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Results for "

BCRP

" in MedChemExpress (MCE) Product Catalog:

By Targets:	BCRP (33) 5-HT Receptor (1) Acyltransferase (2) Antibiotic (2) Cytochrome P450 (2) Dopamine β-hydroxylase (1) HCV Protease (1) Isotope-Labeled Compounds (2) LRRK2 (1) OAT (2) P-glycoprotein (10) Parasite (6) Topoisomerase (3)
By Research Areas:	Cancer (30) Cardiovascular Disease (1) Infection (9) Inflammation/Immunology (2) Metabolic Disease (6) Neurological Disease (3)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Antibodies

Targets Recommended: BCRP

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-12757

YHO-13177 2 Publications Verification	BCRP	Cancer
YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC₅₀ value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express *BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP* xenograft model .

HY-N5011

5,7-Dimethoxyflavone	Cytochrome P450	Metabolic Disease Inflammation/Immunology Cancer
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor .

HY-108347

CP-100356 hydrochloride 4 Publications Verification	P-glycoprotein BCRP	Metabolic Disease
CP-100356 hydrochloride 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 hydrochloride is also a weak inhibitor of OATP1B1 (IC₅₀=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC₅₀>15 µM) .

HY-129037

BCRP-IN-1	BCRP	Cancer
BCRP-IN-1 (compound 48) is a potent inhibitor of breast cancer resistance protein (BCRP), with IC₅₀s of 2.92 μM and 2.46 μM in Hoechst 33342 assay and Pheophorbide A assay, respectively .

HY-144393

*P-gp/BCRP-IN-1*	BCRP	Cancer
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) .

HY-155152

*P-gp/BCRP-IN-2*	P-glycoprotein BCRP	Cancer
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 .

HY-146676

UR-MB108	BCRP	Cancer
UR-MB108 (Compound 57) is a potent, selective ABCG2 (BCRP) inhibitor with an IC₅₀ of 79 nM. UR-MB108 is stable in blood plasma .

HY-168041

LRRK2-IN-15	LRRK2 BCRP	Neurological Disease
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 .

HY-N5011R

5,7-Dimethoxyflavone (Standard)	Cytochrome P450	Metabolic Disease Inflammation/Immunology Cancer
5,7-Dimethoxyflavone (Standard) is the analytical standard of 5,7-Dimethoxyflavone. This product is intended for research and analytical applications. 5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor .

HY-14833

Atiratecan TP300	Topoisomerase	Cancer
Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models .

HY-16278

Pradigastat 2 Publications Verification LCQ-908	Acyltransferase BCRP OAT	Infection Metabolic Disease
Pradigastat (LCQ-908) 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 .

HY-16278A

Pradigastat sodium LCQ 908 sodium	Acyltransferase BCRP OAT	Infection Metabolic Disease
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 .

HY-100390

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

HY-132934

Ac32Az19 1 Publications Verification	BCRP	Cancer
Ac32Az19 is a potent, nontoxic, and highly selective BCRP inhibitor with an EC₅₀ value of 13 nM in the BCRP-overexpressed HEK293/R2 cells.

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-149469

3,7,2',4'-Tetramethoxy-5-hydroxyflavone	BCRP	Cancer
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 .

HY-10010

Ko 143 Maximum Cited Publications 36 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-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[1][2].

HY-136450R

Triclabendazole sulfoxide (Standard)	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-12758

YHO-13351	BCRP	Cancer
YHO-13351 is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.

HY-B0777

Moxidectin 1 Publications Verification CL301423	Antibiotic BCRP P-glycoprotein Parasite	Infection
Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .

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[1][2].

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-12758A

YHO-13351 free base	BCRP	Cancer
YHO-13351 free base is the prodrug of YHO-13177, which is a potent and specific inhibitor of BCRP.

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-B0777R

Moxidectin (Standard) CL301423 (Standard)	Antibiotic BCRP P-glycoprotein Parasite	Infection
Moxidectin (Standard) is the analytical standard of Moxidectin. This product is intended for research and analytical applications. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .

HY-128685

FD 12-9 Ac12Az9	P-glycoprotein BCRP	Cancer
FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and *BCRP, with EC₅₀*s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity .

HY-W740060

Dipyridamole Mono-O-β-D-glucuronide	Others	Others
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 .

HY-19753

KS176 2 Publications Verification	BCRP	Cancer
KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively).

HY-50879

Elacridar 25+ Cited Publications GF120918; GW0918; GG918; GW120918	P-glycoprotein BCRP	Cancer
Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer .

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-50880

Elacridar hydrochloride 25+ Cited Publications GF120918A	P-glycoprotein BCRP	Cancer
Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer .

HY-116494

ML753286	BCRP	Cancer
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 .

HY-107096

CH-0793076 TP3076	Topoisomerase	Cancer
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC₅₀ of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein) .

HY-107096B

CH-0793076 TFA TP3076 TFA	Topoisomerase	Cancer
CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC₅₀ of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein) .

HY-161246

uPSEM792	Others	Neurological Disease
uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM ⁴-GlyR, with an affinity of K_i of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM ⁴-GlyR .

HY-162753

ZW-1226	Others	Cancer
ZW-1226 is a selective inhibitor of MRP1, reducing the uptake activity of MRP1 vesicles by 65 % at 5 μM. ZW-1226 shows inhibition of MRP1 in a GSH dependent way and good selectivity for MRP1 over other major ABC transporters, including P-gp, BCRP, MRP2 and MRP3 .

