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

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

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.

TTT-28 is a thiazole-valine peptidomimetic and a selective ABCB1 (P-gp/MDR1) inhibitor with high efficacy and low toxicity, reversing ABCB1-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.

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).

Elodeoidileon A acts as an agonist to RXRα, exhibiting a dissociation constant (Kd) of 5.85 μM when interacting with the RXRα-LBD protein. It enhances the expression of ATP Binding Cassette Transporter A1 (ABCA1). Furthermore, Elodeoidileon A holds potential in Alzheimer's disease research.

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.

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

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.

DL-threo dihydrosphingosine is a cell-permeable inhibitor of the extracellular signal-regulated kinase (ERK) signalling cassette in mammalian cells. DL-threo dihydrosphingosine is effective against both growth factor- and G-protein-dependent activation of

MK-571 sodium (L-660711 sodium salt) is a selective, orally active antagonist of the CysLT1 receptor. MK-571 sodium is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics, and their conjugates. MK-571 sodium can inhibit the synthesis of K-4′-O-GlcA (19.7 μM). MK571 dose-dependently inhibits the intracellular biosynthesis of all flavonol sulphates and glucuronides by Caco-2 cells. MK-571 sodium significantly inhibits phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-4′-O-glucuronide was competitively inhibited. In addition to inhibiting MRP2, MK571 is a potent inhibitor of enterocyte phase-2 conjugation.

HM30181AK is an inhibitor of the adenosine triphosphate (ATP) binding cassette (ABC) transporter P-glycoprotein (P-gp) with adjuvant activity.

Olomoucine II is an inhibitor of cyclin-dependent kinases (CDKs; IC50s = 7.6, 0.1, 19.8, 0.45, and 0.06 μM for Cdk1, -2, -4, -7, and -9, respectively).1It is selective for CDKs over 10 additional kinases (IC50s = >100 μM for all) but does inhibit ERK2 (IC50= 32 μM) and the ATP-binding cassette transporter B1 (ABCB1; IC50= 6.4 μM).1,2Olomoucine II inhibits proliferation of a variety of cancer cells, including those expressing wild-type p53 or mutant p53 (mean IC50s = 7.4 and 10.1 μM, respectively), and it acts synergistically with daunorubicin to inhibit proliferation of HCT-8 cells that endogenously express ABCB1. Olomoucine also inhibits replication of herpes simplex virus 1 (HSV-1), HSV-2, vaccinia virus, human adenovirus type 4 (Ad4), and human CMV (IC50s = 5, 4.7, 3.8, 2.4, and 3.2 μM, respectively) but not measles virus or influenza virus (IC50s = >20 μM for both).3

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.

Ibutilide Fumarate (U70226E) is the fumarate salt form of ibutilide, a class III antiarrhythmic agent. Ibutilide exerts its effect by activating a slow, inward, predominately sodium current rather than by blocking outward potassium currents. This results in prolongation of atrial and ventricular action potential duration and refractory periods. Ibutilide slightly decreases the sinus rate and atrioventricular (AV) conduction and produces a dose-related prolongation of the QT interval.

MsbA-IN-6 is a potent antibiotic and inhibitor of the gram-negative ATP-binding cassette (ABC) transporter MsbA, an essential protein for transporting lipopolysaccharide across the inner bacterial membrane. It exerts a bactericidal effect on Escherichia coli by inhibiting the ATPase and transport activity of MsbA, while retaining efficacy against multidrug-resistant clinical strains [1] [2].

st-Ht31, a cell-permeable stearated peptide derived from the amphipathic helix domain of A-kinase anchoring proteins (AKAPs), effectively binds protein kinase A (PKA), impacting PKA's cellular interactions without altering its activity. Specifically, at a 50 µM concentration, it reduces PKA's membrane anchoring in BHK-21 fibroblast reporter assays. Moreover, st-Ht31 at concentrations of 1 and 3 µM decreases both capacitance and hyperactivation in mouse sperm, thereby inhibiting in vitro fertilization. Additionally, at 50 µM, this compound facilitates cholesterol export in BHK-21 cells and RAW 264.7 macrophages expressing ATP-binding cassette transporter 1 (ABCA1), showcasing its multifaceted cellular impacts.

C3N-Dbn-Trp2 is an inhibitor of the ATP-binding cassette transporter ABCB1. It inhibits the efflux of Rhodamine 123 mediated by ABCB1 in HEK293T and HCT-15 cells, with IC50 values of 5.9 µM and 2.2 µM, respectively. Additionally, C3N-Dbn-Trp2 inhibits the efflux of Doxorubicin, thereby enhancing the cytotoxicity of Doxorubicin in cells expressing ABCB1.

CS-6253TFA is the TFA salt form of CS-6253. This compound serves as an activator for the ATP Binding Cassette 1 (ABCA1). It effectively modulates the amyloid-beta Aβ42 40 ratio and influences the metabolism of lipoproteins in plasma. Additionally, CS-6253TFA facilitates the production of cholesterol-rich high-density lipoprotein (HDL) particles and induces the release of microparticles.

CS-6253 is an agonist of ATP Binding Cassette 1 (ABCA 1). It modulates the amyloid beta Aβ42 40 ratio, influencing lipoprotein metabolism in the plasma. Additionally, CS-6253 promotes the production of cholesterol-rich high-density lipoprotein (HDL) particles and induces the release of microparticles.

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