2. MAPK/ERK Pathway
  3. MAPKAPK2 (MK2) p38 MAPK
  4. PF-3644022

PF-3644022 是一种有效的，选择性的，口服活性的，具有 ATP 竞争性的 MAPKAPK2 (MK2) 抑制剂，IC50 为 5.2 nM，Ki 为 3 nM。PF-3644022 还抑制 MK3 和 p38 调节/激活激酶 (PRAK)，IC50 分别为 53 nM 和 5.0 nM。PF-3644022 有效抑制 TNFα 的产生并具有抗炎作用。

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PF-3644022 Chemical Structure

PF-3644022 Chemical Structure

CAS No. : 1276121-88-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3960
In-stock
1 mg ￥1440
In-stock
5 mg ￥3000
In-stock
10 mg ￥4354
In-stock
25 mg 现货 询价
50 mg   询价  
100 mg   询价  

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Customer Review

PF-3644022 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect[1].

IC50 & Target

IC50: 5.2 nM (MK2), 5.0 nM (PRAK) and 53 nM (MK3)[1].
Ki: 3 nM (MK2)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MDCK IC50
7 μM
Compound: 30; PF-3644022; PF022
Inhibition of MRP2 in MDCK cells after 15 mins by Calcein-AM assay
Inhibition of MRP2 in MDCK cells after 15 mins by Calcein-AM assay
[PMID: 26502061]
Sf9 IC50
7 μM
Compound: 30; PF-3644022; PF022
Inhibition of human BSEP expressed in recombinant baculovirus infected insect Sf9 cell membrane vesicles assessed as [3H]-taurocholate transport preincubated for 5 mins followed by ATP or AMP addition measured after 5 mins by scintillation counting method
Inhibition of human BSEP expressed in recombinant baculovirus infected insect Sf9 cell membrane vesicles assessed as [3H]-taurocholate transport preincubated for 5 mins followed by ATP or AMP addition measured after 5 mins by scintillation counting method
[PMID: 26502061]
U-937 IC50
150 nM
Compound: 30; PF-3644022; PF022
Inhibition of LPS-induced TNFalpha production in human U937 cells preincubated for 1 hr followed by LPS addition measured after 4 hrs by electro-chemiluminescence method
Inhibition of LPS-induced TNFalpha production in human U937 cells preincubated for 1 hr followed by LPS addition measured after 4 hrs by electro-chemiluminescence method
[PMID: 26502061]
U-937 IC50
201 nM
Compound: 30; PF-3644022; PF022
Inhibition of MK2 in human U937 cells assessed as reduction in LPS-stimulated HSP27 phosphorylation at Ser82 preincubated for 1 hr followed by LPS addition measured after 30 mins by Western blot analysis
Inhibition of MK2 in human U937 cells assessed as reduction in LPS-stimulated HSP27 phosphorylation at Ser82 preincubated for 1 hr followed by LPS addition measured after 30 mins by Western blot analysis
[PMID: 26502061]
体外研究
(In Vitro)

The inhibitory activity of PF-3644022 against other MAPKAP kinase family members is evaluated. Other than MNK2 with an IC50 of 148 nM, other family members are largely not inhibited, showing at least several hundred-fold selectivity versus MK2[1].
In the human U937 monocytic cell line or peripheral blood mononuclear cells, PF-3644022 potently inhibits TNFα production with similar activity (IC50 of 160 nM). PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood with IC50 values of 1.6 and 10.3 μM, respectively. Inhibition of TNFα in U937 cells and blood correlates closely with inhibition of phospho-heat shock protein 27, a target biomarker of MK2 activity[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PF-3644022 相关抗体:
体内研究
(In Vivo)

PF-3644022 (3-100 mg/kg; oral gavage; twice a day; for 12 days; Lewis rats) treatment shows dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing, with ED50 value of 20 mg/kg[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Lewis rats (125-140 g) injected with streptococcal cell wall[1]
Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral gavage; twice a day; for 12 days
Result: Showed dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing.
分子量

374.46

Formula

C21H18N4OS
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 41.67 mg/mL (111.28 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6705 mL 13.3526 mL 26.7051 mL
5 mM 0.5341 mL 2.6705 mL 5.3410 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制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

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (5.55 mM); 悬浊液; 超声助溶

    此方案可获得 2.08 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.65%

COA (193 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献

PF-3644022 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6705 mL 13.3526 mL 26.7051 mL 66.7628 mL
5 mM 0.5341 mL 2.6705 mL 5.3410 mL 13.3526 mL
10 mM 0.2671 mL 1.3353 mL 2.6705 mL 6.6763 mL
15 mM 0.1780 mL 0.8902 mL 1.7803 mL 4.4509 mL
20 mM 0.1335 mL 0.6676 mL 1.3353 mL 3.3381 mL
25 mM 0.1068 mL 0.5341 mL 1.0682 mL 2.6705 mL
30 mM 0.0890 mL 0.4451 mL 0.8902 mL 2.2254 mL
40 mM 0.0668 mL 0.3338 mL 0.6676 mL 1.6691 mL
50 mM 0.0534 mL 0.2671 mL 0.5341 mL 1.3353 mL
60 mM 0.0445 mL 0.2225 mL 0.4451 mL 1.1127 mL
80 mM 0.0334 mL 0.1669 mL 0.3338 mL 0.8345 mL
100 mM 0.0267 mL 0.1335 mL 0.2671 mL 0.6676 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-36440221276121-88-0PF3644022PF 3644022MAPKAPK2 (MK2)p38 MAPKMitogen-activated protein kinase activated protein kinase 2MAP kinase activated protein kinase 2MAPK activated protein kinase 2MAPKAP kinase 2Anti-inflammatorysafetyTNFαIL-6lipopolysaccharidemonocyticorallyefficaciousPRAKMK3Inhibitorinhibitorinhibit

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