An inhibitor of USP2
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ML-364

Item No. 21774

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[(4-methylphenyl)sulfonyl]amino]-N-(4-phenyl-2-thiazolyl)-4-(trifluoromethyl)-benzamide
CAS Number
1991986-30-1
Molecular Formula
C24H18F3N3O3S2
Formula Weight
517.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/mlEthanol: 20 mg/ml
λmax
232, 329 nm
SMILES
[H]N(C(C1=C(N(S(C2=CC=C(C)C=C2)(=O)=O)[H])C=C(C(F)(F)F)C=C1)=O)C3=NC(C4=CC=CC=C4)=CS3
InChi Code
InChI=1S/C24H18F3N3O3S2/c1-15-7-10-18(11-8-15)35(32,33)30-20-13-17(24(25,26)27)9-12-19(20)22(31)29-23-28-21(14-34-23)16-5-3-2-4-6-16/h2-14,30H,1H3,(H,28,29,31)
InChi Key
QZUGMNXETPARLI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

    $436

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    Cayman Chemical
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    Product Description

    ML-364 is a reversible inhibitor of ubiquitin-specific protease 2 (USP2), a deubiquitinase, that has an IC50 value of 1.1 µM in a fluorescence-based assay using di-ubiquitin substrates.1 It inhibits USP8, which is closely related to USP2, with an IC50 value of 0.95 µM in the same assay. It has no activity at the proteases caspase-6, caspase-7, MMP-1, MMP-9, and USP15 or at 102 kinases in a panel including cell cycle regulators. ML-364 increases cyclin D1 degradation (IC50 = 0.97 µM) in HCT116 colorectal carcinoma cells. It induces arrest of the cell cycle at the G1 phase in Mino mantle cell lymphoma and HCT116 cells and inhibits proliferation of HCT116 cells (IC50 = 3.6 µM). It also decreases homologous recombination-mediated DNA repair in DR-GFP U2OS cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Davis, M.I., Pragani, R., Fox, J.T., et al. 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. The Journal of Biological Chemisty 291(47), 24628-24640 (2016).