ML792

Catalog No.S8697

For research use only.

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.

ML792 Chemical Structure

CAS No. 1644342-14-2

Selleck's ML792 has been cited by 4 Publications

Purity & Quality Control

Choose Selective E1 Activating Inhibitors

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 (from reference)

Cell Research:

[1]

  • 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).

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 551.41
Formula
C21H23BrN6O5S
CAS No. 1644342-14-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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