Darbufelone, Inhibitor

Darbufelone

Cat. Num. AAA5752984

• Purity: 98.00%
• Synonyms: Darbufelone; CI-1004; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• Formula: C18H24N2O2S
• SMILES: O=C1N=C(N)S/C1=C\C2=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C2
• CAS Number: 139226-28-1
• Target & IC50: PGHS-2: ic50 0.19uM; PGHS-1: ic50 20uM
• In Vitro: Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Dabfilon has oral activity in animal models of inflammation and arthritis and does not cause ulcers. When the mice were treated with bufafenone at a dose of 80 mg/kg/day, the tumor volume decreased in a time-dependent manner. In contrast, the lower dose of bufafenone (20 or 40 mg/kg/day) did not show any significant inhibition of tumor weight. At necropsy, the tumor weight of the mice treated with bufafenone (80 mg/kg/day) was reduced by 30.2% compared to the control group.
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Darbufelone, inhibitor

Darbufelone is a dual inhibitor of cellular PGF2alpha and LTB4 production. Dabfilon effectively inhibited PGHS-2 (IC50 = 0.19 uM), but had a much smaller effect on PGHS-1 (IC50 = 20uM).

References

Johnson AR, et al. Slow-binding inhibition of human prostaglandin endoperoxide synthase-2 with darbufelone, an isoform-selective antiinflammatory di-tert-butyl phenol. Biochemistry.2001 Jun 26;40(25):7736-45.
Johnson AR, et al. Slow-binding inhibition of human prostaglandin endoperoxide synthase-2 with darbufelone, an isoform-selective antiinflammatory di-tert-butyl phenol. Biochemistry.2001 Jun 26;40(25):7736-45.
Ye X, et al. Darbufelone, a novel anti-inflammatory drug, induces growth inhibition of lung cancer cells both in vitro and in vivo. Cancer Chemother Pharmacol. 2010 Jul;66(2):277-85.
Ye X, et al. Darbufelone, a novel anti-inflammatory drug, induces growth inhibition of lung cancer cells both in vitro and in vivo. Cancer Chemother Pharmacol. 2010 Jul;66(2):277-85.