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Isofistularin-3 Catalog number: BADC-00845
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Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
Category
ADCs Cytotoxin
Product Name
Isofistularin-3
Catalog Number
BADC-00845
Molecular Formula
C31H30Br6N4O11
Molecular Weight
1114.01
Target
Ordering Information
| Catalog Number | Size | Price | Quantity |
|---|---|---|---|
| BADC-00845 | -- | $-- |
Description
Isofistularin-3 is a direct, DNA-competitive DNMT1 inhibitor, with an IC50 of 13.5 μM. Isofistularin-3, as a DNA demethylating agent, induces cell cycle arrest and sensitization to TRAIL in cancer cells. Isofistularin-3 can be used as an ADC cytotoxin.
Solubility
10 mm in DMSO
In Vitro
Isofistularin-3 (Iso-3) induced growth arrest of cancer cells in G0/G1 concomitant with increased p21 and p27 expression and reduced cyclin E1, PCNA and c-myc levels. Reduced proliferation was accompanied by morphological changes typical of autophagy revealed by fluorescent and transmission electron microscopy and validated by LC3I-II conversion. Furthermore, Iso-3 strongly synergized with tumor-necrosis-factor related apoptosis inducing ligand (TRAIL) in RAJI [combination index (CI) = 0.22] and U-937 cells (CI = 0.21) and increased TRAIL-induced apoptosis via a mechanism involving reduction of survivin expression but not of Bcl-2 family proteins nor X-linked inhibitor of apoptosis protein (XIAP). Iso-3 treatment decreased FLIPL expression and triggered activation of endoplasmatic reticulum (ER) stress with increased GRP78 expression, eventually inducing TRAIL receptor death receptor (DR)5 surface expression.
Purity
≥95%
Shelf Life
0-4℃ for short term (days to weeks), or -20℃ for long term (months).
Shipping
Room temperature
Storage
-20°C
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