Unesbulin (PTC596)

Catalog No.S8820 Batch:S882001

Print

Technical Data

Formula
C19H13F5N6
 
Molecular Weight 420.34 CAS No. 1610964-64-1
Solubility (25°C)* In vitro DMSO 84 mg/mL (199.83 mM)
Ethanol 7 mg/mL (16.65 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.1mg/ml Taking the 1 mL working solution as an example, add 50 μL of 42 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
1.05mg/ml Taking the 1 mL working solution as an example, add 50 μL of 21 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Unesbulin (PTC596) is a second-generation BMI-1 inhibitor that accelerates BMI-1 degradation. PTC596 downregulates MCL-1 and induces p53-independent mitochondrial apoptosis. IC50 values at 72 hours ranged from 68 to 340 nM in mantle cell lymphoma (MCL) cell lines.
Targets
BMI-1 [1]
In vitro

PTC596 induces mitochondrial apoptosis in BMI-1-expressing MCL cells in a p53-independent manner. MCL SP cells were susceptible to PTC596-induced apoptosis[1].
In vivo

PTC596 inhibits myeloid leukemia cell growth in vivo while sparing normal hematopoietic cells[2].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Z-138 and REC-1 cells

  • Concentrations

    300 nM

  • Incubation Time

    24 h

  • Method

    Z-138 and REC-1 cells were treated for 24 hours with 300 nM PTC596, after which BCL-2, BCL-XL and MCL-1 protein levels were determined.
Animal Study:

[2]
  • Animal Models

    Non-obese diabetic-severe combined immunodeficiency (NOD-SCID)/IL2Rγ-KO (NSG) mice

  • Dosages

    5 mg/kg

  • Administration

    by oral gavage

Selleck's Unesbulin (PTC596) has been cited by 5 publications

Proteogenomic analysis of enriched HGSOC tumor epithelium identifies prognostic signatures and therapeutic vulnerabilities [ NPJ Precis Oncol, 2024, 8(1):68] PubMed: 38480868
Identification of therapeutic sensitivities in a spheroid drug combination screen of Neurofibromatosis Type I associated High Grade Gliomas [ PLoS One, 2023, 18(2):e0277313] PubMed: 36730269
PIC recruitment by synthetic reader-actuators to polycomb-silenced genes blocks triple-negative breast cancer invasion [ bioRxiv, 2023, 2023.01.23.525196] PubMed: 36747762
BMI1 regulates multiple myeloma-associated macrophage's pro-myeloma functions [ Cell Death Dis, 2021, 12(5):495] PubMed: 33993198
Inhibition of BMI-1 Induces Apoptosis through Downregulation of DUB3-Mediated Mcl-1 Stabilization [ Int J Mol Sci, 2021, 22(18)10107] PubMed: 34576269

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.