MK2-IN-1 (hydrochloride)

MK2-IN-1 hydrochloride (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 hydrochloride impaires the phosphorylation level of serine residues in the Tfcp2l1 protein[1][2].

Product Specifications

CAS Number

[1314118-94-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

HSP; MAPKAPK2 (MK2)

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; MAPK/ERK Pathway; Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/MK2-IN-1-hydrochloride.html

Concentration

10mM

Purity

98.36

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : ≥ 100 mg/mL

Smiles

O=C(C1=CC=C(C2=CC=C(Cl)C=C2)O1)N(C3=CC=C(N4CCNCC4)C=C3)CC5=NC=CC=C5.[H]Cl

Molecular Formula

C27H26Cl2N4O2

Molecular Weight

509.43

Precautions

H302, H315, H319, H335

References & Citations

[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.|[2]Huang X, et al. A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors. Bioorg Med Chem Lett. 2012 Jan 1;22 (1) :65-70.|[3]Huang X, et al. Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors. ACS Med Chem Lett. 2011 Jun 24;2 (8) :632-7.|[4]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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, stored under nitrogen)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Citation 01

Cell Death Dis. 2021 Oct 23;12 (11) :994.|University of Minnesota. 2025.|Biol Pharm Bull. 2025;48 (2) :172-176.|Cell Rep. 2021 Nov 2;37 (5) :109949.|J Pharmacol Exp Ther. 2019 Aug;370 (2) :219-230.