A UAE inhibitor (IC50 = 1 nM); selective for UAE over NAE

MLN7243 – 1 mg

Brand:
Cayman
CAS:
1450833-55-2
Storage:
-20
UN-No:
Non-Hazardous - /

MLN7243 is an inhibitor of ubiquitin-activating enzyme (UAE; IC50 = 1 nM).{52441} It is selective for UAE over NEDD8-activating enzyme (NAE), SUMO-activating enzyme (SAE), and the autophagy-activating enzyme ATG7 (IC50s = 28, 850, and >10,000 nM, respectively). MLN7243 inhibits proliferation in a panel of 30 cancer cell lines (EC50s = 0.006-1.1 µM). It activates the unfolded protein response (UPR) and expansion of the endoplasmic reticulum surface area, a marker of ER stress, in HCT116 cells. In vivo, MLN7243 (12.5-25 mg/kg) reduces tumor growth in WSU-DLCL2, HCT116, Calu-6, THP-1, CWR22, HCC70, and MM.1S mouse xenograft models, as well as patient-derived xenograft (PDX) mouse models of colon, lung, breast, ovarian, and neck cancer.  

 

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SKU: 30108 - 1 mg Category:

Description

A UAE inhibitor (IC50 = 1 nM); selective for UAE over NAE, SAE, and ATG7 (IC50s = 28, 850, and >10,000 nM, respectively); inhibits proliferation in a panel of 30 cancer cell lines (EC50s = 0.006-1.1 µM); activates the UPR and expansion of the endoplasmic reticulum surface area in HCT116 cells; reduces tumor growth in various mouse xenograft models and PDX mouse models from 12.5-25 mg/kg

Formal name: sulfamic acid, [(1R,2R,3S,4R)-2,3-dihydroxy-4-[[2-[3-[(trifluoromethyl)thio]phenyl]pyrazolo[1,5-a]pyrimidin-7-yl]amino]cyclopentyl]methyl ester

Synonyms:  TAK-243

Molecular weight: 519.5

CAS: 1450833-55-2

Purity: ≥98%

Formulation: A crystalline solid

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