5.31535

AP-1/NF-κB Dual Inhibitor, SP100030

• 别名: AP-1/NF-κB Dual Inhibitor, SP100030, 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3ʹ,5ʹ-bis(trifluoromethyl)phenyl)-carboxamide, N-(3,5-bis(Trifluoromethyl)phenyl)-2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxamide, Activator Protein-1 Activation Inhibitor; AP-1 Acti, SP-100030, Nuclear Factor-κB Activation Inhibitor XI, 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3ʹ,5ʹ-bis(trifluoromethyl)phenyl)-carboxamide, N-(3,5-bis(Trifluoromethyl)phenyl)-2-chloro-4-(trifluoromethyl)pyrimidine-5-carboxamide, Activator Protein-1 Activation Inhibitor; AP-1 Activation Inhibitor, NF-κB Activation Inhibitor XI
• 经验公式（希尔记法）: C₁₄H₅ClF₉N₃O
• CAS号: 154563-54-9
• 分子量: 437.65
• 分類程式碼代碼: 51111800
• NACRES: NA.77

属性

• 化驗: ≥95% (HPLC)
• 品質等級: 100
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: off-white
• 溶解度: DMSO: 100 mg/mL
• 儲存溫度: 2-8°C

说明

一般說明

A cell-permeable, conformationally restricted pyrimidinecarboxamide compound that is reported to inhibit against the activation of AP-1- & NF-κB-, but not &beta-actin-, mediated transcriptions (IC₅₀ = 50 nM in Jurkat-based reporter assays; 0.5 h drug pretreatment prior to 5 h stimulation with 1 µg/mL PHA/526511 & 50 ng/mL PMA/500582 & 524400) and target genes expressions, including IL-2, IL-8, TNF-α, in 6 T cell cultures (by >85% at 3 µM), while exhibiting little inhibitory potency against cytokine inductions in 10 non-T cell cultures (by <5% at 10 µM), including endothelial, epithelial, fibroblast, monocytic, and osteoblast cultures. Intraperitoneal injection is shown to display in vivo anti-inflammatory efficacy in a murine model of collagen-induced arthritis (10 mg/kg/d) and a rodent model of Ova-induced asthma response (20 mg/kg/d). Dual AP-1 & NF-κB inhibition via daily SP100030 subcutaneous injection is also reported to suppress AH-130 Yoshida ascites hepatoma tumor expansion in rats in vivo (5 mg/kg/d).

A cell-permeable, non-toxic, conformationally restricted pyrimidinecarboxamide compound that acts as a potent, reversible T-cell specific inhibitor of both AP-1 and NF-κB transcriptional activation (IC₅₀ = 50 nM). Reduces DNA binding activity of NF-κB and downregulates NF-κB driven cytokine gene expression. Displays only trivial inhibitory effect against cytokine induction in a variety of other cells. Exhibits anti-inflammatory activity in a murine model of collagen-induced arthritis (~ 10 mg/kg/d, i.p.) and suppresses the expansion of AH-130 Yoshida ascites hepatoma in rats (~ 5 mg/kg/d, i.p.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化／生理作用

Cell permeable: yes

Primary Target
AP-1 and NF-κB

Reversible: yes

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Use only fresh DMSO for reconstitution.

其他說明

Ye, N., et al. 2014. J. Med. Chem.57, 6930.
Moore-Carrasco, R., et al. 2009. Anticancer Res.29, 1315.

Huang, T.J., et al. 2001. Br. J. Pharmacol.134, 1029.
Gerlag, D.M., et al. 2000. J. Immunol.165,1652.
Sullivan, R.W., et al. 1998. J. Med. Chem.41, 413.
Goldman, M.E., et al. 1996. Transplant. Proc.28, 3106.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable