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% | |||||||||||||||||
| Adezmapimod | 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. |
| Concentration | Treated Time | Description | References | |
| HL-60 cells | 5 µM | 48 hours | Inhibited p38 MAPK activity, reduced complex-induced apoptosis | Redox Biol. 2019 Jan;20:182-194. |
| Human islet cells | 100 µM | 1 hour | PD169316 was able to inhibit p38 activation in response to the isolation procedure as well as cytokine stimulation. | Ann Surg. 2001 Jan;233(1):124-33. |
| Canine islet cells | 100 µM | 1 hour | PD169316 was able to inhibit p38 activation in response to the isolation procedure as well as cytokine stimulation. | Ann Surg. 2001 Jan;233(1):124-33. |
| Rabbit lacrimal gland acinar cells | 2 µM | 30 minutes | To investigate the effect of p38 inhibition on LG secretion, results showed PD 169316 significantly decreased carbachol-induced secretion | Cell Mol Biol Lett. 2012 Mar;17(1):1-10. |
| HEK-293 cells | 10 µM | 30 minutes | To investigate the effect of PD169316 on SERT expression, results showed that PD169316 inhibited SERT insertion to the plasma membrane and reduced 5-HT uptake. | J Neurosci. 2005 Jan 5;25(1):29-41. |
| Rat midbrain synaptosomes | 10 µM | 30 minutes | To investigate the effect of PD169316 on 5-HT uptake, results showed that PD169316 significantly inhibited 5-HT uptake and reduced transport capacity (Vmax). | J Neurosci. 2005 Jan 5;25(1):29-41. |
| Bone-marrow derived macrophages (BMMs) | 10 µM | 4 hours | To investigate the effect of PD 169316 on IFN-γ-activated macrophage bactericidal activity, results showed that PD 169316 inhibited p38 MAPK-mediated autophagy and bactericidal activity. | Immunology. 2014 Jan;141(1):61-9. |
| RAW 264.7 cells | 10 µM | 4 hours | To investigate the effect of PD 169316 on IFN-γ-activated macrophage bactericidal activity, results showed that PD 169316 inhibited p38 MAPK-mediated autophagy and bactericidal activity. | Immunology. 2014 Jan;141(1):61-9. |
| Mouse mesenchymal limb bud cells | 2 µM | from day 2 onwards | To investigate the role of p38 MAP kinases in hypertrophic chondrocyte differentiation. Results showed that PD169316 treatment markedly delayed the induction of alkaline phosphatase activity and matrix mineralization, and reduced the expression of hypertrophic marker genes such as collagen X, matrix metalloproteinase 13, and bone sialoprotein. | Biochem J. 2004 Feb 15;378(Pt 1):53-62. |
| Y79 cells | 10 µM | PD169316 increased the sensitivity of Y79 cells to SN50-induced cell death | Am J Pathol. 2002 Dec;161(6):2229-40. | |
| 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 |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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