Fascaplysin (chloride)

Fascaplysin is an inhibitor of cyclin D kinase 4/ cyclin D1 (IC50 = 0.35 µM) that was originally isolated from the marine sponge Thorectandra. It is significantly less selective for Cdk6/cyclin D1 (IC50 = 3.4 µM) and does not inhibit other Cdks and tyrosine kinases. Fascaplysin is reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest. Inhibition of Cdk4 via fascaplysin has been shown to induce peroxisome-proliferator-activated receptor gamma-1alpha 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.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: DMF: 0.14 mg/mL, DMSO: 16 mg/mL, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/mL. lambdamax: 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.