MK2-IN-1
Based on 6 publication(s) in Google Scholar
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.
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- 純度: 99.04%
- CAS 番号: 1314118-92-7
- 分子式: C27H25ClN4O2
- 分子量:472.97
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 MK2-IN-1
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW1353 | CC50 |
>20 μM
Compound: 25
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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
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[PMID: 24900358] |
| SW1353 | EC50 |
0.35 μM
Compound: 25
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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
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[PMID: 24900358] |
| SW1353 | IC50 |
5.7 μM
Compound: 25
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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
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[PMID: 24900358] |
| THP-1 | EC50 |
0.35 μM
Compound: 1
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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
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[PMID: 22182499] |
| THP-1 | EC50 |
350 nM
Compound: 1
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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
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[PMID: 24900435] |
| THP-1 | EC50 |
5 μM
Compound: 2a
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Inhibition of LPS-stimulated TNFalpha production in human THP1 cells by ELISA
Inhibition of LPS-stimulated TNFalpha production in human THP1 cells by ELISA
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[PMID: 22169260] |
| THP-1 | IC50 |
4.4 μM
Compound: 25
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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
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[PMID: 24900358] |
| THP-1 | IC50 |
5.2 μM
Compound: 25
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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
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[PMID: 24900358] |
MK2-IN-1 (purchased from MCE; 5 μM; 0.5-8 h) gradually increases Tfcp2l1 protein level without a change in the Tfcp2l1 transcript level within 2 h[2].
MK2-IN-1 induces more alkaline phosphatase (AP)-positive colonies than the other factors in a short time[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:46C mouse embryonic stem cells (mESCs)
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Concentration:5 μM
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Incubation Time:0.5, 1, 2, 8 h
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Result:The Tfcp2l1 protein level gradually increased without a change in the Tfcp2l1 transcript level within 2 h.
化学情報
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CAS 番号 1314118-92-7
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性状 Solid
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分子量 472.97
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分子式 C27H25ClN4O2
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Color White to off-white
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SMILES
O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)N(C3=CC=C(N4CCNCC4)C=C3)CC5=NC=CC=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
Quantitative analysis of phosphoproteome in necroptosis reveals a role of TRIM28 phosphorylation in promoting necroptosis-induced cytokine production. [Abstract]2021 Oct 23;12(11):994. PMID: 34689152 -
Cell Rep
MK2 promotes Tfcp2l1 degradation via β-TrCP ubiquitin ligase to regulate mouse embryonic stem cell self-renewal. [Abstract]2021 Nov 2;37(5):109949. PMID: 34731635 -
J Pharmacol Exp Ther
Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. [Abstract]2019 Aug;370(2):219-230. PMID: 31189728 -
Biol Pharm Bull
Stress Response Kinase MK2 Induces Non-canonical Activation of EphA2 in EML4-ALK Lung Cancer Cells. [Abstract]2025;48(2):172-176. PMID: 40024717 -
純度とドキュメンテーション
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データシート (274 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Rao AU, et al. Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1068-72. [Content Brief]
[2]. Yan Zhang, et al. MK2 promotes Tfcp2l1 degradation via β-TrCP ubiquitin ligase to regulate mouse embryonic stem cell self-renewal. Cell Rep. 2021 Nov 2;37(5):109949. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MK2-IN-1 関連分類
HY-12834 関連分類
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