin-proteasome pathway, downregulates the expression of downstream target genes of MITF, and inhibits the colony formation and migration abilities of cancer cells. WZS0347 can be used in melanoma-related research.
(Pink: Microphthalmia Associated Transcription Factor (MITF) ligand (HY-179718); Blue: Cereblon ligand (HY-131717); Black: linker (HY-22391)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.06%
- 分子式: C41H42N8O9
- 分子量:790.82
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
Cereblon |
体外実験
WZS0347 (10 nM-10000 nM; 24 h) induces concentration-dependent degradation of MITF in B16F10 mouse melanoma cells[1].
WZS0347 (1 μM; 1-24 h) induces time-dependent degradation of MITF in B16F10 mouse melanoma cells[1].
WZS0347 (1 nM-1000 nM; 12 h) induces MITF degradation in human melanoma A375 cells in a concentration-dependent manner[1].
WZS0347 (1 nM-1000 nM; 24 h) induces concentration-dependent degradation of MITF in GAK human melanoma cells[1].
WZS0347 (1 μM; 24 h) induces MITF degradation in B16F10 mouse melanoma cells through binding to MITF, as pretreatment with the MITF ligand TT-012 (HY-156483) reverses this degradation effect[1].
WZS0347 (1 μM; 24 h)-induced MITF degradation in B16F10 mouse melanoma cells is dependent on CRBN, as pretreatment with the CRBN ligand Lenalidomide (HY-A0003) reverses this degradation process[1].
WZS0347 (1 μM; 24 h) induces proteasome-dependent degradation of MITF in B16F10 mouse melanoma cells, as pretreatment with a proteasome inhibitor abrogates this degradation[1].
WZS0347 (1 μM; 0-24 h) shortens the half-life of MITF protein in B16F10 mouse melanoma cells, reducing the basal half-life from 12 h[1].
WZS0347 (0.3 μM) downregulates the mRNA levels of MITF and its downstream target genes TYR and Trpm1 in B16F10 mouse melanoma cells[1].
WZS0347 (100 nM-1000 nM; 5 days) inhibits colony formation of B16F10 mouse melanoma cells in a dose-dependent manner[1].
WZS0347 (0.5-1 μM; 24 h) inhibits the migration of B16F10 mouse melanoma cells and A375 human melanoma cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:B16F10 mouse melanoma cells
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Concentration:0.1 μM, 1 μM
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Incubation Time:48 h
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Result:Induced 78% MITF degradation at 0.1 μM after 48 h.
Induced 80% MITF degradation at 1 μM after 48 h.
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Cell Line:B16F10 mouse melanoma cells
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Concentration:10 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM, 10000 nM
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Incubation Time:24 h
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Result:Caused concentration-dependent reduction of MITF protein levels over 24 h.
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Cell Line:B16F10 mouse melanoma cells
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Concentration:1 μM
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Incubation Time:1 h, 2 h, 4 h, 12 h, 24 h
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Result:Caused significant MITF depletion starting at 12 h of treatment.
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Cell Line:A375 human melanoma cells
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Concentration:1 nM, 3 nM, 7 nM, 15 nM, 30 nM, 62 nM, 125 nM, 250 nM, 500 nM, 1000 nM
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Incubation Time:12 h
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Result:Caused concentration-dependent reduction of MITF protein levels over 12 h.
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Cell Line:GAK human melanoma cells
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Concentration:1 nM, 3 nM, 7 nM, 15 nM, 30 nM, 62 nM, 125 nM, 250 nM, 500 nM, 1000 nM
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Incubation Time:24 h
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Result:Caused concentration-dependent reduction of MITF protein levels over 24 h.
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Cell Line:B16F10 mouse melanoma cells
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Concentration:1 μM TT-012 (HY-156483) (pre-incubation), 1 μM this compound
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Incubation Time:2 h (TT-012 pre-incubation), 24 h (this compound)
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Result:Reversed MITF degradation when cells were pretreated with TT-012.
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Cell Line:B16F10 mouse melanoma cells
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Concentration:1 μM Lenalidomide (HY-A0003) (pre-incubation), 1 μM this compound
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Incubation Time:2 h (lenalidomide pre-incubation), 24 h (this compound)
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Result:Reversed MITF degradation when cells were pretreated with lenalidomide.
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Cell Line:B16F10 mouse melanoma cells
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Concentration:1 μM
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Incubation Time:2 h (proteasome inhibitor pre-incubation), 24 h (this compound)
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Result:Abolished MITF degradation when cells were pretreated with proteasome inhibitor.
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Cell Line:B16F10 mouse melanoma cells
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Concentration:1 μM Cycloheximide (HY-12320) + 1 μM this compound
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Incubation Time:0 h, 1 h, 2 h, 4 h, 12 h, 24 h
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Result:Significantly shortened MITF's basal half-life from 12 h.
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Cell Line:B16F10 mouse melanoma cells
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Concentration:100 nM, 300 nM, 1000 nM
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Incubation Time:5 days
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Result:Caused dose-dependent suppression of colony formation over 5 days.
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Cell Line:B16F10 mouse melanoma cells, A375 human melanoma cells
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Concentration:0.5 μM, 1 μM
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Incubation Time:24 h
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Result:Suppressed cell migration in both B16F10 and A375 cells in a dose-dependent manner over 24 h.
化学情報
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性状 Solid
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分子量 790.82
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分子式 C41H42N8O9
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Color White to yellow
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SMILES
O=C(NCCCCCCCNC1=CC(NC(/C=C/C2=CC=CO2)=O)=NC(NC(/C=C/C3=CC=CO3)=O)=C1)CNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (126.45 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.16 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
純度とドキュメンテーション
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データシート (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
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- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 1.2645 mL | 6.3226 mL | 12.6451 mL | 31.6128 mL |
| 5 mM | 0.2529 mL | 1.2645 mL | 2.5290 mL | 6.3226 mL | |
| 10 mM | 0.1265 mL | 0.6323 mL | 1.2645 mL | 3.1613 mL | |
| 15 mM | 0.0843 mL | 0.4215 mL | 0.8430 mL | 2.1075 mL | |
| 20 mM | 0.0632 mL | 0.3161 mL | 0.6323 mL | 1.5806 mL | |
| 25 mM | 0.0506 mL | 0.2529 mL | 0.5058 mL | 1.2645 mL | |
| 30 mM | 0.0422 mL | 0.2108 mL | 0.4215 mL | 1.0538 mL | |
| 40 mM | 0.0316 mL | 0.1581 mL | 0.3161 mL | 0.7903 mL | |
| 50 mM | 0.0253 mL | 0.1265 mL | 0.2529 mL | 0.6323 mL | |
| 60 mM | 0.0211 mL | 0.1054 mL | 0.2108 mL | 0.5269 mL | |
| 80 mM | 0.0158 mL | 0.0790 mL | 0.1581 mL | 0.3952 mL | |
| 100 mM | 0.0126 mL | 0.0632 mL | 0.1265 mL | 0.3161 mL |
WZS0347 関連分類
HY-179717 関連分類
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Keywords
- WZS0347
- WZS 0347
- WZS-0347
- PROTACs
- Microphthalmia Associated Transcription Factor (MITF)
- PROTAC
- Microphthalmia Associated Transcription Factor
- Trpm1
- CRBN
- cereblon-dependent ubiquitin-proteasome pathway
- Microphthalmia-associated transcription factor
- TYR
- GAK human melanoma cells
- B16F10 mouse melanoma cells
- A375 human melanoma cells
- melanoma
- MITF
- Inhibitor
- inhibitor
- inhibit