For research use only.

Catalog No.S7372

8 publications

PTC-209 Chemical Structure

CAS No. 315704-66-6

PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).

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Selleck's PTC-209 has been cited by 8 publications

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  • Immunoblot analysis of BMI-1 and H2AK119Ub levels following 72 h treatment with 10 µM PTC-209. β-actin and total H2A served as loading controls.

    Oncotarget, 2017, doi: 10.18632/oncotarget.18002. PTC-209 purchased from Selleck.

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Choose Selective BMI-1 Inhibitors

Biological Activity

Description PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).
Features BMI-1-selective inhibitor targeting self-renewal of cancer cells.
BMI-1 [1]
(HEK293T cells)
0.5 μM
In vitro

PTC-209 inhibits both the UTR-mediated reporter expression and endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells. PTC-209 decreases colorectal tumor cell growth in a BMI-1-dependent way. In addition, PTC-209 impairs colorectal cancer-initiating cells (CICs) through irreversible growth inhibition. [1]

In vivo PTC-209 (60 mg/kg/day, s.c.) effectively inhibits BMI-1 production in tumor tissue, and halts growth of preestablished tumors in mice bearing primary human colon cancer xenograft, human colon cancer cell lines LIM1215 or HCT116 xenografts. PTC-209 also reduces the frequency of functional colorectal CICs in vivo. [1]


Kinase Assay:[1]
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Untranslated region-mediated luciferase reporter expression:

HEK293 cells are transfected with a GEMS reporter vector that contains the luciferase open-reading frame flanked by and under post-transcriptional control of the BMI-1 5′ and 3′ UTRs. The resulting stable cells (F8) are treated with PTC-209 or vehicle control overnight, and then luciferase reporter activity is determined using Bright-Glo assays. The assays are run in triplicate for each point, and the percentage of inhibition was calculated against vehicle control.
Cell Research:[1]
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  • Cell lines: Human lymphoma U937 and HT1080 tumor cells, primary human peripheral blood mononuclear cells and human hematopoietic stem cells.
  • Concentrations: ~10 μM
  • Incubation Time: 4 days
  • Method: To determine whether pretreatment with the inhibitor affects tumor cell growth, cells are plated with the inhibitor for 4 d in vitro and plated in limiting doses in vitro without adding further inhibitor. Trypan blue exclusion is used to count viable cells. The in vitro sphere-initiating cell frequency is calculated after inhibitor treatment by evaluating the number of wells containing spheres. For the experiments where LDAs are set up following recovery of PTC-209 treated cells, 6-well plates were seeded with 1E6 cells per well and incubated overnight. Cells are subsequently treated for 4 d in triplicate with either DMSO vehicle or PTC-209 (0.01, 0.1, 1 and 10 μM). Drug treatments are washed off and 4 mL fresh suspension medium added to all wells. To assess cell viability following the 4 d treatment window, cells are trypsinized and counted at 0, 24, 72 and 120 h after removal of the drug. Long-lasting effects of the drug treatment on sphere-forming ability are assessed by plating LDAs (50,000, 10,000, 1,000,100, 10 and 1 cell per well) using the cells obtained 120 h after the 4-d drug treatment.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Primary human colon cancer xenograft, human colon cancer cell lines LIM1215 and HCT116 xenografts in nude mice.
  • Dosages: ~60 mg/kg/day
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 99 mg/mL (199.92 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 495.19


CAS No. 315704-66-6
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID