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FB23 is a potent and selective FTO demethylase inhibitor with an IC50 of 60 nM. FB23 binds to FTO and selectively inhibits FTO's mRNA N6-methyladenosine (m6A) demethylase activity.
FB23 treatment inhibits acute myeloid leukemia (AML) cells proliferation with IC50 values of 44.8 μM, 23.6 μM for NB4 and MONOMAC6 AML cells. FB23 treatment causes the significant suppression of MYC targets, E2F targets, and G2M checkpoint signal cascades, which may contribute to the inhibitory effects of FTO inhibitors and FTO KD on cell cycle and proliferation. FB23 treatments activates apoptosis and p53 pathways.
A single dose of 3 mg/kg FB23 is i.p. administrated to Sprague Dawley (SD) rats for the pharmacokinetic profile. The Cmax and Tmax value of FB23 are 142.5 ng/mL and 0.4 hr, respectively.
| Molecular Weight | 377.22 |
| Formula | C18H14Cl2N2O3 |
| CAS Number | 2243736-35-6 |
| Form | Solid |
| Solubility (25°C) | DMSO >55 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related FTO Products |
|---|
| Entacapone
Entacapone is an inhibitor of FTO demethylation with IC50 of 3.5 μM, Entacapone also inhibits catechol-O-methyltransferase (COMT) with IC50 of 151 nM. |
| Rhein
Rhein, also known as cassic acid, is a substance in the anthraquinone group obtained from rhubarb. |
| FB23-2
FB23-2 is a potent and selective FTO inhibitor with an IC50 of 2.6 μM, directly binds to FTO and selectively inhibit FTO's m6A demethylase activity. |
| Dac51
Dac51 (FTO-IN-1 TFA) is an effective FTO inhibitor with an IC50 of 0.4 μM against FTO demethylation. |
| Meclofenamic acid
Meclofenamic acid (Meclofenamate) is a non-steroidal anti-inflammatory agent. Meclofenamic acid is a highly selective FTO (fat mass and obesity-associated) enzyme inhibitor. Meclofenamic acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker. Meclofenamic acid inhibits hKv2.1 and hKv1.1, with IC50 values of 56.0 and 155.9 μM, respectively. |
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