ML792

For research use only.

Catalog No.S8697

ML792 Chemical Structure

CAS No. 1644342-14-2

ML-792 is a potent and selective inhibitor of SUMO (small ubiquitin-like modifier)-activating enzyme (SAE). ML-792 inhibits SAE/SUMO1 and SAE/SUMO2 in ATP–inorganic pyrophosphate (PPi) exchange assays with IC50 of 3 nM and 11 nM, respectively.

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Biological Activity

Description ML-792 is a potent and selective inhibitor of SUMO (small ubiquitin-like modifier)-activating enzyme (SAE). ML-792 inhibits SAE/SUMO1 and SAE/SUMO2 in ATP–inorganic pyrophosphate (PPi) exchange assays with IC50 of 3 nM and 11 nM, respectively.
Targets
SAE/SUMO1 [1]
(Cell-free assay)
SAE/SUMO2 [1]
(Cell-free assay)
3 nM 11 nM
In vitro

ML-792 is a mechanism-based SUMO-activating enzyme (SAE) inhibitor with nanomolar potency in cellular assays. ML-792 selectively blocks SAE enzyme activity and total SUMOylation, thus decreasing cancer cell proliferation. Induction of the MYC oncogene increases the ML-792-mediated viability effect in cancer cells, thus indicating a potential application of SAE inhibitors in treating MYC-amplified tumors.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: HCT116 cells
  • Concentrations: 0.5 μM
  • Incubation Time: 48 h
  • Method:

    HCT116 cells are plated (0.2 × 106 cells/well) and incubated overnight in six-well tissue culture dishes. To study ML-792-induced DNA damage, cells are then treated with DMSO or 0.5 μM ML-792 for 24 h. A 4-h treatment with 20 μM etoposide is used as a positive control for induction of DNA-strand breaks. To study how loss of SUMOylation contributes to repair of DNA damage by cisplatin, individual wells of HCT116 cells are treated with the following treatments: DMSO (6 h); 0.5 μM ML-792 (6 h); DMSO (2 h) followed by treatment with 10 μM cisplatin (4 h); and 0.5 μM ML-792 (2 h) followed by treatment with 10 μM cisplatin (4 h).


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (181.35 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 551.41
Formula
C21H23BrN6O5S
CAS No. 1644342-14-2
Storage powder
in solvent
Synonyms N/A
Smiles C1C(CC(C1COS(=O)(=O)N)O)NC2=NC=NC=C2C(=O)C3=NN(C=C3)CC4=CC(=CC=C4)Br

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID