PD 169316是一种强效、细胞可渗透和选择性的 p38 MAP 激酶抑制剂,IC50 为 89 nM。它选择性地抑制磷酸化的 p38 激酶活性,不妨碍上游激酶磷酸化 p38,显示出对肠病毒 71 的抗病毒活性。
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | p38 MAPK ↓ ↑ | p38α ↓ ↑ | p38β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BMS-582949 |
+++
p38 MAPK, IC50: 13 nM |
98% | |||||||||||||||||
SB 203580 | 99%+ | ||||||||||||||||||
Pexmetinib | ✔ | Tie-2 | 99%+ | ||||||||||||||||
Skepinone-L |
++++
p38α, IC50: 5 nM |
98% | |||||||||||||||||
Doramapimod |
++++
p38α, Kd: 0.1 nM p38α, IC50: 38 nM |
99%+ | |||||||||||||||||
VX-702 | 99%+ | ||||||||||||||||||
Ralimetinib dimesylate |
++++
p38α, IC50: 7 nM |
98% | |||||||||||||||||
SB 202190 |
++
p38α, IC50: 50 nM |
++
p38β, IC50: 100 nM |
99%+ | ||||||||||||||||
Losmapimod |
++++
p38α, pKi: 8.1 |
+++
p38β, pKi: 7.6 |
99%+ | ||||||||||||||||
Neflamapimod |
+++
p38α, IC50: 10 nM |
+
p38β, IC50: 220 nM |
99%+ | ||||||||||||||||
PH-797804 |
++
p38α, IC50: 26 nM |
+
p38β, IC50: 102 nM |
98% | ||||||||||||||||
TAK-715 |
++++
p38α, IC50: 7.1 nM |
+
p38β, IC50: 0.20 μM |
99%+ | ||||||||||||||||
SB 239063 |
++
p38α, IC50: 44 nM |
++
p38β, IC50: 44 nM |
99%+ | ||||||||||||||||
Pamapimod |
+++
p38α, IC50: 0.014 μM |
+
p38β, IC50: 0.48 μM |
98%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | PD 169316 is a potent and selective p38 MAP kinase inhibitor. It blocked p38 enzyme activity activated by serum-starvation and apoptosis by approximately 80% in Rat-1 fibroblasts at concentration of 10μM. PD169316 at 5μM or higher abrogated signaling initiated by both TGFβ and Activin A, but not BMP4, in CaOV3 cells. PD169316 at 10μM blocked the apoptotic process induced upon LIF withdrawal, without impairing cell differentiation, in mouse ES cells, with decreased FGF-5 and increased Bcl-2 expression on RNA level observed post 3 days. |
Dose | Mice: 60 mg/kg[4] (p.o.); 1 mg/kg[5] (i.m.) |
Administration | p.o., i.m. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.78mL 0.56mL 0.28mL |
13.88mL 2.78mL 1.39mL |
27.75mL 5.55mL 2.78mL |
CAS号 | 152121-53-4 |
分子式 | C20H13FN4O2 |
分子量 | 360.341 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
溶解度 |
DMSO: 12 mg/mL(33.3 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |