Protein Inhibitors - Ko 143 (CAS: 461054-93-3)

Ko 143 (CAS: 461054-93-3)

Catalog #：EBC51113

Biological Activity

Synonyms

BCRP inhibitor, Ko-143

Chemical 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

Application

Ko 143 is a selective BCRP multidrug transporter inhibitor

CAS Number

461054-93-3

Purity

≥99.0%

Molecular Weight

469.57

Molecular Formula

C₂₆H₃₅N₃O₅

SMILES

CC(C)C[C@H]1C2=C(C[C@@H]3N1C(=O)[C@@H](NC3=O)CCC(=O)OC(C)(C)C)C4=C(N2)C=C(C=C4)OC

Target & IC50

ABCG2: IC50 = 5 nM (human)
MRP1: IC50 = 2 μM (human)
MRP2: IC50 >50 μM (human)

Shipping

Gel Pack

Storage

Store at -20°C

Preparing Stock Solutions

Molecular Structure

ConcentrationSolventMass	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
50 mM	0.0426 ml	0.2130 ml	0.4259 ml

Solubility
DMSO: 48 mg/mL (100.22 mM)

Product Description
Ko 143 is a potent and selective ABCG2 (breast cancer resistance protein multidrug transporter, BCRP) inhibitor (EC90 = 26 nM). It displays > 200-fold selectivity over P-gp and MRP-1 transporters. Ko 143 also increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance.