PPACK dihydrochloride
Based on 2 publication(s) in Google Scholar
PPACK dihydrochloride is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PPACK dihydrochloride binds to CRBN, recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (Treg) into effector-like T cells, enhances CD8+ T cell responses, and modulates the Teff:Treg balance. PPACK dihydrochloride also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PPACK dihydrochloride can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1.
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: 99.07%
- CAS 番号: 82188-90-7
- 分子式: C21H33Cl3N6O3
- 分子量:523.88
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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Immunology/Inflammation Compound Library
HY-L007
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Anti-Cardiovascular Disease Compound Library
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Ubiquitination Compound Library
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MedChemExpress（MCE）の使用を引用している文献 PPACK dihydrochloride
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Flow Cytometry
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In Vivo Efficacy Study
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Histological Imaging/Staining
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Cell Imaging/Staining
生物活性
PPACK dihydrochloride rapidly and completely degrades IKZF2, reduces the expression of CD25 and FOXP3 in inhibitory regulatory T cells (Treg), converts them into effector-like T cells, and simultaneously promotes the proliferation of effector T cells (Teff)[1].
PPACK dihydrochloride promotes the production of inflammatory cytokines IL-2 and IFNγ, enhances CD8+ T cell responses, regulates the Teff:Treg balance, and exerts a selective degradation effect on IKZF2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar ST (male, 8-10 weeks old)[2]
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Dosage:0.05 mg/kg; 0.1 mg/kg; 0.25 mg/kg; 0.5 mg/kg
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Administration:i.v.; single bolus injection
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Result:Exerted a significant, dose-dependent antithrombotic effect in both arterioles and venules.
Required a significantly higher number of laser irradiations to induce occlusive thrombi in both vessel types relative to controls at 0.5 mg/kg dose, with maximal effect immediately after injection that persisted for 60 minutes.
Identified minimal effective dose of 0.1 mg/kg for both arterioles and venules.
Increased the number of laser irradiations needed for thrombus occlusion at all active doses, with effect magnitude increasing with higher doses.
化学情報
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CAS 番号 82188-90-7
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性状 Solid
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分子量 523.88
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分子式 C21H33Cl3N6O3
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Color White to off-white
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SMILES
O=C([C@H]1N(CCC1)C([C@H](N)CC2=CC=CC=C2)=O)N[C@@H](CCCNC(N)=N)C(CCl)=O.[H]Cl.[H]Cl
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別名
Pebac; D-Phenylalanyl-prolyl-arginyl Chloromethyl Ketone; D-Phe-Pro-Arg-CH2Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Nature
2025 Feb;638(8050):490-498. PMID: 39814882
PPACK dihydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2025 Feb;638(8050):490-498. [Abstract]
Summary statistics showing the number of different immune cells in the BALF of PPACK (PPACK TFA) (62.5 μg per mouse; i.p.; every 2 days) treated mice. Each symbol indicates one mouse, and lines denote means.
PPACK dihydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2025 Feb;638(8050):490-498. [Abstract]
Airway hypersensitivity of the vehicle or PPACK (PPACK TFA) (62.5 μg per mouse; i.p.; every 2 days) treated mice measured using the forced oscillation technique. Each symbol indicates one mouse, and bars denote means.
PPACK dihydrochloride purchased from MedChemExpress. Usage Cited in: Nature. 2025 Feb;638(8050):490-498. [Abstract]
Representative AB-PAS staining of lung tissue sections of vehicle or PPACK (PPACK TFA) (62.5 μg per mouse; i.p.; every 2 days) treated mice. Scale bar, 100 μm. Statistics summarizing the PAS+ areas in the airway of indicated mice. Each symbol indicates one mouse, and lines denote means.
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J Thromb Thrombolysis
The inhibitory effect of antiplatelet drugs on spontaneous platelet aggregation on glass surfaces: an analysis based on microscopic three-dimensional topography. [Abstract]2025 Sep 9. PMID: 40924280
PPACK dihydrochloride purchased from MedChemExpress. Usage Cited in: J Thromb Thrombolysis. 2025 Sep 9. [Abstract]
PPACK (PPACK TFA)-anticoagulated PRP droplets deposited on the glass surface. The results showed that 100 μM PPACK-anticoag-ulated PRP on the glass surface retained the ability to form platelet aggregates on the glass surface.
溶剤 & 溶解度
DMSO : 100 mg/mL (190.88 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (4.77 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 (4.77 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 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.
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 (sealed storage, away from moisture)
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 (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[2]. Chen Z, et al. Development of PVTX-405 as a potent and highly selective molecular glue degrader of IKZF2 for cancer immunotherapy. Nat Commun. 2025 May 1;16(1):4095. [Content Brief]
[3]. Zhang X, et al. Discovery of a Novel Series of iso-Indolinone-Based Glutarimides as Highly Efficacious and Selective IKZF2 Molecular Glue Degraders. J Med Chem. 2025 Sep 11;68(17):18230-18257. [Content Brief]
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 (sealed storage, away from moisture). 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 | 1.9088 mL | 9.5442 mL | 19.0883 mL | 47.7209 mL |
| 5 mM | 0.3818 mL | 1.9088 mL | 3.8177 mL | 9.5442 mL | |
| 10 mM | 0.1909 mL | 0.9544 mL | 1.9088 mL | 4.7721 mL | |
| 15 mM | 0.1273 mL | 0.6363 mL | 1.2726 mL | 3.1814 mL | |
| 20 mM | 0.0954 mL | 0.4772 mL | 0.9544 mL | 2.3860 mL | |
| 25 mM | 0.0764 mL | 0.3818 mL | 0.7635 mL | 1.9088 mL | |
| 30 mM | 0.0636 mL | 0.3181 mL | 0.6363 mL | 1.5907 mL | |
| 40 mM | 0.0477 mL | 0.2386 mL | 0.4772 mL | 1.1930 mL | |
| 50 mM | 0.0382 mL | 0.1909 mL | 0.3818 mL | 0.9544 mL | |
| 60 mM | 0.0318 mL | 0.1591 mL | 0.3181 mL | 0.7953 mL | |
| 80 mM | 0.0239 mL | 0.1193 mL | 0.2386 mL | 0.5965 mL | |
| 100 mM | 0.0191 mL | 0.0954 mL | 0.1909 mL | 0.4772 mL |
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