Formulation: A solid
Formal Name: sulfamic acid, [(1R,2S,4R)-4-[[5-[[1-[(3-bromophenyl)methyl]-1H-pyrazol-3-yl]carbonyl]-4-pyrimidinyl]amino]-2-hydroxycyclopentyl]methyl ester
Purity: ≥98%
Formula Markup: C21H23BrN6O5S
Formula Weight: 551,4
Shelf life (days): 1460
CAS Number: 1644342-14-2
Notes: ML-792 is an inhibitor of SUMO-activating enzyme (SAE; IC50s = 0.003 and 0.011 µM with small ubiquitin-related modifier 1 (SUMO-1) or SUMO-2, respectively, as the ubiquitin-like proteins).{69035} It is selective for SAE over NEDD8-activating enzyme (NAE) and ubiquitin-activating enzyme (UAE; IC50s = 32 and >100 µM, respectively). ML-792 inhibits SAE activity and decreases global SUMOylation in HCT116 human colon cancer cells (EC50 = 0.019 µM), as well as decreases the viability of MDA-MB-468 human breast and A375 human melanoma cells (EC50s = 0.06 and 0.45 µM, respectively). It also induces mitotic defects in HCT116 cells and impairs chromosomal segregation in HCT116, A375, and COLO 205 cells. ML-792 reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 150 and 200 mg/kg twice per day.{69036}
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