bcrp — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T83892	33-BCRP Inhibitor	33-Breast Cancer Resistance Protein Inhibitor
	33-BCRP inhibitor is a compound that blocks the action of breast cancer resistance protein (BCRP), enhancing the susceptibility of mitoxantrone-resistant H460/MX20 lung cancer cells to the cytotoxic effects of mitoxantro...
T79353	P-gp/BCRP-IN-2
	P-gp/BCRP-IN-2 (compound 15), an oxadiazole derivative, functions as a dual inhibitor targeting both the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). Additionally, it bolsters the anti-prolifera...
T63267	P-gp/BCRP-IN-1
	P-gp/BCRP-IN-1 (compound 19) is a relatively safe, orally active, and efficient inhibitor of the efflux transporters P-gp and BCRP. By inhibiting their efflux function, it reverses resistance and enhances the oral bioava...
TQ0186	Ko 143		BCRP , ABC
	Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP).		BCRP , ABC
T3581	KS176		Potassium Channel , BCRP
	KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter, showing no inhibitory activity against P-gp or MRP1.		Potassium Channel , BCRP
T4595	YHO-13177	YHO 13177,YHO13177	BCRP
	YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.		BCRP
T38400	Triclabendazole sulfoxide	TCBZ-SO	BCRP , Parasite
	Triclabendazole sulfoxide (TCBZ-SO) is a main plasma metabolite of Triclabendazole. Triclabendazole sulfoxide inhibits membrane transporter ABCG2/BCRP and exhibits anti-parasite effects.		BCRP , Parasite
T8596	Ceefourin 1		MRP
	Ceefourin 1 is a highly selective multidrug resistance protein 4 (MRP4) inhibitor.		MRP
T4337	PCI 29732	PCI29732,PCI-29732	Others , BCRP , BTK
	PCI 29732 is a selective and irreversible Btk inhibitor with IC50 of 8.2 nM in a FRET based biochemical enzymology assay.		Others , BCRP , BTK
T13383	Zamicastat	BIA 5-1058	BCRP , Hydroxylase , P-gp
	Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH), and is also a concentration-dependent dual inhibitor of P-gp and BCRP(IC50 values of 73.8 μM and 17.0 μM, respectively).		BCRP , Hydroxylase , P-gp
T2657	Elacridar	GW0918,GW120918,GF120918,GG918	BCRP , P-gp
	Elacridar (GG918) (GF120918) is an effective BCRP and P-gp (MDR-1) inhibitor.		BCRP , P-gp
T13365	YHO-13351 free base		BCRP
	YHO-13351 free base is the water-soluble prodrug of YHO-13177 which is an inhibitor of BCRP .		BCRP
T19649	PF-06273340	PF 6273340,PF 06273340,PF6273340,PF-6273340	Trk receptor
	PF-06273340 is an effective, Selective, and Peripherally Restricted Pan-Trk inhibitor (IC50: Trk-A = 6 nM; Trk-B = 4 nM; Trk-C = 3 nM). PF-06273340 has low metabolic turnover in HLM and hHep is a good substrate for efflu...		Trk receptor
T67821	GS-9191 PM		BCRP , Antiviral
	GS-9191 PM is a novel antitumorviral compound, a bis-amide prodrug of the nucleotide analog 9-(2-phosphonomethoxyethyl)-N6-cyclopropyl-2,6-diaminopurine (cPrPMEDAP).GS-9191 PM is a potent inhibitor of MDR1 and BCRP.GS-91...		BCRP , Antiviral
T16113	ML753286		AMPK
	ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions. ML753286 is an orally active and selective inhibitor of BCRP (IC50: 0.6 μM). It is also stable in plasma across species.		AMPK
T10490	(S)-ML753286		Others
	(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor (IC50: 0.6 μM on BCRP efflux transporter).		Others
T22680	CP-100356 hydrochloride	CP-100356 HCl,CP 100356 hydrochloride	BCRP
	CP-100356 hydrochloride is an orally active and low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue with inhibitory effects on MDR1-mediated Calcein-AM transporter and BCRP-medi...		BCRP
T11268	FD 12-9	Ac12Az9	Others
	FD 12-9, Anti-glioblastoma activity. is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively.		Others
T14340	Atiratecan	TP300	Others
	Atiratecan (TP300) is a prodrug of camptothecin analog CH0793076. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models[1]. A...		Others
T69897	MC-70 hydrochloride
	MC-70 hydrochloride is a potent P-gp inhibitor with good selectivity towards BCRP pump (EC50 values 0.05 μM, 0.69 μM, 9.3 μM, and 73 μM for Caco-2, MDR1, MRP1, and BCRP inhibition, respectively).
T13366	YHO-13351		Epigenetic Reader Domain
	YHO-13351 is the water-soluble prodrug of YHO-13177, which is a potent and specific BCRP inhibitor.		Epigenetic Reader Domain
T73356	Ac32Az19
	Ac32Az19 is a potent, non-toxic, and highly selective inhibitor of Breast Cancer Resistance Protein (BCRP), demonstrating an EC50 of 13 nM in BCRP-overexpressed HEK293/R2 cells.
T73369	UR-MB108
	UR-MB108 is a potent and selective inhibitor of ABCG2 (BCRP), displaying an IC50 value of 79 nM, and exhibits stability in blood plasma.
T72521	Efflux inhibitor-1
	Efflux inhibitor-1 is a pyrazolopyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC 50 s of 0.45 μM and 2.17 μM, respectively .
T1405L	Cefditoren sodium	Cefditoren pivoxil,Cefditoren,ME-1206,ME1206,ME 1206
	Cefditoren sodium is a cephalosporin antibiotic potentially for the treatment of bacterial infection. The expression levels of Mrp2, Bcrp, Oat2 mRNA were markedly increased, while P-gp and Oct1 mRNA were decreased. In co...
T14945	CH-0793076	TP3076	Topoisomerase
	CH-0793076, a hexacyclic camptothecin analog, is an active drug and major metabolite of TP300. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein). CH-0793076 inhibits DNA topoisome...		Topoisomerase
T73672	CH-0793076 TFA
	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 IC 50 of 2.3 μM. CH-0793076 TFA is efficacious against cells ex...
T72861	(6R)-ML753286
	'(6R)-ML753286, an isomer of ML753286, is an orally active, selective Breast Cancer Resistance Protein (BCRP) inhibitor, demonstrating an IC50 of 0.6 μM. It exhibits high permeability and low to medium clearance in roden...

