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Rhein (50µM) causes apoptosis in rat primary hepatocytes by generation of reactive oxygen species (ROS), increase in intracellular Ca++ , decrease in the mitochondrial membrane potential and depletion of intracellular glutathione (GSH) content. At molecular level rhein induced DNA damage results in over expression of γ-H2AX protein (2.5 fold) thereby causing enhancement of p53 (4.5 fold) and p21 (3.6 fold) leading to intrinsic pathway mediated apoptosis involving Bax, bcl2, cytochrome c, caspases 3, 9 and poly ADP ribose polymerase (PARP). Rhein induced ROS generation was also involved in the modulation of signaling molecules like MAPK kinases including ERK1/2, p38 and JNK; and mitochondrial energetics proteins including complex II-V, p-AMPK and Sirt-1.
Animals (Basel). 2024 Aug 22;14(16):2434.
Inhibitor of FTO, Rhein, Restrains the Differentiation of Myoblasts and Delays Skeletal Muscle Regeneration
Rhein purchased from AbMole
Front Immunol. 2022 Oct 27;13:971409.
The effects of rhein on D-GalN/LPS-induced acute liver injury in mice: Results from gut microbiome-metabolomics and host transcriptome analysis
Rhein purchased from AbMole
| Molecular Weight | 284.22 |
| Formula | C15H8O6 |
| CAS Number | 478-43-3 |
| Solubility (25°C) | DMSO: 6 mg/mL (Need ultrasonic and warming) |
| 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. |
| FB23
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. |
| FB23-2
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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