Cat. No.: HY-183626

PAI-1-IN-1

고객리뷰

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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity: 99.45%
CAS No.: 1247823-40-0
화학식: C₂₃H₁₄ClN₂NaO₃
분자량:424.81

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PAI-1-IN-1 Chemical Structure

CAS No.: 1247823-40-0

사이즈

가격

재고

수량

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- In Vitro
- In Vivo
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

All MMP Isoforms :

In Vitro

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.

Apoptosis Analysis^[2]

Cell Line:

PAI-1/K562-1 and PAI-1/K562-2 cells
Concentration:

62.7 μM
Incubation Time:

72 h
Result:

Significantly increased the proportion of early and late apoptosis.

In Vivo

PAI-1-IN-1 (10 mg/kg; p.o.; daily; for 3-7 consecutive days) promotes skeletal muscle regeneration and alleviates inflammation in a cardiotoxin (CTX)-induced mouse model of skeletal muscle injury by downregulating pro-inflammatory cytokine expression, upregulating anti-inflammatory cytokine expression, and accelerating tissue repair. It enhances the phagocytic activity of macrophages (as a surrogate marker of efferocytosis), increasing the dextran uptake rate of macrophages by 14.5 percentage points^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6J (12- to 20-week-old male; CTX-induced skeletal muscle injury)^[1]
Dosage:

10 mg/kg
Administration:

p.o.; daily; 7 consecutive days/ daily; 3 consecutive days
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

CAS No. 1247823-40-0
Appearance Solid
분자량 424.81
화학식 C₂₃H₁₄ClN₂NaO₃
SMILES

O=C(C1=CC(Cl)=CC=C1NC(C2=CC=CC(C3=C4N=CC=CC4=CC=C3)=C2)=O)O[Na]
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3540 mL

11.7700 mL

23.5399 mL

5 mM

0.4708 mL

2.3540 mL

4.7080 mL

10 mM

0.2354 mL

1.1770 mL

2.3540 mL

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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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PAI-1-IN-1

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Neuronal Signaling Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Osteogenesis Compound Library

Coagulation and Anti-coagulation Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Protease Inhibitor Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Macrophage Related Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

All MMP Isoforms

Biological Activity

Chemical Information

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

PAI-1-IN-1 Related Classifications

HY-183626 Related Classifications