XMD17-109

Name: XMD17-109
Brand: MedChemExpress
SKU: HY-15665
Rating: 5.0 (6 reviews)

Cat. No.: HY-15665 Purity: 99.20%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC₅₀ of 162 nM.

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

XMD17-109 Chemical Structure

CAS No. : 1435488-37-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 138	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 138	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 46	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 98	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 460	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 695	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

5 Publications Citing Use of MCE XMD17-109

: XMD17-109 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Jun 7;7(23):34322-40. [Abstract]; HCT116 parental cells are treated for up to 48 h with increasing doses of 5-FU in combination with 4 μM XMD8-92 or 2 μM XMD17-109, two highly-selective ERK5 pharmacological inhibitors.

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ERK ERK1 ERK2 ERK5 ERK8

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

XMD17-109 is a novel, specific ERK-5 inhibitor, with an IC₅₀ of 162 nM.

IC₅₀ & Target^[1]

ERK5

162 nM (IC₅₀)

LRRK2[G2019S]

339 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	4.2 μM Compound: 26, ERK5-IN-1	Inhibition of GST-tagged full length human ERK5 transfected in HEK293 cells assessed as inhibition of AP1 transcriptional activity after 24 hrs by dual luciferase reporter gene assay Inhibition of GST-tagged full length human ERK5 transfected in HEK293 cells assessed as inhibition of AP1 transcriptional activity after 24 hrs by dual luciferase reporter gene assay	[PMID: 23656407]
HEK-293T	IC₅₀	> 10000 nM Compound: ERK5-IN-1	Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]
MM1.S	IC₅₀	280 nM Compound: ERK5-IN-1	Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay	[PMID: 34710325]

In Vitro

XMD17-109 (Compound 26) inhibits ERK5 biochemically with an IC₅₀ of 0.162 ± 0.006 μM, and blocks pidermal growth factor induced ERK5 autophosphorylation with an EC₅₀ of 0.09 ± 0.03 μM in cells. XMD17-109 also inhibits LRRK2[G2019S] with an IC₅₀ of 339 nM^[1]. XMD17-109 demonstrats low nanomolar cellular activity judged by the significant dose-dependent reduction of mobility shifted phosphorylated ERK5 bands from sorbitol stimulated cells. XMD17-109 completely inhibits the ERK5-mediated AP1 transcriptional activity at 30 μM and has an EC₅₀ of 4.2 μM^[2].

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

Molecular Weight

638.80

Formula

C₃₆H₄₆N₈O₃

CAS No.

1435488-37-1

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(C=CC=C2)N(C3CCCC3)C4=NC(NC5=C(OCC)C=C(C(N6CCC(N7CCN(C)CC7)CC6)=O)C=C5)=NC=C4N1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (156.54 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5654 mL	7.8272 mL	15.6544 mL
5 mM	0.3131 mL	1.5654 mL	3.1309 mL
10 mM	0.1565 mL	0.7827 mL	1.5654 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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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: ≥ 2.5 mg/mL (3.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.20%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (260 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[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;70:758-67. [Content Brief]

[2]. Elkins, Jonathan M., et al. X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor. Journal of Medicinal Chemistry (2013), 56(11), 4413-4421. [Content Brief]

[3]. Wilhelmsen K, et al. Extracellular signal-regulated kinase 5 promotes acute cellular and systemic inflammation. Sci Signal. 2015 Aug 25;8(391):ra86. [Content Brief]

Cell Assay
^[2]

HeLa cells are maintained in DMEM supplemented with 10% FBS, 2 mM l-glutamine, 50 U/mL penicillin G, and 50 μg/mL streptomycin. Before use HeLa cells are serum starved for 16 h in DMEM supplemented with 2 mM l-glutamine, 50 U/mL penicillin G, and 50 μg/mL streptomycin. HeLa cells are then incubated with ERK5-IN-1 at the indicated concentrations for 1 h prior to stimulation with 0.5mol/Lsorbitol for 30 min. Cells are lysed in Triton lysis buffer (50 mM Tris-HCl, pH 7.5, 1 mM EGTA, 1 mM EDTA, 1 mM sodium orthovanadate, 50 mM sodium fluoride, 1 mM sodium pyrophosphate, 0.27mol/Lsucrose, 1 μM microcystin-LR, 1% (v/v) Triton X-100, 0.1% (v/v) 2-mercaptoethanol) and 20 μg of protein loaded per well. Samples are run on 8% polyacrylamide gels using standard methods. Proteins are transferred onto nitrocellulose membranes and specific proteins detected by immunoblotting.

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

References

[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;70:758-67. [Content Brief]

[2]. Elkins, Jonathan M., et al. X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor. Journal of Medicinal Chemistry (2013), 56(11), 4413-4421. [Content Brief]

[3]. Wilhelmsen K, et al. Extracellular signal-regulated kinase 5 promotes acute cellular and systemic inflammation. Sci Signal. 2015 Aug 25;8(391):ra86. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.5654 mL	7.8272 mL	15.6544 mL	39.1359 mL
	5 mM	0.3131 mL	1.5654 mL	3.1309 mL	7.8272 mL
	10 mM	0.1565 mL	0.7827 mL	1.5654 mL	3.9136 mL
	15 mM	0.1044 mL	0.5218 mL	1.0436 mL	2.6091 mL
	20 mM	0.0783 mL	0.3914 mL	0.7827 mL	1.9568 mL
	25 mM	0.0626 mL	0.3131 mL	0.6262 mL	1.5654 mL
	30 mM	0.0522 mL	0.2609 mL	0.5218 mL	1.3045 mL
	40 mM	0.0391 mL	0.1957 mL	0.3914 mL	0.9784 mL
	50 mM	0.0313 mL	0.1565 mL	0.3131 mL	0.7827 mL
	60 mM	0.0261 mL	0.1305 mL	0.2609 mL	0.6523 mL
	80 mM	0.0196 mL	0.0978 mL	0.1957 mL	0.4892 mL
	100 mM	0.0157 mL	0.0783 mL	0.1565 mL	0.3914 mL

XMD17-109 Related Classifications

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:

XMD17-1091435488-37-1ERKExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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XMD17-109

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XMD17-109 Related Antibodies

5 Publications Citing Use of MCE XMD17-109

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View All ERK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

XMD17-109 Related Antibodies

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Complete Stock Solution Preparation Table

XMD17-109 Related Classifications

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