abcg

Prazosin hydrochloride (Vasoflex) reduces peripheral resistance and relaxes vascular smooth muscles as a selective adrenergic alpha-1 antagonist by a mechanism not completely known. Prazosin hydrochloride is a synthetic piperazine derivative with hypotensive antiadrenergic properties, It is used in the treatment of heart failure, hypertension, pheochromocytoma, Raynaud's syndrome, prostatic hypertrophy, and urinary retention.

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.

ABCB1/ABCG2-IN-1 (Compound (S,Z)-4b) is an inhibitor of ABCB1 and ABCB2 transport proteins. It exhibits moderate activity against SW620M, -V, and -Mito variants with an IC50 of approximately 50 μM. In vitro, ABCB1/ABCG2-IN-1 can influence methotrexate resistance and is applicable in cancer research.

ABCG2-IN-5 (Compound 10) is a selective ABCG2 inhibitor with an IC50 value of 0.34 µM. ABCG2-IN-5 is applicable in research involving tumors that overexpress ABCG2, such as non-small cell lung cancer (NSCLC).

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].

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

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.

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).

Lycorine (Narcissine) inhibits protein synthesis and may inhibit ascorbic acid biosynthesis, although studies on the latter are controversial and inconclusive.

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.

N3-PEG8-Phe-Lys-PABC-Gefitinib is an antibody-drug conjugate (ADC) agent-linker complex exhibiting potent antitumor activity. It incorporates the orally active EGFR tyrosine kinase inhibitor Gefitinib, tethered by the cleavable linker N3-PEG8-Phe-Lys-PABC. As a click chemistry reagent, it features an azide group facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAC) with alkyne-bearing molecules. Additionally, it can engage in strain-promoted alkyne-azide cycloaddition (SPAAC) with compounds presenting DBCO or BCN groups.

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

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