PPACK TFA
Based on 2 publication(s) in Google Scholar
PPACK TFA is an orally active, selective molecular glue degrader targeting IKZF2. Through a molecular glue mechanism, PPACK TFA 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 TFA also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of Treg. PPACK TFA can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti-PD1.
For research use only. We do not sell to patients.
- Purity: 96.79%
- CAS No.: 157379-44-7
- Formula: C23H32ClF3N6O5
- Molecular Weight:564.99
-
Storage:
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 Citing Use of MedChemExpress (MCE) PPACK TFA
More-
Flow Cytometry
-
In Vivo Efficacy Study
-
Histological Imaging/Staining
-
Cell Imaging/Staining
Biological Activity
PPACK TFA 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 TFA 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.
-
Animal Model:Wistar ST (male, 8-10 weeks old)[2]
-
Dosage:0.05 mg/kg; 0.1 mg/kg; 0.25 mg/kg; 0.5 mg/kg
-
Administration:i.v.; single bolus injection
-
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.
Chemical Information
-
CAS No. 157379-44-7
-
Appearance Solid
-
Molecular Weight 564.99
-
Formula C23H32ClF3N6O5
-
Color White to off-white
-
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.O=C(C(F)(F)F)O
-
Sequence
{d-Phe}-Pro-{Arg-Chloromethylketone}
-
Sequence Shortening
{d-Phe}-P-{Arg-Chloromethylketone}
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
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)
-
Journal Impact Factor
-
Most Recent
-
Nature
2025 Feb;638(8050):490-498. PMID: 39814882
PPACK TFA 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 TFA 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 TFA 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.
-
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 TFA 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.
Solvent & Solubility
DMSO : 250 mg/mL (442.49 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (283 KB)
-
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)
-
Handling Instructions (2659 KB)
References
[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 | 1.7699 mL | 8.8497 mL | 17.6994 mL | 44.2486 mL |
| 5 mM | 0.3540 mL | 1.7699 mL | 3.5399 mL | 8.8497 mL | |
| 10 mM | 0.1770 mL | 0.8850 mL | 1.7699 mL | 4.4249 mL | |
| 15 mM | 0.1180 mL | 0.5900 mL | 1.1800 mL | 2.9499 mL | |
| 20 mM | 0.0885 mL | 0.4425 mL | 0.8850 mL | 2.2124 mL | |
| 25 mM | 0.0708 mL | 0.3540 mL | 0.7080 mL | 1.7699 mL | |
| 30 mM | 0.0590 mL | 0.2950 mL | 0.5900 mL | 1.4750 mL | |
| 40 mM | 0.0442 mL | 0.2212 mL | 0.4425 mL | 1.1062 mL | |
| 50 mM | 0.0354 mL | 0.1770 mL | 0.3540 mL | 0.8850 mL | |
| 60 mM | 0.0295 mL | 0.1475 mL | 0.2950 mL | 0.7375 mL | |
| 80 mM | 0.0221 mL | 0.1106 mL | 0.2212 mL | 0.5531 mL | |
| 100 mM | 0.0177 mL | 0.0885 mL | 0.1770 mL | 0.4425 mL |