Indisulam

Biological Activity

Indisulam is an acts as a molecular glue to induce proteosomal degradation of mRNA splicing factor RBM39 (also designated CAPERα, HCC1, FSAP59, and RNPC2), via binding to DCAF15. Acts as a pre-mRNA splicing modulator (SPLAMs; splicing inhibitor sulfonamides), causes aberrant pre-mRNA splicing. Suppresses proliferation of cancer cell lines. Reduces viability of HCT-116 cells (IC₅₀ = 0.56 μM). Induces cell cycle arrest in the G₁ phase in cancer cell lines. Also a high affinity carbonic anhydrase isozyme XII (hCA XII) inhibitor (K_i = 3.0-5.7 nM).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15.
   Han et al.
   Science, 2017;28:356
2. Selective degradation of splicing factor CAPERa by anticancer sulfonamides.
   Uehara et al.
   Nat.Chem.Biol., 2017;13:675
3. E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo.
   Ozawa et al.
   Eur.J.Cancer., 2001;37:2275
4. Discovery of novel antitumor sulfonamides targeting G₁ phase of the cell cycle.
   Owa et al.
   J.Med.Chem., 1999;42:3789
5. Function, clinical application, and strategies of Pre-mRNA splicing in cancer.
   Di et al.
   Cell Death Differ., 2018;:doi: 10.1038/s41418-
6. Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs?
   Vullo et al.
   Bioorg.Med.Chem.Lett., 2005;15:963

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