1358099-18-9
1358099-18-9 structure
- Name: C25-140
- Chemical Name: C25-140
- CAS Number: 1358099-18-9
- Molecular Formula: C26H31N7O
- Molecular Weight: 457.57
- Catalog: Signaling Pathways Apoptosis TNF Receptor
- Create Date: 2019-06-01 15:26:45
- Modify Date: 2024-01-14 20:58:10
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C25-140, a first-in-class TRAF6-Ubc13 inhibitor, directly binds to TRAF6, thereby blocks the interaction of TRAF6 with Ubc13 and as a consequence lowers TRAF6 activity. C25-140 expands studying the impact of the ubiquitin system on immune signaling and underscores the importance of TRAF6 E3 ligase activity in psoriasis and rheumatoid arthritis (RA)[1].
| Name | C25-140 |
|---|
| Description | C25-140, a first-in-class TRAF6-Ubc13 inhibitor, directly binds to TRAF6, thereby blocks the interaction of TRAF6 with Ubc13 and as a consequence lowers TRAF6 activity. C25-140 expands studying the impact of the ubiquitin system on immune signaling and underscores the importance of TRAF6 E3 ligase activity in psoriasis and rheumatoid arthritis (RA)[1]. |
|---|---|
| Related Catalog | |
| Target |
TRAF6-Ubc13[1] |
| In Vitro | C25-140 dose-dependently impedes TRAF6-Ubc13 interaction[1]. C25-140 (10-30 μM; 2 hours) effectively reduces TRAF6-mediated ubiquitin chain formation[1]. C25-140 affects TNFα-induced phosphorylation of IκBα as well as NF-κB-induced target gene expression[1]. C25-140 efficiently inhibits IL-1β- and TNFα-mediated receptor signaling in the context of cytokine activation[1]. Western Blot Analysis[1] Cell Line: TRAF6WT Concentration: 10 μM, 20 μM, 30 μM Incubation Time: 2 hours Result: Effectively reduced TRAF6-mediated ubiquitin chain formation. |
| In Vivo | C25-140 (~1.5 mg/kg; topically to the shaved back and the right ear; twice daily for 6 days) ameliorates symptoms of autoimmune psoriasis in Imiquimod-induced psoriasis mouse model[1]. C25-140 (6-14 mg/kg; given i.p.; twice daily for 14 days) shows a dose-dependent improvement of RA disease outcome in Collagen-induced arthritis (CIA) model[1]. Animal Model: Imiquimod-induced psoriasis mouse model (male BALB/c mice)[1] Dosage: ~1.5 mg/kg Administration: Topically to the shaved back and the right ear; twice daily for 6 days Result: Showed a dose-dependent improvement of RA disease outcome. Animal Model: Collagen-induced arthritis (CIA) model in DBA1/J mice[1] Dosage: 6 mg/kg, 10 mg/kg, 14 mg/kg Administration: Given i.p.; twice daily for 14 days Result: Ameliorated the arthritic index to almost baseline levels in this efficacy model at doses of 10 and 14 mg/kg. Dose-dependently improved symptoms of RA including inflammation and structural damage. |
| References |
| Molecular Formula | C26H31N7O |
|---|---|
| Molecular Weight | 457.57 |
| Storage condition | 2-8℃ |