4-CPPC |
Catalog No.GC46630
One-Click Copy Product Info
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4-CPPC is a reversible, selective small molecule inhibitor of the pro-inflammatory protein macrophage migration inhibitor-2 (MIF-2), with Ki values of 431±37 and 33±0.7µM for MIF-1 and MIF-2, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 29553-70-6
Sample solution is provided at 25 µL, 10mM.
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4-CPPC is a reversible, selective small molecule inhibitor of the pro-inflammatory protein macrophage migration inhibitor-2 (MIF-2), with Ki values of 431±37 and 33±0.7µM for MIF-1 and MIF-2, respectively[1]. 4-CPPC inhibits MIF-1 by specifically binding to its C-terminal region and inducing conformational changes[1].
In vitro, pre-treatment with 10μM 4-CPPC for 30min, followed by overnight incubation with 1μg/mL MIF-2, attenuated Low-Density Lipoprotein (LDL) uptake in PBMC-derived macrophages[2]. Treatment of primary astrocytes with 100μM 4-CPPC for 24h attenuated MIF-2 (1μg/mL)-induced activation of the COX-2/PGE2 (Cyclooxygenase-2/Prostaglandin E2) pathway[3].
In vivo, intraperitoneal administration of 4-CPPC (5mg/kg, every other day over 4.5 weeks) markedly reduced aortic root lesion size, along with lesional macrophages and circulating cytokines/chemokines (e.g., IL-1α, IL-6, IL-15, and IFN-γ) in Apolipoprotein E knockout (Apoe–/–) mice[2]. In a rat spinal cord injury (SCI) model, intrathecal injection of 8μL 100mM 4-CPPC at the lesion site increased BBB (Basso, Beattie, and Bresnahan) scores within 21 days, significantly improving hindlimb motor recovery[3].
References:
[1] Pantouris G, Bucala R, Lolis EJ. Structural Plasticity in the C-Terminal Region of Macrophage Migration Inhibitory Factor-2 Is Associated with an Induced Fit Mechanism for a Selective Inhibitor. Biochemistry. 2018;57(26):3599-3605.
[2] El Bounkari O, Zan C, Yang B, et al. An atypical atherogenic chemokine that promotes advanced atherosclerosis and hepatic lipogenesis. Nat Commun. 2025;16(1):2297.
[3] Ji H, Zhang Y, Chen C, et al. D-dopachrome tautomerase activates COX2/PGE2 pathway of astrocytes to mediate inflammation following spinal cord injury. J Neuroinflammation. 2021;18(1):130.
| Cell experiment [1]: | |
Cell lines | PBMC-derived macrophages |
Preparation Method | Macrophages were cultured in the full RPMI 1640 medium at 37°C, and then changed to MEM medium containing 0.2% BSA for 2-4h to achieve starvation. Later, cells were pre-incubated with inhibitors (10µM AMD3100, 4-IPP, or 4-CPPC) for 30min along with 1µg/mL MIF-2 overnight. The second day, cells were cultured in the same medium added with 1% 2-hydroxypropyl-β-cyclodextrin (HPCD) at 37°C for 45min. After rinsing with PBS three times, macrophages were maintained in 25µg/mL DiI-LDL solution at 4°C for 30min and subsequently moved to 37°C for 20min. Measure cellular uptake of DiI-LDL. |
Reaction Conditions | 10µM; overnight |
Applications | 4-CPPC inhibits MIF-2-induced enhancement of LDL uptake in cells. |
| Animal experiment [1]: | |
Animal models | Male Apoe–/– mice (C57BL/6) |
Preparation Method | Eight-week-old male Apoe–/– mice were randomly divided into two groups of 11 mice each. The experimental group was administered with 100µg of 4-CPPC dissolved in physiological saline (0.9% NaCl) intraperitoneally every other day for 4.5 weeks; while the control group received saline at the same time intervals. |
Dosage form | 5mg/kg; i.p. |
Applications | Atherosclerotic lesion size in aortic root was markedly decreased in 4-CPPC-treated mice compared with controls. Similarly, there was a reduction in lesional macrophages and circulating cytokines and chemokines, such as IL-1α, IL-6, IL-15, and IFN-γ |
References: | |
| Cas No. | 29553-70-6 | SDF | |
| Canonical SMILES | OC(C1=NC=C(C(O)=O)C(C2=CC=CC(C(O)=O)=C2)=C1)=O | ||
| Formula | C14H9NO6 | M.Wt | 287.2 |
| Solubility | DMSO : 100 mg/mL (348.17 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4819 mL | 17.4095 mL | 34.8189 mL |
| 5 mM | 696.4 μL | 3.4819 mL | 6.9638 mL |
| 10 mM | 348.2 μL | 1.7409 mL | 3.4819 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)