Referencia número: HY-168438

ERBB agonist-1

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

ERBB agonist-1 is a ERBB4 agonist with an EC₅₀ of 10.5 μM. ERBB agonist-1 enhances NRG1-induced ERBB4 homodimerization and activates the PI3K/Akt and MAPK/ERK signaling pathways. ERBB agonist-1 acts as a cell survival promoter, anti-hypertrophic agent, anti-fibrotic agent, and cardioprotective agent. ERBB agonist-1 is applicable to the research of heart failure.

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Pureza: 99.16%
No. CAS: 930856-19-2
Fòrmula: C₂₄H₂₅N₃O₂S
Peso molecular:419.54

Almacenamiento:

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

ERBB agonist-1 Chemical Structure

No. CAS: 930856-19-2

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

ErbB4

10.5 μM (EC₅₀)

Ver todos los productos específicos de isoformas EGFR :

Ver todos los productos específicos de isoformas Akt :

Ver todos los productos específicos de isoformas ERK :

In Vitro

ERBB agonist-1 (EF-1) (0.0625-32 μM; 6 h, or 1-32 μM; 10 min pre-incubation + 6 h) potently induces ERBB4 homodimerization in U2OS ERBB4/ERBB4 osteosarcoma cells, with an EC₅₀ of 10.5 μM. This compound acts via a non-competitive binding site relative to NRG1, and enhances NRG1-mediated ERBB4 homodimerization at high concentrations^[1].
ERBB agonist-1 (0.0625-32 μM; 6 h) weakly induces ERBB2/ERBB4 heterodimerization and ERBB2/ERBB3 and ERBB1/ERBB1 dimerization in U2OS ERBB2/ERBB4 osteosarcoma cells (EC₅₀ > 32 μM)^[1].
ERBB agonist-1 (32 μM; 0-240 min) activates the PI3K/Akt and MAPK/ERK signaling pathways in cardiomyocyte-differentiated iAMs^[1].
ERBB agonist-1 (32 μM; 16 h) alters the gene expression of cardiomyocyte-differentiated iAM and HCF, significantly downregulates the TGF-β and MAPK/ERK pathways in HCF, and shares overlapping gene expression changes with NRG1 in both cell types^[1].
ERBB agonist-1 (4-32 μM; 10 min pre-incubation + 24 h) reduces TGF-β1-induced COL3A1 mRNA expression in human cardiac fibroblasts (HCFs) in a dose-dependent manner via an ERBB4-dependent mechanism^[1].
ERBB agonist-1 (4-32 μM; 10 min pre-incubation + 4 h) reduces H₂O₂-induced iAMs cell death in a dose-dependent manner via an Erbb4- and PI3K/Akt signaling pathway-dependent mechanism^[1].
ERBB agonist-1 (4-32 μM; 1 h pre-incubation + 24 h) attenuates AngII-induced cardiomyocyte hypertrophy in iAMs in a dose-dependent manner via an ERK1/2-dependent mechanism^[1].

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

Western Blot Analysis^[1]

Cell Line:

cardiomyogenically differentiated conditionally immortalized rat atrial myocytes (iAMs)
Concentration:

32 μM
Incubation Time:

0, 15, 60, 120, 240 min
Result:

Induced time-dependent phosphorylation of Akt, with peak levels at 120 min.
Induced transient phosphorylation of ERK1/2, with peak levels at 15 min.

Cell Cytotoxicity Assay^[1]

Cell Line:

cardiomyogenically differentiated iAMs
Concentration:

4, 8, 16, 32 μM (10 min pre-incubation + 4 h co-incubation with H₂O₂)
32 μM (10 min pre-incubation with LY294002 (HY-10108) + 4 h co-incubation with H₂O₂)
Incubation Time:

10 min pre-incubation + 4 h (H₂O₂ co-treatment)
10 min pre-incubation with LY294002 + 4 h (H₂O₂ co-treatment)
Result:

Dose-dependently decreased H₂O₂-induced total cell death by more than 75% at the highest dose.
Had its pro-survival effect diminished by Erbb4 knockdown.
Had its pro-survival effect blocked by pre-treatment with PI3K/Akt inhibitor LY294002.
Increased cell viability and reduced apoptotic cell number in H₂O₂-treated iAMs, confirmed by WST-1 and TUNEL assays.

Cell Proliferation Assay^[1]

Cell Line:

proliferating iAMs
Concentration:

32 μM
Incubation Time:

24 h, followed by 24 h EdU incubation
Result:

Significantly decreased the number of EdU-positive nuclei compared to vehicle.

