Ko143

BML-EI396

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BCRP inhibitor

Analog of the fungal toxin fumitremorgin C (Prod. No. ALX-350-127). Potent and selective inhibitor of the breast cancer resistance protein multidrug transporter (BCRP, EC₉₀=26nM). Highly effective for increasing the intracellular drug accumulation and reversing BCRP-mediated multidrug resistance yet has little activity against P-glycoprotein, multidrug resistance-associated protein (MRP1) and other known drug transporters. In mouse models Ko143 was able to restore the intracellular accumulation and abolish the directionality in net flux of dasatinib. It is a highly useful tool for the identification of drug transport processes in complex experimental systems.

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Product Details

Alternative Name	(3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino-[1′,2′:1,6]pyrido[3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester
Appearance	White solid.
CAS	461054-93-3
Couple Target	BCRP
Couple Type	Inhibitor
Formula	C₂₆H₃₅N₃O₅
MW	469.6
Purity	≥96% (HPLC)
Solubility	Soluble in DMSO (>25mg/ml) or 100% ethanol (>25mg/ml).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Store solutions at -20°C for up to 3 months.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

ABCB1 as a potential beneficial target of midostaurin in acute myeloid leukemia: S. Sucha, et al.; Biomed. Pharmacother. 150, 112962 (2022), Abstract
Folium Sennae Increased the Bioavailability of Methotrexate through Modulation on MRP 2 and BCRP: C.P. Yu, et al.; Pharmaceuticals 14, 1036 (2021), Abstract
Apoptosis Induced by the Curcumin Analogue EF-24 Is Neither Mediated by Oxidative Stress-Related Mechanisms nor Affected by Expression of Main Drug Transporters ABCB1 and ABCG2 in Human Leukemia Cells: Skoupa, N., Dolezel, P., et al.; Int. J. Mol. Sci. 18, (2017), Abstract
Increased Systemic Exposure of Methotrexate by a Polyphenol-Rich Herb via Modulation on Efflux Transporters Multidrug Resistance-Associated Protein 2 and Breast Cancer Resistance Protein: C.P. Yu, et al.; J. Pharm. Sci. 105, 343 (2016), Application(s): Positive inhibitor of BCRP, Abstract
Influence of drug transporters and stereoselectivity on the brain penetration of pioglitazone as a potential medicine against Alzheimer’s disease: K.L. Chang, et al.; Sci. Rep. 5, 9000 (2015), Application(s): Cell Culture, Abstract — Full Text
Dinaciclib, a cyclin-dependent kinase inhibitor, is a substrate of human ABCB1 and ABCG2 and an inhibitor of human ABCC1 in vitro: D. Cihalova, et al.; Biochem. Pharmacol. 98, 465 (2015), Application(s): MDCKII monolayer transport assay, Abstract
ABC transporter activity linked to radiation resistance and molecular subtype in pediatric medulloblastoma: W.J. Ingram, et al.; Exp. Hematol. Oncol. 2, 26 (2013), Abstract — Full Text
P-glycoprotein and breast cancer resistance protein influence brain distribution of dasatinib: Y. Chen, et al.; J. Pharmacol. Exp. Ther. 330, 956 (2009), Abstract
Identification of novel specific and general inhibitors of the three major human ATP-binding cassette transporters P-gp, BCRP and MRP2 among registered drugs: P. Matsson, et al.; Pharm. Res. 26, 1816 (2009), Abstract
Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C: J.D. Allen, et al.; Mol. Cancer Ther. 1, 417 (2002), Abstract

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Ko143

BML-EI396

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