abcg2

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

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).

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.

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

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.

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

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

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).

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).

MZ82, a derivative of Ko 143, is a potent inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2 BCRP), with an IC50 of approximately 23 nM. Compared to Ko 143, MZ82 exhibits significantly enhanced metabolic stability in liver microsomes and shows marked improvement in mice, along with the ability to penetrate the brain.

AZ99 (compound 7) serves as an effective inhibitor of ABCG2. It impedes the transport of estrone-3-sulfate (E1S) to proteoliposomes and inhibits ABCG2 ATPase activity mediated by ABCG2.

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.

NSC636795 is an ABCG2 transporter function inhibitor.

Methyl Streptonigrin is an ABCG2 transporter function inhibitor.

NSC103054 is an ABCG2 transporter function inhibitor.