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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related FTO Products |
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| ZLD115
ZLD115 is a FB23-derivated inhibitor of Fat Mass and Obesity-associated Protein (FTO). |
| Meclofenamic acid sodium hydrate
Meclofenamic acid sodium hydrate is a highly selective FTO (fat mass and obesity-associated) enzyme inhibitor. Meclofenamic acid sodium hydrate inhibits hKv2.1 and hKv1.1, with IC50 values of 56.0 and 155.9 μM, respectively. |
| 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. |
| Dac51
Dac51 is an effective FTO inhibitor with an IC50 of 0.4 μM against FTO demethylation. |
| 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. |
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