Ko 143

Name: Ko 143
Brand: MedChemExpress
SKU: HY-10010
Rating: 5.0 (39 reviews)

Cat. No.: HY-10010 Purity: 99.97%: FAQs
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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.

For research use only. We do not sell to patients.

Ko 143 Chemical Structure

CAS No. : 461054-93-3

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
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10 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 39 publication(s) in Google Scholar

36 Publications Citing Use of MCE Ko 143

Proliferation Assay

: Ko 143 purchased from MedChemExpress. Usage Cited in: Drug Deliv. 2017 Nov;24(1):1453-1459. [Abstract]; Fluorescent substrates accumulate in the organoids. The organoids are incubated in Hoechst 33342 with or without YHO-13177 or Ko143 for 20, 60 and 100 minutes, respectively. Ko143 and YHO-13177 notably decrease the fluorescence intensity of Hoechst 33342 in the organoids.

: Ko 143 purchased from MedChemExpress. Usage Cited in: J Drug Target. 2016;24(5):441-9. [Abstract]; Cells are co-treated with 5 μM of free LY156758 or an equivalent dose of SMA-LY156758 and either vehicle control (0.01% DMSO), Elacridar (1 μM), KO143 (5 μM), Valspodar (1 μM) or a combination of efflux inhibitors for 6 h.

: Ko 143 purchased from MedChemExpress. Usage Cited in: J Pharm Biomed Anal. 2012 Jul;66:232-9. [Abstract]; Effect of pharmacological inhibition of drug efflux transporters on brain distribution of FLZ in rats. The rats receive 35 mg/kg FLZ via tail vein injection 10 min after intravenous administration of 20 mg/kg Zosuquidar or 7.5 mg/kg ko143.

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Description

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^[1]^[2].

