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].

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

1114.01

C₃₁H₃₀Br₆N₄O₁₁

COC1=C(Br)[C@H](O)[C@@]2(ON=C(C(NC[C@H](O)COC3=C(Br)C=C([C@H](O)CNC(C4=NO[C@]5(C4)C=C(Br)C(OC)=C(Br)[C@H]5O)=O)C=C3Br)=O)C2)C=C1Br

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• [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]