ABCG2

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].

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].

Avapritinib (BLU-285) is a dual inhibitor targeting the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM).

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).

CCTA-1523 is an efflux function of ABCG2 inhibitor. CCTA-1523 selectively reverses ABCG2-mediated MDR in cancer cells.

A-803467 is a selective NaV1.8 channel blocker.

MY-5445 (N-(3-chlorophenyl)-4-phenylphthalazin-1-amine) is a specific inhibitor of phosphodiesterase type 5 (PDE5). MY-5445 selectively inhibits cGMP PDE (Ki:1.3 μM).

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

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.

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.

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

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.

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

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.

NSC636795 is an ABCG2 transporter function inhibitor.

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.

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.

Vismodegib-d7 is a deuterated compound of Vismodegib. Vismodegib has a CAS number of 879085-55-9. Vismodegib is a hedgehog pathway inhibitor (IC50: 3 nM). It also inhibits P-gp (IC50: 3.0 μM), ABCG2 (IC50: 1.4 μM).

Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.

Methyl Streptonigrin is an ABCG2 transporter function inhibitor.

NSC107392 is a substrate of ABCG2.

UR-MB108 is a potent and selective inhibitor of ABCG2 (BCRP), displaying an IC50 value of 79 nM, and exhibits stability in blood plasma.

NSC265473 is an ABCG2 substrate.

Becatecarin is a water-soluble, diethylaminoethyl analog of the antineoplastic antibiotic rebeccamycin. It intercalates into DNA, stabilizing the DNA-topoisomerase complex. This results in the potent catalytic inhibition of both topoisomerases I and II, initiating DNA cleavage and apoptosis. Becatecarin, alone or in combination with other compounds, has anti-cancer as well as myelosuppressive effects in vivo. It is also a transport substrate of the ATP-binding cassette (ABC) transporter ABCG2.

LL-37(17-32) is a biologically active peptide fragment derived from the C-terminal domain of human cathelicidin antimicrobial peptide. This segment reverses ABCG2-mediated multidrug resistance in cancer cell lines, highlighting its potential therapeutic role against drug resistance.

Antitumor Photosensitizer-4 (compound 10b), a conjugate of dasatinib and imatinib, serves as a potent tyrosine kinase inhibitor (TKI) targeting ABCG2. This photosensitizer (PS) induces apoptosis and reactive oxygen species (ROS) production, while demonstrating significant phototoxicity against both HepG2 and B16-F10 cells [1].

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).

Glafenine Hydrochloride is an anti-inflammatory agent.

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.

Vismodegib-d4 is a deuterated compound of Vismodegib. Vismodegib has a CAS number of 879085-55-9. Vismodegib is a hedgehog pathway inhibitor (IC50: 3 nM). It also inhibits P-gp (IC50: 3.0 μM), ABCG2 (IC50: 1.4 μM).

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)

Efflux inhibitor-1 is a pyrazolopyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC 50 s of 0.45 μM and 2.17 μM, respectively .

KPH2f, a dual URAT1/GLUT9 inhibitor, demonstrates safety, oral activity, and efficacy, with inhibitory concentrations (IC50s) of 0.24 μM for URAT1 and 9.37 μM for GLUT9. It exhibits minimal effects on OAT1 and ABCG2, with IC50 values of 32.14 μM and 26.74 μM, respectively [1].

NSC103054 is an ABCG2 transporter function inhibitor.

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

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

1. Tectochrysin (Techtochrysine) has antioxidant effect. 2. Tectochrysin is promising inhibitors for the reversal of ABCG2-mediated drug transport. 3. Tectochrysin leads to apoptotic cell death in NSC-LC cells through activation of DR3 and Fas expression via inhibition of STAT3 phosphorylation.

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