IC₅₀ & Target

EC90: 26 nM (BCRP)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	122.83 nM Compound: Ko143	Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 1625.4 +/-413.42 nM) Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 1625.4 +/-413.42 nM)	[PMID: 34496204]
A549	IC₅₀	127.7 nM Compound: Ko143	Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 1162.92 +/-250.73 nM) Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 1162.92 +/-250.73 nM)	[PMID: 34496204]
A549	IC₅₀	236.09 nM Compound: Ko143	Chemo-sensitizing activity against human A549 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 376.13 +/-60.17 nM) Chemo-sensitizing activity against human A549 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 376.13 +/-60.17 nM)	[PMID: 34496204]
A549	IC₅₀	326.96 nM Compound: Ko143	Chemo-sensitizing activity against human A549 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb =555.44 +/-125.7 nM) Chemo-sensitizing activity against human A549 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb =555.44 +/-125.7 nM)	[PMID: 34496204]
A549	IC₅₀	37.17 nM Compound: Ko143	Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 552.97 +/-106.74 nM) Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 552.97 +/-106.74 nM)	[PMID: 34496204]
A549	IC₅₀	41.83 nM Compound: Ko143	Chemo-sensitizing activity against human A549 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 82.47 +/-24.25 nM) Chemo-sensitizing activity against human A549 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 82.47 +/-24.25 nM)	[PMID: 34496204]
Caco-2	IC₅₀	> 30 μM Compound: Ko143	Inhibition of P-gp transporter in human Caco2 cells using [3H]-digoxin as substrate measured at 30 to 120 mins by microplate scintillation and luminescence counting analysis Inhibition of P-gp transporter in human Caco2 cells using [3H]-digoxin as substrate measured at 30 to 120 mins by microplate scintillation and luminescence counting analysis	[PMID: 26642765]
HEK293	EC₅₀	0.012 μM Compound: Ko143	Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux at 5 uM after 30 mins in presence of 0.1 uM (2E,2'E)-1,1'-(1,4-Phenylene)bis(3-(2,6-dimethoxyphenyl)-prop-2-en-1-one) by flow cytometry Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux at 5 uM after 30 mins in presence of 0.1 uM (2E,2'E)-1,1'-(1,4-Phenylene)bis(3-(2,6-dimethoxyphenyl)-prop-2-en-1-one) by flow cytometry	[PMID: 24611893]
HEK293	EC₅₀	0.029 μM Compound: Ko143	Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux after 30 mins by flow cytometry relative to control Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux after 30 mins by flow cytometry relative to control	[PMID: 24611893]
HEK293	IC₅₀	0.05 μM Compound: Ko143	Inhibition of ABCG2-mediated mitoxantrone efflux in HEK293 cells by flow cytometry Inhibition of ABCG2-mediated mitoxantrone efflux in HEK293 cells by flow cytometry	[PMID: 22165858]
HEK293	EC₅₀	0.074 μM Compound: Ko143	Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by flow cytometric analysis Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by flow cytometric analysis	[PMID: 27376492]
HEK293	IC₅₀	0.09 μM Compound: Ko143	Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by FACS method Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by FACS method	[PMID: 25272055]
HEK293	EC₅₀	0.09 μM Compound: Ko143	Inhibition of ABCG2 (unknown origin)-mediated mitoxantrone efflux expressed in HEK293 cells after 30 mins by flow cytometric analysis Inhibition of ABCG2 (unknown origin)-mediated mitoxantrone efflux expressed in HEK293 cells after 30 mins by flow cytometric analysis	[PMID: 24304387]
HEK293	IC₅₀	2.53 nM Compound: Ko143	Chemo-sensitizing activity against human HEK293 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 2.74 +/-0.69 nM) Chemo-sensitizing activity against human HEK293 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 2.74 +/-0.69 nM)	[PMID: 34496204]
HEK293	IC₅₀	2.69 nM Compound: Ko143	Chemo-sensitizing activity against human HEK293 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 2.78 +/-0.58 nM) Chemo-sensitizing activity against human HEK293 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 2.78 +/-0.58 nM)	[PMID: 34496204]
HEK293	IC₅₀	38.59 nM Compound: Ko143	Chemo-sensitizing activity against human HEK293 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 35.17 +/-8.65 nM) Chemo-sensitizing activity against human HEK293 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 35.17 +/-8.65 nM)	[PMID: 34496204]
HEK293	IC₅₀	8.36 nM Compound: Ko143	Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 99.55 +/-7.35 nM) Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 99.55 +/-7.35 nM)	[PMID: 34496204]
HEK293	IC₅₀	9.94 nM Compound: Ko143	Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 239.91 +/-25 nM) Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 239.91 +/-25 nM)	[PMID: 34496204]
HEK293	IC₅₀	96.43 nM Compound: Ko143	Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 558.68 +/-81.31 nM) Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 558.68 +/-81.31 nM)	[PMID: 34496204]
K562	IC₅₀	71.53 μM Compound: Ko143	Cytotoxicity against human K562 cells incubated for 48 hrs by MTT assay Cytotoxicity against human K562 cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
K562/A02	IC₅₀	58.74 μM Compound: Ko143	Cytotoxicity against P-gp overexpressing human K562/A02 cells incubated for 48 hrs by MTT assay Cytotoxicity against P-gp overexpressing human K562/A02 cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
