Art. -Nr.: HY-14403

ERK5-IN-1

Name: ERK5-IN-1
Brand: MedChemExpress
SKU: HY-14403
Price: 150.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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ERK5-IN-1 is a potent ERK5 inhibitor with an IC₅₀ of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC₅₀ of 26 nM.

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Reinheit : 99.55%
CAS. Nr.: 1234479-76-5
Formel: C₂₅H₂₉N₇O₂
Molecular Weight:459.54

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ERK5-IN-1 Chemical Structure

CAS. Nr.: 1234479-76-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (1)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

ERK5-IN-1 is a potent ERK5 inhibitor with an IC₅₀ of 87±7 nM. ERK5-IN-1 also inhibits LRRK2[G2019S] with an IC₅₀ of 26 nM.

IC₅₀ & Target

^[1]

ERK5

87 nM (IC₅₀)

LRRK2[G2019S]

26 nM (IC₅₀)

Alle ERK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.56 μM Compound: XMD8-85	Inhibition of TNK2 D163E mutant in human BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay Inhibition of TNK2 D163E mutant in human BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 31928839]
HeLa	IC₅₀	0.19 μM Compound: 11	Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysis Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysis	[PMID: 21412406]
HeLa	IC₅₀	87 nM Compound: XMD8-85	Inhibition of ERK5 in human HeLa cells assessed as reduction in EGF-induced ERK5 autophosphorylation pretreated for 1 hr followed by EGF stimulation and measured after 17 mins by 32p kinase assay Inhibition of ERK5 in human HeLa cells assessed as reduction in EGF-induced ERK5 autophosphorylation pretreated for 1 hr followed by EGF stimulation and measured after 17 mins by 32p kinase assay	[PMID: 32530623]

In Vitro

ERK5-IN-1 (Compound 5) exhibits a cellular EC₅₀ for inhibiting epidermal growth factor (EGF) induced ERK5 autophosphorylation of 0.19±0.04 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Chemical Information

CAS. Nr. 1234479-76-5
Appearance Solid
Molecular Weight 459.54
Formel C₂₅H₂₉N₇O₂
Color Light yellow to yellow
SMILES

O=C1C2=C(C=CC=C2)N(C)C3=NC(NC4=C(OC)C=C(N5CCN(C)CC5)C=C4)=NC=C3N1C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (217.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.1761 mL

10.8804 mL

21.7609 mL

5 mM

0.4352 mL

2.1761 mL

4.3522 mL

10 mM

0.2176 mL

1.0880 mL

2.1761 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.75 mg/mL (5.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.75 mg/mL (5.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.75 mg/mL (5.98 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Handling Instructions (2659 KB)

Verweise

[1]. Deng X, et al. Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones. Eur J Med Chem. 2013;70:758-767. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1761 mL	10.8804 mL	21.7609 mL	54.4022 mL
	5 mM	0.4352 mL	2.1761 mL	4.3522 mL	10.8804 mL
	10 mM	0.2176 mL	1.0880 mL	2.1761 mL	5.4402 mL
	15 mM	0.1451 mL	0.7254 mL	1.4507 mL	3.6268 mL
	20 mM	0.1088 mL	0.5440 mL	1.0880 mL	2.7201 mL
	25 mM	0.0870 mL	0.4352 mL	0.8704 mL	2.1761 mL
	30 mM	0.0725 mL	0.3627 mL	0.7254 mL	1.8134 mL
	40 mM	0.0544 mL	0.2720 mL	0.5440 mL	1.3601 mL
	50 mM	0.0435 mL	0.2176 mL	0.4352 mL	1.0880 mL
	60 mM	0.0363 mL	0.1813 mL	0.3627 mL	0.9067 mL
	80 mM	0.0272 mL	0.1360 mL	0.2720 mL	0.6800 mL
	100 mM	0.0218 mL	0.1088 mL	0.2176 mL	0.5440 mL

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ERK5-IN-1

Alle ERK Isoform-spezifische Produkte anzeigen