Carnosic acid (Carnosate) | ERAP1 inhibitor, BCL9/β-catenin inhibitor

Chemical Structure : Carnosic acid

CAS No.: 3650-09-7

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Carnosic acid (Compound 3-23, Carnosate)

货号: PC-22853Not For Human Use, Lab Use Only.

Carnosic acid (Carnosate) is a highly selective inhibitor targeting the orthosteric site of ERAP1 with IC50 of 10.73 uM, inhibits oxidative stress and inflammation, suppressescell proliferation, and has antibacterial activity, also inhibits the BCL9/β-catenin interaction with Ki of 3.3 uM.

规格	价格	库存
25 mg	￥880	In stock
50 mg	￥1280	In stock
100 mg	￥1980	In stock
250 mg		Get quote

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生物&药学活性

Carnosic acid (Carnosate) is a highly selective inhibitor targeting the orthosteric site of ERAP1 with IC50 of 10.73 uM, inhibits oxidative stress and inflammation, suppressescell proliferation, and has antibacterial activity, also inhibits the BCL9/β-catenin interaction with Ki of 3.3 uM.

Carnosic acid shows little inhibitory effect on the homologous enzyme ERAP2, IRAP, related families of aminopeptidase APs and MMP1, and several classical proteases, Trypsin, and Furin.

Carnosic acid binds stably and dose-dependently to ERAP1 at the molecular level with a dissociation KD value of 9.05 μM.

Carnosic acid regulates the endoplasmic reticulum stress response caused by ERAP1-mediated misfolding of HLA-B27.

Carnosic acid impacts the presentation of endogenous antigenic peptides in living cells by inhibiting ERAP1, thereby reducing disease-related phenotypes.

Carnosic acid inhibits β-catenin-dependent transcription, and destabilizes oncogenic β-catenin in colon cancer cells.

Carnosic acid reduces the expression of Sox2 and the number of SOX2+ cells in MB sphere cultures.

物理化学性质&存储条件

分子量	332.44
分子式	C20H28O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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Solubility	10 mM in DMSO
Chemical Name/SMILES	(4aR,10aS)-5,6-Dihydroxy-7-isopropyl-1,1-dimethyl-1,2,3,4,4a,9,10,10a-octahydrophenanthrene-4a-carboxylic acid

参考文献

1. Wu J, et al. J Agric Food Chem. 2024 Jul 18. doi: 10.1021/acs.jafc.4c00957.

Carnosic acid (Compound 3-23, Carnosate)

生物&药学活性

物理化学性质&存储条件

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Carnosic acid (Compound 3-23, Carnosate)

生物&药学活性

物理化学性质&存储条件

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