1. Cell Cycle/DNA Damage
  2. p97

ML240 

Cat. No.: HY-19795 Purity: 99.49%
Handling Instructions

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

ML240 Chemical Structure

CAS No. : 1346527-98-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
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5 mg USD 84 In-stock
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10 mg USD 132 In-stock
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25 mg USD 276 In-stock
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50 mg USD 480 In-stock
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100 mg USD 840 In-stock
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Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 100 nM (p97)[1]

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 Ki 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].

References
Preparing Stock Solutions
Concentration Volume 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
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

ML240 is dissolved in DMSO, and diluted before use[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
Molecular Weight

396.44

Formula

C₂₃H₂₀N₆O

CAS No.

1346527-98-7

SMILES

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

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 16.5 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
ML240
Cat. No.:
HY-19795
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