fto

FTO-IN-3, a FTO inhibitor, impairs self-renewal in glioblastoma stem cells (GSCs).

UUN44923 is a FTO inhibitor. It may be useful for treating diseases assocd. with FTO targets, obesity, metabolic syndrome (MS) , type 2 diabetes (T2D) , Alzheimer's diseases, breast cancers, small- cell lung cancers, a human bone marrow striated muscle cancer, a pancreatic cancer, malignant glioblastoma and the like.

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.

FB23 directly binds to FTO and selectively inhibits FTO's m6A demethylase activity. (FTO, an mRNA N6-methyladenosine (m6A) demethylase, was reported to promote leukemogenesis.)

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.

N6-Methyl-2'-O-methyladenosine (N6,2′-O-Dimethyladenosine), a substrate for adiposity and obesity-related genes (FTO), is a reversible modifier compound found on a wide variety of RNA molecules.N6,2′-O-Dimethyladenosine can be used to study obesity and its related diseases.

FTO-IN-13 (compound 8t) is a potent FTO inhibitor with antiproliferative properties. It induces apoptosis (cell apoptosis) and reduces the expression of Bcl-2 and Caspase 3 active proteins. Additionally, FTO-IN-13 lowers the expression of MYC and CEBPA genes and demonstrates anticancer activity.

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.

FTO-IN-7d is the first inhibitor of the RNA demethylase FTO with anticonvulsant activity.

FTO-IN-2, a FTO inhibitor, impairs self-renewal in glioblastoma stem cells.

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].

FTO-IN-1 TFA is an inhibitor of adiposity and obesity-related enzymes (FTO) (IC50 < 1 μM).FTO-IN-1 TFA can be used to study cancer.

FTO-IN-4 is a potent and selective inhibitor of the adiposity and obesity-associated protein (FTO).

FTO-IN-5 is a potent, selective inhibitor targeting the fat mass obesity-associated protein (FTO).

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].

FTO-IN-12 (Compound 2), an inhibitor of fat mass and obesity-related protein (FTO), exhibits Kd and IC50 values of 185 nM and 1.46 μM, respectively. This compound is utilized in researching neurodegenerative diseases.

Elexacaftor (VX-445) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. It promotes the processing and trafficking of CFTR, increases the amount of CFTR on the cell surface, and improves the processing and trafficking of Phe508del CFTR protein.

Ceftolozane sulfate (FR-264205) is a cephalosporin antibiotic with broad-spectrum antimicrobial activity, inhibits P. aeruginosa PAO1, inhibits Pseudomonas aeruginosa, and is used in the study of pneumonia.

Aminaftone, a derivative of 4-aminobenzoic acid, inhibits endothelin-1 (ET-1) production and is used to study hypertension and systemic sclerosis.

Bamocaftor is a CFTR channel (DeltaF508-CFTR mutation) corrector for CF transmembrane conductance regulators designed to restore F508del-CFTR protein function. Combined use of tezacaftor and VX-561 for the treatment of cystic fibrosis patients with F508del/MF.

Naftopidil (KT-611) (INN, marketed under the brand name Flivas), an antihypertensive medicine, is used as a selective α1-adrenergic receptor antagonist or α-blocker.

Ivacaftor (VX-770) (VX-770) is a potentiator of CFTR targeting G551D-CFTR (EC50: 100 nM) and F508del-CFTR (EC50: 25 nM) in Fisher rat thyroid cells, respectively.

Lumacaftor (VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein. It enhances F508del-CFTR protein maturation in FRT cells (EC50: 100 nM).