MCF7	IC₅₀	0.23 μM Compound: Ko143	Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining	[PMID: 19932960]
MCF7	IC₅₀	0.39 μM Compound: Ko143	Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining	[PMID: 21354800]
MDCK	IC₅₀	> 50000 nM Compound: 2, Ko143	Inhibition of ABCC2 overexpressed in MDCK cells at 100 uM by flow cytometric-based chloromethylfluorescein-diacetate accumulation assay Inhibition of ABCC2 overexpressed in MDCK cells at 100 uM by flow cytometric-based chloromethylfluorescein-diacetate accumulation assay	[PMID: 19170519]
MDCK	IC₅₀	0.074 μM Compound: Ko143	Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay	[PMID: 19932960]
MDCK	IC₅₀	0.21 μM Compound: Ko143	Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining	[PMID: 21354800]
MDCK	IC₅₀	93.27 μM Compound: Ko143	Cytotoxicity against dog MDCK cells after 48 hrs by MTT assay Cytotoxicity against dog MDCK cells after 48 hrs by MTT assay	[PMID: 35247755]
MDCK-II	IC₅₀	0.128 μM Compound: Ko143	Inhibition of GFP-tagged human BCRP expressed in MDCK2 cells pre-incubated for 30 mins followed by Hoechst 33342 addition and further incubated for 120 mins by Hoechst 33342 accumulation assay Inhibition of GFP-tagged human BCRP expressed in MDCK2 cells pre-incubated for 30 mins followed by Hoechst 33342 addition and further incubated for 120 mins by Hoechst 33342 accumulation assay	[PMID: 25855895]
MDCK-II	IC₅₀	0.215 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay	[PMID: 23851114]
MDCK-II	IC₅₀	0.221 μM Compound: Ko143	Inhibition of recombinant human GFP-fused ABCG2 expressed in MDCK2 cells assessed as reduction in Hoechst 33342 efflux preincubated for 30 mins followed by Hoechst 33342 addition measured immediately at 60 sec time interval for 120 mins by fluorescence as Inhibition of recombinant human GFP-fused ABCG2 expressed in MDCK2 cells assessed as reduction in Hoechst 33342 efflux preincubated for 30 mins followed by Hoechst 33342 addition measured immediately at 60 sec time interval for 120 mins by fluorescence as	[PMID: 27676469]
MDCK-II	IC₅₀	0.24 μM Compound: Ko143	Inhibition of human C-terminal GFP-tagged ABCG2 expressed in MDCK2 cells using pheophorbide A as substrate preincubated for 20 mins followed by substrate addition measured after 120 mins by flow cytometry Inhibition of human C-terminal GFP-tagged ABCG2 expressed in MDCK2 cells using pheophorbide A as substrate preincubated for 20 mins followed by substrate addition measured after 120 mins by flow cytometry	[PMID: 27100033]
MDCK-II	IC₅₀	0.25 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation treated 30 mins before Hoechst 33342 addition measured up to 120 mins by fluorescence assay Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation treated 30 mins before Hoechst 33342 addition measured up to 120 mins by fluorescence assay	[PMID: 24184213]
MDCK-II	IC₅₀	0.25 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells preincubated for 30 mins prior to Hoechst 33342 addition measured every 60 secs up to 120 mins by Hoechst 33342 accumulation assay Inhibition of human BCRP expressed in MDCK2 cells preincubated for 30 mins prior to Hoechst 33342 addition measured every 60 secs up to 120 mins by Hoechst 33342 accumulation assay	[PMID: 23017888]
MDCK-II	IC₅₀	0.26 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation preincubated for 30 mins by fluorimetry Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation preincubated for 30 mins by fluorimetry	[PMID: 22112540]
MDCK-II	IC₅₀	0.276 μM Compound: Ko143	Inhibition of recombinant human GFP-fused ABCG2 expressed in MDCK2 cells assessed as reduction in pheophorbide A efflux preincubated for 30 mins followed by pheophorbide A addition measured after 2 hrs by flow cytometry Inhibition of recombinant human GFP-fused ABCG2 expressed in MDCK2 cells assessed as reduction in pheophorbide A efflux preincubated for 30 mins followed by pheophorbide A addition measured after 2 hrs by flow cytometry	[PMID: 27676469]
MDCK-II	IC₅₀	0.33 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells assessed as pheophorbide A accumulation treated 30 mins before pheophorbide A addition measured up to 120 mins by flow cytometry Inhibition of human BCRP expressed in MDCK2 cells assessed as pheophorbide A accumulation treated 30 mins before pheophorbide A addition measured up to 120 mins by flow cytometry	[PMID: 24184213]
MDCK-II	IC₅₀	0.354 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry	[PMID: 23851114]
MDCK-II	GI₅₀	10.9 μM Compound: Ko143	Cytotoxicity against wild-type MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against wild-type MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27280693]
MDCK-II	GI₅₀	10.9 μM Compound: Ko143	Intrinsic cytotoxicity against parental MDCK2 cells incubated for 72 hrs by MTT assay Intrinsic cytotoxicity against parental MDCK2 cells incubated for 72 hrs by MTT assay	[PMID: 27148793]
MDCK-II	GI₅₀	10.9 μM Compound: Ko143	Cytotoxicity against MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
MDCK-II	GI₅₀	11.1 μM Compound: Ko143	Cytotoxicity against MDCK2 cells expressing human ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells expressing human ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27280693]
