Fascaplysin A selective CDK4/cyclin D1 inhibitor

Fascaplysin (CAS 114719-57-2)

Fascaplysin | CAS 114719-57-2 is rated 5.0 out of 5 by 1.
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Synonym: Fascaplysin Chloride
Application: A selective CDK4/cyclin D1 inhibitor
CAS Number: 114719-57-2
Purity: ≥98%
Molecular Weight: 306.75
Molecular Formula: C18H11N2O•Cl
* Refer to Certificate of Analysis for lot specific data (including water content).
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Fascaplysin was originally isolated from a marine sponge and is involved in signal transduction and dna synthesis. Selective CDK4/cyclin D1 (IC50 = 350 nM) inhibitor (in an ATP competitive manner). Fascaplysin is an inhibitor of Cdk6.


References

1. Fascaplysin, an unusual antimicrobial pigment from the marine sponge Fascaplysinopsis sponge: D.M. Roll, et al.; J. Org. Chem. 53, 3276 (1988)
2. Kirsch, G., et al., 2000. A new bioactive sesterterpene and antiplasmodial alkaloids from the marine sponge hyrtios cf. erecta. Journal of natural products. 63(6): 825-9. PMID: 10869210
3. Soni, R., et al., 2000. Inhibition of cyclin-dependent kinase 4 (Cdk4) by fascaplysin, a marine natural product. Biochemical and biophysical research communications. 275(3): 877-84. PMID: 10973815
4. Hörmann, A., et al., 2001. DNA binding properties of the marine sponge pigment fascaplysin. Bioorganic & medicinal chemistry. 9(4): 917-21. PMID: 11354674

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (10 mg/ml), and methanol (1 mg/ml).
Storage :
Store at -20° C
IC50 :
Cdk4/cyclin D1 : IC50 = 0.35 µM; CDK4: IC50 = 0.35 µM; Cdk6/cyclin D1: IC50 = 3.4 µM; Plasmodium falciparum: IC50 = 0.034 ug/ml; Plasmodium falciparum (isolate K1 / Thailand): IC50 = 0.05 ug/ml (Plasmodium falciparum K1)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
73292
MDL Number :
MFCD04036980
SMILES :
C1=CC=C2C(=C1)C3=C(N2)C4=[N+](C=C3)C5=CC=CC=C5C4=O.[Cl-]

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Certificate of Analysis

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Fascaplysin  Product Citations

See how others have used Fascaplysin. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 28922657  Jemaà, M. et al. 2017. Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology. 43: 431-444.

PMID: # 27626793  Mischitelli, M. et al. 2016. Cell. Physiol. Biochem. 39: 1638-47.

PMID: # 26569265  Ampofo, E. et al. 2015. Mar Drugs. 13: 6774-91.

PMID: # 26370090  Lee, JG. et al. 2015. J. Biol. Chem. 290: 26752-64.

Citations 1 to 4 of 4 total
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Rated 5 out of 5 by from Kumar Kumar, S. et al. (PubMed 25561006) reported that Fascaplysin induces caspase mediated crosstalk between apoptosis and autophagy through the inhibition of PI3K/AKT/mTOR signaling cascade in human leukemia HL-60 cells. -SCBT Publication Review
Date published: 2015-03-04
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