GSK256066 | Phosphodiesterase 4 Inhibitor | AmBeed-信号通路专用抑制剂

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GSK256066 {[allProObj[0].p_purity_real_show]}

货号：A541549

GSK256066 is a selective PDE4B (equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, showing > 380,000-fold selectivity versus PDE1/2/3/5/6 and > 2500-fold selectivity against PDE4B versus PDE7.

GSK256066 化学结构
CAS号：801312-28-7

GSK256066 3D分子结构
CAS号：801312-28-7

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GSK256066 纯度/质量文件产品仅供科研

货号：A541549 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]; • Cell, 2025. Ambeed. [ A122167 ]; • Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]; • Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]; • Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]; 更多 >

PDE 亚型比较

产品名称	PDE ↓ ↑	PDE1 ↓ ↑	PDE10A ↓ ↑	PDE2 ↓ ↑	PDE3 ↓ ↑	PDE4 ↓ ↑	PDE5 ↓ ↑	PDE6 ↓ ↑	其他靶点	纯度
Doxofylline	✔									99+%
Deltarasin	+++ PDEδ , Kd: 38 nM									95%
7-(2,3-Dihydroxypropyl)theophylline	✔									98%
Aminophylline	+ PDE, IC50: 0.12 mM									98+%
Anagrelide HCl	✔									99%+
Irsogladine	✔								AChR,mAChR	99%
PF-8380	+++ Autotaxin, IC50: 2.8 nM									99%+
Dipyridamole	✔									98%
Balipodect			++++ PDE10A, IC50: 0.3 nM							99%+
Luteolin		+ PDE1, Ki: 15.0 μM		++ PDE2, Ki: 6.4 μM	+ PDE3, Ki: 13.9 μM	+ PDE4, Ki: 11.1 μM	+ PDE5, Ki: 9.5 μM			98%
Milrinone				++ PDE2, IC50: 5.2 μM	++ PDE3, IC50: 2.1 μM				ATPase	99%
Pimobendan					++ PDE3, IC50: 0.32 μM					98%
Cilostazol					++ PDE3, IC50: 0.2 μM					98%
Fenspiride HCl					+ PDE3, pIC50: 3.44	+ PDE4, pIC50: 4.16				99% (HPLC)
(S)-(+)-Rolipram						++ PDE4, IC50: 0.75 μM				99% (HPLC)
Apremilast						+++ PDE4, IC50: 74 nM				98%
GSK256066						++++ PDE4B, IC50: 3.2 pM				98+%
Roflumilast						++++ PDE4A1, IC50: 0.7 nM PDE4A4, IC50: 4.3 nM				99%
Rolipram						+++ PDE4B, IC50: 130 nM				99%+
Cilomilast						+++ LPDE4, IC50: 100 nM HPDE4, IC50: 120 nM				99%
Avanafil							++++ PDE5, IC50: 1 nM			98%
Vardenafil HCl Trihydrate							++++ PDE5, IC50: 0.7 nM			98%
Tadalafil							++++ PDE5, IC50: 1.8 nM			98%
Icariin							++ PDE5, IC50: 0.432 μM			98%
Sildenafil							✔	+++ PDE6, IC50: 33 nM		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。

GSK256066 生物活性

靶点

PDE4

PDE4B, IC50:3.2 pM

描述

Phosphodiesterases (PDEs) are a class of enzymes that hydrolyze cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) which are composed of 11 different families and each family contains different subtypes^[3]. GSK256066 is a selective PDE4B inhibitor with IC₅₀ of 3.2 pM. Consistent with its potency, GSK256066 inhibited tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with 0.01 nM IC₅₀ and by LPS-stimulated whole blood with 126 pM IC₅₀^[4]. When administered intratracheally to rats, GSK256066 inhibited LPS-induced pulmonary neutrophilia with ED₅₀ values of 1.1 μg/kg (aqueous suspension) and 2.9 μg/kg (dry powder formulation) and was more potent than an aqueous suspension of the corticosteroid fluticasone propionate (ED₅₀ 9.3 μg/kg)^[4].

GSK256066 参考文献

[1]Tralau-Stewart CJ, Williamson RA, et al. GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization. J Pharmacol Exp Ther. 2011 Apr;337(1):145-54.

[2]Woodrow MD, Ballantine SP, et al. Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5261-5.

[3]Peng T, Gong J, Jin Y, et al. Inhibitors of phosphodiesterase as cancer therapeutics. Eur J Med Chem. 2018;150:742–756.

[4]Tralau-Stewart CJ, Williamson RA, Nials AT, et al. GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization. J Pharmacol Exp Ther. 2011;337(1):145–154.

GSK256066 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.64mL

1.93mL

0.96mL

19.28mL

3.86mL

1.93mL

GSK256066 技术信息

CAS号	801312-28-7
分子式	C₂₇H₂₆N₄O₅S
分子量	518.58
SMILES Code	O=C(C1=C(NC2=CC=CC(OC)=C2)C3=CC(S(=O)(C4=CC=CC(C(N(C)C)=O)=C4)=O)=CC(C)=C3N=C1)N
MDL No.	MFCD18206923

别名
运输	蓝冰
InChI Key	JFHROPTYMMSOLG-UHFFFAOYSA-N
Pubchem ID	9827968

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature

溶解方案

细胞实验：

DMSO: 25 mg/mL(48.21 mM)，配合低频超声，并水浴加热至45℃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

GSK256066 {[allProObj[0].p_purity_real_show]}

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GSK256066 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

GSK256066 质控信息

GSK256066 生物活性

GSK256066 参考文献

GSK256066 实验方案

GSK256066 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

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