MDCK-II	GI₅₀	11.1 μM Compound: Ko143	Intrinsic cytotoxicity against MDCK2 cells over-expressing human ABCG2 incubated for 72 hrs by MTT assay Intrinsic cytotoxicity against MDCK2 cells over-expressing human ABCG2 incubated for 72 hrs by MTT assay	[PMID: 27148793]
MDCK-II	GI₅₀	11.1 μM Compound: Ko143	Cytotoxicity against MDCK2 cells expressing human C-terminal GFP-tagged ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells expressing human C-terminal GFP-tagged ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
MDCK-II	GI₅₀	12.5 μM Compound: Ko143	Growth inhibition of MDCK2 cells after 72 hrs by MTT assay Growth inhibition of MDCK2 cells after 72 hrs by MTT assay	[PMID: 30390439]
MDCK-II	GI₅₀	12.5 μM Compound: 59; Ko143	Intrinsic cytotoxicity in parental MDCK2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Intrinsic cytotoxicity in parental MDCK2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 30075623]
MDCK-II	GI₅₀	12.5 μM Compound: Ko143	Cytotoxicity against MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 28841513]
MDCK-II	GI₅₀	12.5 μM Compound: 55; Ko143	Cytotoxicity against MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 28471656]
MDCK-II	GI₅₀	12.6 μM Compound: Ko143	Growth inhibition of MDCK2 cells harboring GFP-fused human ABCG2 after 72 hrs by MTT assay Growth inhibition of MDCK2 cells harboring GFP-fused human ABCG2 after 72 hrs by MTT assay	[PMID: 30390439]
MDCK-II	GI₅₀	12.6 μM Compound: 59; Ko143	Intrinsic cytotoxicity in MDCK2 cells overexpressing BCRP assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Intrinsic cytotoxicity in MDCK2 cells overexpressing BCRP assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 30075623]
MDCK-II	GI₅₀	12.6 μM Compound: Ko143	Cytotoxicity against MDCK2 cells harboring human ABCG2 assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells harboring human ABCG2 assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 28841513]
MDCK-II	GI₅₀	12.6 μM Compound: 55; Ko143	Cytotoxicity against ABCG2 over-expressing MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against ABCG2 over-expressing MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 28471656]
MDCK-II	GI₅₀	13 μM Compound: 56; Ko143	Cytotoxicity against MDCK2 cells expressing human BCRP assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells expressing human BCRP assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 29547272]
MDCK-II	GI₅₀	13 μM Compound: 56; Ko143	Cytotoxicity against MDCK2 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 29547272]
MDCK-II	IC₅₀	58.26 μM Compound: Ko143	Cytotoxicity against BCRP-overexpressing MDCK-II cells incubated for 48 hrs by MTT assay Cytotoxicity against BCRP-overexpressing MDCK-II cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
MDCK-II	IC₅₀	87.19 μM Compound: Ko143	Cytotoxicity against MDCK-II cells incubated for 48 hrs by MTT assay Cytotoxicity against MDCK-II cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
NCI-H460	IC₅₀	0.21 μM Compound: Ko143	Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 4.33 +/-1.18 microM) Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 4.33 +/-1.18 microM)	[PMID: 34496204]
NCI-H460	IC₅₀	102.95 nM Compound: Ko143	Chemo-sensitizing activity against human NCI-H460 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 279.69 +/-31.94 nM) Chemo-sensitizing activity against human NCI-H460 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 279.69 +/-31.94 nM)	[PMID: 34496204]
NCI-H460	IC₅₀	12.27 nM Compound: Ko143	Chemo-sensitizing activity against human NCI-H460 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 20.7 +/-6.32 nM) Chemo-sensitizing activity against human NCI-H460 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 20.7 +/-6.32 nM)	[PMID: 34496204]
NCI-H460	IC₅₀	144.61 nM Compound: Ko143	Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 3262.6 +/-811.81 nM) Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 3262.6 +/-811.81 nM)	[PMID: 34496204]
NCI-H460	IC₅₀	42.61 nM Compound: Ko143	Chemo-sensitizing activity against human NCI-H460 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 128.27 +/-22.6 nM) Chemo-sensitizing activity against human NCI-H460 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 128.27 +/-22.6 nM)	[PMID: 34496204]
NCI-H460	IC₅₀	53.43 nM Compound: Ko143	Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 963.32 +/-120.89 nM) Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 963.32 +/-120.89 nM)	[PMID: 34496204]
Sf9	IC₅₀	0.004 μM Compound: Ko143	Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive basal ATPase activity after 20 mins by colorimetric method Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive basal ATPase activity after 20 mins by colorimetric method	[PMID: 27280693]
Sf9	IC₅₀	0.028 μM Compound: Ko143	Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive quercetin-stimulated ATPase activity after 20 mins by colorimetric method Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive quercetin-stimulated ATPase activity after 20 mins by colorimetric method	[PMID: 27280693]
Sf9	IC₅₀	0.17 μM Compound: Ko143	Inhibition of human ABCG2 expressed in Sf9 insect cell membranes assessed as inhibition of quercetin-stimulated ATPase activity after 30 mins by colorimetric analysis in presence of sodium orthovanadate Inhibition of human ABCG2 expressed in Sf9 insect cell membranes assessed as inhibition of quercetin-stimulated ATPase activity after 30 mins by colorimetric analysis in presence of sodium orthovanadate	[PMID: 24304387]

