Bmi-1 inhibitor,cell-permeable and small-molecule
CAS：315704-66-6
分子式：C17H13Br2N5OS
分子量：495.19
纯度：98%
存储：Store at -20°C

Background:

PTC-209 is a small-molecule inhibitor of BMI-1 with IC50 value of 0.5 μM [1].

PTC-209 is screened out by using gene expression modulation by small molecules (GEMS) technology. It can lower BMI-1 transcript levels. PTC-209 is demonstrated to inhibit not only the UTR-mediated expression but also endogenous BMI-1 expression in HCT116 cell line. For HEK293 and HT1080 cell lines, PTC-209 doesn’t show any inhibition of the growth, suggesting that PTC-209 has no cytotoxicity. And for tumor cells or stem cells, such as U937, HT1080 and human hematopoietic stem cells, PTC-209 can inhibit the proliferation of them. As BMI-1 plays its role through the PRC1 complex, PTC-209 reduces the ability of PRC1 selectively. It is also reported that PTC-209 suppresses the growth of colorectal tumor cells through irreversible growth inhibition of CICs [1].

参考文献:
[1] Kreso A, van Galen P, Pedley NM, Lima-Fernandes E, Frelin C, Davis T, Cao L, Baiazitov R, Du W, Sydorenko N, Moon YC, Gibson L, Wang Y, Leung C, Iscove NN, Arrowsmith CH, Szentgyorgyi E, Gallinger S, Dick JE, O'Brien CA. Self-renewal as a therapeutic target in human colorectal cancer. Nat Med. 2014 Jan;20(1):29-36.