Product Name: MLN-7243

Request MLN-7243

CAT#: A-1384


  Synonym:MLN-7243,

MLN-7243 Chemical Structure
MLN-7243 chemical structure


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Biological Activity
MLN7243 is the first-in-class inhibitor specifically targeting this class of enzyme to be studied clinically.

A small molecule inhibitor of ubiquitin-activating enzyme (UAE), with potential antineoplastic activity. UAE inhibitor MLN7243 binds to and inhibits UAE, which prevents both protein ubiquitination and subsequent protein degradation by the proteasome. This results in an excess of proteins in the cells and may lead to endoplasmic reticulum (ER) stress-mediated apoptosis. This inhibits tumor cell proliferation and survival. UAE, also called ubiquitin E1 enzyme (UBA1; E1), is more active in cancer cells than in normal, healthy cells.
Technical Data
CAS#: 1450833-55-2
Chemical Formula:C19H20F3N5O5S2
M.Wt.: 519.52
Purity: >99%
Chiral HPLC: 100%
Storage Conditions: 2ºC to 8 ºC, or -20ºC for 3 years.

MLN-7243 reference
From: http://www.winsymposium.org/wp-content/uploads/2014/06/L2.04_GOMEZ_NAVARRO_JESUS.pdf
Clinical Trials:A Phase 1, Dose Escalation Study of MLN7243 in Adult Patients With Advanced Solid Tumors
https://clinicaltrials.gov/ct2/show/NCT02045095