Cat. No.: HY-10010

Ko 143

49 Cited Publications

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Based on 49 publication(s) in Google Scholar

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.

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Purity: 99.97%
CAS No.: 461054-93-3
Formula: C₂₆H₃₅N₃O₅
Molecular Weight:469.57

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

Ko 143 Chemical Structure

CAS No.: 461054-93-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (49)
Solvent & Solubility
- In Vitro
- In Vivo
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Biological Activity

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]
A549	CC₅₀	22.3 μM Compound: Ko143	Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 37482017]
B16-F10	IC₅₀	0.75 μM Compound: Ko143	Synergistic photodynamic antitumor activity against mouse B16-F10 cells assessed as inhibition of cell proliferation incubated for 48 hrs under 10 J/cm2 light irradiation at 660 nm in presence of chlorin e6 by CCK-8 assay Synergistic photodynamic antitumor activity against mouse B16-F10 cells assessed as inhibition of cell proliferation incubated for 48 hrs under 10 J/cm2 light irradiation at 660 nm in presence of chlorin e6 by CCK-8 assay	[PMID: 37690263]
B16-F10	IC₅₀	12.26 μM Compound: Ko143	Synergistic photodynamic antitumor activity against mouse B16-F10 cells assessed as inhibition of cell proliferation incubated for 48 hrs under dark condition in presence of chlorin e6 by CCK-8 assay Synergistic photodynamic antitumor activity against mouse B16-F10 cells assessed as inhibition of cell proliferation incubated for 48 hrs under dark condition in presence of chlorin e6 by CCK-8 assay	[PMID: 37690263]
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	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	0.09 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	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	0.09 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	0.074 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	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]
HepG2	IC₅₀	0.99 μM Compound: Ko143	Synergistic photodynamic antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs under 10 J/cm2 light irradiation at 660 nm in presence of chlorin e6 by CCK-8 assay Synergistic photodynamic antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs under 10 J/cm2 light irradiation at 660 nm in presence of chlorin e6 by CCK-8 assay	[PMID: 37690263]
HepG2	IC₅₀	84.76 μM Compound: Ko143	Synergistic photodynamic antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs under dark condition in presence of chlorin e6 by CCK-8 assay Synergistic photodynamic antitumor activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs under dark condition in presence of chlorin e6 by CCK-8 assay	[PMID: 37690263]
HFF-1	IC₅₀	56.5 μM Compound: Ko 143	Cytotoxicity against human HFF1 cells assessed as reduction in cell viability Cytotoxicity against human HFF1 cells assessed as reduction in cell viability	[PMID: 31465686]
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	0.26 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	0.25 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	0.215 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	0.354 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	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	0.33 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	0.128 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	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 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	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	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	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	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	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	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	0.276 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	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: 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	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	12.6 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	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	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	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	12.6 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	12.5 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	12.6 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	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]
NIH3T3	IC₅₀	>100 μM Compound: Ko 143	Cytotoxicity against mouse 3T3 cells assessed as reduction in cell viability Cytotoxicity against mouse 3T3 cells assessed as reduction in cell viability	[PMID: 31465686]
Sf9	IC₅₀	5 nM Compound: Ko143	TP_TRANSPORTER: efflux of Hoechst33342 in BCRP-expressing Sf9 cells TP_TRANSPORTER: efflux of Hoechst33342 in BCRP-expressing Sf9 cells	[PMID: 15155841]
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]
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]

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.

Chemical Information

CAS No. 461054-93-3
Appearance Solid
Molecular Weight 469.57
Formula C₂₆H₃₅N₃O₅
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

Publications (49)

All IFCell Proliferation/Viability Assay

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Journal Impact Factor

Nat Nanotechnol

Annexin A1 mRNA-loaded liposomes alleviate acute pancreatitis by suppressing STING pathway and promoting efferocytosis in macrophages. [Abstract]

2025 Aug 11. PMID: 40789923
Nat Commun

Inhibition of ABCG2 prevents phototoxicity in a mouse model of erythropoietic protoporphyria. [Abstract]

2024 Dec 4;15(1):10557. PMID: 39632884
Adv Sci (Weinh)

Fusidic Acid Reverses Chemoresistance in Breast Cancer via Targeting DDX6 to Downregulate GSK-3β/β-Catenin Signaling. [Abstract]

2025 Aug 4:e04680. PMID: 40757496
Adv Sci (Weinh)

Metabolomic and Cellular Mechanisms of Drug-Induced Ototoxicity and Nephrotoxicity: Therapeutic Implications of Uric Acid Modulation. [Abstract]

2025 Apr;12(16):e2415041. PMID: 40041973
Acta Biomater

A nanotherapeutic strategy to overcome chemoresistance to irinotecan/7-ethyl-10-hydroxy-camptothecin in colorectal cancer. [Abstract]

