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

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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MK2-IN-1

MK2-IN-1 Estructura química

No. CAS : 1314118-92-7

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Based on 5 publication(s) in Google Scholar

Other Forms of MK2-IN-1:

MK2-IN-1 Related Antibodies

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Ver todos los productos específicos de isoformas HSP:

Ver todas las isoformas
HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

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Descripciòn

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].

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 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
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 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]
In Vitro

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.

MK2-IN-1 Related Antibodies

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.
Peso molecular

472.97

Fòrmula

C27H25ClN4O2
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)N(C3=CC=C(N4CCNCC4)C=C3)CC5=NC=CC=C5
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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Referencias
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MK2-IN-1 Related Classifications

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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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Nombre del producto:
MK2-IN-1
Cat. No.:
HY-12834
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