Isofistularin-3 

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^[1].

Isofistularin-3 (1-50 μM; 24-72 hours) shows a marked reduction of cell proliferation^[1].
Isofistularin-3 (5-50 μM; 24 hours) increases arrests cancer cells in G0/G1 cell cycle phase^[1].
Isofistularin-3 (25 μM; 72 hours) increases AHR expression^[1]. Isofistularin-3 induces AHR promoter demethylation. Isofistularin-3 (72 hours) inhibits a broader panel of cancer cell lines proliferation, with the GI₅₀s ranging from 7.3-14.8 μM. Isofistularin-3 induces morphological changes and autophagy in RAJI cells. Isofistularin-3 induces caspase-dependent and -independent cell death. Isofistularin-3 sensitizes lymphoma cells to TRAIL-induced apoptosis^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1114.01

C₃₁H₃₀Br₆N₄O₁₁

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Florean C, et al. Discovery and characterization of Isofistularin-3, a marine brominated alkaloid, as a new DNA demethylating agent inducing cell cycle arrest and sensitization to TRAIL in cancer cells. Oncotarget. 2016 Apr 26;7(17):24027-49.  [Content Brief]