Breast cancer resistance protein

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

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

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

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.

(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).

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

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.

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.

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.

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.

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].'

Ac32Az19 is a potent, non-toxic, and highly selective inhibitor of Breast Cancer Resistance Protein (BCRP), demonstrating an EC50 of 13 nM in BCRP-overexpressed HEK293 R2 cells.

CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC 50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein) [1] .

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.

Ledipasvir-d6 is a deuterated compound of Ledipasvir. Ledipasvir has a CAS number of 1256388-51-8. Ledipasvir 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.