1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK
  3. ERK5-IN-1

ERK5-IN-1 

Cat. No.: HY-14403 Purity: 99.92%
Handling Instructions

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.

For research use only. We do not sell to patients.

ERK5-IN-1 Chemical Structure

ERK5-IN-1 Chemical Structure

CAS No. : 1234479-76-5

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 462 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 462 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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Based on 1 publication(s) in Google Scholar

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Description

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)

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].

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

Molecular Weight

459.54

Formula

C₂₅H₂₉N₇O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (217.61 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Kinase activity is determined in an assay volume of 40 μL in kinase buffer (50 mM Tris-HCl, pH 7.5, 0.1 mM EGTA, 1 mM 2-mercaptoethanol) containing 200 ng of pure active ERK5 and the indicated amount of inhibitor. Reaction started by adding 10 mM magnesium acetate, and 50 μM [γ-32P]-ATP (500 cpm/pmol) and 250 μM PIMtide (ARKKRRHPSGPPTA) as substrates. Assays are carried out for 20 min at 30°C, terminated by applying the reaction mixture onto p81 paper and the incorporated radioactivity measured[1].

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

References
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Product Name:
ERK5-IN-1
Cat. No.:
HY-14403
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