1644342-14-2

1644342-14-2 structure

Name: ML 792
Chemical Name: {(1R,2S,4R)-4-[(5-{[1-(3-Bromobenzyl)-1H-pyrazol-3-yl]carbonyl}-4-pyrimidinyl)amino]-2-hydroxycyclopentyl}methyl sulfamate
CAS Number: 1644342-14-2
Molecular Formula: C₂₁H₂₃BrN₆O₅S
Molecular Weight: 551.414
Create Date: 2020-01-12 07:38:50
Modify Date: 2024-01-16 23:03:50
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.

Name	{(1R,2S,4R)-4-[(5-{[1-(3-Bromobenzyl)-1H-pyrazol-3-yl]carbonyl}-4-pyrimidinyl)amino]-2-hydroxycyclopentyl}methyl sulfamate
Synonyms	Sulfamic acid, [(1R,2S,4R)-4-[[5-[[1-[(3-bromophenyl)methyl]-1H-pyrazol-3-yl]carbonyl]-4-pyrimidinyl]amino]-2-hydroxycyclopentyl]methyl ester {(1R,2S,4R)-4-[(5-{[1-(3-Bromobenzyl)-1H-pyrazol-3-yl]carbonyl}-4-pyrimidinyl)amino]-2-hydroxycyclopentyl}methyl sulfamate

Description	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.
References	References 1. He X, et al. Nat Chem Biol. 2017 Sep 11. doi: 10.1038/nchembio.2463. View Related Products by Target Ubiquitin-activating Enzyme (E1)