SP600125
作者：齊岳
發(fā)布時間：2023-09-11
09:05:17
點擊數(shù)：
產(chǎn)品名稱：SP600125
產(chǎn)品描述：
| 產(chǎn)品描述 | SP600125 is a JNK1/2/3 inhibitor (IC50: 40/40/90 nM) and 10-fold higher selectivity than MKK4, 25-fold higher selectivity than MKK3, MKK6, PKCα, and PKB. |
| 靶點活性 | JNK1:40 nM (cell free), JNK2:40 nM (cell free), JNK3:90 nM (cell free) |
| 體外活性 | In cells, SP600125 dose-dependently inhibited the phosphorylation of c-Jun ( IC50s: 5–10 μM), the expression of inflammatory genes COX-2, IL-2, IFN-gamma, TNF-alpha, and prevented the activation and differentiation of primary human CD4 cell cultures [1]. Fas agonistic antibody CH11-induced autophagy was blocked by SP600125, and the CH11-induced apoptosis was increased by SP600125 [2]. In synchronized cells, SP600125 prevents the entry of cells into mitosis and leads to endoreplication of DNA from G2 phase. The inhibitory effect of SP600125 on mitotic entry predominantly occurs upstream of Aurora A kinase and Polo-like kinase 1, resulting in a failure to remove the inhibitory phosphorylation of Cdk1 [3]. |
| 體內(nèi)活性 | In control animals, CD4+ CD8+ thymocytes represented just less than 40% of total thymocytes. Forty-eight hours after exposure to CD3 Ab in vivo, the percentage of CD4+ CD8 + cells had declined to 10%. Mice receiving SP600125 showed almost complete resistance to CD3 Ab-mediated apoptosis with CD4+ CD8+ numbers the same as control animals [1]. Pulmonary edema, the expression of inflammatory cytokines and pathological alterations were found to be significantly attenuated in LPS-induced ALI following treatment with SP600125 in vivo [4]. |
| 細(xì)胞實驗 | Multiarray plate screening of mRNA was performed by High Throughput Genomics. In brief, cell lysates were prepared by using a single-step proprietary lysis buffer. Lysates were incubated with a 16-gene capture array manufactured into each well of a 96-well plate. Detection was by luminescence and was performed by HTG. SDs for triplicate samples were typically 3–8% for samples with high levels of gene expression and 15–25% for samples with very low (near-threshold) levels of cytokine gene expression [1]. |
| 動物實驗 | Mouse LPS/TNF assay was performed as follows: Female CD-1 mice (8–10 weeks of age) were dosed i.v. or per os with SP600125 in PPCES vehicle (30% PEG-400/20% polypropylene glycol/15% Cremophor EL/5% ethanol/30% saline), final volume of 5 ml/kg, 15 min before i.v. injection with LPS in saline (0.5 mg/kg; Escherichia coli 055:B5). At 90 min, a terminal bleed was obtained from the abdominal vena cava, and the serum was recovered. Samples were analyzed for mouse TNF-α by using an ELISA. The in-life phase of the thymocyte apoptosis assay was performed in female C57BL/6 mice. SP600125 was administered at 0, 12, 24, and 36 h, 15 mg/kg s.c. in PPCES vehicle. Anti-CD3 (50 μg) i.p. (clone 145-2C11) was administered as a single dose immediately after SP600125 at time 0. After 48 h, mice were killed, and the thymus was dissected for thymocyte isolation. Treated and untreated mice thymuses were excised and immediately placed in complete medium (RPMI medium 1640 with 10% FBS, penicillin/streptomycin, and l-glutamine) on ice. Each thymus was then pressed between the frosted ends of 2 microscope slides to form a single cell suspension and collected through a 30 μm nylon mesh. Cells were stained for cell surface CD4 and CD8 and apoptosis and measured by flow cytometry [1]. |
| 別名 | JNK Inhibitor II, 1PMV, Nsc75890, Pyrazolanthrone |
| 分子量 | 220.23 |
| 分子式 | C14H8N2O |
| CAS No. | 129-56-6 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 22 mg/mL (100 mM)
Ethanol: 1.1 mg/mL (5 mM)),with gentle warming
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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