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Results for "

ABCG2-IN-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (1) Bacterial (2) BCRP (14) Btk (1) c-Kit (3) DNA-PK (1) Isotope-Labeled Compounds (3) Parasite (4) PDGFR (3) Reference Standards (2) Topoisomerase (1)
By Research Areas:	Cancer (13) Infection (5) Inflammation/Immunology (1) Metabolic Disease (1)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Dan family AIM2 NEKs CD44

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N2143

Fumitremorgin C 3 Publications Verification 12α-FumitremorgIN C	BCRP Bacterial Antibiotic	Infection Cancer
Fumitremorgin C is a potent and selective *ABCG2/BRCP* inhibitor.

HY-136450

Triclabendazole sulfoxide TCBZ-SO	Parasite BCRP	Infection
Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter *ABCG2/BCRP* .

HY-10010

Ko 143 Maximum Cited Publications 41 Publications Verification	BCRP	Cancer
Ko 143 is a potent and selective ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor. Ko 143 displays >200-fold selectivity over P-gp and MRP-1 transporters .

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-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-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 the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .

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 the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .

HY-163919

N,N-Dimethyl-idarubicin-trisaccharide	Topoisomerase	Cancer
N,N-Dimethyl-idarubicin-trisaccharide (compound 26) is an efficient intercalating agent. N,N-Dimethyl-idarubicin-trisaccharide shows excellent cytotoxicity against ABCG2-overexpressing and ABCB1-overexpressing cells with IC₅₀s of 19 and 32 nM, respectively .

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 the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .

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-112505

Efflux inhibitor-1	BCRP	Cancer
Efflux inhibitor-1 (compound 2) is a pyrazolo[1,5-a]pyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward *ABCG2/BCRP* over ABCB1 with IC₅₀s of 0.45 μM and 2.17 μM, respectively .

HY-P5391

LL-37(17-32)	Bacterial	Others
LL-37(17-32) is a biological active peptide. (This peptide is an active segment of LL-37, a peptide derived from the C-terminal domain of human cathelicidin antimicrobial peptide. It has been reported that the LL17-32 peptide exhibits reversal effect on ABCG2-mediated multidrug resistance in cancer cell lines.)

HY-168572

MZ82	BCRP	Cancer
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 .

HY-18010

PCI 29732 3 Publications Verification	Btk BCRP	Inflammation/Immunology
PCI 29732 is a potent, orally active, reversible BTK inhibitor with K_i ^app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of *ABCG2* by competitively binding to the ATP-binding site of ABCG2 .

HY-101570

Nedisertib 20+ Cited Publications Peposertib; M3814	DNA-PK BCRP	Cancer
Nedisertib (Peposertib) is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC₅₀ value of less than 3 nM. Nedisertib also acts as a modulator of *ABCG2, capable of reversing ABCG2*-mediated multidrug resistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity .

HY-101561

Avapritinib 5+ Cited Publications BLU-285	c-Kit PDGFR	Cancer
Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .

HY-122416

6,8-Diprenylnaringenin Lonchocarpol A; SenegalensIN	BCRP	Metabolic Disease 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 .

HY-101561R

Avapritinib (Standard) BLU-285 (Standard)	Reference Standards c-Kit PDGFR	Cancer
Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .

HY-W754911

Avapritinib-d3 BLU-285-d₃	Isotope-Labeled Compounds PDGFR c-Kit	Cancer
Avapritinib-d₃ (BLU-285-d₃) is deuterium labeled Avapritinib. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .

Cat. No.	Product Name	Target	Research Area

HY-P5391

LL-37(17-32)	Bacterial	Others
LL-37(17-32) is a biological active peptide. (This peptide is an active segment of LL-37, a peptide derived from the C-terminal domain of human cathelicidin antimicrobial peptide. It has been reported that the LL17-32 peptide exhibits reversal effect on ABCG2-mediated multidrug resistance in cancer cell lines.)

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N2143

Fumitremorgin C 3 Publications Verification 12α-FumitremorgIN C	Infection Alkaloids Structural Classification Microorganisms Classification of Application Fields Source classification Disease Research Fields Indole Alkaloids	BCRP Bacterial Antibiotic
Fumitremorgin C is a potent and selective *ABCG2/BRCP* inhibitor.

HY-122416

6,8-Diprenylnaringenin Lonchocarpol A; SenegalensIN	Structural Classification Classification of Application Fields Erythrinasenegalensis DC. Source classification Metabolic Disease Plants Moraceae Flavonoids Leguminosae Humulus lupulus L. Flavonones Phenols Polyphenols Disease Research Fields Cancer	BCRP
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 .

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 the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .

HY-136450S1

Triclabendazole sulfoxide-13C,d3
Triclabendazole sulfoxide- ¹³C,d₃ is the ¹³C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is the main plasma metabolite of Triclabendazole, and exhibits anti-parasite effects. Triclabendazole sulfoxide can inhibit membrane transporter ABCG2/BCRP .

HY-W754911

Avapritinib-d3
Avapritinib-d₃ (BLU-285-d₃) is deuterium labeled Avapritinib. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .

Avapritinib-d3

Avapritinib-d₃ (BLU-285-d₃) is deuterium labeled Avapritinib. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC₅₀s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .

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