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C25-140 

目录号: HY-120934
产品使用指南

C25-140 是 TRAF6–Ubc13 相互作用的抑制剂,通过阻断 TRAF6 和 Ubc13 的相互作用,从而降低 TRAF6 活性。C25-140扩展了研究泛素系统对免疫信号的影响,并强调了 TRAF6 E3 连接酶活性在银屑病和类风湿性关节炎中的重要性。

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C25-140 Chemical Structure

C25-140 Chemical Structure

CAS No. : 1358099-18-9

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥2310 In-stock
5 mg ¥2100 In-stock
10 mg ¥3500 In-stock
50 mg ¥12500 In-stock
100 mg ¥20000 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Description

C25-140 is an inhibitor of the TRAF6–Ubc13 interaction by blocking the interaction of TRAF6 with Ubc13 to lower 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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× = ×
C1   V1   C2   V2

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产品名称:
C25-140
目录号:
HY-120934
需求量:

C25-140

Cat. No.: HY-120934