In Vitro

Ko143 (10 nM) significantly decreases (2.5-fold) the IC₅₀ of MTX for HEK G2 cells and mouse G2 cells. Ko143 (1-100 μM) metabolite does not inhibit the function of ABC Transporters^[1].
Reversal of drug resistance in SKF 104864A-selected mouse MEF3.8/T6400 cells and human IGROV1/T8 cells by FTC analogue Ko143. Ko143 is applied at zero, one, or eight times the EC₉₀ concentration of 25 nM^[2].
Ko143 inhibits BCRP-mediated transport of ZD 4522 in Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC (wild type) cells and MDCK2-BCRP421AA (mutant type) cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ko143 (10 mg/kg, p.o.) increases the oral availability of SKF 104864A in mice^[2].
Ko143 significantly affects the pharmacokinetics of ZD 4522 in rats^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

469.57

Formula

C₂₆H₃₅N₃O₅

CAS No.

461054-93-3

Appearance

Solid

Color

White to off-white

SMILES

O=C1N2[C@]([H])(C3=C(C[C@]2(C(N[C@H]1CCC(OC(C)(C)C)=O)=O)[H])C4=CC=C(OC)C=C4N3)CC(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (212.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1296 mL	10.6480 mL	21.2961 mL
5 mM	0.4259 mL	2.1296 mL	4.2592 mL
10 mM	0.2130 mL	1.0648 mL	2.1296 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.32 mM); Suspended solution; Need ultrasonic and warming and heat to 50°C

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.32 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (5.32 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.97%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (249 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Weidner LD, et al. The Inhibitor Ko143 Is Not Specific for ABCG2. J Pharmacol Exp Ther. 2015 Sep;354(3):384-93. [Content Brief]

[2]. JD Allen et al. 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. Mol. Cancer Ther. 2002, 1, 417-425. [Content Brief]

[3]. Wen JH, et al. Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of ZD 4522 In Vivo and Vitro. Chin Med Sci J. 2015 Dec;30(4):218-25. [Content Brief]

[4]. Hou J, et al. Quantitative determination and pharmacokinetic study of the novel anti-Parkinson's disease candidate drug FLZ in rat brain by high performance liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2012 Jul;66:232-9. [Content Brief]

[5]. Liu K, et al. Metabolism of KO143, an ABCG2 inhibitor. Drug Metab Pharmacokinet. 2017 Aug;32(4):193-200. [Content Brief]

