PD169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor (IC50 = 89 nM).
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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 |
99% | ||||||||||||||||
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 | 360.34 |
SMILES Code | O=[N+](C1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1)[O-] |
MDL No. | MFCD12405019 |
别名 | |
运输 | 蓝冰 |
InChI Key | BGIYKDUASORTBB-UHFFFAOYSA-N |
Pubchem ID | 4712 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, 2-8°C |