1. Epigenetics
    Antibody-drug Conjugate/ADC Related
    Autophagy
    Apoptosis
  2. DNA Methyltransferase
    ADC Cytotoxin
    Autophagy
    Apoptosis
  3. Isofistularin-3

Isofistularin-3 

Cat. No.: HY-19826
Handling Instructions

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.

For research use only. We do not sell to patients.

Isofistularin-3 Chemical Structure

Isofistularin-3 Chemical Structure

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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[1].

IC50 & Target[1]

DNMT1

13.5 μM (IC50)

Traditional Cytotoxic Agents

 

In Vitro

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].

Cell Proliferation Assay[1]

Cell Line: RAJI and U-937 lymphoma cells
Concentration: 1, 5, 15, 25, 50 μM
Incubation Time: 24 and 72 hours
Result: A marked reduction of cell proliferation.

Cell Cycle Analysis[1]

Cell Line: RAJI and U-937 cells
Concentration: 5, 50 μM
Incubation Time: 24 hours
Result: An arrest in the G0/G1 phase of the cell cycle for both cell lines.

RT-PCR[1]

Cell Line: RAJI cells
Concentration: 25 μM
Incubation Time: 72 h
Result: AHR mRNA expression level was 5.1 times higher.
Molecular Weight

1114.01

Formula

C₃₁H₃₀Br₆N₄O₁₁

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

Isofistularin-3Isofistularin3Isofistularin 3DNA MethyltransferaseADC CytotoxinAutophagyApoptosisDNMTsDNA MTasesAHRpromoterdemethylationRAJIcellsproliferationDNA-competitiveTRAILautophagyInhibitorinhibitorinhibit

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Isofistularin-3
Cat. No.:
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