Drug intelligence / Profile preview

mkc-1

Development stage
Phase 2
Lead developer
CASI Pharmaceuticals
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

MKC-1 is an orally bioavailable small-molecule bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. It acts by inhibiting tubulin polymerization and blocking the formation of the mitotic spindle, leading to cell cycle arrest at the G2/M phase and apoptosis. MKC-1 also inhibits cyclin-dependent kinase 1 (CDK1) and targets pathways including Akt/mTOR. The drug has demonstrated broad antitumor activity in preclinical studies and has been investigated for use in various cancers such as breast cancer, leukemia, lung cancer, and solid tumors[1][2][4][5]. It was initially developed by F. Hoffmann-La Roche[7].

Other names
bisindolylmaleimide cell cycle inhibitorR-440R440R 440
02

Targets

KPNB1 (Importin subunit beta-1)TUBB (Tubulin (alpha and beta subunits))CDK1 (Cyclin-dependent kinase 1)Mechanistic target of rapamycin kinase complex 2

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