fat mass and obesity-associated protein (fto)

Meclofenamic acid (Meclofenamate) is a non-selective gap-junction blocker and a selective inhibitor of the fat mass and obesity-associated (FTO) enzyme, with notable anti-inflammatory activities.

FTO-IN-14 (Compound F97) is an inhibitor of the RNA demethylase Fat mass and obesity-associated protein (FTO), with an IC50 of 0.45 μM. It modulates the expression of the ASB2, RARA, and MYC proteins. FTO-IN-14 demonstrates antiproliferative activity in AML cancer cells, with IC50 values of 0.7-5.5 μM against MOLM13, NB4, HEL, OCI-AML3, MV4-11, and MONOMAC6, and induces apoptosis in NB4 cells. Additionally, FTO-IN-14 exhibits antitumor activity in a mouse NB4 xenograft model.

PROTACFTO degrader 1 is a PROTAC designed to target and degrade fat mass and obesity-associated protein (FTO). It leverages the VHL E3 ligase and the ubiquitin-proteasome system for the selective degradation of FTO. This compound enhances m6A modifications on mRNAs related to ribosome biogenesis and promotes their YTHDF2-mediated degradation. Furthermore, PROTACFTO degrader 1 effectively inhibits cancer cell proliferation and induces apoptosis, making it a valuable candidate for cancer research, particularly in acute myeloid leukemia (AML).

FTO-IN-6 is a selective inhibitor of the fat mass and obesity-associated protein (FTO).

FTO-IN-8, also known as FTO-43, is an inhibitor of N6-methyladenosine demethylase FTO (fat mass- and obesity-associated protein). It exhibits an IC50 value of 5.5 μM and displays anti-cancer cell proliferative activity [1].

ZLD115 (compound 44), a derivative of FB23, functions as an inhibitor of the Fat Mass and Obesity-associated Protein (FTO) and demonstrates antiproliferative properties as an antileukemic agent against leukemic cell lines [1].

FTO-IN-10 (compound 7), a potent inhibitor of the human demethylase FTO (fat mass and obesity-associated protein), exhibits an IC50 of 4.5 μM. It interacts with the binding pocket of FTO's structural domain II via hydrophobic and hydrogen bonding interactions, and promotes DNA damage and autophagic cell death in A549 cells [1].

Clausine E is an inhibitor of fat mass and obesity-associated protein (FTO) demethylase activity. The binding of Clausine E to FTO was driven by positive entropy and negative enthalpy changes.