A selective Cdk4 inhibitor
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Fascaplysin (chloride)

Item No. 21715

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
12,13-dihydro-13-oxo-pyrido[1,2-a:3,4-b']diindol-5-ium, monochloride
CAS Number
114719-57-2
Synonyms
  • NSC 622398
Molecular Formula
C18H11N2O • Cl
Formula Weight
306.7
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.14 mg/mLDMSO: 16 mg/mLDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mL
λmax
215, 262, 299, 407 nm
SMILES
O=C1C2=[N+](C=CC3=C2C4=C(C=CC=C4)N3[H])C5=CC=CC=C51.[Cl-]
InChi Code
InChI=1S/C18H10N2O.ClH/c21-18-12-6-2-4-8-15(12)20-10-9-14-16(17(18)20)11-5-1-3-7-13(11)19-14;/h1-10H;1H
InChi Key
XZKREMDIWZNGDA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $213

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    Cayman Chemical
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    Product Description

    Fascaplysin is an inhibitor of cyclin D kinase 4/ cyclin D1 (IC50 = 0.35 μM) that was originally isolated from the marine sponge Thorectandra.1 It is significantly less selective for Cdk6/cyclin D1 (IC50 = 3.4 μM) and does not inhibit other Cdks and tyrosine kinases.1 Fascaplysin is reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest.1 Inhibition of Cdk4 via fascaplysin has been shown to induce peroxisome-proliferator-activated receptor γ-1α deacetylation (IC50 = 0.7 µM) and has been used to demonstrate a role for insulin-activated cyclinD1-Cdk4 signaling in the control of glucose metabolism.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Soni, R., Muller, L., Furet, P., et al. Inhibition of cyclin-dependent kinase 4 (Cdk4) by fascaplysin, a marine natural product. Biochem. Biophys. Res. Commun. 275(3), 877-884 (2000).

    2. Lee, Y., Dominy, J.E., Choi, Y.J., et al. Cyclin D1-Cdk4 controls glucose metabolism independently of cell cycle progression. Nature 510(7506), 547-551 (2014).