ML792

製品コードS8697 バッチS869701

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
化学式
C21H23BrN6O5S
分子量 551.41 CAS No. 1644342-14-2
Solubility (25°C)* 体外 DMSO 100 mg/mL (181.35 mM)
Water Insoluble
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

5.000mg/ml (9.07mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

0.625mg/ml (1.13mM) Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or 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.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 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.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HCT116 cells
濃度 0.5 μM
反応時間 48 h
実験の流れ

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 is used as a positive control for induction of DNA-strand breaks. To study how loss of SUMOylation contributes to repair of DNA damage, individual wells of HCT116 cells are treated with the following treatments: DMSO (6 h); 0.5 μM ML-792 (6 h).

参考

  • https://pubmed.ncbi.nlm.nih.gov/28892090/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

SUMO4 promotes SUMO deconjugation required for DNA double-strand-break repair [ Mol Cell, 2025, 85(5):877-893.e9] PubMed: 40054443
Transcription-coupled DNA-protein crosslink repair by CSB and CRL4CSA-mediated degradation [ Nat Cell Biol, 2024, 10.1038/s41556-024-01394-y] PubMed: 38600236
SUMO promotes DNA repair protein collaboration to support alternative telomere lengthening in the absence of PML [ Genes Dev, 2024, 38(13-14):614-630] PubMed: 39038850
SUMO Promotes DNA Repair Protein Collaboration to Support Alterative Telomere Lengthening in the Absence of PML [ bioRxiv, 2024, 2024.02.29.582813] PubMed: 38463993
The SUMO-NIP45 pathway processes toxic DNA catenanes to prevent mitotic failure [ Nat Struct Mol Biol, 2023, 10.1038/s41594-023-01045-0] PubMed: 37474739
PML and PML-like exonucleases restrict retrotransposons in jawed vertebrates [ Nucleic Acids Res, 2023, 51(7):3185-3204] PubMed: 36912092
Heat-shock protein 90α protects NME1 against degradation and suppresses metastasis of breast cancer [ Br J Cancer, 2023, 10.1038/s41416-023-02435-3] PubMed: 37731021
Knockdown of UBE2I inhibits tumorigenesis and enhances chemosensitivity of cholangiocarcinoma via modulating p27kip1 nuclear export [ Mol Carcinog, 2023, 62(5):700-715] PubMed: 36825757
SUMOylation of Nuclear γ-Actin by SUMO2 supports DNA Damage Repair against Myocardial Ischemia-Reperfusion Injury [ Int J Biol Sci, 2022, 18(11):4595-4609] PubMed: 35864967
Neddylation is essential for β-catenin degradation in Wnt signaling pathway [ Cell Rep, 2022, 38(12):110538] PubMed: 35320710

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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