2. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. ATM/ATR Checkpoint Kinase (Chk) MDM-2/p53 E1/E2/E3 Enzyme CDK Mitosis Reactive Oxygen Species (ROS) Apoptosis
  4. Americanin A

Americanin A is a Neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizes p27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer.

For research use only. We do not sell to patients.

Americanin A

Americanin A Chemical Structure

CAS No. : 69506-79-2

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Americanin A Related Antibodies

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Description

Americanin A is a Neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizes p27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer[1].

IC50 & Target[1]

Chk1

 

Chk2

 

ATM

 

ATR

 

In Vitro

Americanin A (24–72 h) selectively inhibits proliferation of human cancer cells (IC50 9.0–66.4 μM) with no significant effect on MRC-5 normal cells, and inhibits HCT116 cells in a concentration- and time-dependent manner[1].
Americanin A (7.5-30 μM; 24 h) induces G2/M cell-cycle arrest in HCT116 cells, with 30 μM increasing G2/M phase cells to 38.9%[1].
Americanin A (7.5–30 μM; 24 h) induces DNA damage in HCT116 cells, as indicated by increased phosphorylated H2A.X and decreased acetylated H3[1].
Americanin A (7.5–30 μM; 48 h) induces apoptosis in HCT116 cells after 48 h treatment, with 30 μM increasing sub-G1 cells to 52.0%[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Americanin A Related Antibodies

Cell Proliferation Assay[1]

Cell Line: A549, Caki-1, K562, HCT116, SW480, HCT-15, RKO, MRC-5
Concentration: IC₅₀ values (9.0–66.4 μM for cancer cells; >100 μM for MRC-5)
Incubation Time: 24 h, 48 h, 72 h
Result: Inhibited proliferation of A549 (IC50 39.1 μM), Caki-1 (IC50 66.4 μM), K562 (IC50 12.9 μM), HCT116 (IC50 9.0 μM), SW480 (IC50 27.4 μM), HCT-15 (IC50 12.5 μM), RKO (IC50 24.4 μM) cells; measured HCT116 IC50 values of 24.1 μM (24 h), 9.6 μM (48 h), 8.7 μM (72 h); showed no significant inhibition of MRC-5 cells (IC50 > 100 μM).

Cell Cycle Analysis[1]

Cell Line: HCT116
Concentration: 7.5, 15, 30 μM
Incubation Time: 24 h
Result: Increased the proportion of G₂/M phase cells from 20.6% (untreated) to 38.9% at 30 μM; increased sub-G₁ cell proportion (apoptosis indicator) concentration-dependently, but the increase was not significant at 24 h.

Western Blot Analysis[1]

Cell Line: HCT116
Concentration: 7.5, 15, 30 μM
Incubation Time: 24 h
Result: Suppressed expression of cyclin A, cyclin B1, phosphorylated cyclin B1 (Ser147), CDK2, and cdc2 in a concentration-dependent manner.\nIncreased phosphorylation of histone H2A.X (Ser139) and decreased acetylation of histone H3 (Lys9) concentration-dependently.

Apoptosis Analysis[1]

Cell Line: HCT116
Concentration: 7.5, 15, 30 μM
Incubation Time: 48 h
Result: Increased sub-G₁ cell proportion from 6.5% (untreated) to 52.0% at 30 μM; showed increased early and late apoptotic cells concentration-dependently via annexin V/FITC staining.
In Vivo

Americanin A (5-10 mg/kg; i.p.; three times a week) inhibits HCT116 tumor xenograft growth in nude mice with 45.0% and 55.7% tumor volume reduction at 5 and 10 mg/kg, respectively, via Skp2-dependent p27 stabilization[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c-nu (female, 4-6 weeks old, HCT116 tumor xenograft)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: i.p.; three times a week
Result: Reduced tumor volumes by 45.0% (5 mg/kg) and 55.7% (10 mg/kg) compared to vehicle; Increased expressions of p21 and p27, and decreased Skp2 expression in excised tumors; Showed pronounced p27 staining and diminished Skp2 and Ki-67 staining via immunohistochemistry; Observed no overt toxicity or body weight changes.
Molecular Weight

328.32

Formula

C18H16O6
CAS No.
SMILES

OC[C@H]1[C@H](C2=CC(O)=C(C=C2)O)OC3=CC=C(/C=C/C=O)C=C3O1
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Americanin A Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Americanin A69506-79-2ATM/ATRCheckpoint Kinase (Chk)MDM-2/p53E1/E2/E3 EnzymeCDKMitosisReactive Oxygen Species (ROS)ApoptosisAtaxia telangiectasia mutatedATM and RAD3 relatedE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseCyclin dependent kinasecyclin B1ATRHCT116 cellscdc2p53Chk2Chk1colon cancerATMSkp2Inhibitorinhibitorinhibit

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