Compounds

33-BCRP Inhibitor

T83892

Synonym: 33-Breast Cancer Resistance Protein Inhibitor

Target: Potassium Channel, BCRP

YHO-13177

T4595

Synonym: YHO 13177,YHO13177

Target: BCRP

Triclabendazole sulfoxide

T38400

Synonym: TCBZ-SO

Target: BCRP, Parasite

Synonym: PCI29732,PCI-29732

Target: Others, BCRP, BTK

Zamicastat

T13383

Synonym: BIA 5-1058

Target: BCRP, Hydroxylase, P-gp

Elacridar

T2657

Synonym: GW0918,GW120918,GF120918,GG918

Synonym: PF 6273340,PF 06273340,PF6273340,PF-6273340

Target: BCRP, Antiviral

CP-100356 hydrochloride

T22680

Synonym: CP-100356 HCl,CP 100356 hydrochloride

Target: Epigenetic Reader Domain

Synonym: Cefditoren pivoxil,Cefditoren,ME-1206,ME1206,ME 1206

Target: Topoisomerase

Cat No.	Product Name	Synonyms	Targets
T5778	5,7-DIMETHOXYFLAVONE		Anti-infection , P450
	5,7-DIMETHOXYFLAVONE possessed remarkable leishmanicidal potential.		Anti-infection , P450
T15355	Fumitremorgin C	12α-Fumitremorgin C	BCRP , Antibacterial , Antibiotic , ABC
	Fumitremorgin C (12α-Fumitremorgin C) is a mycotoxin and inhibits ABCG2/BRCP.		BCRP , Antibacterial , Antibiotic , ABC
TN3150	6,8-Diprenylnaringenin	Senegalensin,Lonchocarpol A	BCRP , ABC
	6,8-Diprenylnaringenin (Senegalensin) is a natural product from hop Humulus lupulus. 6,8-Diprenylnaringenin is a breast cancer resistance protein(BCRP) inhibitor with some estrogenicity.		BCRP , ABC

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