PT-65
Based on 1 Customer Validation
PT-65 is a GSK3α and GSK3β PROTAC degrader with DC50 values of 28.3 nM and 34.2 nM, respectively. PT-65 inhibits excessive tau phosphorylation mediated by GSK3β, Aβ and Okadaic acid (HY-N6785). PT-65 is applicable for the research of Alzheimer's disease.
(Pink: GSK-3α and GSK-3β ligand (HY-15761); Blue: Cereblon ligand (HY-10984); Black: linker).
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: 99.48%
- CAS 番号: 2721998-87-2
- 分子式: C51H63N13O12S
- 分子量:1082.19
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保管条件:Powder -20°C, 3 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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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GSK-3α 28.3 nM (DC50) |
GSK-3β 34.2 nM (DC50) |
PT-65 (62.5-1000 nM; 48 h) dose-dependently reduces GSK3β-mediated tau hyperphosphorylation at serine 396, serine 404, and threonine 205 sites in GSK3β-overexpressing HEK-293T cells by inducing GSK3β degradation, with phosphorylated tau levels recovering fully 12 h after compound washout[1].
PT-65 (0-100 μM; 72 h) protects SH-SY5Y cells from Aβ42-induced neurotoxicity by dose-dependently reducing GSK3 levels and subsequent tau hyperphosphorylation, with no intrinsic cytotoxicity up to 100 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GSK3β-overexpressing HEK-293T cells
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Concentration:62.5, 125, 250, 500 and 1000 nM (24 h dose-dependent); 1 μM (washout recovery)
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Incubation Time:24 h (dose-dependent); 24 h treatment followed by up to 36 h washout recovery
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Result:Induced dose-dependent degradation of GSK3β, accompanied by dose-dependent reduction of phosphorylated tau at serine 396, serine 404, and threonine 205 sites; total tau levels remained unchanged.
Recovered GSK3β levels gradually after washout of 1 μM PT-65, and restored phosphorylated tau levels fully by 12 h post-washout.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 3 months old, 280-300 g, unilateral hippocampal microinjection of okadaic acid to induce AD-like pathology)[1]
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Dosage:200 μM/5 μL; 600 μM/5 μL
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Administration:i.c.v.; two doses: 72 h pre-model establishment and 72 h post-model establishment
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Result:Reduced escape latency times on day 3, day 4, and day 5 posttreatment (high dose: 600 μM/5 μL) compared to OA-treated rats.
Reduced escape latency compared to OA-treated rats (low dose: 200 μM/5 μL).
Increased time spent in the target quadrant in probe trial compared to OA-treated rats (both doses).
Dose-dependently reduced hippocampal levels of GSK3α, GSK3β, and hyperphosphorylated tau at the S404, S396, and T205 sites compared to OA-treated rats.
Reduced the density of p-T205-tau-positive staining in hippocampal tissue compared to OA-treated rats.
化学情報
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CAS 番号 2721998-87-2
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性状 Solid
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分子量 1082.19
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分子式 C51H63N13O12S
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Color Light yellow to green yellow
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SMILES
O=C(C1=C(N)N=CC(C2=CC=C(S(=O)(N3CCN(CCCCC4=CN(CCOCCOCCOCCOCCOCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)N=N4)CC3)=O)C=C2)=N1)NC8=CC=CN=C8
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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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (92.41 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)
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 (2.31 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.
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 (271 KB)
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SDS (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 | 0.9241 mL | 4.6203 mL | 9.2405 mL | 23.1013 mL |
| 5 mM | 0.1848 mL | 0.9241 mL | 1.8481 mL | 4.6203 mL | |
| 10 mM | 0.0924 mL | 0.4620 mL | 0.9241 mL | 2.3101 mL | |
| 15 mM | 0.0616 mL | 0.3080 mL | 0.6160 mL | 1.5401 mL | |
| 20 mM | 0.0462 mL | 0.2310 mL | 0.4620 mL | 1.1551 mL | |
| 25 mM | 0.0370 mL | 0.1848 mL | 0.3696 mL | 0.9241 mL | |
| 30 mM | 0.0308 mL | 0.1540 mL | 0.3080 mL | 0.7700 mL | |
| 40 mM | 0.0231 mL | 0.1155 mL | 0.2310 mL | 0.5775 mL | |
| 50 mM | 0.0185 mL | 0.0924 mL | 0.1848 mL | 0.4620 mL | |
| 60 mM | 0.0154 mL | 0.0770 mL | 0.1540 mL | 0.3850 mL | |
| 80 mM | 0.0116 mL | 0.0578 mL | 0.1155 mL | 0.2888 mL |
PT-65 関連分類
HY-153166 関連分類
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