MK2-IN-1 (hydrochloride)
Product Specifications
UNSPSC Description
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].
Target Antigen
HSP; MAPKAPK2 (MK2)
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage;MAPK/ERK Pathway;Metabolic Enzyme/Protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/MK2-IN-1-hydrochloride.html
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 Weight
509.43
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.Cell Death Dis. 2021 Oct 23;12(11):994.|Cell Rep. 2021 Nov 2;37(5):109949.|J Pharmacol Exp Ther. 2019 Aug;370(2):219-230.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, stored under nitrogen)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-12834A/MK2-IN-1-hydrochloride-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-12834A/MK2-IN-1-hydrochloride-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
1314118-94-9
Available Sizes
Curated Selection
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