| 产品编号 |
产品名称 |
产品包装 |
产品价格 |
| SD5946-5mg |
PD169316 (p38 MAPK抑制剂) |
5mg |
506.00元 |
化学信息：
|
化学名
|
4-[4-(4-fluorophenyl)-2-(4-nitrophenyl)-1H-imidazol-5-yl]pyridine
|
|
|
简称
|
PD169316
|
|
别名
|
PD 169316, PD-169316
|
|
中文名
|
N/A
|
|
化学式
|
C20H13FN4O2
|
|
分子量
|
360.34
|
|
CAS号
|
152121-53-4
|
|
纯度
|
98%
|
|
溶剂/溶解度
|
Water<1mg/ml; DMSO10mg/ml; Ethanol<1mg/ml
|
|
溶液配制
|
5mg加入1.39ml DMSO，或者每3.6mg加入1ml DMSO，配制成10mM溶液。SD5946-10mM用DMSO配制。
|
生物信息：
|
产品描述
|
PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor (IC50=89nM).
|
|
信号通路
|
MAPK
|
|
靶点
|
p38 MAPK
|
－
|
－
|
－
|
－
|
|
IC50
|
89nM
|
－
|
－
|
－
|
－
|
|
体外研究
|
PD169316, a p38 MAPK inhibitor, abrogates signaling initiated by both TGFbeta and Activin A, but not bone morphogenetic protein (BMP) 4. Inhibition of TGFbeta signaling is dose dependent and results in reduced Smad2 and Smad3 phosphorylation, nuclear translocation, and up-regulation of the TGFbeta target gene Smad7. Reduced TGFbeta signaling is not due to abrogation of p38 MAPK activity, since blocking p38 MAPK activity with a dominant negative form of p38 MAPK has no effect on TGFbeta/Smad signaling. PD169316 at 5μM or higher can block TGFβ signaling activity and thus caution must be used when attributing cellular activities exclusively to p38 MAPK signaling when these inhibitors are used experimentally. PD169316 significantly attenuated apoptosis in potassium-deprived cells in a dose dependent manner. PD169316 rescued the inhibitory effect of sphingosine on the formation of inositol phosphates by PGF(2alpha) or NaF in osteoblast-like MC3T3-E1 cells. 6-keto-PGF(1alpha) release was increased in a concentration-dependent manner following LPS exposure (maximal at 10(-6)g/ml; EC(50)=1 x 10(-9)g/ml), and was significantly inhibited by p38 MAPK blockade (reduced from 1.6+/-0.3 x 10(-9)g/ml to 4+/-1 x 10(-10)g/ml and 4+/-2 x 10(-10)g/ml with 10(-6) M SB203580 or 10(-6) M PD169316, respectively).
|
|
体内研究
|
N/A
|
|
临床实验
|
N/A
|
|
特征
|
N/A
|
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
|
酶活性检测实验
|
|
方法
|
N/A
|
|
细胞实验
|
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细胞系
|
N/A
|
|
浓度
|
N/A
|
|
处理时间
|
N/A
|
|
方法
|
N/A
|
|
动物实验
|
|
动物模型
|
N/A
|
|
配制
|
N/A
|
|
剂量
|
N/A
|
|
给药方式
|
N/A
|
参考文献：
1. Fu Y, et al. Biochem Biophys Res Commun. 2003 Oct 17, 310(2), 391-7.
2. Nath R, et al. Cell Mol Biol Lett. 2001, 6(2), 173-84.
3. Kozawa O, et al. Cell Signal. 2000 Jul, 12(7), 447-50.
4. Brooks AC, et al. Vet Immunol Immunopathol. 2009 Jun 15, 129(3-4), 174-80.
包装清单：
|
产品编号
|
产品名称
|
包装
|
|
SD5946-10mM
|
PD169316 (p38 MAPK抑制剂)
|
10mM×0.2ml
|
|
SD5946-5mg
|
PD169316 (p38 MAPK抑制剂)
|
5mg
|
|
SD5946-25mg
|
PD169316 (p38 MAPK抑制剂)
|
25mg
|
|
—
|
说明书
|
1份
|
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品对人体有害，操作时请小心，并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。