DC Chemicals Limited
China
Product Name: AM-114
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Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

856849-35-9

856849-35-9 structure

Name: AM 114
Chemical Name: AM-114
CAS Number: 856849-35-9
Molecular Formula: C₂₀H₂₁B₂NO₅
Molecular Weight: 377.006
Catalog: Signaling Pathways Metabolic Enzyme/Protease Proteasome
Create Date: 2018-06-17 12:17:30
Modify Date: 2024-01-10 15:23:51
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity[1][2].

Name	AM-114
Synonyms	4H5Y396039 Boronic acid, B,B'-[(1-methyl-4-oxo-3,5-piperidinediylidene)bis[(Z)methylidyne-4,1-phenylene]]bis- AM-114 {(1-Methyl-4-oxo-3,5-piperidinediylidene)bis[(Z)methylylidene-4,1-phenylene]}diboronic acid

Description	Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53+/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity[1][2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome
Target	IC50: 1 μM (20S proteasome)[1]
In Vitro	Proteasome inhibitor IX (AM114; 0.1-10 µM; 14 days; HCT116 p53+/+ cells) treatment causes a loss of cell survival in the p53+/+ and p53-/- cells by approximately 70 and 20%, respectively at a concentration of 1 µM[1]. Proteasome inhibitor IX (AM114) exhibits potent activity against p53+/+ cells in colony formation assay, with an IC50 value of 0.6 µM[1]. Incubation of HCT116 p53+/+ cells with 1 µM Proteasome inhibitor IX (AM114) causes 28% of the cells to exhibit positive Annexin V staining at 48 h, and this fraction of dead cells increased to 76% at 72 h[1]. Proteasome inhibitor IX (AM114) treatment inhibits the chymotrypsin-like activity of the 20S proteasome in vitro, leading to a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells[1].
References	[1]. Geetha Achanta , et al. A Boronic-Chalcone Derivative Exhibits Potent Anticancer Activity Through Inhibition of the Proteasome. Mol Pharmacol. 2006 Jul;70(1):426-33. [2]. Encouse B Golden, et al. Green Tea Polyphenols Block the Anticancer Effects of Bortezomib and Other Boronic Acid-Based Proteasome Inhibitors. Blood. 2009 Jun 4;113(23):5927-37.

Density	1.3±0.1 g/cm3
Boiling Point	695.4±65.0 °C at 760 mmHg
Molecular Formula	C₂₀H₂₁B₂NO₅
Molecular Weight	377.006
Flash Point	374.3±34.3 °C
Exact Mass	377.160583
LogP	4.14
Vapour Pressure	0.0±2.3 mmHg at 25°C
Index of Refraction	1.644
Storage condition	-20°C

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