AM 114 is a novel compound with significant cytotoxic effects on cancer cells, primarily through the inhibition of the cellular proteasome. This property makes it a promising candidate for the development of cancer chemotherapeutic agents.
856849-35-9
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Basic information
- Product Name: AM 114
- Synonyms: AM 114;3,5-Bis-[benzylidene-4-boronicacid]-1-methylpiperidin-4-one
- CAS NO:856849-35-9
- Molecular Formula: C20H21B2NO5
- Molecular Weight: 377.01
- EINECS: -0
- Product Categories: Inhibitor
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Chemical Properties
- Melting Point: N/A
- Boiling Point: N/A
- Flash Point: N/A
- Appearance: /
- Density: N/A
- Refractive Index: N/A
- Storage Temp.: Store at +4°C
- Solubility: insoluble in H2O; ≥16.65 mg/mL in DMSO; ≥4.11 mg/mL in EtOH with ultrasonic
- CAS DataBase Reference: AM 114(CAS DataBase Reference)
- NIST Chemistry Reference: AM 114(856849-35-9)
- EPA Substance Registry System: AM 114(856849-35-9)
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Safety Data
- Hazard Codes: N/A
- Statements: N/A
- Safety Statements: N/A
- WGK Germany:
- RTECS:
- HazardClass: N/A
- PackingGroup: N/A
- Hazardous Substances Data: 856849-35-9(Hazardous Substances Data)
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856849-35-9 Usage
Uses
Used in Cancer Chemotherapy:AM 114 is used as a chemotherapeutic agent for its ability to induce significant cytotoxic effects in cancer cells. The inhibition of the cellular proteasome by AM 114 provides a rationale for further development of this class of compounds as novel cancer treatments.
Biological Activity
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.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.Check Digit Verification of cas no
The CAS Registry Mumber 856849-35-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,5,6,8,4 and 9 respectively; the second part has 2 digits, 3 and 5 respectively.Calculate Digit Verification of CAS Registry Number 856849-35:
(8*8)+(7*5)+(6*6)+(5*8)+(4*4)+(3*9)+(2*3)+(1*5)=229
229 % 10 = 9
So 856849-35-9 is a valid CAS Registry Number.
856849-35-9Upstream product
856849-35-9Downstream Products
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AM 114
