ML-792 |
| رقم الكتالوجGC36631 |
ML-792 هو مثبط قوي وانتقائي لـ SAE / SUMO1 و SAE / SUMO2 في المقايسات الأنزيمية (قيم IC من 3 و 11 نانومتر ، على التوالي) مقارنة مع NAE / NEDD8 و UAE / ubiquitin (قيم IC من 32 ميكرومتر و> 100 ميكرومتر ، على التوالى).
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 |
| الذوبان | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8135 mL | 9.0677 mL | 18.1353 mL |
| 5 mM | 0.3627 mL | 1.8135 mL | 3.6271 mL |
| 10 mM | 0.1814 mL | 0.9068 mL | 1.8135 mL |
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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