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Product name : PTC-209
Item : CR1800
Price : 200mg, $945; 500mg, $1485
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CAS : 315704-66-6
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Details:
 Chemical Information
M.Wt 495.19 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C17H13Br2N5OS
CAS No 315704-66-6
Solubility

DMSO



Biological Activity of PTC-209

 

PTC-209 is a specific inhibitor  for BMI-1 with IC50 of 0.5 uM in in both GEMS reporter and ELISA assays.
IC50 value: 0.5 uM [1]
Target: BMI-1
PTC-209 inhibited not only the UTR-mediated reporter expression but also endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells. PTC-209 caused no inhibition of cell growth or viability in HEK293 human embryonic kidney cells after overnight treatment and had limited effects on cell proliferation in HT1080 cells after a 48-h treatment. PTC-209 selectively reduced global ubiquitinated histone H2A (uH2A) but not total H2A and RING1A levels indicating its ability to specifically reduce PRC1 activity. Compound PTC-209 preferentially inhibits the proliferation of  human lymphoma U937 and HT1080 tumor cells, whereas it is lesseffective in primary human peripheral blood mononuclear cells and human hematopoietic stem cells.

 

[1]. Kreso A, et al. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.


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