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

C25-140 

目录号: HY-120934 纯度: 99.84%
产品使用指南

C25-140 是一种一流的,具有一定选择性的 TRAF6-Ubc13 相互作用的抑制剂,直接与 TRAF6 结合,阻断 TRAF6 和 Ubc13 的相互作用,从而降低 TRAF6 活性,降低 NF-κB 的活性,并对抗自身免疫。

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C25-140 Chemical Structure

C25-140 Chemical Structure

CAS No. : 1358099-18-9

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2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

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, a first-in-class, fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity[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[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 R 837-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: R 837-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.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (136.59 mM; Need ultrasonic)

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
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

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

    此方案可获得 ≥ 2.17 mg/mL (4.74 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

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

    此方案可获得 ≥ 2.17 mg/mL (4.74 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定溶至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

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

    此方案可获得 ≥ 2.17 mg/mL (4.74 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
References

Purity: 99.84%

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

C25-140TNF ReceptorE1/E2/E3 EnzymeTumor Necrosis Factor ReceptorTNFRE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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产品名称:
C25-140
目录号:
HY-120934
需求量: