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Fumitremorgin C (FTC) is a fungal toxin of the diketopiperazines family of compounds. In mammalian cells, FTC is tremorgenic and causes cell cycle arrest. Fumitremorgin C has been shown to reverse resistance to doxorubicin, mitoxantrane, and topotecan in non-Pgp (P-glycoprotein), non-MRP (multidrug resistance protein) multidrug-resistance (MDR) cells. This reversal of resistance is associated with an increase in drug accumulation.
Fumitremorgin C is a specific, selective, and potent inhibitor at micromolar concentrations of the breast cancer resistant protein (BCRP/ABCG2), an ABC transporter associated with chemotherapy resistance. FTC, in combination with mitoxantrone, can be used for the detection of ABCG2 functional activity in several cell lines.
| Molecular Weight | 379.45 |
| Formula | C22H25N3O3 |
| CAS Number | 118974-02-0 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related BCRP/ABCG2/MXR/ABCP Products |
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| KS176
KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter with IC50 values of 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays, respectively. |
| Ko 143
Ko 143 is a potent and selective BCRP inhibitor. |
| YHO-13177
YHO-13177 is a potent and specific inhibitor of breast cancer resistance protein (BCRP/ABCG2). |
| Zamicastat
Zamicastat is a dopamine β-hydroxylase (DBH) inhibitor that crosses the blood-brain barrier and causes central and peripheral effects. In addition, Zamicastat is a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively. |
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