Ko 143
- Product Name
- Ko 143
- CAS No.
- 461054-93-3
- Chemical Name
- Ko 143
- Synonyms
- Ko 143;12aS)-;4-dioxo-;6]pyrido[3;Ko143 ,99%;Pyrazino[1';Ko143 hydrate;KO 143;KO-143;KO143;4-b]indole-3-propanoicacid;12a-octahydro-9-Methoxy-6-(2-Methylpropyl)-1
- CBNumber
- CB81562442
- Molecular Formula
- C26H35N3O5
- Formula Weight
- 469.57
- MOL File
- 461054-93-3.mol
Ko 143 Property
- Melting point:
- 147 ºC
- Boiling point:
- 689.8±55.0 °C(Predicted)
- Density
- 1.24
- storage temp.
- Desiccate at -20°C
- solubility
- DMSO: >10mg/mL
- form
- powder
- pka
- 13.31±0.60(Predicted)
- color
- white to off-white
- Stability:
- Stable for 2 years from date of purchase as supplied. Protect from exposure to moisture. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- K2144
- Product name
- Ko143 hydrate
- Purity
- ≥98% (HPLC)
- Packaging
- 1mg
- Price
- $125
- Updated
- 2024/03/01
- Product number
- K2144
- Product name
- Ko143 hydrate
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $497
- Updated
- 2024/03/01
- Product number
- 15215
- Product name
- Ko 143
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $120
- Updated
- 2024/03/01
- Product number
- 15215
- Product name
- Ko 143
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $216
- Updated
- 2024/03/01
- Product number
- 15215
- Product name
- Ko 143
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $448
- Updated
- 2024/03/01
Ko 143 Chemical Properties,Usage,Production
Description
Breast cancer resistance protein (BCRP) is an ATP-
Uses
A potent BCRP (breast cancer resistance protein) inhibitor
Uses
Ko143 hydrate has been used:
- to determine the role of ATP-binding cassette sub-family G member 2 (ABCG2), human embryonic kidney (HEK)-C1 and HEK-ABCG2 in tumor microenvironment
- to inhibit ABCG2 for sphere formation assay
- in calcein-AM efflux inhibition to monitor multidrug resistance protein (MRP)-function in kidney
- for cell viability assay
Definition
ChEBI: LSM-6260 is a member of beta-carbolines and a tert-butyl ester.
Biological Activity
Potent and selective breast cancer resistance protein multidrug transporter (BCRP) inhibitor (EC 90 = 26 nM). Displays > 200-fold selectivity over P-gp and MRP-1 transporters. Increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance.
Biochem/physiol Actions
Ko143 has been used as a positive control inhibitor on functions of breast cancer resistance protein (BCRP) using a BCRP prototypical substrate mitoxantrone. BCRP, an ABCG2 transporter, plays an important role in disposition of many drugs and environmental toxins. Ko143 displays > 200-fold selectivity over P-gp and MRP-1 transporters and thus is more specific than other known BCRP inhibitors such as fumitremorgin C and GF120918. It increases intracellular drug accumulation and reverses BCRP-mediated multidrug resistance. It blocks topotecan and ABZSO transport in a concentration-dependent manner.
storage
Store at -20°C
References
1) Allen et al. (2002), Potent and specific inhibition of breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C; Mol. Cancer Ther., 1 417 2) Weidner et al. (2015), The Inhibitor Ko143 Is Not Specific for ABCG2; J. Pharmacol. Exp. Ther., 354 384 3) Palasuberniam et al. (2015), ABCG2 transporter inhibitor restores the sensitivity of triple negative breast cancer cells to aminolevulinic acid-mediated photodynamic therapy; Sci. Rep., 5 13298 4) Moreno-Sanz et al. (2011), The ABC membrane transporter ABCG2 prevents access of FAAH inhibitor URB937 to the central nervous system; Pharmacol. Res., 64 359 5) Sabnis et al. (2017),?The Efflux Transporter ABCG2 Maintains Prostate Stem Cells;? Mol. Cancer Res., 15 128
Ko 143 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Ko 143 manufacturers
- Product
- Ko 143 461054-93-3
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- Min98% HPLC
- Supply Ability
- g/kg/ton
- Release date
- 2020-01-01