ML240

Name: ML240
Brand: MedChemExpress
SKU: HY-19795
Rating: 5.0 (3 reviews)

Cat. No.: HY-19795 Purity: 99.87%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC₅₀ value of 100 nM.

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

ML240 Chemical Structure

CAS No. : 1346527-98-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 101	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 101	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 92	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 138	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 249	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 640	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE ML240

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC₅₀ value of 100 nM.

IC₅₀ & Target

IC50: 100 nM (p97)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	3.26 μM Compound: 7	Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by Celltiter-Glo assay Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by Celltiter-Glo assay	[PMID: 26565666]
A549	IC₅₀	6.14 μM Compound: 7	Inhibition of p97 ATPase in human A549 cells assessed as accumulation of K48 poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay Inhibition of p97 ATPase in human A549 cells assessed as accumulation of K48 poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay	[PMID: 26565666]
A549	IC₅₀	6.61 μM Compound: 7	Inhibition of p97 ATPase in human A549 cells assessed as accumulation of CHOP poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay Inhibition of p97 ATPase in human A549 cells assessed as accumulation of CHOP poly-ubiquitinated proteins incubated for 6 hrs by immunofluorescence assay	[PMID: 26565666]

In Vitro

ML240 is a potent p97 inhibitor, with an IC₅₀ of 100 nM. ML240 is active in the UbG76V-GFP stabilization assay (IC₅₀, 0.9 μM). ML240 inhibits p97 competitively with respect to ATP with a K_i values of 0.22 μM. ML240 also inhibits labeling of only three protein kinase domains by >50% when tested at 20 μM: PIP5 K3 (belongs to phosphoinositide-3 kinase family), JAK1 JH2 (N-terminal pseudokinase domain of JAK1), and DNAPK (DNA-dependent protein kinase). ML240 (1.1, 3.3, 10, or 20 μM) induces executioner caspases 3 and 7 and triggers cell death independently of apical caspases 8 and 9^[1]. ML240 is cytotoxic to HCT15 and SW403 cells, with GI₅₀s of 0.76 and 0.5 μM after treatment for 24 h, and 0.54 and 0.5 μM after treatment for 72 h, respectively^[2].

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

Molecular Weight

396.44

Formula

C₂₃H₂₀N₆O

CAS No.

1346527-98-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

COC1=CC=CC2=C(NCC3=CC=CC=C3)N=C(N4C(N)=NC5=CC=CC=C45)N=C12

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 : 12.5 mg/mL (31.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : < 1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5224 mL	12.6122 mL	25.2245 mL
5 mM	0.5045 mL	2.5224 mL	5.0449 mL
10 mM	0.2522 mL	1.2612 mL	2.5224 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 (6.31 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (6.31 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (6.31 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: 99.87%

Select Batch:

Data Sheet (281 KB) SDS (392 KB)

COA (257 KB) HNMR (249 KB) LCMS (95 KB) Elemental Analysis Report (115 KB)

Handling Instructions (2659 KB)

References

[1]. Chou TF et al. Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase. ChemMedChem, 2013 Feb, 8(2):297-312. [Content Brief]

[2]. Chou TF, et al. Selective, reversible inhibitors of the AAA ATPase p97. Probe Reports from the NIH Molecular Libraries Program. April 14, 2011. [Content Brief]

Cell Assay
^[2]

HeLa cells stably expressing ODD-luciferase are seeded onto a 96-well white solid bottom plate (5000 cells/well) and cells are grown for 16 h. Cells are treated with DMEM containing MG132 (4 μM) for 1h and washed with 100 μL PBS twice. DMEM containing 2.5% FBS, cycloheximide (50 μg/mL) and ML240 are added into the well. Four 96-well plates are prepared and one of the plates is taken out from incubator at each time point (70, 90, 120, or 150 min). Luciferin (50 μL of 1 mg/mL in PBS) is added into each well containing 50 μL of medium and incubated at room temperature with shaking at 500 rpm for 5 min. Luminescence intensity is determined with 0.1 ms integration time on the Synergy HT Microplate Reader^[2].

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

References

[1]. Chou TF et al. Structure-activity relationship study reveals ML240 and ML241 as potent and selective inhibitors of p97 ATPase. ChemMedChem, 2013 Feb, 8(2):297-312. [Content Brief]

[2]. Chou TF, et al. Selective, reversible inhibitors of the AAA ATPase p97. Probe Reports from the NIH Molecular Libraries Program. April 14, 2011. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.5224 mL	12.6122 mL	25.2245 mL	63.0612 mL
	5 mM	0.5045 mL	2.5224 mL	5.0449 mL	12.6122 mL
	10 mM	0.2522 mL	1.2612 mL	2.5224 mL	6.3061 mL
	15 mM	0.1682 mL	0.8408 mL	1.6816 mL	4.2041 mL
	20 mM	0.1261 mL	0.6306 mL	1.2612 mL	3.1531 mL
	25 mM	0.1009 mL	0.5045 mL	1.0090 mL	2.5224 mL
	30 mM	0.0841 mL	0.4204 mL	0.8408 mL	2.1020 mL

ML240 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:

ML2401346527-98-7ML 240ML-240p97VCPCdc48Inhibitorinhibitorinhibit

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ML240

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ML240 Related Antibodies

3 Publications Citing Use of MCE ML240

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Customer Review

ML240 Related Antibodies

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Complete Stock Solution Preparation Table

ML240 Related Classifications

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