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Results for "

ABCG2-IN-2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Antibiotic (1) Bacterial (2) BCRP (22) Btk (1) c-Kit (3) DNA-PK (3) Drug Metabolite (1) Isotope-Labeled Compounds (4) P-glycoprotein (1) Parasite (4) PDGFR (3) Reference Standards (4)
By Research Areas:	Cancer (22) Infection (5) Inflammation/Immunology (1) Metabolic Disease (1)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

GMP Molecules

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10010

Ko 143 Maximum Cited Publications 49 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-101570

Nedisertib 25+ 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 10+ 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-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-10873

N-Desethyl Sunitinib 5+ Cited Publications SU-12662	Drug Metabolite	Cancer
N-Desethyl Sunitinib (SU-12662) is a metabolite of Sunitinib (HY-10255A). N-Desethyl Sunitinib serves as a good transport substrate for human ABCB1, ABCG2 and murine ABCG2 .

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 .

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-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-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-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-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-101570G

Nedisertib Peposertib; M3814	DNA-PK BCRP	Cancer
Nedisertib (GMP) (Peposertib (GMP)) is Nedisertib (HY-101570) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Nedisertib 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-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-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 .

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-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-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-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-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-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-181731S

(R,S,R)-Altenuene-13C15	Isotope-Labeled Compounds	Others
(R,S,R)-Altenuene- ¹³C₁₅ is the ¹³C-labeled (R,S,R)-Altenuene. Fumitremorgin C is a potent and selective *ABCG2/BRCP* inhibitor.

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-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-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-10010R

Ko 143 (Standard)	BCRP Reference Standards	Cancer
Ko 143 (Standard) is the analytical standard of Ko 143 (HY-10010). This product is intended for research and analytical applications. 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-101570R

Nedisertib (Standard) Peposertib (Standard); M3814 (Standard)	DNA-PK Reference Standards BCRP	Cancer
Nedisertib (Standard) is the analytical standard of Nedisertib (HY-101570). This product is intended for research and analytical applications. 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 .

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 Microorganisms Classification of Application Fields Disease Research Fields Indole Alkaloids Source Classification	BCRP Bacterial Antibiotic
Fumitremorgin C is a potent and selective *ABCG2/BRCP* inhibitor.

HY-122416

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

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 .