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Results for "

ABCG2 ATPase activity

" in MedChemExpress (MCE) Product Catalog:

By Targets:	BCRP (10) Akt (3) Apoptosis (3) EGFR (3) ERK (3) Isotope-Labeled Compounds (2) P-glycoprotein (1) Parasite (4) PARP (1) Reference Standards (1) TRP Channel (3)
By Research Areas:	Cancer (10) Infection (5) Metabolic Disease (1) Neurological Disease (1)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: BCRP Na+/K+ ATPase

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 ATP*ase 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 .

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 ATP*ase 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 .

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 .

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-178100

PARP1-IN-45	PARP BCRP	Cancer
PARP1-IN-45 (Compound 15) is a PARP1 inhibitor with an IC₅₀ of 17  nM. PARP1-IN-45 effectively stimulates ATPase activity of *ABCG2*. PARP1-IN-45 can be used for cancers like ovarian cancer research .

HY-119724

ABCG2-IN-3	BCRP	Cancer
ABCG2-IN-3 (Compound 52) is a selective inhibitor for breast cancer resistance protein (ABCG2), with an IC₅₀ of 0.238 µM. ABCG2-IN-3 reverses the ABCG2-mediated resistance toward SN-38 and inhibit the *ATPase* activity .

HY-181803

MRS8432	BCRP	Cancer
MRS8432 is an ABCG2 modulator with an EC₅₀ of 7.5 nM against human *ABCG2. MRS8432 activates ABCG2* ATPase activity. MRS8432 partially inhibits *ABCG2*-mediated substrate transport. MRS8432 is applicable to research related to cancer multidrug resistance .

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 .

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 .

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 .

HY-181804

MRS8288	BCRP P-glycoprotein	Cancer
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 .

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 ATP*ase 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 .

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 .

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 .

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 .

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 .

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