4-CPPC是一种可逆的，选择性的促炎蛋白巨噬细胞迁移抑制因子-2（MIF-2）的小分子抑制剂，对MIF-1和MIF-2的Ki值分别为431±37和33±0.7µM。
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.
4-CPPC是一种可逆的，选择性的促炎蛋白巨噬细胞迁移抑制因子-2（MIF-2）的小分子抑制剂，对MIF-1和MIF-2的Ki值分别为431±37和33±0.7µM。4-CPPC通过特异性结合MIF-1的C端区域并诱导构象变化，从而发挥抑制作用[1]。
体外实验中，10μM 4-CPPC预处理30分钟后，与1μg/mL MIF-2共同孵育过夜，可抑制PBMC来源巨噬细胞中的低密度脂蛋白（LDL）摄取[2]。用100μM 4-CPPC处理原代星形胶质细胞24小时，可减弱1μg/mL MIT-2诱导的胞内环氧合酶-2/前列腺素E2（COX-2/PGE2）通路的激活[3]。
体内实验中，在载脂蛋白E敲除（Apoe⁻/⁻）小鼠中，以5mg/kg剂量腹腔注射4-CPPC（每隔一天一次，持续4.5周）可显著降低主动脉根部斑块面积，并伴随病灶巨噬细胞及循环细胞因子/趋化因子的减少（如IL-1α、IL-6、IL-15和IFN-γ）[2]。在大鼠脊髓损伤模型中，于病变部位鞘内注射8μL 100mM 4-CPPC，可在21天内提高BBB运动评分，显著改善后肢运动功能恢复[3]。
| 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 | ||
| 分子式 | C14H9NO6 | 分子量 | 287.2 |
| 溶解度 | DMSO : 100 mg/mL (348.17 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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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 |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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- Purity: >95.00% Appearance: A solid
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