MK2-IN-1

Name: MK2-IN-1
Brand: MedChemExpress
SKU: HY-12834
Rating: 5.0 (3 reviews)

Cat. No.: HY-12834 Purity: 99.04%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

MK2-IN-1 Chemical Structure

CAS No. : 1314118-92-7

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of MK2-IN-1:

MK2-IN-1 hydrochloride In-stock

3 Publications Citing Use of MCE MK2-IN-1

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View All Isoforms

HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

Biological Activity
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References
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Description

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]

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.

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.

Molecular Weight

472.97

Formula

C₂₇H₂₅ClN₄O₂

CAS No.

1314118-92-7

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Purity & Documentation

Purity: 99.04%

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Data Sheet (274 KB) SDS (251 KB)

COA (251 KB) HNMR (282 KB) RP-HPLC (288 KB) LCMS (141 KB)

Handling Instructions (2659 KB)

References

[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]

MK2-IN-1 Related Classifications

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The molarity calculator equation

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(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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MK2-IN-1

Customer Review

Other Forms of MK2-IN-1:

MK2-IN-1 Related Antibodies

3 Publications Citing Use of MCE MK2-IN-1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HSP Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

MK2-IN-1 Related Antibodies

MK2-IN-1 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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