Indisulam

Product Description

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).

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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	1.30 mL	2.59 mL
50 mM	0.05 mL	0.26 mL	0.52 mL

Calculators

Background References

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

• Vullo 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. 2005 PMID: 15686894
• Di Function, clinical application, and strategies of Pre-mRNA splicing in cancer. Cell Death Differ. 2018 PMID: 30464224
• Owa Discovery of novel antitumor sulfonamides targeting G₁ phase of the cell cycle. J.Med.Chem. 1999 PMID: 10508428
• Ozawa E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo. Eur.J.Cancer. 2001 PMID: 11677118
• Uehara Selective degradation of splicing factor CAPERa by anticancer sulfonamides. Nat.Chem.Biol. 2017 PMID: 28437394
• Han Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15. Science 2017 PMID: 28302793