YE6144 is a prototypical interferon regulatory factor 5 (IRF5) inhibitor. YE6144 selectively suppresses IRF5 activity through inhibition of IRF5 phosphorylation[1].
In Vitro
YE6144 (1 or 3 μM; 30 min) inhibits the phosphorylation of IRF5 in both human PBMCs and mouse splenocytes[1].
YE6144 (0-10 μM; 30 min) inhibits the production of type I IFNs with an IC50 of approximately 0.09 μM in human HC PBMCs[1].
Western Blot Analysis[1]
| Cell Line: |
Human HC PBMCs and mouse WT splenocytes |
| Concentration: |
1 μM (PBMCs) and 3 μM (splenocytes) |
| Incubation Time: |
30 min |
| Result: |
Inhibited the phosphorylation of IRF5. |
In Vivo
YE6144 (40.0 mg/kg; s.c.; once) suppresses the progression of mouse systemic lupus erythematosus[1].
| Animal Model: |
NZB/W F1 mouse model of systemic lupus erythematosus (SLE)[1] |
| Dosage: |
40.0 mg/kg |
| Administration: |
Subcutaneous injection, once |
| Result: |
Suppressed the exacerbation of autoantibody production. Splenomegaly and renal dysfunction were also suppressed by the treatment after disease onset. |