A 20S proteasome inhibitor
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AM114

Item No. 42040

Technical Information
Formal Name
B,B′-[(1-methyl-4-oxo-3,5-piperidinediylidene)bis(methylidyne-4,1-phenylene)]bis-boronic acid
CAS Number
856849-35-9
Synonyms
  • Proteasome Inhibitor IX
Molecular Formula
C20H21B2NO5
Formula Weight
Purity
≥95%
Formulation
A solid
Methanol: Slightly soluble: 0.1-1 mg/ml
SMILES
OB(C1=CC=C(C=C(CN(CC2=CC(C=C3)=CC=C3B(O)O)C)C2=O)C=C1)O
InChi Code
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
InChi Key
SRPIKXGUPAKTIZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    AM114 is an inhibitor of the 20S proteasome (IC50 = ~1 µM).1 It induces the accumulation of ubiquitinated proteins in HCT116 colon cancer cells when used at a concentration of 1 µM. AM114 sensitizes HCT116 p53+/+ and HCT116 p53-/- cells to ionizing radiation-induced cytotoxicity in an additive and synergistic manner, respectively. It decreases the viability of macrophages isolated from patients with rheumatoid arthritis (IC50 = 0.88 µM).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Achanta, G., Modzelewska, A., Feng, L., et alA boronic-chalcone derivative exhibits potent anticancer activity through inhibition of the proteasome. Mol. Pharmacol. 70(1), 426-433 (2006).

    2. Chitra, S., Nalini, G., Lokeswari, T.S., et alThe effect of proteasome inhibitor (AM114) on apoptosis in IL-1β-treated peripheral blood macrophage cultured cells from rheumatoid arthritis patients. Indian J. Rheumato. 11(1), 7-13 (2016).