ML-792 |
Catalog No.GC36631
One-Click Copy Product Info
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ML-792 is a specific inhibitor of small ubiquitin-like modifier (SUMO) activating enzyme (SAE), which can inhibit SAE/SUMO1 and SAE/SUMO2 with IC50 of 3nM and 11nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1644342-14-2
Sample solution is provided at 25 µL, 10mM.
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ML-792 is a specific inhibitor of small ubiquitin-like modifier (SUMO) activating enzyme (SAE), which can inhibit SAE/SUMO1 and SAE/SUMO2 with IC50 of 3nM and 11nM, respectively[1]. The SUMO protein pathway can control a series of important biological processes, including cell death, proliferation, differentiation, metabolism and signal transduction, by diversifying the functions, half-lives and partnerships of in situ target proteins[2]. ML-792 is often used to study the role of SUMOylation in cancer, neurodegenerative diseases and viral infection[3, 4].
In vitro, ML-792 (0, 1, 5μM) treatment of 5-FU-resistant cell lines (HCT-8/5-FU cells) for 12-16 days significantly reduced the number of cell colony formation and reversed the cell's 5-FU resistance[5].
In vivo, ML-792 (50, 100mg/kg) was intraperitoneally injected into mice bearing HOS cell xenografts, which inhibited tumor growth in a dose-dependent manner[6]. ML-792 (150, 200mg/kg) was subcutaneously injected into mice bearing HCT-116 cell xenografts, which inhibited tumor growth in a dose-dependent manner[7].
References:
[1] He X, Riceberg J, Soucy T, et al. Probing the roles of SUMOylation in cancer cell biology by using a selective SAE inhibitor[J]. Nature chemical biology, 2017, 13(11): 1164-1171.
[2] Connolly J G, Plant L D. SUMO regulation of ion channels in health and disease[J]. Physiology, 2025, 40(2).
[3] Celen A B, Sahin U. Sumoylation on its 25th anniversary: mechanisms, pathology, and emerging concepts[J]. The FEBS journal, 2020, 287(15): 3110-3140.
[4] Sahin U, de Thé H, Lallemand-Breitenbach V. Sumoylation in physiology, pathology and therapy[J]. Cells, 2022, 11(5): 814.
[5] Deng Y, Chen Y, Gao S, et al. RREB1-mediated SUMOylation enhancement promotes chemoresistance partially by transcriptionally upregulating UBC9 in colorectal cancer[J]. Frontiers in Pharmacology, 2024, 15: 1381860.
[6] Jin X, Yin H, Bao J, et al. ML792 inhibits growth and TGF-β1-induced EMT of osteosarcoma cells via TGF-β1/Smad and PI3K/AKT pathways[J]. All Life, 2022, 15(1): 1222-1235.
[7] Langston S P, Grossman S, England D, et al. Discovery of TAK-981, a first-in-class inhibitor of SUMO-activating enzyme for the treatment of cancer[J]. Journal of medicinal chemistry, 2021, 64(5): 2501-2520.
| Cell experiment [1]: | |
Cell lines | 5-FU-resistant cell line HCT-8/5-FU |
Preparation Method | 1000 HCT-8/5-FU cells/well were seeded in 6-well plates and incubated with 100µM 5-FU and 0, 1, or 5µM ML-792 for 12-16 days. Colony formation assay was performed. |
Reaction Conditions | 0, 1, 5μM; 12-16 days |
Applications | ML-792 significantly reduced colony formation numbers in HCT-8/5-FU cells. |
| Animal experiment [2]: | |
Animal models | BALB/c-nude mice |
Preparation Method | HOS cells were suspended in culture media at a density of 1.0×106/mL and subcutaneously transplanted onto the 6-week-old female BALB/c-nude mice (200μL). After weighing, the nude mice were randomly divided into three groups (6 in each group): control group, 50mg/kg ML-792, and 100mg/kg ML-792. Treatment begins when subcutaneous tumors form. The intraperitoneal administration regimen was two days a week. Tumors were measured weekly using calipers. The nude mice were killed before the tumor reached ethical size. |
Dosage form | 50, 100mg/kg; two days a week; i.p. |
Applications | ML-792 significantly inhibited the growth of tumors, and the effect of the high concentration group was more obvious. |
References: | |
| Cas No. | 1644342-14-2 | SDF | |
| Canonical SMILES | O=S(OC[C@@H]1[C@@H](O)C[C@H](NC2=NC=NC=C2C(C3=NN(CC4=CC=CC(Br)=C4)C=C3)=O)C1)(N)=O | ||
| Formula | C21H23BrN6O5S | M.Wt | 551.41 |
| Solubility | DMSO: 100 mg/mL (181.35 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8135 mL | 9.0677 mL | 18.1353 mL |
| 5 mM | 362.7 μL | 1.8135 mL | 3.6271 mL |
| 10 mM | 181.4 μL | 906.8 μL | 1.8135 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)