Carnosol - CAS# 5957-80-2

Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM[1]. Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1).

Product information

CAS Number: 5957-80-2

Molecular Weight: 330.42

Formula: C20H26O4

Chemical Name: (1R, 8S, 10S)-3, 4-dihydroxy-11, 11-dimethyl-5-(propan-2-yl)-16-oxatetracyclo[6.6.2.0, .0, ]hexadeca-2(7), 3, 5-trien-15-one

Smiles: CC1(C)CCC[C@]23[C@H]1C[C@H](OC2=O)C1=CC(C(C)C)=C(O)C(O)=C31

InChiKey: XUSYGBPHQBWGAD-PJSUUKDQSA-N

InChi: InChI=1S/C20H26O4/c1-10(2)11-8-12-13-9-14-19(3,4)6-5-7-20(14,18(23)24-13)15(12)17(22)16(11)21/h8,10,13-14,21-22H,5-7,9H2,1-4H3/t13-,14-,20+/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 125 mg/mL (378.31 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

It is showed that carnosol has no cytotoxic effects on GES1 cells and 10 μM carnosol strongly suppresses RSK2 activity, but has little effect on any other kinase. Carnosol exerts strong dose-dependent inhibitory effects against RSK2 autophosphorylation and phosphorylation of its substrate ATF1.

In Vivo:

Results indicate that Carnosol significantly decreaseS the volume and weight of gastric tumors relative to the vehicle-treated group. Additionally, mice tolerate treatment with carnosol without significant loss of body weight similar to the vehicle-treated group. The phosphorylation of CREB, a direct downstream protein of RSK2, Is strongly inhibited in the carnosol-treated group but the expression of total CREB is relatively unchanged.

References:

1. Wang L, et al. Carnosol suppresses patient-derived gastric tumor growth by targeting RSK2. Oncotarget. 2018 Feb 6;9(76):34200-34212.
2. Li X, et al. Carnosol as a Nrf2 Activator Improves Endothelial Barrier Function Through Antioxidative Mechanisms. Int J Mol Sci. 2019;20(4):880. Published 2019 Feb 18.
3. Martin D, et al. Regulation of heme oxygenase-1 expression through the phosphatidylinositol 3-kinase/Akt pathway and the Nrf2 transcription factor in response to the antioxidant phytochemical carnosol. J Biol Chem. 2004;279(10):8919-8929.

Products are for research use only. Not for human use.