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Merck

197227

BCRP Inhibitor III, YHO-13177

The BCRP Inhibitor III, YHO-13177 controls the biological activity of BCRP.

Synonym(s):

BCRP Inhibitor III, YHO-13177, ( Z)-2-(3,4-Dimethoxyphenyl)-3-(5-(4-hydroxypiperidin-1-yl)thiophen-2-yl)acrylonitrile, (Z)-2-(3,4-Dimethoxyphenyl)-3-(5-(4-hydroxypiperidin-1-yl)thiophen-2-yl)acrylonitrile

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About This Item

Empirical Formula (Hill Notation):
C20H22N2O3S
CAS Number:
912287-56-0
Molecular Weight:
370.47
UNSPSC Code:
12352200
MDL number:
MFCD28900680

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Product Name

BCRP Inhibitor III, YHO-13177, The BCRP Inhibitor III, YHO-13177 controls the biological activity of BCRP.

SMILES string

OC(CC1)CCN1C(S2)=CC=C2/C=C(C#N)/C3=CC(OC)=C(OC)C=C3

assay

≥98% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange

solubility

DMSO: 100 mg/mL

shipped in

wet ice

storage temp.

2-8°C

Quality Level

100

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable acrylonitrile compound that potently inhibits breast cancer resistance protein (BCRP/ABCG2)-mediated drug export and reverses BCRP-mediated drug resistance in vitro (half maximal in the range 0.01 - 1 µM) without altering the BCRP expression levels (in ≤ 6 hrs.). Shown to selectively enable the intracellular accumulation of anticancer drugs and potentiate the cytotoxicity of BCRP-expressing carcinoma cells with no effect either on the P-glycoprotein/ABCB1- and MDRP1-mediated export or on the drug sensitivity of parental cells (IC50 >10 µM in A549 cells). An in vivo bioavailable and readily water soluble prodrug of YHO-13177, BCRP Inhibitor IV, YHO-13351 is also available (Cat. No. 197228).

Other Notes

Yamazaki, R., et al. 2011. Mol. Cancer Ther.10, 1252.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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