ROCK inhibition impairs macrophage trailing-edge retraction
Cell-based study · RAW264.7 mouse macrophages expressing blue opsin-mCh, stimulated locally by optical activation [1]
GSK 269962 prevented complete cell migration and trailing-edge retraction while leading-edge lamellipodia activity remained largely intact. Combined wortmannin and GSK treatment suppressed both edge activities; this combination is distinguished from GSK alone. The result supports a ROCK-associated contractility phenotype in this model, without establishing exclusive on-target action at this concentration.
| Endpoint | Reported result | Reference |
|---|---|---|
| Trailing-edge retraction and leading-edge activity | Qualitative response No trailing-edge retraction; leading-edge activity largely retained | [1] |
Literature-Reported Treatment Conditions
- Treatment concentration
- 12.5 μM
- Exposure duration
- 30 min preincubation at 37 °C; images compare 0 and 20 min during optical activation
- Method
- Drug exposure followed by live-cell optical activation and imaging
- Vehicle
- DMSO stock diluted in HBSS or culture medium; final DMSO percentage not reported in reagent paragraph
- Co-treatment
- GSK-alone phenotype is selected; 50 nM wortmannin plus GSK is a separate comparison in Fig. 3B(IV).
- Reported limits
- No biochemical target-engagement measurement or concentration-response series for GSK in this experiment.
Methods and source locations
Compound reported in the paper: GSK 269962
Named compound only; no salt equivalence, analytical purity or current Adooq lot validation is established.
Fig. 3B(III–IV), caption; ROCK inhibition Results paragraph; Experimental procedures, DNA constructs and reagents; cell culture and imaging
Trailing-edge retraction and leading-edge activity — Fig. 3B(III), caption and corresponding Results paragraph