JPS036
Based on 1 Customer Validation
JPS036 is a HDAC3 PROTAC degrader with a DC50 of 0.44 μM. JPS036 recruits the VHL E3 ligase to form a ternary complex with HDAC3, driving proteasome-mediated degradation. JPS036 is applicable to relevant research on colon cancer.
(Pink: HDAC3 Target protein ligand; Blue: VHL ligand (HY-125905); Black: linker (HY-W105741)).
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: 99.31%
- CAS 番号: 2669785-85-5
- 分子式: C51H66FN7O7S
- 分子量:940.18
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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
- 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
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HDAC3 0.44 μM (DC50) |
VHL |
JPS036 (Compound 22) (0.1-10 μM; 24 h) selectively degrades HDAC3 in HCT116 cells, with a DC50 of 0.44 μM and a maximum HDAC3 degradation rate of 77%, while causing only minimal degradation of HDAC1 and HDAC2[1].
JPS036 is a weak inhibitor of purified class I HDAC complexes, with the strongest inhibitory activity against the HDAC3-SMRT complex (IC50 = 9.67 μM), and significantly lower inhibitory activity against the HDAC1/2-CoREST complex[1].
Treatment of HCT116 cells with JPS036 (10 μM; 24 h) induces only minimal genome-wide transcriptomic changes[1].
JPS036 (10 μM; 24-48 h) induces extremely low levels of apoptosis in HCT116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 human colon carcinoma cells
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Concentration:0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Reduced HDAC3 abundance to approximately 30% of control levels at 0.1 μM, while HDAC1 and HDAC2 remained at ~95% and ~85% of control levels, respectively.
Reduced HDAC3 abundance to ~40% of control at 1 μM, with HDAC1 and HDAC2 at ~85% and ~90% of control, respectively.
Reduced HDAC3 abundance to ~80% of control at 10 μM, with HDAC1 and HDAC2 at ~60% and ~85% of control, respectively.
Exhibited a standard dose-response curve for HDAC3 degradation with no hook effect, and achieved a maximum degradation (Dmax) of 77% for HDAC3, with a DC50 of 0.44 μM.
Achieved Dmax values of 41% and 18% for HDAC1 and HDAC2, respectively, with no measurable DC50 values.
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Cell Line:HCT116 human colon carcinoma cells
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Concentration:10 μM
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Incubation Time:24 h, 48 h
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Result:Increased the sub-G1 population to ~10% of total cells after 24 h of treatment with 10 μM JPS036.
Increased the sub-G1 population to ~20% of total cells after 48 h of treatment with 10 μM JPS036, showing minimal induction of apoptosis compared to HDAC1/2-targeting PROTACs.
化学情報
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CAS 番号 2669785-85-5
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性状 Solid
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分子量 940.18
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分子式 C51H66FN7O7S
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Color White to off-white
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SMILES
O=C(C1(CC1)F)N[C@@H](C(C)(C)C)C(N2[C@@H](C[C@H](C2)O)C(NCC3=C(C=C(C4=C(N=CS4)C)C=C3)OCCCCCCCCCCCC(NC5=CC=C(C=C5)C(NC6=C(C=CC=C6)N)=O)=O)=O)=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
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
DMSO : 100 mg/mL (106.36 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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)
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 (2.66 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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 (273 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 (protect from light, stored under nitrogen). 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 | 1.0636 mL | 5.3181 mL | 10.6363 mL | 26.5907 mL |
| 5 mM | 0.2127 mL | 1.0636 mL | 2.1273 mL | 5.3181 mL | |
| 10 mM | 0.1064 mL | 0.5318 mL | 1.0636 mL | 2.6591 mL | |
| 15 mM | 0.0709 mL | 0.3545 mL | 0.7091 mL | 1.7727 mL | |
| 20 mM | 0.0532 mL | 0.2659 mL | 0.5318 mL | 1.3295 mL | |
| 25 mM | 0.0425 mL | 0.2127 mL | 0.4255 mL | 1.0636 mL | |
| 30 mM | 0.0355 mL | 0.1773 mL | 0.3545 mL | 0.8864 mL | |
| 40 mM | 0.0266 mL | 0.1330 mL | 0.2659 mL | 0.6648 mL | |
| 50 mM | 0.0213 mL | 0.1064 mL | 0.2127 mL | 0.5318 mL | |
| 60 mM | 0.0177 mL | 0.0886 mL | 0.1773 mL | 0.4432 mL | |
| 80 mM | 0.0133 mL | 0.0665 mL | 0.1330 mL | 0.3324 mL | |
| 100 mM | 0.0106 mL | 0.0532 mL | 0.1064 mL | 0.2659 mL |
JPS036 関連分類
HY-145819 関連分類
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