Brief Description

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
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.

Solubility

DMSO

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Density

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Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

Light yellow to yellow solid