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Chemical Structure : MS0621
Catalog No.: PC-49739Not For Human Use, Lab Use Only.
MS0621 (UNC0621, MS 0621) is a small-molecule modulator of EWSR1::FLI1-mediated chromatin, reverses EWSR1::FLI1-mediated chromatin accessibility, persistently and selectively inhibits cell proliferation in Ewing sarcoma cell lines (SK-N-MC, IC50=128 nM).
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MS0621 (UNC0621, MS 0621) is a small-molecule modulator of EWSR1::FLI1-mediated chromatin, reverses EWSR1::FLI1-mediated chromatin accessibility, persistently and selectively inhibits cell proliferation in Ewing sarcoma cell lines (SK-N-MC, IC50=128 nM).
MS0621 displays no activity against clear cell sarcoma cell line with the oncogenic EWS::ATF1 rearrangement (SU-CCS-1), and two primary cell lines that either express FLI1 (HUVEC) or do not express FLI1 (RPTEC).
MS0621 induces a G1/S arrest in Ewing sarcoma cell lines.
MS0621 interacts with a core complex of proteins that includes hnRNPH1, EWSR1, BRG1, and EWSR1::FLI1 in the absence of RNA or intact chromatin.
hnRNPH1 knockdown recapitulates the effect of MS0621 on Ewing sarcoma cell proliferation.
MS0621 affects EWSR1::FLI1-mediated gene expression and alternative splicing.
MS0621 treatment recapitulated the effects of EWSR1::FLI1 loss on FAIRE, cell cycle, and gene expression through a mechanism independent of regulating EWSR1::FLI1 gene expression.
MS0621 decreases FAIRE signal at EWSR1::FLI1-bound loci without displacing the oncoprotein from chromatin.
| M.Wt | 567.82 | |
| Formula | C32H53N7O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Tamara Vital, et al. Front Oncol. 2023 Jan 30;13:1099550.
2. Cueva JP, et al. J Med Chem 58:4242–4249.
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