1. Protein Tyrosine Kinase/RTK
  2. Ephrin Receptor
  3. EPHA4 antagonist-1

EPHA4 antagonist-1 (Compound 2) is an EphA4 receptor antagonist. EPHA4 antagonist-1 is also an EphA2 receptor antagonist. EPHA4 antagonist-1 inhibits ephrin-A5 AP binding to EphA4 Fc receptor, with an IC50 of 10 μM.

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EPHA4 antagonist-1

EPHA4 antagonist-1 Chemical Structure

CAS No. : 313701-92-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Description

EPHA4 antagonist-1 (Compound 2) is an EphA4 receptor antagonist. EPHA4 antagonist-1 is also an EphA2 receptor antagonist. EPHA4 antagonist-1 inhibits ephrin-A5 AP binding to EphA4 Fc receptor, with an IC50 of 10 μM[1].

IC50 & Target[1]

EPHA2

 

EPHA4

 

Cellular Effect
Cell Line Type Value Description References
MT2 CC50
133.4 μM
Compound: NB-2
Cytotoxicity against human MT2 cells after 4 days by XTT assay
Cytotoxicity against human MT2 cells after 4 days by XTT assay
[PMID: 23673219]
MT2 CC50
133.46 μM
Compound: A12
Cytotoxicity against human MT2 cells after 4 days by XTT assay
Cytotoxicity against human MT2 cells after 4 days by XTT assay
[PMID: 19053778]
MT2 CC50
333.84 μM
Compound: A12
Cytotoxicity against human MT2 cells after 4 days by XTT assay
Cytotoxicity against human MT2 cells after 4 days by XTT assay
[PMID: 19932616]
MT2 EC50
0.69 μM
Compound: A12
Antiviral activity against HIV1 3B in human MT2 cells assessed as inhibition of p24 antigen level after 4 days by ELISA
Antiviral activity against HIV1 3B in human MT2 cells assessed as inhibition of p24 antigen level after 4 days by ELISA
[PMID: 19053778]
MT2 EC50
0.7 μM
Compound: NB-2
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA
[PMID: 23673219]
MT2 IC50
28.19 μM
Compound: A12
Antiviral activity against HIV1 3B in human MT2 cells assessed as inhibition of p24 antigen level after 4 days by ELISA
Antiviral activity against HIV1 3B in human MT2 cells assessed as inhibition of p24 antigen level after 4 days by ELISA
[PMID: 19932616]
MT2 IC50
43.24 μM
Compound: A12
Antiviral activity against HIV1 3B in human MT2 cells assessed as inhibition of cell-cell fusion
Antiviral activity against HIV1 3B in human MT2 cells assessed as inhibition of cell-cell fusion
[PMID: 19932616]
MT2 IC50
55.45 μM
Compound: A12
Antiviral activity against HIV1 3B in human MT2 cells assessed as reduction of virus-induced cytopathogenicity
Antiviral activity against HIV1 3B in human MT2 cells assessed as reduction of virus-induced cytopathogenicity
[PMID: 19932616]
Molecular Weight

231.25

Formula

C13H13NO3

CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C(C1=CC(N2C(C)=CC=C2C)=CC=C1O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (540.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.3243 mL 21.6216 mL 43.2432 mL
5 mM 0.8649 mL 4.3243 mL 8.6486 mL
View the 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

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 (protect from light). 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 4.3243 mL 21.6216 mL 43.2432 mL 108.1081 mL
5 mM 0.8649 mL 4.3243 mL 8.6486 mL 21.6216 mL
10 mM 0.4324 mL 2.1622 mL 4.3243 mL 10.8108 mL
15 mM 0.2883 mL 1.4414 mL 2.8829 mL 7.2072 mL
20 mM 0.2162 mL 1.0811 mL 2.1622 mL 5.4054 mL
25 mM 0.1730 mL 0.8649 mL 1.7297 mL 4.3243 mL
30 mM 0.1441 mL 0.7207 mL 1.4414 mL 3.6036 mL
40 mM 0.1081 mL 0.5405 mL 1.0811 mL 2.7027 mL
50 mM 0.0865 mL 0.4324 mL 0.8649 mL 2.1622 mL
60 mM 0.0721 mL 0.3604 mL 0.7207 mL 1.8018 mL
80 mM 0.0541 mL 0.2703 mL 0.5405 mL 1.3514 mL
100 mM 0.0432 mL 0.2162 mL 0.4324 mL 1.0811 mL
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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.

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Product Name:
EPHA4 antagonist-1
Cat. No.:
HY-W078239
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