SB 202190

SB 202190是一种高度选择性、强效且能够透过细胞膜的 p38 MAP 激酶抑制剂，IC50 值分别为 50 nM 和 100 nM，针对 p38α 和 p38β；此外，它对 BRD4 也有略微的抑制作用（Kd = 3.4 μM）。

Mitogen-activated protein kinase (MAPK) cascades regulate signal transduction involved in cell proliferation and death. SB-202190 is a potent cell-permeable inhibitor of p38 MAPK that inhibits p38 and p38β with IC50 values of 50 nM and 100 nM, respectively³. SB-202190 at 5 μM inhibited the activation of p38 in HaCaT cells. The protein expression of COX-2 was almost completely blocked by 5 μM SB-202190 at 8 and 12 h post the exposure to UVB irradiation (250 J/m²). SB-202190 at the same concentration also significantly abrogated UVB induced cox-2mRNA in HaCaT cells. The inhibitory effect of SB-202190 on PGE₂ production after UVB was observed in HaCaT cells treated by 5 μM SB-202190 for one hour⁴. Bull serum albumin induced the gene expression of the inflammation marker MCP-1 more than 30-fold in renal tubular cells, while pre-incubation with 10 μM SB-202190 decreased the gene expression to the basal level. In HK-2 cells, 10 μM SB202190 treatment significantly reduced TGF-β1-induced gene expression⁵. Two doses of SB-202190 (6.25 μg/dose, i.d. administered) prevented the development of blisters and a positive Nikolsky’s skin induced by PV IgG injection (1.5 mg of IgG/g body weight) in neonatal mice. The PV IgG-mediated activation of phospho-p38MAPK immunoreactivity in the skin was abrogated in SB-202190-treated mice⁶.

溶解方案(细胞实验)

DMSO 中的溶解度 : 100 mg/mL (301.80 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

溶解方案(动物实验)

"方案一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.08 mg/mL (6.28 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"

"方案二": "请依序添加每种溶剂：10% DMSO 90% (20% SBE-β-CD in Saline)Solubility: ≥ 2.08 mg/mL (6.28 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。以 1 mL 工作液为例，取 100 μL 20.8 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。20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。"

"方案三": "请依序添加每种溶剂：10% DMSO 90% Corn OilSolubility: ≥ 2.08 mg/mL (6.28 mM); 澄清溶液 此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。"