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ML364

Cat. No. M9785
ML364 Structure
Size Price Availability Quantity
10mg USD 122  USD122 In stock
25mg USD 304  USD304 In stock
50mg USD 528  USD528 In stock
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Quality Control & Documentation
Biological Activity

ML364 is a small molecule inhibitor of the deubiquitinase USP2 (IC50=1.1 μM) with potential anticancer activity. Direct binding of ML364 to USP2 (Kd=5.2 μM) was demonstrated using microscale thermophoresis. ML364 induced an increase in cellular cyclin D1 degradation and caused cell cycle arrest as shown in Western blottings and flow cytometry assays utilizing both Mino and HCT116 cancer cell lines. ML364 also increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP.

Chemical Information
Molecular Weight 517.54
Formula C24H18F3N3O3S2
CAS Number 1991986-30-1
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Mayuko Hashimoto, et al. Physiol Rep. Inhibition of ubiquitin-specific protease 2 causes accumulation of reactive oxygen species, mitochondria dysfunction, and intracellular ATP decrement in C2C12 myoblasts

[2] Mindy I Davis, et al. J Biol Chem. Small Molecule Inhibition of the Ubiquitin-specific Protease USP2 Accelerates cyclin D1 Degradation and Leads to Cell Cycle Arrest in Colorectal Cancer and Mantle Cell Lymphoma Models

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