2022 Jan 1:137:262-275. PMID: 34718178
Proc Natl Acad Sci U S A

CDK7 inhibition suppresses aberrant hedgehog pathway and overcomes resistance to smoothened antagonists. [Abstract]

2019 Jun 25;116(26):12986-12995. PMID: 31182587
Drug Deliv

A novel biosensor based on intestinal 3D organoids for detecting the function of BCRP. [Abstract]

2017 Nov;24(1):1453-1459. PMID: 28949254

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.
Food Res Int

Hydroxypropyl-β-cyclodextrin as a co-delivery vehicle for synergistically enhancing fucoxanthin oral bioavailability through dual regulation of SR-B1 and ABCB1 transporters. [Abstract]

2026 Mar 31:228:118352. PMID: 41703824
Arch Pharm Res

Dual inhibitors of P-glycoprotein and breast cancer resistance protein for overcoming the blood-brain barrier: in silico discovery and preclinical evaluation. [Abstract]

2025 Sep 25. PMID: 40996599
Arch Toxicol

Using the lentiviral vector system to stably express chicken P-gp and BCRP in MDCK cells for screening the substrates and studying the interplay of both transporters. [Abstract]

2018 Jun;92(6):2027-2042. PMID: 29725709
Int J Nanomedicine

The Optimization Design Of Lactoferrin Loaded HupA Nanoemulsion For Targeted Drug Transport Via Intranasal Route. [Abstract]

2019 Nov 27;14:9217-9234. PMID: 31819426
Commun Chem

Exploring bat-inspired cyclic tryptophan diketopiperazines as ABCB1 Inhibitors. [Abstract]

2024 Jul 13;7(1):158. PMID: 39003409
Talanta

High-throughput BCRP inhibitors screening system based on styrene maleic acid polymer membrane protein stabilization strategy and surface plasmon resonance biosensor. [Abstract]

2024 Jul 1:274:125987. PMID: 38552478
JCI Insight

A genome-wide CRISPR/Cas9 screen in acute myeloid leukemia cells identifies regulators of TAK-243 sensitivity. [Abstract]

2021 Mar 8;6(5):e141518. PMID: 33476303
Cancer Cell Int

ABCB1 and ABCG2 restricts the efficacy of gedatolisib (PF-05212384), a PI3K inhibitor in colorectal cancer cells. [Abstract]

2021 Feb 16;21(1):108. PMID: 33593355
Eur J Med Chem

Metabolism-guided development of Ko143 analogs as ABCG2 inhibitors. [Abstract]

2023 Nov 5:259:115666. PMID: 37482017
Biochem Pharmacol

Precision-engineered reporter cell lines reveal ABCG2 regulation in live lung cancer cells. [Abstract]

2020 May;175:113865. PMID: 32142727
Pharmaceutics

Study on the Effect of Pharmaceutical Excipient PEG400 on the Pharmacokinetics of Baicalin in Cells Based on MRP2, MRP3, and BCRP Efflux Transporters. [Abstract]

2024 May 29;16(6):731. PMID: 38931853
J Ethnopharmacol

Intestinal absorption mechanism of rotundic acid: Involvement of P-gp and OATP2B1. [Abstract]

2022 May 10:289:115006. PMID: 35051604
Food Funct

Transepithelial transport mechanisms of 7,8-dihydroxyflavone, a small molecular TrkB receptor agonist, in human intestinal Caco-2 cells. [Abstract]

2019 Aug 1;10(8):5215-5227. PMID: 31384856
Crit Rev Anal Chem

A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]

2022;52(7):1557-1571. PMID: 33691566
Pharmaceuticals (Basel)

Potential Interaction of Pinocembrin with Drug Transporters and Hepatic Drug-Metabolizing Enzymes. [Abstract]

2025 Jan 1;18(1):42. PMID: 39861105
Pharmaceuticals (Basel)

NHERF1/EBP50 as a Target for Modulation of MRP Function in HepG2 Cells. [Abstract]

2021 Mar 8;14(3):239. PMID: 33800412
Pharm Res

Profiling Interactions Between Bicyclol and SLC/ABC Transporters: Advancing Clinical Safety and Efficacy in Combination Therapy. [Abstract]

2025 Oct 27. PMID: 41145746
Pharm Res

Functional Evaluation of P-gp and Bcrp at the Murine Blood-Cerebrospinal Fluid Barrier. [Abstract]

2023 Nov;40(11):2667-2675. PMID: 37704894
Poult Sci

Chicken xenobiotic receptor upregulates the BCRP/ABCG2 transporter. [Abstract]

