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.
Product information
CAS Number: 856849-35-9
Molecular Weight: 377.01
Formula: C20H21B2NO5
Chemical Name: {4-[(5-{[4-(dihydroxyboranyl)phenyl]methylidene}-1-methyl-4-oxopiperidin-3-ylidene)methyl]phenyl}boronic acid
Smiles: CN1CC(=CC2C=CC(=CC=2)B(O)O)C(=O)C(C1)=CC1C=CC(=CC=1)B(O)O
InChiKey: SRPIKXGUPAKTIZ-OTYYAQKOSA-N
InChi: InChI=1S/C20H21B2NO5/c1-23-12-16(10-14-2-6-18(7-3-14)21(25)26)20(24)17(13-23)11-15-4-8-19(9-5-15)22(27)28/h2-11,25-28H,12-13H2,1H3/b16-10+,17-11+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 6.25 mg/mL (16.58 mM; Need ultrasonic).
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:
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. Proteasome inhibitor IX (AM114) exhibits potent activity against p53+/+ cells in colony formation assay, with an IC50 value of 0.6 µM. 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. 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.
Products are for research use only. Not for human use.
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