abc transporter

G907 is a selective and potent antagonist of the small molecule ATP-binding cassette (ABC) transporter protein MsbA, with bactericidal activity, which traps MsbA in the inner lipopolysaccharide. G907 inhibits E. coli MsbA with an IC50 value of 18 nM.

Probucol (DH-581), an anti-hyperlipidemic drug, can lower the level of cholesterol in the bloodstream by increasing the LDL catabolic rate.

Chlorpropamide (Diabinese) is a sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification.

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.

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.

Glipizide (CP 28720) is a short-acting, second-generation sulfonylurea with hypoglycemic activity.

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.

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

Thiethylperazine dimaleate (Thiethylperazine maleate) is an antagonist of the D2 receptor and H1 receptor. Thiethylperazine dimaleate is an activator of ABCC1 and possesses antimicrobial, anti-emetic, and antipsychotic effects.

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

Isosilybin A is a partial PPARγ agonist, it significantly induced ABCA1 protein expression, it inhibited both monophenolase (IC50=1.7-7.6μM) and diphenolase (IC50=12.1-44.9μM) of tyrosinase. Isosilybin A shows anti-angiogenic efficacy, it has anti-prostate cancer (PCA) activity that is mediated via cell cycle arrest and apoptosis induction.

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.

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

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

Vigabatrin (Sabril), an analogue of gamma-aminobutyric acid, is an irreversible inhibitor of 4-aminobutyrate Transaminase responsible for the catabolism of γ-aminobutyric acid.

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.

MMAF sodium is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as Vorsetuzumab mafodotin and SGN-CD19A. MMAF sodium is an effective tubulin polymerization inhibitor and is used as an antitumor agent.

Thiethylperazine (Tietilperazina) is an orally available, highly potent D2 receptor and H1 receptor antagonist and selective ABCC1 activator with antimicrobial and antiemetic activity that reduces amyloid β (Aβ) load in mice, is used to relieve vertigo, and can be used in studies of neurological diseases such as Alzheimer's disease and Parkinson's disease. Alzheimer's and Parkinson's diseases.

Erythrodiol, an olive oil component, promotes Cholesterol efflux (ChE) by selectively inhibiting the degradation of ABCA1 protein.

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.

G0507 is a pyrrolopyrimidinedione compound that serves as a potent inhibitor of Escherichia coli growth, effectively inducing the extracytoplasmic σE stress response. It acts as a valuable chemical probe, specifically designed to dissect lipoprotein trafficking in Gram-negative bacteria. Notably, G0507 demonstrates strong inhibitory activity against the LolCDE ABC Transporter.

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).