HY-116494A

(6R)-ML753286	Others	Cancer
(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 .

HY-120464

PF-05212377 SAM-760	5-HT Receptor	Neurological Disease
PF-05212377 (SAM-760) is an inhibitor for serotonin receptor 5-HT6. PF-05212377 is a substrate for P-gp/non-BCRP human transporter. PF-05212377 exhibits blood brain barrier permeability in non-human primates. PF-05212377 can be used for Alzheimer’s Disease research .

HY-106004

Zamicastat BIA 5-1058	Dopamine β-hydroxylase P-glycoprotein BCRP	Cardiovascular Disease Cancer
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 .

HY-157876

Anticancer agent 191	P-glycoprotein BCRP	Cancer
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 .

HY-16773

Vedroprevir GS-9451	HCV Protease BCRP P-glycoprotein	Infection
Vedroprevir (GS-9451) is an inhibitor for HCV NS3/4A protease with an IC₅₀ of 3.2 nM. Vedroprevir is also an inhibitor for breast cancer resistant protein (BCRP) with an IC₅₀ of 1.4 μM. Vedroprevir inhibits P-gp, MRP1 and MRP2 with IC₅₀ of 34, 14.9 and 12 μM, respectively. Vedroprevir exhibits good pharmacokinetic characteristics in rats and dogs .

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-101453

Ceefourin 1	Others	Cancer
Ceefourin 1 is a potent and highly selective multidrug resistance protein 4 (MRP4) inhibitor. Ceefourin 1 inhibits transport of a broad range of MRP4 substrates, yet is highly selective for MRP4 over other ABC transporters. Ceefourin 1 is a benzothiazol and primarily as a chemosensitizer for high-risk neuroblastoma .

Cat. No.	Product Name

HY-L011

Membrane Transporter/Ion Channel Compound Library	1,476 compounds
Most of molecules enter or leave cells mainly via membrane transport proteins, which play important roles in several cellular functions, including cell metabolism, ion homeostasis, signal transduction, the recognition process in the immune system, energy transduction, etc. There are three major types of transport proteins, ATP-powered pumps, channel proteins and transporters. Transport proteins such as channels and transporters play important roles in the maintenance of intracellular homeostasis, and mutations in these transport protein genes have been identified in the pathogenesis of a number of hereditary diseases. In the central nervous system, ion channels have been linked to, but not limited to, many diseases such asataxias, paralyses, epilepsies, and deafness. This indicates the roles of ion channels in the initiation and coordination of movement, sensory perception, and encoding and processing of information. Ion channels are a major class of drug targets in drug development. MCE designs a unique collection of 1,476 smal-molecule modulators that can be used for the research of Ion Channel and Membrane Transporter or high throughput screening (HTS) related drug discovery.

Membrane Transporter/Ion Channel Compound Library

1,476 compounds

Most of molecules enter or leave cells mainly via membrane transport proteins, which play important roles in several cellular functions, including cell metabolism, ion homeostasis, signal transduction, the recognition process in the immune system, energy transduction, etc. There are three major types of transport proteins, ATP-powered pumps, channel proteins and transporters. Transport proteins such as channels and transporters play important roles in the maintenance of intracellular homeostasis, and mutations in these transport protein genes have been identified in the pathogenesis of a number of hereditary diseases. In the central nervous system, ion channels have been linked to, but not limited to, many diseases such asataxias, paralyses, epilepsies, and deafness. This indicates the roles of ion channels in the initiation and coordination of movement, sensory perception, and encoding and processing of information. Ion channels are a major class of drug targets in drug development.

MCE designs a unique collection of 1,476 smal-molecule modulators that can be used for the research of Ion Channel and Membrane Transporter or high throughput screening (HTS) related drug discovery.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N5011

5,7-Dimethoxyflavone	Structural Classification Flavonoids Classification of Application Fields Flavones Kaempferia parviflora Wall. ex Baker Plants Inflammation/Immunology Disease Research Fields Zingiberaceae Cancer	Cytochrome P450
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor .

HY-N5011R

5,7-Dimethoxyflavone (Standard)	Structural Classification Flavonoids Flavones Kaempferia parviflora Wall. ex Baker Plants Zingiberaceae	Cytochrome P450
5,7-Dimethoxyflavone (Standard) is the analytical standard of 5,7-Dimethoxyflavone. This product is intended for research and analytical applications. 5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor .

HY-149469

3,7,2',4'-Tetramethoxy-5-hydroxyflavone	Structural Classification Mortonia palmeri Hemsl. Flavonoids Flavones Source classification Celastraceae Plants	BCRP
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 .

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 .

Species:	Human (2)
Tag:	Tag Free (2)
Source:	HEK293 (2)

Cat. No.	Compare	Product Name	Species	Source

HY-P703266

	ABCG2 Protein, Human (HEK293) ABCP; BCRP; BCRP1; MXR	Human	HEK293
	ABCG2 Protein, Human (HEK293) is the recombinant human-derived ABCG2, expressed by HEK293 , with tag Free labeled tag. The total length of ABCG2 Protein, Human (HEK293) is 655 a.a.,

HY-P703267

	ABCG2 Protein, Human (HEK293, E211Q) ABCP; BCRP; BCRP1; MXR	Human	HEK293
	ABCG2 Protein, Human (HEK293, E211Q) is the recombinant human-derived ABCG2, expressed by HEK293 , with tag Free labeled tag. ,

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