2. Metabolic Enzyme/Protease Stem Cell/Wnt Neuronal Signaling Apoptosis
  3. PAI-1 Ser/Thr Protease Furin MMP Notch Apoptosis
  4. TM5614 sodium

TM5614 sodium is an orally active and specific PAI-1 inhibitor with an IC50 of <6.95 μM. TM5614 sodium blocks the interaction between PAI-1 and serine proteases or LRP-1, and enhances plasmin generation. TM5614 sodium restores macrophage efferocytosis and promotes macrophage polarization. TM5614 sodium alleviates PAI-1-mediated inhibition of Furin, promotes MT1-MMP maturation, activates the NOTCH1 signaling pathway, inhibits proliferation and induces apoptosis. TM5614 sodium promotes skeletal muscle regeneration and alleviates inflammation in a mouse model of skeletal muscle injury. TM5614 sodium can be used in research on skeletal muscle injury-induced inflammation and chronic myeloid leukemia.

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TM5614 sodium

TM5614 sodium Chemical Structure

CAS No. : 1247823-40-0

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TM5614 sodium Related Antibodies

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Description

TM5614 sodium is an orally active and specific PAI-1 inhibitor with an IC50 of <6.95 μM. TM5614 sodium blocks the interaction between PAI-1 and serine proteases or LRP-1, and enhances plasmin generation. TM5614 sodium restores macrophage efferocytosis and promotes macrophage polarization. TM5614 sodium alleviates PAI-1-mediated inhibition of Furin, promotes MT1-MMP maturation, activates the NOTCH1 signaling pathway, inhibits proliferation and induces apoptosis. TM5614 sodium promotes skeletal muscle regeneration and alleviates inflammation in a mouse model of skeletal muscle injury. TM5614 sodium can be used in research on skeletal muscle injury-induced inflammation and chronic myeloid leukemia[1][2].

In Vitro

TM5614 (2 h) sodium enhances efferocytosis in mouse bone marrow-derived CCR2+Ly6C+ macrophages and J774.1-GFP cells via an LRP-1-dependent mechanism[1].
TM5614 (62.7 μM; 72 h) sodium 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].
TM5614 sodium 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.

TM5614 sodium Related Antibodies

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

TM5614 (10 mg/kg; p.o.; daily; for 3-7 consecutive days) sodium 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%.
Molecular Weight

424.81

Formula

C23H14ClN2NaO3
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TM5614 sodium Related Classifications

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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:

TM56141247823-40-0TM 5614TM-5614PAI-1Ser/Thr ProteaseFurinMMPNotchApoptosisPlasminogen activator inhibitor-1Serine proteasesSerine endopeptidasesThreonine proteasesMatrix metalloproteinasesPAI-1/K562-2 cellschronic myeloid leukemiaLRP-1J774.1-GFP cellsPAI-1/K562-1 cellsmacrophage polarizationCTX-induced mouse skeletal muscle injury modelmurine bone marrow-derived CCR2+Ly6C+ macrophagesmacrophage efferocytosisInhibitorinhibitorinhibit

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