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

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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 429 In-stock
Solution
10 mM * 1 mL in DMSO USD 429 In-stock
Solid
5 mg USD 390 In-stock
10 mg USD 650 In-stock
25 mg USD 1250 In-stock
50 mg USD 2000 In-stock
100 mg USD 3300 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

MPT0B392 Related Antibodies

Top Publications Citing Use of Products

View All JNK Isoform Specific Products:

View All Isoforms
JNK1 JNK2 JNK3 JNK

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View All Isoforms
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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

 

Cellular Effect
Cell Line Type Value Description References
HT-29 IC50
16 nM
Compound: 15
Growth inhibition of human HT-29 cells after 72 hrs by methylene blue assay
Growth inhibition of human HT-29 cells after 72 hrs by methylene blue assay
[PMID: 22060033]
KB IC50
18 nM
Compound: 15
Growth inhibition of human KB cells after 72 hrs by methylene blue assay
Growth inhibition of human KB cells after 72 hrs by methylene blue assay
[PMID: 22060033]
MKN-45 IC50
4 nM
Compound: 15
Growth inhibition of human MKN45 cells after 72 hrs by methylene blue assay
Growth inhibition of human MKN45 cells after 72 hrs by methylene blue assay
[PMID: 22060033]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MPT0B392 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (247.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4726 mL 12.3628 mL 24.7255 mL
5 mM 0.4945 mL 2.4726 mL 4.9451 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4726 mL 12.3628 mL 24.7255 mL 61.8139 mL
5 mM 0.4945 mL 2.4726 mL 4.9451 mL 12.3628 mL
10 mM 0.2473 mL 1.2363 mL 2.4726 mL 6.1814 mL
15 mM 0.1648 mL 0.8242 mL 1.6484 mL 4.1209 mL
20 mM 0.1236 mL 0.6181 mL 1.2363 mL 3.0907 mL
25 mM 0.0989 mL 0.4945 mL 0.9890 mL 2.4726 mL
30 mM 0.0824 mL 0.4121 mL 0.8242 mL 2.0605 mL
40 mM 0.0618 mL 0.3091 mL 0.6181 mL 1.5453 mL
50 mM 0.0495 mL 0.2473 mL 0.4945 mL 1.2363 mL
60 mM 0.0412 mL 0.2060 mL 0.4121 mL 1.0302 mL
80 mM 0.0309 mL 0.1545 mL 0.3091 mL 0.7727 mL
100 mM 0.0247 mL 0.1236 mL 0.2473 mL 0.6181 mL
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MPT0B392 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MPT0B3921346169-92-3Microtubule/TubulinJNKApoptosisCaspasec-Jun N-terminal kinaseInhibitorinhibitorinhibit

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