2. MAPK/ERK Pathway
  3. MAPKAPK2 (MK2)
  4. MK2-IN-6

MK2-IN-6 (Compound 11) 是一种有效的，选择性不可逆的 MK2 抑制剂，其 IC50 值为 2.3 nM。MK2-IN-6 抑制 MK2 激酶活性，实现对 MK2 信号的长时间抑制，降低巨噬细胞的病理性炎症因子。MK2-IN-6 在体外和体内均能抑制巨噬细胞的 M2 样蛋白表型，有望用于结肠癌研究。

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MK2-IN-6 Chemical Structure

MK2-IN-6 Chemical Structure

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MK2-IN-6 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MK2-IN-6 (Compound 11) is a potent and selective irreversible MK2 inhibitor with an IC50 value of 2.3 nM. MK2-IN-6 inhibits MK2 kinase activity, achieving prolonged MK2 signaling suppression and reducing pathological inflammatory cytokines in macrophages. MK2-IN-6 inhibits the M2-like protumor phenotype of macrophages both in vitro and in vivo, which is proming for research of colorectal cancer[1].

IC50 & Target

MK3

>100 nM (IC50)

FGFR4

>1000 nM (IC50)

TTK

>1000 nM (IC50)

p70S6Kb

>1000 nM (IC50)

MK5

>100 nM (IC50)

p38

>1000 nM (IC50)

体外研究
(In Vitro)

MK2-IN-6 (2.3 nM, 70 分钟) 对 MK2 具有高选择性和不可逆的抑制作用，类似 PF-3644022 (HY-107427)[1]。
MK2-IN-6 (1-10 μM, 1.5 或 6 小时) 可深度抑制巨噬细胞中细胞因子的转录和产生，靶向 MK2 的经典下游基因[1]。

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

MK2-IN-6 相关抗体:

Real Time qPCR[1]

Cell Line: Human monocytic THP-1 cell-line-derived macrophage and the mouse RAW264.7 macrophage cell line
Concentration: 1-10 μM
Incubation Time: 6 h
Result: Effectively impeded the transcription and production of TNF-α, IL-6, and IL-1 increased by LPS in macrophages.

Western Blot Analysis[1]

Cell Line: Human monocytic THP-1 cell-line-derived macrophage and the mouse RAW264.7 macrophage cell line
Concentration: 1-10 μM
Incubation Time: 1.5 h
Result: Significantly inhibited the phosphorylation of Hsp27 induced by LPS (100 ng/mL, 30 min) in macrophages, much more potent than that of PF-3644022 (HY-107427) and CC-99677 (HY-139504).
体内研究
(In Vivo)

MK2-IN-6 (10 mg/kg, 腹腔注射, 每天两次，持续 12 天) 显著抑制 MC38 肿瘤模型小鼠的肿瘤生长[1]。

MK2-IN-6 在小鼠体内的药动学参数[1]

药代动力学分析[1]

ip. (10 mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (h·ng/mL) AUCinf_obc (h·ng/mL) MRTinf_obs (h)
Mean ± SD 0.38±0.034 0.05±0.00 125.87±46.0 44.49±21.4 45.19±21.3 1.64±2.08

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

Animal Model: MC38 tumor model of mice[1]
Dosage: 10 mg/kg
Administration: i.p., twice daily for 12 days
Result: The rates of tumor growth inhibition rates at dosages of 25 and 50 mg/kg MK2-IN-6 were 47.5% and 64.0%, respectively in MC38 tumor model of mice.
分子量

442.39

Formula

C22H17F3N4O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MK2-IN-6 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

MK2-IN-6MAPKAPK2 (MK2)Mitogen-activated protein kinase activated protein kinase 2MAP kinase activated protein kinase 2MAPK activated protein kinase 2MAPKAP kinase 2MK2 inhibitorMK2 signalinginflammatory cytokinesmacrophagescolorectal cancerInhibitorinhibitorinhibit

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目录号：
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