1. Apoptosis
  2. Apoptosis
  3. Unesbulin

Unesbulin (Synonyms: PTC596)

Cat. No.: HY-112041 Purity: 98.22%
Handling Instructions

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

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Solution
10 mM * 1 mL in DMSO USD 324 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 324 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 800 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1950 In-stock
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Unesbulin

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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].

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].

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (39.66 mM; Need ultrasonic)

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
10 mM 0.2379 mL 1.1895 mL 2.3790 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Unesbulin
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