ML 792

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ML 792 是一种有效的选择性 SUMO 激活酶 (SAE) 抑制剂，对 SAE/SUMO1 和 SAE/SUMO2 的 IC50 分别为 3 nM 和 11 nM。

ML 792 is a potent, seletive SUMO-activating enzyme (SAE) inhibitor with IC50 of 3 nM and 11 nM for SAE/SUMO1 and SAE/SUMO2, respectively; shows no significant inhibition for closely related E1 enzymes NAE (IC50=32 uM) and ubiquitin-activating enzyme (UAE) (IC50 >100 uM), as well as a panel of 366 ATP-using enzymes; dose-dependently decreases global SUMOylation in HCT116 cells (EC50=19 nM), demonstrates potent antiproliferative effect in HCT116 cells and MDA-MB-231 cells with EC50 of 0.04 and 0.11 uM, respectively.

ML-792 (0.0007-5 μM; 4 hours) inhibits SAE and SUMO-pathway activities in HCT116 cells.ML-792 (0.001-10 μM; 72 hours ) inhibits cell proliferation and decreases cancer cell viability in MDA-MB-468, MDA-MB-231, HCT116, Colo-205, and A375. Cell Viability Assay Cell Line:Human breast cancer cells MDA-MB-468 and MDA-MB-231; human colon carcinoma cells HCT116 and Colo-205; human melanoma cell line A375 Concentration:0.001, 0.01, 0.1, 1, 10 μM Incubation Time:72 hours Result:Demonstrated a dose-dependent viability effect with EC50 values of 0.06 μM in MDA-MB-468 cells to 0.45 μM in A375 cells.Western Blot Analysis Cell Line:HCT116 cells Concentration:0, 0.0007, 0.002, 0.007, 0.02, 0.06, 0.19, 0.56, 1.7, 5 μM Incubation Time:4 hours Result:Revealed a dose-dependent decrease in the SAE and UBC9 thioester levels.

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ML792

Proteasome/Ubiquitin

E1

E1

Cancer

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1644342-14-2

551.416

C21H23BrN6O5S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (181.35 mM)

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

((1R,2S,4R)-4-((5-(1-(3-bromobenzyl)-1H-pyrazole-3-carbonyl)pyrimidin-4-yl)amino)-2-hydroxycyclopentyl)methyl sulfamate

(-20℃)

With Ice Pack

≥ 2 years