2. Signaling Pathways
  3. Cytoskeleton
  4. Cdc42-binding kinase
  5. MRCKβ Isoform

MRCKβ

MRCKβ (myotonic dystrophy kinase-related Cdc42-binding kinase β), encoded by CDC42BPB, is a serine/threonine kinase that functions as a downstream effector of the Rho GTPase Cdc42 and regulates actomyosin cytoskeletal organization, cell polarity, and migration through phosphorylation of substrates involved in myosin contractility[1][2]. Mechanistically, MRCKβ promotes myosin light chain (MLC) phosphorylation and cooperates with additional cytoskeletal regulators to control actin-myosin dynamics required for cell shape remodeling and directional movement[2][3]. MRCKβ shares substantial kinase-domain homology with MRCKα and partially overlapping substrate specificity with ROCK kinases; however, its C-terminal regulatory architecture differs from ROCK family members, supporting distinct signaling functions during cytoskeletal regulation and invasion[2]. In cancer models, Cdc42-MRCK signaling contributes to mesenchymal cell invasion, collective migration, and extracellular matrix penetration by sustaining actomyosin contractility, and combined inhibition of MRCK and ROCK produces stronger suppression of invasive behavior than targeting either pathway alone[2][4]. MRCKβ has therefore emerged as a relevant experimental target in tumor invasion studies, particularly in breast cancer and squamous cell carcinoma models[2][4]. For research applications, selective MRCK inhibitors including BDP-9066, BDP8900, and related small molecules suppress substrate phosphorylation, cell migration, and invasion, providing useful pharmacological tools for dissecting MRCK-dependent signaling networks and evaluating anti-invasive therapeutic strategies[4][5][6].

MRCKβ Related Products (3):

Cat. No. Product Name Effect Purity
  • HY-111424
    BDP9066
    		Inhibitor 98.18%
    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, Ki 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.
  • HY-125221
    DJ4
    		Inhibitor 99.25%
    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.
  • HY-111423
    BDP8900
    		Inhibitor
    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.