BCRP Inhibitor

(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC₅₀ of 0.6 μM on BCRP efflux transporter.

LL-37 (17-32) is an ABCG2 inhibitor. LL-37 (17-32) binds to ABCG2, inhibits its transport activity in a non-competitive manner, and downregulates ABCG2 protein expression via lysosomal degradation. LL-37 (17-32) increases the accumulation of Mitoxantrone (HY-13502) in cancer cells overexpressing ABCG2, thereby reversing mitoxantrone resistance. LL-37 (17-32) can be used in the research of multidrug-resistant cancers.

ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC₅₀ of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species.

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.

Triclabendazole sulfoxide-¹³C,d₃ is the ¹³C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer.

6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and ³H-Methotrexate transport (IC₅₀=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin.

Triclabendazole sulfoxide-d₃ is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer.

Acridone (Standard) is the analytical standard of Acridone. This product is intended for research and analytical applications. Acridone is an organic compound based on the acridine skeleton. Acridone has antibacterial, antimalarial, antiviral and anti neoplastic activities.

WK-X-34 is a low-toxicity, highly effective multidrug resistance reversal agent. By potently inhibiting the transport functions of P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP), WK-X-34 significantly increases the intracellular accumulation of anticancer drugs and radiotracers in drug-resistant cells. WK-X-34 exerts no significant effect on MRP transporters. WK-X-34 not only restores the chemosensitivity of multidrug-resistant ovarian cancer cells, but also significantly enhances the uptake of ^99mTc-Sestamibi in P-gp-positive xenograft tumors, brain and intestinal tissues. WK-X-34 exhibits extremely low toxicity and favorable safety profiles both in vitro and in mice (at doses up to 50 mg/kg), and can be used for research on overcoming multidrug resistance in ovarian cancer.

ABCG2-IN-2 is a potent ABCG2 inhibitor with favorable oral pharmacokinetic profiles in mice. ABCG2-IN-2 can be used for the research of tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP).

Ac22(Az8)2​ is a selective BCRP inhibitor (EC₅₀: 1-2 nM). Ac22(Az8)2 can restore the drug sensitivity of BCRP-overexpressing cells by inhibiting BCRP-ATPase activity, blocking drug efflux, and increasing intracellular drug accumulation. Ac22(Az8)2 can be used in the research of BCRP-mediated multidrug-resistant cancers.

MBL-II-141 is potent ABCG2 inhibitor with an IC₅₀ of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan (HY-16562)) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity (IG₅₀ > 100 μM). MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers.

Pradigastat sodium (LCQ 908 sodium) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC₅₀ at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC₅₀ of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro.

Antitumor photosensitizer-4 (compound 10b) is a potent tyrosine kinase inhibitor (TKI) targeting ABCG2. Antitumor photosensitizer-4 is a photosensitizer (PS) consisting of a conjugate of dasatinib (HY-10181) and imatinib (HY-15463). Antitumor photosensitizer-4 induces apoptosis and ROS production and exhibits strong phototoxicity to HepG2 and B16-F10 cells.

ABCG2-IN-4 (Compound K31) is an orally active inhibitor for ABCG2, which reduces the release of Protoporphyrin IX (PPIX) (HY-B1247) from erythrocytes into plasma, and prevents the reduces phototoxicity. ABCG2-IN-4 exhibits anti-inflammatory and antioxidant activity in mouse models.

AZ99 (compound 7) is a potent ABCG2 inhibitor. AZ99 inhibits ABCG2-mediated transport of estrone-3-sulfate (E1S) into proteoliposomes and ABCG2 ATPase activity.

ABCG2-IN-5 (Compound 10) is a is a selective ABCG2 inhibitor, with an IC₅₀ of 0.34 µM. ABCG2-IN-5 can be used for the study of ABCG2-overexpressing tumors such as non-small cell lung cancer (NSCLC).

Pentamethoxymorin (MRS923) is a selective breast cancer resistance protein (BCRP/ABCG2) inhibitor. Pentamethoxymorin shows selectivity for BCRP over P-gp and MRP1. Pentamethoxymorin inhibits MDCK BCRP cells with IC₅₀ vaues of 5.98 μM and 5.94 μM in Hoechst 33342 (HY-15559) assay and Pheophorbide A (HY-125665) assay, respectively. Pentamethoxymorin can be used for the study of ccancer.

ABCG2-IN-1 (compound K2), a Ko143 analog, is an orally active ABCG2 inhibitor with an IC₅₀ of 0.13 μM. ABCG2-IN-1 has favorable oral pharmacokinetic profiles in mice.

CP-100356 is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC₅₀s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 is also a weak inhibitor of OATP1B1 (IC₅₀ = ∼66 µM). CP-100356 is devoid of inhibition against MRP2 and major human P450 enzymes (IC₅₀ > 15 µM).