2023 Jan;102(1):102278. PMID: 36402040
J Funct Foods

2023 Jun, 105, 105582.
Pestic Biochem Physiol

Overexpression of ATP-binding cassette transporters ABCG10, ABCH3 and ABCH4 in Aphis craccivora (Koch) facilitates its tolerance to imidacloprid. [Abstract]

2022 Aug:186:105170. PMID: 35973758
Drug Metab Dispos

Impairment of Intestinal Monocarboxylate Transporter 6 Function and Expression in Diabetic Rats Induced by Combination of High-Fat Diet and Low Dose of Streptozocin: Involvement of Butyrate-Peroxisome Proliferator-Activated Receptor- γ Activation. [Abstract]

2019 Jun;47(6):556-566. PMID: 30923035
Aquaculture

2025 Sep 17;612:743212.
J Biol Chem

p38 MAPK-dependent phosphorylation of transcription factor SOX2 promotes an adaptive response to BRAF inhibitors in melanoma cells. [Abstract]

2022 Sep;298(9):102353. PMID: 35944584
Oncol Rep

Radixin knockdown improves the accumulation and efficiency of methotrexate in tumor cells. [Abstract]

2019 Jul;42(1):283-290. PMID: 31115547
J Drug Target

Raloxifene nanomicelles reduce the growth of castrate-resistant prostate cancer. [Abstract]

2016;24(5):441-9. PMID: 26373825

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.
Chem Res Toxicol

Inhibitory Effects of Alkaloids on BCRP Implicated in Reversing Multidrug Resistance: A Case Example of Enhancing Temozolomide Cytotoxicity. [Abstract]

2025 Aug 12. PMID: 40793827
BMC Cancer

Preclinical studies of the falnidamol as a highly potent and specific active ABCB1 transporter inhibitor. [Abstract]

2025 Jan 7;25(1):24. PMID: 39773145
Front Oncol

Cryptotanshinone Inhibits ERα-Dependent and -Independent BCRP Oligomer Formation to Reverse Multidrug Resistance in Breast Cancer. [Abstract]

2021 Apr 22:11:624811. PMID: 33968724
J Pharm Biomed Anal

Transport and metabolic profiling studies of amentoflavone in Caco-2 cells by UHPLC-ESI-MS/MS and UHPLC-ESI-Q-TOF-MS/MS. [Abstract]

2020 Sep 10;189:113441. PMID: 32615340
J Pharm Biomed Anal

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. [Abstract]

2012 Jul;66:232-9. PMID: 22472186

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.
J Chromatogr B Analyt Technol Biomed Life Sci

Microdialysis combined with RRLC-MS/MS for the pharmacokinetics of two major alkaloids of Bi qi capsule and the potential roles of P-gp and BCRP on their penetration. [Abstract]

2018 Aug 15:1092:72-81. PMID: 29883892
Photodiagnosis Photodyn Ther

Efficacy of photodynamic therapy using 5-aminolevulinic acid-induced photosensitization is enhanced in pancreatic cancer cells with acquired drug resistance. [Abstract]

2024 Dec:50:104362. PMID: 39395619
Photochem Photobiol

Enhancing PDT efficacy in NMIBC: Efflux inhibitor mediated improvement of PpIX levels and efficacy of the combination of PpIX-PDT and SO-cleavable prodrugs. [Abstract]

2024 Nov-Dec;100(6):1636-1646. PMID: 38866726
Pharmacol Res Perspect

The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco-2 monolayer model by interacting with UDP-glucuronosyltransferases and efflux transport proteins. [Abstract]

2022 Feb;10(1):e00928. PMID: 35148019
Biomed Res Int

A Novel Cryptococcal Meningitis Therapy: The Combination of Amphotericin B and Posaconazole Promotes the Distribution of Amphotericin B in the Brain Tissue. [Abstract]

2020 Nov 29;2020:8878158. PMID: 33313322
Drug Metab Pharmacokinet

Black ginger extract and its active compound, 5,7-dimethoxyflavone, increase intestinal drug absorption via efflux drug transporter inhibitions. [Abstract]

2023 Jun:50:100500. PMID: 36948091
Drug Metab Pharmacokinet

Metabolism of KO143, an ABCG2 inhibitor. [Abstract]

2017 Aug;32(4):193-200. PMID: 28619281
University of Washington

2025.
Preprints

2025 Mar 17.
SSRN

2023 Jun 15.
Research Square Preprint

2020 Sep.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protocol

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.

MedChemExpress (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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

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Ko 143

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Lipid Metabolism Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Ko 143

Biological Activity

Chemical Information

Publications (49)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Ko 143

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Lipid Metabolism Compound Library

Cancer Stem Cells Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Ko 143

Biological Activity

Chemical Information

Publications (49)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Ko 143 Related Classifications

Cat. No.: HY-10010