In Vivo

ERBB agonist-1 (EF-1) (2 mg/kg/day; s.c.; daily; 1-4 weeks) exhibits anti-fibrotic and cardioprotective activity in angiotensin II-induced myocardial fibrosis in both male and female C57BL/6N mice, reducing fibrotic tissue and fibrosis-related gene expression^[1].
ERBB agonist-1 (2 mg/kg/day; s.c.; daily; 28 days) reduces cardiac dilation and interstitial fibrosis in female Balb/cJ mice following myocardial infarction, with no significant effects observed in male mice^[1].
ERBB agonist-1 (2 mg/kg/day; s.c.; daily; 1 week) protects against Doxorubicin (HY-15142A)-induced acute cardiomyocyte injury in female wild-type C57BL/6N mice, with this effect dependent on ERBB4 expression^[1].

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

Animal Model:

C57BL/6N (13-week-old male and female; angiotensin II-induced myocardial fibrosis model)^[1]
Dosage:

2 mg/kg/day (4-week study; 1-week male study)
Administration:

s.c.; daily; 4 weeks; s.c.; daily; 1 week (male mice)
Result:

Significantly reduced angiotensin II-induced total fibrosis, interstitial fibrosis, and perivascular fibrosis in male mice.
Significantly reduced angiotensin II-induced total fibrosis and perivascular fibrosis in female mice.
Significantly reduced angiotensin II-induced Col1a1, Col3a1, and Nppa mRNA expression in male mice in the 1-week study.
Did not significantly alter cardiac dimensions on ultrasound in either sex.

Animal Model:

C57BL/6N (12-week-old male and female; Doxorubicin-induced acute cardiotoxicity model)
Erbb4-null (13-week-old female, Tamoxifen (HY-13757A)-induced (10 mg/kg; in corn oil); Doxorubicin-induced acute cardiotoxicity model)^[1]
Dosage:

2 mg/kg/day
Administration:

s.c.; daily; 1 week
Result:

Significantly prevented the Doxorubicin-induced increase in circulating cTnI plasma levels in female wild-type mice.
Did not prevent the Doxorubicin-induced increase in circulating cTnI plasma levels in male wild-type mice or female Erbb4-null mice.

Animal Model:

Balb/cJ (12-week-old female and male; myocardial infarction model, treatment starting 7 days post-infarction)^[1]
Dosage:

2 mg/kg/day
Administration:

s.c.; daily; 28 days
Result:

Significantly attenuated the infarction-induced increase in left ventricular end-diastolic volume (LVEDV) and left ventricular end-systolic volume (LVESV) in female mice.
Resulted in a trend towards increased left ventricular ejection fraction in female mice.
Significantly reduced interstitial fibrosis in the remote myocardium of female infarcted mice.
Did not affect LVEDV, LVESV, ejection fraction, or interstitial fibrosis in male mice.
Did not alter scar size in either sex.

Chemical Information

No. CAS 930856-19-2
Appearance Solid
Peso molecular 419.54
Fòrmula C₂₄H₂₅N₃O₂S
Color White to off-white
SMILES

O=C(NC1CC1)C(SC(N2C3CCCC3)=NC4=CC=CC=C4C2=O)C5=CC=CC=C5
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (1)

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Stem Cells

LARP7 enhances the potential of dental pulp stem cells to promote peripheral nerve repair. [Abstract]

2026 Mar 11:sxag013. PMID: 41812059

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (238.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3836 mL

11.9178 mL

23.8356 mL

5 mM

0.4767 mL

2.3836 mL

4.7671 mL

10 mM

0.2384 mL

1.1918 mL

2.3836 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (290 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Cools JMT, et al. Small-molecule-induced ERBB4 activation to treat heart failure. Nature communications. 2025 Jan 10;16(1):576. [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	2.3836 mL	11.9178 mL	23.8356 mL	59.5891 mL
	5 mM	0.4767 mL	2.3836 mL	4.7671 mL	11.9178 mL
	10 mM	0.2384 mL	1.1918 mL	2.3836 mL	5.9589 mL
	15 mM	0.1589 mL	0.7945 mL	1.5890 mL	3.9726 mL
	20 mM	0.1192 mL	0.5959 mL	1.1918 mL	2.9795 mL
	25 mM	0.0953 mL	0.4767 mL	0.9534 mL	2.3836 mL
	30 mM	0.0795 mL	0.3973 mL	0.7945 mL	1.9863 mL
	40 mM	0.0596 mL	0.2979 mL	0.5959 mL	1.4897 mL
	50 mM	0.0477 mL	0.2384 mL	0.4767 mL	1.1918 mL
	60 mM	0.0397 mL	0.1986 mL	0.3973 mL	0.9932 mL
	80 mM	0.0298 mL	0.1490 mL	0.2979 mL	0.7449 mL
	100 mM	0.0238 mL	0.1192 mL	0.2384 mL	0.5959 mL

ERBB agonist-1

1 Cited Publications

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ERBB agonist-1

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Publications Citing Use of MedChemExpress (MCE) ERBB agonist-1

Ver todos los productos específicos de isoformas EGFR

Ver todos los productos específicos de isoformas Akt

Ver todos los productos específicos de isoformas ERK

Actividad biológica

Chemical Information

Publications (1)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

ERBB agonist-1 Related Classifications

HY-168438 Related Classifications