Cell Assay ^[2]	cells are plated at 400 or 1000/well in 96-well plates the night before addition of drugs. A concentration series of drug is applied along one plate axis and left for the duration of the assay. Plates are harvested after 4-5 days while untreated wells are still subconfluent. Relative cell proliferation is quantified with CyQuant or Sybr Green I fluorescent nucleic acid stains. Assays with human cell lines are performed in the presence of 0.1 μm PSC833 to inhibit confounding P-gp activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Oral toxicity of FTC analogues in mice is tested by mixing 50 mg/mL stocks in DMSO 1:1 with Tween 80 (polyoxyethylene sorbitan mono-oleate) and diluting with 5% w/v glucose such that the final volume administered by oral gavage is 10 μL/g of body weight. Pairs of mice are administered oral doses of 50 mg/kg Ko132, Ko134, Ko143, or vehicle under light methoxyflurane anesthesia. Final tests of 50 mg/kg Ko134 or Ko143 are performed on additional pairs of unanesthetized animals to observe any behavioral effects. Further, another pair of mice receive the higher dose of 100 mg/kg Ko134. For i.p. toxicity tests, the FTC analogue stocks in DMSO are dispersed in at least 10 volumes of sterile corn oil such that the injected volume is 5 μL/g of body weight. After pilot tests at lower doses show no adverse effects, mice (4 per group) are administered vehicle or 10 mg/kg i.p. of Ko132, Ko134, or Ko143. The mice are observed continuously during the first hour after administration and then at increasing intervals for 2 weeks, after which they are sacrificed for histological examination of major organs and structures including brain, salivary glands, heart, lungs, liver, adrenal glands, kidneys, urinary tract, spleen, thymus, bone marrow, pancreas, stomach, intestines, cecum, colon, testes, epididymus, skin, head, trunk, and limbs. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Weidner LD, et al. The Inhibitor Ko143 Is Not Specific for ABCG2. J Pharmacol Exp Ther. 2015 Sep;354(3):384-93. [Content Brief] [2]. JD Allen et al. 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. Mol. Cancer Ther. 2002, 1, 417-425. [Content Brief] [3]. Wen JH, et al. Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of ZD 4522 In Vivo and Vitro. Chin Med Sci J. 2015 Dec;30(4):218-25. [Content Brief] [4]. Hou J, et al. Quantitative determination and pharmacokinetic study of the novel anti-Parkinson's disease candidate drug FLZ in rat brain by high performance liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2012 Jul;66:232-9. [Content Brief] [5]. Liu K, et al. Metabolism of KO143, an ABCG2 inhibitor. Drug Metab Pharmacokinet. 2017 Aug;32(4):193-200. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1296 mL	10.6480 mL	21.2961 mL	53.2402 mL
	5 mM	0.4259 mL	2.1296 mL	4.2592 mL	10.6480 mL
	10 mM	0.2130 mL	1.0648 mL	2.1296 mL	5.3240 mL
	15 mM	0.1420 mL	0.7099 mL	1.4197 mL	3.5493 mL
	20 mM	0.1065 mL	0.5324 mL	1.0648 mL	2.6620 mL
	25 mM	0.0852 mL	0.4259 mL	0.8518 mL	2.1296 mL
	30 mM	0.0710 mL	0.3549 mL	0.7099 mL	1.7747 mL
	40 mM	0.0532 mL	0.2662 mL	0.5324 mL	1.3310 mL
	50 mM	0.0426 mL	0.2130 mL	0.4259 mL	1.0648 mL
	60 mM	0.0355 mL	0.1775 mL	0.3549 mL	0.8873 mL
	80 mM	0.0266 mL	0.1331 mL	0.2662 mL	0.6655 mL
	100 mM	0.0213 mL	0.1065 mL	0.2130 mL	0.5324 mL

Ko 143 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ko 143461054-93-3Ko143Ko-143BCRPBreast cancer resistance proteinABCG2Inhibitorinhibitorinhibit

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Ko 143

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