PAI-1-IN-1
Based on 1 Customer Validation
PAI-1-IN-1 is an orally active and specific PAI-1 inhibitor with an IC50 of <6.95 μM. PAI-1-IN-1 blocks the interaction between PAI-1 and serine proteases or LRP-1, and enhances plasmin generation. PAI-1-IN-1 restores macrophage efferocytosis and promotes macrophage polarization. PAI-1-IN-1 alleviates PAI-1-mediated inhibition of Furin, promotes MT1-MMP maturation, activates the NOTCH1 signaling pathway, inhibits proliferation and induces apoptosis. PAI-1-IN-1 promotes skeletal muscle regeneration and alleviates inflammation in a mouse model of skeletal muscle injury. PAI-1-IN-1 can be used in research on skeletal muscle injury-induced inflammation and chronic myeloid leukemia.
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 1247823-40-0
- Formula: C23H14ClN2NaO3
- Molecular Weight:424.81
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
PAI-1-IN-1 (2 h) enhances efferocytosis in mouse bone marrow-derived CCR2+Ly6C+ macrophages and J774.1-GFP cells via an LRP-1-dependent mechanism[1].
PAI-1-IN-1 (62.7 μM; 72 h) exerts direct anti-tumor effects on PAI-1/K562-1 and PAI-1/K562-2 chronic myeloid leukemia cells by inhibiting proliferation, inducing apoptosis, and regulating the Furin/NICD signaling pathway[2].
PAI-1-IN-1 upregulates the protein expression level of Furin and enhances the expression level of MT1-MMP on the cell surface[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PAI-1/K562-1 and PAI-1/K562-2 cells
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Concentration:62.7 μM
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Incubation Time:72 h
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Result:Significantly increased the proportion of early and late apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (12- to 20-week-old male; CTX-induced skeletal muscle injury)[1]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 7 consecutive days/ daily; 3 consecutive days
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Result:Reduced relative mRNA expression of pro-inflammatory cytokines TNF-α, IL-1β, IFN-γ, and CCL2 in injured TA muscle on day 4 post-CTX injection.
Increased relative mRNA expression of anti-inflammatory cytokine IL-10 in injured TA muscle on day 4 post-CTX injection.
Accelerated disappearance of EBD blue staining in injured TA muscle by day 8 post-CTX injection.
Increased number of mature/restored skeletal myofibers in injured TA muscle by day 8 post-CTX injection.
Increased the percentage of CD45+CD11b+ macrophages in injured TA muscle that took up TRITC-labeled dextran from 23.9% to 38.4%.
Chemical Information
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CAS No. 1247823-40-0
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Appearance Solid
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Molecular Weight 424.81
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Formula C23H14ClN2NaO3
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SMILES
O=C(C1=CC(Cl)=CC=C1NC(C2=CC=CC(C3=C4N=CC=CC4=CC=C3)=C2)=O)O[Na]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (58.85 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. 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. 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
References
[1]. Ibrahim AA, et al. Inflammatory macrophage-derived plasminogen activator inhibitor-1 exacerbates inflammation through efferocytosis inhibition. Cell Death Discov. 2026;12(1):195. Published 2026 Mar 27. [Content Brief]
[2]. Sasaki K, et al. TM5614, an Inhibitor of Plasminogen Activator Inhibitor-1, Exerts an Antitumor Effect on Chronic Myeloid Leukemia. Tohoku J Exp Med. 2022;257(3):211-224. [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. 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 | 2.3540 mL | 11.7700 mL | 23.5399 mL | 58.8498 mL |
| 5 mM | 0.4708 mL | 2.3540 mL | 4.7080 mL | 11.7700 mL | |
| 10 mM | 0.2354 mL | 1.1770 mL | 2.3540 mL | 5.8850 mL | |
| 15 mM | 0.1569 mL | 0.7847 mL | 1.5693 mL | 3.9233 mL | |
| 20 mM | 0.1177 mL | 0.5885 mL | 1.1770 mL | 2.9425 mL | |
| 25 mM | 0.0942 mL | 0.4708 mL | 0.9416 mL | 2.3540 mL | |
| 30 mM | 0.0785 mL | 0.3923 mL | 0.7847 mL | 1.9617 mL | |
| 40 mM | 0.0588 mL | 0.2942 mL | 0.5885 mL | 1.4712 mL | |
| 50 mM | 0.0471 mL | 0.2354 mL | 0.4708 mL | 1.1770 mL |
PAI-1-IN-1 Related Classifications
Cat. No.: HY-183626
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- PAI-1-IN-1
- 1247823-40-0
- PAI-1
- Ser/Thr Protease
- Furin
- MMP
- Notch
- Apoptosis
- PAI-1/K562-2 cells
- chronic myeloid leukemia
- LRP-1
- J774.1-GFP cells
- PAI-1/K562-1 cells
- macrophage polarization
- CTX-induced mouse skeletal muscle injury model
- murine bone marrow-derived CCR2+Ly6C+ macrophages
- macrophage efferocytosis
- Inhibitor
- inhibitor
- inhibit