1. MAPK/ERK Pathway
    Protein Tyrosine Kinase/RTK
    Apoptosis
  2. Ribosomal S6 Kinase (RSK)
    DYRK
    Apoptosis
  3. MBM-55S

MBM-55S 

Cat. No.: HY-101029A
Handling Instructions

MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice.

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MBM-55S Chemical Structure

MBM-55S Chemical Structure

CAS No. : 2083624-07-9

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Description

MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice[1].

IC50 & Target

IC50: 1 nM (Nek2), 5.4 nM (RSK1), 6.5 nM (DYRK1a), 57 nM (CHK1), 91 nM (GSK-3β), 20 nM (ABL), 370 nM (CDK2), 441nM (CDK4), 608 nM (AKT1), 5300 nM (Aurora A)[1]

In Vitro

MBM-55S inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.53, 0.84, 7.13 μM, respectively[1].
MBM-55S (0.5-1 μM; 24 hours) induces G2/M phase arrest and accumulation of cells with >4N content in HCT-116 cells[1].
MBM-55S (0.5-1 μM; 24 hours) causes cell apoptosis in a concentration-dependent manner in HCT-116 cells[1].

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 1 μM
Incubation Time: 24 hours
Result: Induced G2/M phase arrest and accumulation of cells with >4N content.

Apoptosis Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 1 μM
Incubation Time: 24 hours
Result: Caused cell apoptosis in a concentration-dependent manner.
In Vivo

MBM-55S (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule in nude mice bearing HCT-116 xenografts[1]. MBM-55S (1.0 mg/kg; i.v.) treatment shows the CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively[1].

Animal Model: Female BALB/c nu/nu mice (5-6 weeks, bearing HCT-116 xenografts)[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; twice a day for 21 days
Result: Significantly suppressed tumor growth.
Animal Model: Male Sprague Dawley (SD) rats[1]
Dosage: 1.0 mg/kg
Administration: IV injection (Pharmacokinetic Analysis)
Result: The CL, Vss, T1/2, AUC0-t, and AUC0-∞ values were 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ml/min/kg, respectively.
Molecular Weight

734.73

Formula

C₃₆H₃₉FN₆O₁₀

CAS No.

2083624-07-9

SMILES

NC(C(C=C1)=C(OCC2=CC=CC(F)=C2)C=C1C3=CN=C4N3C=CC(C5=CN(CCN(C)C)N=C5)=C4)=O.O=C(O)CCC(O)=O.O=C(O)CCC(O)=O

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

MBM-55SRibosomal S6 Kinase (RSK)DYRKApoptosisS6KDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseantitumorselectivityNek2proliferationcellcyclearrestapoptosisInhibitorinhibitorinhibit

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