2. MAPK/ERK Pathway Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. MAPKAPK2 (MK2) HSP
  4. MK2-IN-1

MK2-IN-1 (compound 1) 是一种有效的选择性 MAPKAPK2 (MK2) 抑制剂，对 MK2 的 IC50 为 0.11 uM，对 pHSP27 的 EC50 为 0.35 uM。MK2-IN-1 损害 Tfcp2l1 蛋白中丝氨酸残基的磷酸化水平。

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MK2-IN-1 Chemical Structure

MK2-IN-1 Chemical Structure

CAS No. : 1314118-92-7

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规格 价格 是否有货 数量
5 mg ￥585
In-stock
10 mg ￥990
In-stock
50 mg   询价  
100 mg   询价  

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Other Forms of MK2-IN-1:

MK2-IN-1 相关抗体

Top Publications Citing Use of Products

查看 HSP 亚型特异性产品:

查看所有亚型
HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MK2-IN-1 (compound 1) is a potent and selecitve MAPKAPK2 (MK2) inhibitor with an IC50 of 0.11 uM for MK2 and an EC50 of 0.35 uM for pHSP27. MK2-IN-1 impaires the phosphorylation level of serine residues in the Tfcp2l1 protein[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
SW1353 CC50
> 20 μM
Compound: 25
Cytotoxicity against human SW1353 cells after 30 mins by ATP-dependent luciferase luminescence assay
Cytotoxicity against human SW1353 cells after 30 mins by ATP-dependent luciferase luminescence assay
[PMID: 24900358]
SW1353 EC50
0.35 μM
Compound: 25
Inhibition of MK2-mediated HSP27 phosphorylation in IL-1beta stimulated human SW1353 cells incubated for 30 mins prior to IL-1beta-stimulation measured after 27 mins by ELISA
Inhibition of MK2-mediated HSP27 phosphorylation in IL-1beta stimulated human SW1353 cells incubated for 30 mins prior to IL-1beta-stimulation measured after 27 mins by ELISA
[PMID: 24900358]
SW1353 IC50
5.7 μM
Compound: 25
Inhibition of IL1beta-stimulated MMP13 secretion in human SW1353 cells incubated for 30 mins prior to IL1beta-stimulation measured after 24 hrs by ELISA
Inhibition of IL1beta-stimulated MMP13 secretion in human SW1353 cells incubated for 30 mins prior to IL1beta-stimulation measured after 24 hrs by ELISA
[PMID: 24900358]
THP-1 EC50
0.35 μM
Compound: 1
Inhibition of MK2-mediated HSP27 phosphorylation at Ser78 in LPS-stimulated human THP-1 cells pre-incubated for 60 mins before LPS treatment measured after 60 mins
Inhibition of MK2-mediated HSP27 phosphorylation at Ser78 in LPS-stimulated human THP-1 cells pre-incubated for 60 mins before LPS treatment measured after 60 mins
[PMID: 22182499]
THP-1 EC50
350 nM
Compound: 1
Inhibition of MK2 in human THP1 cells assessed as inhibition of LPS-induced HSP27 Ser78 phosphorylation incubated for 60 mins prior to LPS-induction measured after 60 mins
Inhibition of MK2 in human THP1 cells assessed as inhibition of LPS-induced HSP27 Ser78 phosphorylation incubated for 60 mins prior to LPS-induction measured after 60 mins
[PMID: 24900435]
THP-1 IC50
4.4 μM
Compound: 25
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 30 mins prior to LPS-challenge measured after 3 hrs by ELISA
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 30 mins prior to LPS-challenge measured after 3 hrs by ELISA
[PMID: 24900358]
THP-1 EC50
5 μM
Compound: 2a
Inhibition of LPS-stimulated TNFalpha production in human THP1 cells by ELISA
Inhibition of LPS-stimulated TNFalpha production in human THP1 cells by ELISA
[PMID: 22169260]
THP-1 IC50
5.2 μM
Compound: 25
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 30 mins prior to LPS-challenge measured after 18 hrs by immunoabsorbent-based electrochemical luminescence assay
Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 30 mins prior to LPS-challenge measured after 18 hrs by immunoabsorbent-based electrochemical luminescence assay
[PMID: 24900358]
体外研究
(In Vitro)

MK2-IN-1 (购自 MCE；5 μM；0.5-8 h) 逐渐增加 Tfcp2l1 蛋白水平，2 小时内 Tfcp2l1 转录物水平没有变化[2]。
MK2-IN-1 在短时间内比其他因子诱导更多的碱性磷酸酶 (AP) 阳性集落[2]。

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

MK2-IN-1 相关抗体:

Western Blot Analysis[2]

Cell Line: 46C mouse embryonic stem cells (mESCs)
Concentration: 5 μM
Incubation Time: 0.5, 1, 2, 8 h
Result: The Tfcp2l1 protein level gradually increased without a change in the Tfcp2l1 transcript level within 2 h.
分子量

472.97

Formula

C27H25ClN4O2
CAS 号
性状

固体

颜色

White to off-white

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
纯度 & 产品资料
参考文献

MK2-IN-1 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-11314118-92-7MAPKAPK2 (MK2)HSPMitogen-activated protein kinase activated protein kinase 2MAP kinase activated protein kinase 2MAPK activated protein kinase 2MAPKAP kinase 2Heat shock proteinsMK2pHSP27phosphorylationserineTfcp2l1alkaline phosphataseInhibitorinhibitorinhibit

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产品名称：
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目录号：
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