1. Apoptosis
  2. Apoptosis
  3. Unesbulin

Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity.

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

Unesbulin Chemical Structure

Unesbulin Chemical Structure

CAS No. : 1610964-64-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 264 In-stock
Solution
10 mM * 1 mL in DMSO USD 264 In-stock
Solid
1 mg USD 110 In-stock
5 mg USD 240 In-stock
10 mg USD 380 In-stock
25 mg USD 700 In-stock
50 mg USD 1050 In-stock
100 mg USD 1500 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity[1][2].

IC50 & Target

BMI-1[1]

In Vitro

Unesbulin (PTC596; 20-200 nM; for 48 hours) induces apoptosis in AML cells in a p53-independent manner. BMI-1 overexpression desensitizes AML cells to PTC596-induced apoptosis[1].
Unesbulin (200 nM; for 10 hours) leads to an accumulation of cells in G2/M phase[1].
Unesbulin (0.012-1 μM; for 20 hours) significantly reduces protein levels of BMI-1[1].
Unesbulin inhibits APC/CCDC20 activity resulting in the persistent activation of CDK1 and CDK2 which mediate the hyperphosphorylation of BMI1[2].

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

Apoptosis Analysis[1]

Cell Line: AML cell lines (MOLM-13, OCI-AML3, MOLM-14, MV4-11, U-937, HL-60)
Concentration: 20, 50, 100, 200 nM
Incubation Time: For 48 hours
Result: Induced apoptosis in a dose- and time-dependent manner with the average IC50 and ED50 values among six cell lines were 30.7 nM and 60.3 nM, respectively.

Cell Cycle Analysis[1]

Cell Line: MOLM-13 and U-937 cells
Concentration: 200 nM
Incubation Time: For 10 hours
Result: Led to an accumulation of cells in G2/M phase, whereas the percentage of cells in G1 phase decreased.

Western Blot Analysis[1]

Cell Line: MOLM-13 cell
Concentration: 0.012, 0.037, 0.11, 0.33, 1 μM
Incubation Time: For 20 hours
Result: Significantly reduced protein levels of BMI-1 and its downstream target ubiquitinated histone H2A.
Increased cyclin B1 and securin levels.
In Vivo

Unesbulin (PTC596; 5 mg/kg; oral gavage; every 3 days for 13 days) significantly prolongs mouse survival[1].
Unesbulin (20 mg/kg; oral gavage; once a week for 15 days) causes tumor volume significantly smaller than that of control SCID mice with K562 cells[1].
Unesbulin (10 or 12.5  mg/kg; oral gavage; twice a week until death) causes the survival significantly longer than the vehicle-treated group in NOD-SCID mice with HL-60 cells[1].

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

Animal Model: NOD-SCID/IL2Rγ-KO (NSG) mice with MOLM-13 cells[1]
Dosage: 5 mg/kg
Administration: Oral gavage; every 3 days for 13 days
Result: Significantly prolonged mouse survival compared with the vehicle-treated mice in a dose-dependent manner.
Clinical Trial
Molecular Weight

420.34

Formula

C19H13F5N6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=C(F)C(NC2=CC=C(C(F)(F)F)C=C2)=NC(N3C4=CC(F)=CC=C4N=C3C)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (39.66 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 2.3790 mL 11.8951 mL 23.7903 mL
5 mM 0.4758 mL 2.3790 mL 4.7581 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥ 1.67 mg/mL (3.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.67 mg/mL (3.97 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Purity: 99.45%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3790 mL 11.8951 mL 23.7903 mL 59.4757 mL
5 mM 0.4758 mL 2.3790 mL 4.7581 mL 11.8951 mL
10 mM 0.2379 mL 1.1895 mL 2.3790 mL 5.9476 mL
15 mM 0.1586 mL 0.7930 mL 1.5860 mL 3.9650 mL
20 mM 0.1190 mL 0.5948 mL 1.1895 mL 2.9738 mL
25 mM 0.0952 mL 0.4758 mL 0.9516 mL 2.3790 mL
30 mM 0.0793 mL 0.3965 mL 0.7930 mL 1.9825 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Unesbulin 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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Unesbulin
Cat. No.:
HY-112041
Quantity:
MCE Japan Authorized Agent: