2. Immunology/Inflammation
  3. Complement System
  4. EG01377

EG01377 is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1. EG01377 has antiangiogenic, antimigratory, and antitumor effects.

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EG01377 Chemical Structure

EG01377 Chemical Structure

CAS No. : 2227996-00-9

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EG01377 Related Antibodies

Top Publications Citing Use of Products

    EG01377 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 25;14(2):159.  [Abstract]

    EG01377 (20, 40, 80 µM) attenuates the phosphorylation of EGFR, AKT, GSK3β, and mTOR in PC-3 and DU-145 cells.

    EG01377 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 25;14(2):159.  [Abstract]

    EG01377 (20, 40, 80 µM; 14 days) significantly attenuates clone formation ability of PC-3 and DU-145 cells in a concentration-dependent manner.

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    Description

    EG01377 is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of both 609 nM for NRP1-a1 and NRP1-b1. EG01377 has antiangiogenic, antimigratory, and antitumor effects[1].

    IC50 & Target

    IC50: 609 nM (NRP1-a1 and NRP1-b)[1] Kd: 1.32 μM (NRP1-b1)[1]
    In Vitro

    EG01377 (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR[1].
    EG01377 (30 μM) is able to significantly reduce HUVEC cell migration in response to VEGFA[1].
    EG01377 (30 μM; 5 days) can delay the VEGF-induced wound closure[1].
    EG01377 (30 μM) reduces network area, length, and branching points[1].
    EG01377 (30 μM; 7 days) reduces VEGF-induced angiogenesis[1].
    EG01377 (30 μM; 7 days) in combination with VEGFA reduces A375P (malignant melanoma) spheroid outgrowth[1].
    EG01377 (500 nM; 2 hours) blocks the production of transforming growth factor beta (TGFβ) by Nrp1+ regulatory T-cell SMAD3/AKT (Tregs) in the presence of tumor cell-derived factors[1].

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

    EG01377 Related Antibodies

    Western Blot Analysis[1]

    Cell Line: Human umbilical vein endothelial cells (HUVECs)
    Concentration: 3, 10, 30 μM
    Incubation Time: 30 minutes
    Result: Inhibited VEGF-A stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC50 of 30 μM.
    In Vivo

    EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice[1].

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

    Animal Model: 6–8 week-old BABL/c female mice[1]
    Dosage: 2 mg/kg (Pharmacokinetic Analysis)
    Administration: I.v. administration
    Result: The half time (T1/2) of 4.29 h.
    Molecular Weight

    586.68

    Formula

    C26H30N6O6S2
    CAS No.
    SMILES

    O=S(C1=CC(C2=CC=C(CN)C=C2)=CC3=C1OCC3)(NC4=C(C(N[C@@H](CCC/N=C(N)/N)C(O)=O)=O)SC=C4)=O
    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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    EG01377 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:

    EG013772227996-00-9EG 01377EG-01377Complement Systemneuropilin-1NRP1NRP1-a1NRP1-b1antiangiogenicantimigratoryantitumorInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
    HY-112151
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