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Abcg2+Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Akt (3) Apoptosis (3) BCRP (16) EGFR (3) ERK (3) Isotope-Labeled Compounds (2) Parasite (4) Reference Standards (1) TRP Channel (3)
By Research Areas:	Cancer (16) Infection (5) Metabolic Disease (1) Neurological Disease (1)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-109061

Lazertinib 3 Publications Verification YH25448; GNS-1480	Apoptosis Akt TRP Channel EGFR ERK	Infection Neurological Disease Metabolic Disease Cancer
Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an *ABCB1/ABCG2* inhibitor and a TRPA1 activator. Lazertinib exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and *ABCG2, respectively. By inhibiting* mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of *ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC* activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia ^[2] .

HY-12758

YHO-13351	BCRP	Cancer
YHO-13351 is an orally active *ABCG2* inhibitor . YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer ^[2] .

HY-109061B

Lazertinib mesylate 3 Publications Verification YH25448 mesylate; GNS-1480 mesylate	TRP Channel EGFR Akt ERK Apoptosis	Cancer
Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an *ABCB1/ABCG2* inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and *ABCG2, respectively. By inhibiting* mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of *ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC* activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia ^[2] .

HY-136450

Triclabendazole sulfoxide TCBZ-SO	Parasite BCRP	Infection Cancer
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 ^[2].

HY-146676

UR-MB108	BCRP	Cancer
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 .

HY-168573

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

HY-17648

MBL-II-141	BCRP	Cancer
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 ^[2].

HY-129301

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

HY-N2651

5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone	BCRP	Cancer
5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone (compound 1), a flavonoid, is a potent *ABCG2* inhibitor with an IC₅₀ of 6.6 μM .

HY-155653

ABCG2-IN-2	BCRP	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) .

HY-155652

ABCG2-IN-1	BCRP	Cancer
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 .

HY-178386

ABCG2-IN-5	BCRP	Cancer
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) .

HY-W082856A

Butein tetramethyl ether	BCRP	Cancer
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 .

HY-136450R

Triclabendazole sulfoxide (Standard) TCBZ-SO (Standard)	Reference Standards Parasite BCRP	Infection
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 ^[2].

HY-136450S

Triclabendazole sulfoxide-d3 TCBZ-SO-d₃	Isotope-Labeled Compounds Parasite BCRP	Infection
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 ^[2].

HY-136450S1

Triclabendazole sulfoxide-13C,d3 TCBZ-SO-¹³C,d₃	Isotope-Labeled Compounds Parasite BCRP	Infection
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 ^[2].

HY-181802

MRS8431	BCRP	Cancer
MRS8431 is an ABCG2 inhibitor with a IC₅₀ of 160 nM against human ABCG2. MRS8432 partially inhibits ABCG2-mediated substrate transport. MRS8432 is applicable to research related to cancer multidrug resistance .

HY-118083

Pentamethoxymorin MRS923	BCRP	Cancer
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 .

HY-109061A

Lazertinib mesylate hydrate YH25448 mesylate hydrate; GNS-1480 mesylate hydrate	Apoptosis Akt TRP Channel EGFR ERK	Cancer
Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an *ABCB1/ABCG2* inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and *ABCG2, respectively. By inhibiting* mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of *ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC* activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia ^[2] .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2651

5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone	Flavonoids Leguminosae Flavonones Plants Sophora flavescens Aiton Source Classification	BCRP
5,7,3'-Trihydroxy-4'-Methoxy-8-prenylflavanone (compound 1), a flavonoid, is a potent *ABCG2* inhibitor with an IC₅₀ of 6.6 μM .

Cat. No.	Product Name	Chemical Structure

HY-136450S

Triclabendazole sulfoxide-d3
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 ^[2].

Triclabendazole sulfoxide-d3

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 ^[2].

HY-136450S1

Triclabendazole sulfoxide-13C,d3
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 ^[2].

Triclabendazole sulfoxide-13C,d3

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 ^[2].

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