2. PROTAC Immunology/Inflammation
  3. Ligands for E3 Ligase Molecular Glues IKZF Family
  4. PPACK dihydrochloride

PPACK dihydrochloride  (Synonyms: Pebac; D-Phenylalanyl-prolyl-arginyl Chloromethyl Ketone; D-Phe-Pro-Arg-CH2Cl)

Cat. No.: HY-122542A Purity: 99.07%
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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.

For research use only. We do not sell to patients.

PPACK dihydrochloride

PPACK dihydrochloride Chemical Structure

CAS No. : 82188-90-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of PPACK dihydrochloride:

PPACK dihydrochloride Related Antibodies

Top Publications Citing Use of Products

View All Ligands for E3 Ligase Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) MDM2 Cereblon IAP KLHDC2 Fbxo3 RNF4 DCAF11 DCAF1 UHRF1 TRIM21 NEURL1B

View All IKZF Family Isoform Specific Products:

View All Isoforms
IKZF1 IKZF2 IKZF3 IKZF4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][3].

In Vitro

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.

PPACK dihydrochloride Related Antibodies
In Vivo

In humanized CRBN mouse models, PPACK dihydrochloride induces IKZF2 depletion and significantly inhibits MC38 tumor growth. When combined with anti-PD1 or anti-LAG3, PPACK dihydrochloride significantly improves animal survival and induces durable tumor regression compared with monotherapy with anti-PD1 or anti-LAG3[2][3].

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.
Molecular Weight

523.88

Formula

C21H33Cl3N6O3
CAS No.
Appearance

Solid

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.[H]Cl.[H]Cl
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)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9088 mL 9.5442 mL 19.0883 mL
5 mM 0.3818 mL 1.9088 mL 3.8177 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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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PPACK dihydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PPACK82188-90-7Pebac D-Phenylalanyl-prolyl-arginyl Chloromethyl Ketone D-Phe-Pro-Arg-CH2ClLigands for E3 LigaseMolecular GluesIKZF FamilyE3 ligase-recruiting MoietyIkaros zinc finger protein familyrt-PAfibrin degradatioantiplasminplasma proteaseInhibitorinhibitorinhibit

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