breast cancer resistance protein

Elacridar (GG918) is a potent inhibitor of P-glycoprotein and BCRP.

Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH) and a concentration-dependent dual inhibitor of P-gp and BCRP, with IC50 values of 73.8 μM and 17.0 μM, respectively.

Fumitremorgin C (12α-Fumitremorgin C) is a mycotoxin and inhibits ABCG2/BRCP.

Brevianamide F (Cyclo(L-Pro-L-Trp)), also known as cyclo-(L-Trp-L-Pro), is a naturally occurring 2,5-diketopiperazine with notable breast cancer resistance protein inhibitory activity.

KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter, exhibiting no inhibitory activity against P-gp or MRP1.

Triclabendazole sulfoxide (TCBZ-SO), a primary plasma metabolite of Triclabendazole, inhibits the membrane transporter ABCG2/BCRP and demonstrates anti-parasite effects.

PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.

YHO-13177 is a potent and specific inhibitor of BCRP, which enhances the cytotoxicity of SN-38 in cancer cells without affecting P-glycoprotein–mediated paclitaxel resistance in [MDR1]-transduced human leukemia [K562] cells.

6,8-Diprenylnaringenin (Senegalensin) is a natural product from hop Humulus lupulus. 6,8-Diprenylnaringenin is a breast cancer resistance protein(BCRP) inhibitor with some estrogenicity.

Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP).

33-BCRP inhibitor is a compound that blocks the action of breast cancer resistance protein (BCRP), enhancing the susceptibility of mitoxantrone-resistant H460/MX20 lung cancer cells to the cytotoxic effects of mitoxantrone, both individually and when combined with UV radiation. Additionally, it enhances the sensitivity of KB-C2 epidermal carcinoma cells, which overexpress P-glycoprotein (P-gp) or multidrug resistance protein (MDR), to colchicine-induced apoptosis. Furthermore, at a concentration of 5 µM, it boosts the intracellular accumulation of mitoxantrone in H460/MX20 cells.

YHO-13351 free base, the water-soluble prodrug of YHO-13177, is an inhibitor of BCRP (breast cancer resistance protein).

(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on the BCRP efflux transporter.

Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1]. Atiratecan does not inhibit acetylch

CH-0793076, a hexacyclic camptothecin analog, is an active drug and major metabolite of TP300. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein). CH-0793076 inhibits DNA topoisomerase I (IC50: 2.3 μM).

WK-X-34 is an inhibitor of P-glycoprotein and Breast Cancer Resistance Protein (BCRP).

Butein tetramethyl ether (Compound 20) is a potent and selective inhibitor of breast cancer resistance protein / ATP-binding cassette sub-family G member 2 (BCRP/ABCG2). It inhibits MCF-7 MX and MDCKBCRP cells with IC50 values of 2.2 μM and 1.03 μM, respectively. Butein tetramethyl ether holds potential for cancer research.

P7-2302 inhibits PDE7 and PDE4B with IC50 values of 0.18 nM and 77.3 nM, respectively. It also inhibits the efflux of P-gp and BCRP (breast cancer resistance protein) and shows low uptake in rat brains. When labeled with 18F, P7-2302 can be used as a PET tracer.

Anticanceragent 191 (Compound 2) is a probenecid derivative. It functions as an efflux inhibitor targeting cancer cells by inhibiting P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticanceragent 191 enhances the accumulation of vincristine within cancer cells and is utilized for cancer research.

Kahalalide F is a novel marine-derived antitumor agent known for inhibiting DNA synthesis. It exhibits cytotoxicity that is not correlated with the expression levels of the multidrug resistance gene MDR1 or the tyrosine kinase HER2/NEU, and is only slightly related to the expression of the anti-apoptotic protein BCL-2. Kahalalide F hinders the PI3K-Akt signaling pathway by depleting ErbB3. Its effects are rapidly activated with short pulse treatments. The compound primarily induces cell death through oncosis (cellular swelling) in tumor cells. Kahalalide F can be utilized in studies of prostate cancer, breast cancer, vulvar cancer, and non-small cell lung cancer.

Estradiol 17-(β-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile.1It acts as a substrate of the multidrug resistance protein 2 (MRP2; Km= 75 μM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.1,2In addition to binding to the MRP2 transport site, E217G has been shown to bind to an allosteric site that through positive cooperativity activates its own transportviaMRP2 and the transport of other MRP2 substrates, including the non-cholestatic estrogen metabolite, estradiol 3-(β-D-glucuronide) .2,3E217G has also been reported to be transported by MDR1, MRP1, MRP3, MRP4, MRP7, ABCG2 (a breast cancer resistance protein transporter), and the rat organic anion-transporting polypeptides 1-4.2 1.Loe, D.W., Almquist, K.C., Cole, S.P., et al.ATP-dependent 17β-estradiol 17-(β-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroidsThe Journal of Biological Chemisty271(16)9683-9689(1996) 2.Gerk, P.M., Li, W., and Vore, M.Estradiol 3-glucuronide is transported by the multidrug resistance-associated protein 2 but does not activate the allosteric site bound by estradiol 17-glucuronideDrug Metabolism and Disposition32(10)1139-1145(2004) 3.Gerk, P.M., Li, W., Megaraj, W., et al.Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholateJournal of Pharmacology and Experimental Therapeutics320(2)893-899(2007)

CAY10719 is a selective inhibitor of the breast cancer resistance protein ABCG2 (IC50 = 0.23 μM) with little activity at ABCG1. It has been shown to reverse the ABCG2-mediated resistance toward SN 38 and to inhibit ATPase activity.

Ledipasvir (GS-5885) is a Hepatitis C Virus NS5A Inhibitor. The mechanism of action of ledipasvir is as a P-Glycoprotein Inhibitor, and Breast Cancer Resistance Protein Inhibitor.

'(6R)-ML753286, an isomer of ML753286, is an orally active, selective Breast Cancer Resistance Protein (BCRP) inhibitor, demonstrating an IC50 of 0.6 μM. It exhibits high permeability and low to medium clearance in rodent and human liver S9 fractions, with cross-species plasma stability [1].'