A8163-10mg | AM 114 [856849-35-9] Clinisciences

AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC₅₀ of approximately 1 μM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins. AM 114 also exerts anti-cancer activity against cancer cells, which potently inhibits the growth of human colon cancer HCT116 cells with values of IC₅₀ of 1.5 μM and 0.6 μM in MTT and colony formation assays respectively.

Reference

Achanta G, Modzelewska A, Feng L, Khan SR, Huang P. A boronic-chalcone derivative exhibits potent anticancer activity through inhibition of the proteasome. Mol Pharmacol. 2006 Jul;70(1):426-33. Epub 2006 Apr 24.

1. Gunderwala A, Porter J. "A luminescence assay for natural product inhibitors of the Mycobacterium tuberculosis proteasome." Phytochem Anal. 2016 Mar;27(2):126-32. PMID:26778282
2. Chen, Wei, et al. "Competitive Expression of Endogenous Wheat CENH3 May Lead to Suppression of Alien ZmCENH3 in Transgenic Wheat× Maize Hybrids." Journal of Genetics and Genomics (2015).

Physical Appearance	A solid
Storage	Store at 4°C
M.Wt	377.01
Cas No.	856849-35-9
Formula	C₂₀H₂₁B₂NO₅
Solubility	insoluble in H2O; ≥16.65 mg/mL in DMSO; ≥4.11 mg/mL in EtOH with ultrasonic
Chemical Name	[4-[(Z)-[(5Z)-5-[(4-boronophenyl)methylidene]-1-methyl-4-oxopiperidin-3-ylidene]methyl]phenyl]boronic acid
SDF	Download SDF
Canonical SMILES	B(C1=CC=C(C=C1)C=C2CN(CC(=CC3=CC=C(C=C3)B(O)O)C2=O)C)(O)O
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.