FR901464 is a potent spliceosome inhibitor with prominent anti-tumor and anti-cancer effects[1].
FR901464 (10-20 ng/ml; 6-24 hours) inhibits the growth of murine solid tumors, Colon 38 carcinoma and Meth A fibrosarcoma. FR901464 induces characteristic G1 and G2/M phase arrest in the cell cycle and internucleosomal degradation of genomic DNA with the same kinetics as activation of SV40 promoter-dependent cellular transcription in M-8 tumor cells[1].FR901464 (1-10 ng/ml; 16 hours) suppresses the transcription of some inducible endogenous genes but not house keeping genes in M-8 cells[1].FR901464 exhibits potent anticancer activity. It shows enhancement of activity of a promoter of the SV40 DNA tumor virus at 10 nM concentration in M-8 cells[1].
[1]. H Nakajima, et al. New antitumor substances, FR901463, FR901464 and FR901465. II. Activities against experimental tumors in mice and mechanism of action. J Antibiot (Tokyo). 1996 Dec;49(12):1204-11.
[2]. Arun K Ghosh, et al. Enantioselective total syntheses of FR901464 and spliceostatin A and evaluation of splicing activity of key derivatives. J Org Chem. 2014 Jun 20;79(12):5697-709.