MK2-IN-1 (hydrochloride)

MK2-IN-1 (hydrochloride)

• CAS Number: 1314118-94-9
• 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)
• Clinical Information: No Development Reported