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Description: Molecular glue; pre-mRNA splicing modulator
Chemical Name: N1-(3-Chloro-1H-indol-7-yl)-1,4-benzenedisulfonamide
Purity: ≥98% (HPLC)
Literature (3)

Biological Activity for Indisulam

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 (Ki = 3.0-5.7 nM).

Technical Data for Indisulam

M. Wt 385.84
Formula C14H12ClN3O4S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 165668-41-7
PubChem ID 216468
Smiles NS(=O)(C1=CC=C(S(=O)(NC2=CC=CC3=C2NC=C3Cl)=O)C=C1)=O

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.

Solubility Data for Indisulam

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 38.58 100

Preparing Stock Solutions for Indisulam

The following data is based on the product molecular weight 385.84. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.59 mL 12.96 mL 25.92 mL
5 mM 0.52 mL 2.59 mL 5.18 mL
10 mM 0.26 mL 1.3 mL 2.59 mL
50 mM 0.05 mL 0.26 mL 0.52 mL

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References for Indisulam

References are publications that support the biological activity of the product.

Han et al (2017) Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15. Science 28 356 PMID: 28302793

Uehara et al (2017) Selective degradation of splicing factor CAPERa by anticancer sulfonamides. Nat.Chem.Biol. 13 675 PMID: 28437394

Ozawa et al (2001) E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo. Eur.J.Cancer. 37 2275 PMID: 11677118

Owa et al (1999) Discovery of novel antitumor sulfonamides targeting G1 phase of the cell cycle. J.Med.Chem. 42 3789 PMID: 10508428

Di et al (2018) Function, clinical application, and strategies of Pre-mRNA splicing in cancer. Cell Death Differ. doi: 10.1038/s41418- PMID: 30464224

Vullo et al (2005) Carbonic anhydrase inhibitors. Inhibition of the transmembrane isozyme XII with sulfonamides-a new target for the design of antitumor and antiglaucoma drugs? Bioorg.Med.Chem.Lett. 15 963 PMID: 15686894

If you know of a relevant reference for Indisulam, please let us know.

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Literature in this Area

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