Molecular Weight(MW): 576.10
PTC-209 HBr is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs).
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b Reduced viability 96 h post treatment was observed in all MM cell lines in a dose-dependent manner, but not in BMSCs or PBMCs (c). d Downregulation of CCND1 and MYC as well as upregulation of CDNK1A and CDKN1B was noted 5 h post treatment. e Deregulation of proliferation-associated genes translated into a significant increase of cells in the G1 phase and concurrent decrease in the S and G2M phase of the cell cycle 24 h post treatment. ***P < 0.001, **P < 0.01 and *P < 0.05 vs DMSO control
J Hematol Oncol, 2016, 9:17. PTC-209 HBr purchased from Selleck.
C. Western blot images of GBC cells treated with 1.25 μM PTC-209 for 72 h (n = 4, cropped). Abbreviations: BMI1: BMI1 polycomb ring finger oncogene; h: hours; H2AK119ub: mono-ubiquitylation of histone 2A at lysine 119; PRC1: polycomb repressive complex 1; RING1B: ring finger protein 2.
Oncotarget, 2016, 7(1):745-58. PTC-209 HBr purchased from Selleck.
Purity & Quality Control
|Description||PTC-209 HBr is the hydrobromide salt of PTC-209, which is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM, and results in irreversible reduction of cancer-initiating cells (CICs).|
|Features||BMI-1-selective inhibitor, targeting the BMI-1 self-renewal machinery.|
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. 
|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. |
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.
|In vitro||DMSO||100 mg/mL warmed (173.58 mM)|
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