- Cat. No.
- A11080
Valspodar (PSC-833)
Synonyms: PSC833; Amdray
PSC-833 is a kind of P-glycoprotein (P-gp) modulator that inhibits P-gp-mediated multidrug-resistance (MDR).
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P-glycoprotein (P-gp) inhibitors block a drug efflux pump that contributes to multidrug resistance in cells. P-gp, also called multidrug resistance protein 1 (MDR1) or ATP-binding cassette subfamily B member 1 (ABCB1), uses energy from adenosine triphosphate (ATP) hydrolysis. It was first described in 1976 as a surface glycoprotein of drug-resistant Chinese hamster ovary cells. A crystal structure later showed a large drug-binding pocket that accounts for its broad substrate range. Verapamil and its metabolite norverapamil hydrochloride are early inhibitors, and verapamil is also listed under Calcium Channels. Later inhibitors include valspodar, tariquidar, LY335979 and elacridar, which also blocks breast cancer resistance protein (BCRP).
Synonyms: PSC833; Amdray
PSC-833 is a kind of P-glycoprotein (P-gp) modulator that inhibits P-gp-mediated multidrug-resistance (MDR).
Synonyms: XR 9576??XR9576??D06008; XR9576
Tariquidar (XR9576) is a P-glycoprotein drug efflux pump inhibitor.
Synonyms: RS-33295-198; Zosuquidar 3HCl
LY335979 (Zosuquidar trihydrochloride) is a potent highly selective P-gp inhibitor.
Synonyms: GF120918
Elacridaris a prototypical BCRP inhibitor which inhibits the Bcrp1-mediated transport.
Synonyms: (±)-Norverapamil hydrochloride; D591 hydrochloride
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity.
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
Synonyms: OC144-093
ONT-093 is an orally bioavailable P-glycoprotein pump inhibitor, for the potential reversal of multidrug resistance in patients undergoing cancer chemotherapy.
Synonyms: R101933
Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters.
Synonyms: VX-710 dicitrate; VX-710
Biricodar dicitrate (VX-710 dicitrate) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
Synonyms: Tariquidar methanesulfonate hydrate
XR9576 is a P-glycoprotein inhibitor undergoing research as an adjuvant against multidrug resistance in cancer
Synonyms: GF 120918A
Elacridar hydrochloride is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.
Synonyms: LY335979
Zosuquidar is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.
KS-176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 uM in Pheo A and Hoechst 33342 assays respectively).
Synonyms: CP 76136-27
Danofloxacin mesylate is a fluoroquinolone antimicrobial agent that exerts its bactericidal activity primarily through the inhibition of bacterial DNA gyrase, a crucial enzyme for DNA replication. This compound displays a broad spectrum of effectiveness against various bacterial strains. Additionally, Danofloxacin mesylate is recognized as a substrate for ATP-dependent efflux transporters, including P-glycoprotein (P-gp) and multidrug resistance protein 2 (MRP2), making it relevant for studies on drug resistance mechanisms in bacteria. This agent is primarily utilized in veterinary medicine and research on antibiotic efficacy and resistance.
NSC 23925 is a plasma membrane glycoprotein 1 (Pgp1) inhibitor to reverse multidrug resistance (MDR1).
FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity.
Synonyms: CBLC4H10
Reversan (CBLC4H10) is a potent and nontoxic multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (Pgp) inhibitor.
P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
Synonyms: HM30181; HM30181A
Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.
Synonyms: VX-710
Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
Synonyms: HM30181 mesylate; HM 30181; HM30181A mesylate; HM 30181A
Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
Synonyms: MS-209
Dofequidar, also known as MS-209, is a quinolone-derived sphingomyelin synthase inhibitor that blocks P-glycoprotein and multidrug resistance-associated protein-1, is under development by Schering for the potential treatment of multidrug resistant tumors.
Isosinensetin is a bioactive flavonoid compound with diverse pharmacological properties. It acts as a dual inhibitor of HIV-1 protease and protein tyrosine phosphatase 1B (PTP1B), with an IC₅₀ of 2.61 µM and a Kᵢ of 0.92 µM for PTP1B, indicating its potential in antiviral and metabolic disease research. Additionally, isosinensetin inhibits P-glycoprotein (P-gp) activity in MDR1-MDCKII cells, suggesting its utility in overcoming multidrug resistance. Isosinensetin exhibits multiple therapeutic effects, including anti-tumor, anti-viral, anti-inflammatory, and antioxidant activities. These properties support its application in the research of various conditions such as cancer, chronic inflammation, osteoporosis, diabetes, and infectious diseases.