Butein

Additional information:
Butein, isolated from Dalbergia odorifera T. Chen, is a cAMP-specific PDE inhibitor with an IC50 of 10.PMID:33148043 4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).|Product information|CAS Number: 487-52-5|Molecular Weight: 272.25|Formula: C15H12O5|Synonym:|2’, 3, 4, 4’-tetrahydroxy Chalcone|Chemical Name: (2E)-1-(2, 4-dihydroxyphenyl)-3-(3, 4-dihydroxyphenyl)prop-2-en-1-one|Smiles: OC1=CC(O)=C(C=C1)C(=O)/C=C/C1=CC(O)=C(O)C=C1|InChiKey: AYMYWHCQALZEGT-ORCRQEGFSA-N|InChi: InChI=1S/C15H12O5/c16-10-3-4-11(14(19)8-10)12(17)5-1-9-2-6-13(18)15(20)7-9/h1-8,16,18-20H/b5-1+|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 35 mg/mL (128.56 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: ≥360 days 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:|Butein potently inhibits cAMP-specific phosphodiesterase (type IV) activity with an IC50 of 10.4±0.4 μM. In contrast, phosphodiesterase I, III and V activities were inhibited by Butein above 100 μM. Butein, a plant polyphenol, is a specific protein tyrosine kinase inhibitor. Butein inhibits not only the EGF-stimulated auto-phosphotyrosine level of EGFR in HepG2 cells but also tyrosine-specific protein kinase activities of EGFR (IC50=16 μM) and p60c-src (IC50=65 μM) in vitro. Butein (10, 20, and 40 μM; 24, 48, and 72 hours) inhibits cell growth in a dose- and time-dependent manner. Butein exhibits anticancer activity through the inhibition of the activation of PKB/AKT and MAPK pathways, which are two pathways known to be involved in resistance to cisplatin. Butein (20 µM) decreases phosphorylation of AKT, ERK and p38 following 24 h of co-treatment with Cisplatin (20 µM).|In Vivo:|Butein (2 mg/kg every 2 days) in combination with Cisplatin (2 mg/kg every 2 days) for 3 weeks suppresses tumor growth in vivo.|References:|Yu SM, et al. Endothelium-dependent relaxation of rat aorta by butein, a novel cyclic AMP-specific phosphodiesterase inhibitor.Eur J Pharmacol. 1995 Jun 23;280(1):69-77.Zhang L, et al. Butein sensitizes HeLa cells to cisplatin through the AKT and ERK/p38 MAPK pathways by targeting FoxO3a.Int J Mol Med. 2015 Oct;36(4):957-66.Yang EB, et al. Butein, a specific protein tyrosine kinase inhibitor.Biochem Biophys Res Commun. 1998 Apr 17;245(2):435-8.Products are for research use only. Not for human use.|