1. Apoptosis
    Metabolic Enzyme/Protease
  2. TNF Receptor
    E1/E2/E3 Enzyme
  3. C25-140

C25-140 

Cat. No.: HY-120934
Handling Instructions

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).

For research use only. We do not sell to patients.

C25-140 Chemical Structure

C25-140 Chemical Structure

CAS No. : 1358099-18-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 990 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Technical Information

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  • References

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].

IC50 & 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. Taken together, 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.
Solvent & Solubility
In Vitro: 

DMSO : ≥ 130 mg/mL (284.11 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1855 mL 10.9273 mL 21.8546 mL
5 mM 0.4371 mL 2.1855 mL 4.3709 mL
10 mM 0.2185 mL 1.0927 mL 2.1855 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (4.74 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (4.74 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (4.74 mM); Clear solution

References
Molecular Weight

457.57

Formula

C₂₆H₃₁N₇O

CAS No.

1358099-18-9

SMILES

O=C(N1CCC(CC2=CC=CC=C2)CC1)CCC3=C(C)N(C4=NN5C(C=C4)=NN=C5C)N=C3C

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
C25-140
Cat. No.:
HY-120934
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C25-140

Cat. No.: HY-120934