IP Library › Granted Patent US 12667570
Granted Patent B2
US 12667570 · App. 17/791,364 · Granted Jun 30, 2026

Small molecule modulators of KSR-bound MEK

Inventors: Arvin Dar (New York, NY); Alexander P. Scopton (New York, NY); Jayasudhan Reddy Yerabolu (New York, NY); Zaigham M. Khan (New York, NY); Alexander Michael Real (Newton, MA); William Michael Marsiglia (New York, NY)
Assignee: Icahn School of Medicine at Mount Sinai
A61K31/519
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Quick Facts
Patent No.
US 12667570
App. No.
17/791,364
Granted
Jun 30, 2026
Kind
B2
Abstract

An ATP non-competitive inhibitor of mitogen-activated protein kinase (MEK), inter alia, human MEK (MEK1 or MEK2) having the properties: (i) allosterically binds an inhibitor pocket formed at an interaction interface between human MEK (MEK1 or MEK2) and human Kinase Suppressor of Ras (KSR1 or KSR2 or BRAF) adjacent to ATP in a physiological complex between MEK and KSR (or BRAF), forming an inhibitor-inhibitor pocket complex; (ii) is an ATP non-competitive kinase inhibitor; (iii) a structure such that when bound to the inhibitor-inhibitor pocket complex, the complex comprises the structural elements: (a) at least one moiety of the inhibitor engaging A825 of KSR1, or P878 of KSR2; or R662 of BRAF (b) at least one moiety engaging R234 of MEK, wherein where R234 is within 5 Å from any atoms of KSR1 or KSR2 or BRAF is disclosed.

Claims (3)

1 . An ATP non-competitive inhibitor of mitogen-activated protein kinase, having the following structure:

2 . Pharmaceutically acceptable salts of the ATP non-competitive inhibitor of mitogen-activated protein kinase of claim 1 .

3 . Enantiomers of the ATP non-competitive inhibitor of mitogen-activated protein kinase of claim 1 .