abcg2

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

Novobiocin Sodium (Albamycinsodium) binds to DNA gyrase and blocks adenosine triphosphatase (ATPase) activity. Novobiocin sodium is an antibiotic compound derived from Streptomyces niveus. It has a chemical structure similar to coumarin.

Acridone could induce cell apoptosis, inhibited ABCG2 (ATP-binding cassette sub-family G member 2) protein, and adjusted hormone level.

Vismodegib (GDC-0449) is a hedgehog pathway inhibitor (IC50: 3 nM). It also inhibits P-gp (IC50: 3.0 μM), ABCG2 (IC50: 1.4 μM).

Glafenine Hydrochloride is an anti-inflammatory agent.

YHO-13351 is an ABCG2 inhibitor, an acrylonitrile derivative, that induces sensitization of cancer stem/initiating-like side population cells to irinotecan.GSK1702934A can be used to study diabetes.

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.

ML230 is a selective ATP-binding cassette (ABC) transporter ABCG2 inhibitor. It 36-fold selective for ABCG2 over ABCB1 (EC50s: 0.13 μM and 4.65 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.

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.

Vorolanib (X-82) is an orally active VEGFR/PDGFR dual inhibitor.

Ceefourin 1 is a highly selective multidrug resistance protein 4 (MRP4) inhibitor.

Tepotinib hydrochloride(1 : x) is an orally bioavailable, mesenchymal-epithelial transition (MET) TKI developed mainly for selected NSCLC patients with METex14 skipping mutations.

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.

5-Hydroxy-2′,3,4′,7-tetramethoxyflavone shows weak ABCG2 inhibitory potency with IC50s of 3.27 and 3.89 µM in the Hoechst 33342 and pheophorbide A assays.

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

ABCG2-IN-4 (Compound K31) is an orally active ABCG2 inhibitor that reduces the release of Protoporphyrin IX (PPIX) from red blood cells into the plasma and prevents phototoxicity. In mouse models, ABCG2-IN-4 also demonstrates anti-inflammatory and antioxidant properties.

ABCG2-IN-1 (compound K2), an analog of Ko143, is an orally active inhibitor of ABCG2 with an IC50 of 0.13 μM, demonstrating favorable oral pharmacokinetics in mice and showing promise for further research [1].

ABCG2-IN-2 is a potent inhibitor of ABCG2, showing favorable oral pharmacokinetic profiles in mice, and is applicable for investigating tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP) [1].

Avapritinib (BLU-285) is a selective, highly potent, and orally active inhibitor of KIT and PDGFRA activation loop mutant kinases, targeting KIT D816V (IC50:0.27 nM) and PDGFRA D842V (IC50:0.24 nM), and attenuates the transport functions of ABCB1 and ABCG2. It binds to the active conformation of the kinases and exhibits antitumor activity.

GW 583340 dihydrochloride is a potent and orally available dual EGFR/ErbB2 (epidermal growth factor receptor/tyrosine kinase) inhibitor and is capable of reversing ABCG2- and ABCB1-mediated resistance.GW 583340 dihydrochloride selectively inhibits the growth of human tumor cells overexpressing EGFR and ErbB2, selectively inhibits the growth of human tumor cells overexpressing EGFR and ErbB2, and inhibits 80% of tumor growth in a mouse xenograft model, with potential anticancer activity.