1. Cell Cycle/DNA Damage
    Cytoskeleton
    MAPK/ERK Pathway
    Apoptosis
  2. Microtubule/Tubulin
    JNK
    Apoptosis
    Caspase
  3. MPT0B392

MPT0B392 

Cat. No.: HY-101287
Handling Instructions

MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.

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

MPT0B392 Chemical Structure

MPT0B392 Chemical Structure

CAS No. : 1346169-92-3

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Description

MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line[1].

IC50 & Target[1]

JNK

 

Caspase

 

In Vitro

MPT0B392 (B392) (0.001-0.1 μM; 24 and 48 hours) inhibits the cell viability of HL60, MOLT-4, and CCRF-CEM cells with IC50s of 0.02 μM, 0.03 μM and 0.02 μM, respectively[1].
MPT0B392 (0.1 μM; 48 hours) induces apoptosis in HL60 cancer cells[1].
MPT0B392 (0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours) triggers cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner[1].
MPT0B392 (0.1 μM; 48 hours) increases the phosphorylation of Bcl-2, Mcl-1S and decreases in Mcl-1L[1].

Cell Viability Assay[1]

Cell Line: HL60 (acute promyelocytic leukemia), MOLT-4 (acute lymphoblastic leukemia), CCRF-CEM (acute lymphoblastic leukemia) cells
Concentration: 0.001, 0.003, 0.01, 0.03, 0.1 μM
Incubation Time: 24 and 48 hours
Result: Inhibited the cell viability.

Apoptosis Analysis[1]

Cell Line: HL60 cells
Concentration: 0.1 μM
Incubation Time: 48 hours
Result: Induced apoptosis in cancer cells.

Cell Cycle Analysis[1]

Cell Line: HL60 cells
Concentration: 0.1 μM or 0.01, 0.03, 0.1 μM
Incubation Time: 0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours
Result: Triggered cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner.

Western Blot Analysis[1]

Cell Line: HL60 cells
Concentration: 0.1 μM
Incubation Time: 48 hours
Result: Increased the phosphorylation of Bcl-2, Mcl-1S and decreased in Mcl-1L.
In Vivo

The effects of MPT0B392 (oral gavage; 50 mg/kg or 100 mg/kg for 12 or 14 days) shows relative potent anti-leukemia activity in a vivo xenograft model[1].

Animal Model: Severe combined immunodeficient (SCID) mice [1]
Dosage: 50 mg/kg or 100 mg/kg
Administration: Oral gavage; 12 or 14 days
Result: Resulted in significant tumor growth delay (83.3%) and tumor volume inhibition without loss of body weight.
Molecular Weight

404.44

Formula

C₁₉H₂₀N₂O₆S

CAS No.

1346169-92-3

SMILES

NC1=C2C(N=C(S(=O)(C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C2)=CC=C1OC

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MPT0B392
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