Cdc42-binding kinase Inhibitor

BDP9066 is a potent and selective myotonic dystrophy-related Cdc42-binding kinase MRCK inhibitor with an IC₅₀ of 64 nM for MRCKβ in SCC12 cells, K_i values of 0.0136 nM and 0.0233 nM for MRCKα/β in house determinations, respectively. BDP9066 has therapeutic effect on skin cancer by reducing substrate phosphorylation.

(R)-BDP9066 is an isomer of BDP9066 and has lower activity compared to BDP9066. BDP9066 is a potent inhibitor of myotonic dystrophy kinase-related Cdc42-binding kinase (MRCK). (R)-BDP9066 is derived from patent WO2019034890A1 (E118).

DJ4 is a ATP-competitive inhibitor of ROCK1/2 (IC₅₀ values:5 and 50 nM) and MRCKα/β (IC₅₀ values:10 and 100 nM). DJ4 blocks stress fiber formation and inhibits migration and invasion of cancer cells. DJ4 can be used for study of lung cancer, breast cancer, and pancreatic (PANC-1) cancer.

Rac/Cdc42-IN-1, the major phase I metabolite of the oral Rac/Cdc42 inhibitor MBQ-167 (HY-112842) in vivo, is a selective Rac inhibitor. Rac/Cdc42-IN-1 functions by blocking the GTP-binding activation of Rac1, targeting the autophosphorylation of Thr⁴²³/Thr⁴⁰²/Thr⁴³⁶ and Ser¹⁴¹/Ser¹⁴⁴/Ser¹⁵⁴ in downstream PAK1/2/3, with an inhibitory effect superior to that of MBQ-167. Rac/Cdc42-IN-1 significantly inhibits cell migration, and suppresses tumor growth and distant metastasis to the lung, liver and kidney in HER2+ breast cancer mouse models. Rac/Cdc42-IN-1 can be used for targeted research on metastatic breast cancer.

BDP8900 is a potent and selective inhibitor of myotonic dystrophy-related Cdc42-binding kinases (MRCKα and MRCKβ). BDP8900 reduces substrate phosphorylation, leading to morphological changes, motility inhibition and invasiveness of cancer cells.