BCRP Inhibitor

CCTA-1523 is a potent, selective, reversible and orally active ABCG2 inhibitor. CCTA-1523 shows cytotoxicity. CCTA-1523 shows anticancer activity.

Butein tetramethyl ether (Compound 20) is a potent and selective breast cancer resistance protein/ATP-binding cassette subfamily G member 2 (BCRP/ABCG2) inhibitor. Butein tetramethyl ether has inhibitory potencies against MCF-7 MX and MDCK BCRP cells with IC₅₀ values of 2.2 and 1.03 μM, respectively. Butein tetramethyl ether is promising for research of cancers.

LRRK2-IN-15 is an LRRK2 inhibitor. The IC₅₀ value for PBMC cells is 5 nM, and the IC₅₀ value for BCRP is 1.5 μM. LRRK2-IN-15 can be used for research on Parkinson's disease.

UR-MB108 is a selective ABCG2 inhibitor with an IC₅₀ value of 79 nM. UR-MB108 acts as a potent inhibitor of ABCG2 transport and ATPase activity. UR-MB108 can be used in cancer-related research.

Rhinacanthin C is an orally active naphthoquinone ester and P-gp inhibitor (IC₅₀ = 5.20 μM). Rhinacanthin C exerts effects in ameliorating hepatic steatosis, insulin resistance, and inflammation by inhibiting P-gp, BCRP, OATP1B1/1B3, and multiple CYP enzymes, downregulating lipid synthesis-related factors such as ACC and FAS, and upregulating AMPKα phosphorylation and SIRT1. Rhinacanthin C can be used in research on non-alcoholic fatty liver disease, diabetes, abnormal osteolysis, Alzheimer's disease, and inflammation.

(6R)-ML753286 is an isomer of ML753286 (HY-116494). 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.

MRS8288 is a ABCG2 and P-glycoprotein inhibitor, with an IC₅₀ of 0.96 μM against ABCG2 and an IC₅₀ of 1.39 μM against P-glycoprotein. MRS8288 inhibits the ATPase activity of ABCG2 and P-glycoprotein, and suppresses ABCG2-mediated substrate transport. MRS8288 is applicable for cancer research.

P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC₅₀: 1.6 nM) and BCRP (IC₅₀: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells.

P-gp/BCRP-IN-1 (compound 19) is a potential, relatively safe, orally active and efficient efflux transporter (P-gp and BCRP) inhibitor. P-gp/BCRP-IN-1 exerts resistance reversal by inhibiting the efflux function of P-gp and BCRP. P-gp/BCRP-IN-1 can overcome the resistance and improve the oral bioavailability of PTX (Paclitaxel).

Anticancer agent 191 (Compound 2) is a derivative of probenecid (HY-B0545). As a cancer cell efflux inhibitor, Anticancer agent 191 is designed to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticancer agent 191 increases the accumulation of vinblastine in cancer cells, which is used for cancer research.

Triclabendazole sulfoxide (Standard) is the analytical standard of Triclabendazole sulfoxide. This product is intended for research and analytical applications. 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.

ML230 (Standard) is the analytical standard of ML230 (HY-111678). This product is intended for research and analytical applications. ML230 (CID44640177; SID 88095709) is a selective inhibitor of ATP-binding cassette (ABC) transporter ABCG2, and 36-fold selective for ABCG2 over ABCB1 with EC₅₀s values of 0.13 μM and 4.65 μM, respectively.

6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin) is a potent BCRP/ABCG2 inhibitor (IC₅₀ = 0.410 μM) and a non-competitive allosteric PTP1B inhibitor (IC₅₀ = 1.04 μM; K_i = 1.56 μM) that is isolated from Humulus lupulus. 6,8-Diprenylnaringenin produces non-competitive allosteric inhibition by locking the WPD catalytic loop of PTP1B in an inactive open conformation, while simultaneously binding to and inhibiting the ABCG2 drug efflux pump. 6,8-Diprenylnaringenin also exhibits antibacterial activity against MRSA (MIC = 6-13 μM) and antioxidant activity. 6,8-Diprenylnaringenin is used in research on type 2 diabetes, obesity, MRSA infection, and atherosclerosis.

BCRP-IN-2 has BCRP inhibitory activity and shows even greater inhibition of BCRP after activation by ultraviolet light. BCRP-IN-2 can be a valuable probe for studying the interactions of quinazolinamine derivatives with BCRP, as it stimulates ATP hydrolysis of the BCRP transport protein, increasing the accumulation of mitoxantrone (HY-13502) in H460/MX20 cells with BCRP overexpression.

Dipyridamole Mono-O-β-D-glucuronide (compound M4) is a derivative of the phosphodiesterase (PDE) and BCRP inhibitor Dipyridamole (HY-B0312) and is an O-glucuronide.

Nuvisertib (Standard) (TP-3654 (Standard)) is the analytical standard of Nuvisertib (HY-101126). This product is intended for research and analytical applications. Nuvisertib (TP-3654) is an orally active second-generation pan-PIM kinase inhibitor with K_i values of 5 nM, 239 nM, and 42 nM against PIM-1, PIM-2, and PIM-3, respectively. Nuvisertib inhibits JAK-independent inflammatory and survival signaling pathways, reduces the production of proinflammatory cytokines, restores apoptotic sensitivity, inhibits mTORC1, MYC, and TGF-β signaling pathways, and decreases the expression of fibrosis markers. Nuvisertib selectively impairs the transport function of ABCG2, resensitizes multidrug-resistant cancer cells to cytotoxic drugs, and overcomes JAK2 inhibitor resistance. Nuvisertib can be used in research related to myelofibrosis, renal cell carcinoma, multidrug-resistant cancer, advanced solid tumors, urothelial carcinoma, and prostate adenocarcinoma.

BCRP/ABCG2-IN-1 is the inhibitor of breast cancer resistance protein (BCRP/ABCG2), with IC₅₀ of 5.98 μM, that can be used in multidrug resistance of breast cancer.

Zamicastat (Standard) is the analytical standard of Zamicastat (HY-106004). This product is intended for research and analytical applications. Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC₅₀ values of 73.8 μM and 17.0 μM, respectively. Zamicastat reduces high blood pressure.

(S)-ML753286 (Standard) is the analytical standard of (S)-ML753286 (HY-100390). This product is intended for research and analytical applications. (S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.

MZ82, Ko 143 (HY-10010) derivative, is a ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor with the IC₅₀ of ~23 nM. MZ82 not only shows greatly improved metabolic stability over Ko 143 (HY-10010) in liver microsomes but also in mice, and is able to penetrate into the brain.