Indisulam

SKU: orb1302953

Description

Indisulam (E 7070) is a dual-action small molecule inhibitor of carbonic anhydrase and cyclin-dependent kinase 2 (CDK2). It induces G1 phase arrest by depleting cyclin E, upregulating p53 and p21, thereby blocking the G1/S transition. This compound is utilized in cancer research for studying cell cycle mechanisms in both in vitro and in vivo models.

Research Area

Cell Biology, Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 165668-41-7
• MW: 385.8
• Purity: >98%
• Formula: C₁₄H₁₂ClN₃O₄S₂
• SMILES: NS(=O)(=O)c1ccc(cc1)S(=O)(=O)Nc1cccc2c(Cl)c[nH]c12
• Target: Molecular glue
• Solubility: Soluble in DMSO (up to 25 mg/ml)

Bioactivity

• In Vivo:
  In vivo, indisulam suppresses tumor growth and decreases tumor volume in murine HCT116, SW620, and HCT15 colorectal and LX-1 and PC9 lung cancer xenograft models. Indisulam induces proteasomal degradation of RNA binding motif protein 39 (RBM39) through association with the CUL4-DCAF15 E3 ubiquitin ligase in vitro.It is also an inhibitor of carbonic anhydrase in H. pylori (Ki = 310-562 nM). Formulations containing indisulam are under Clinicalal investigation for the treatment of solid tumors.
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• In Vitro:
  In vitro, indisulam has antiproliferative effects on a wide range of human tumor lines with HCT116 colorectal being the most sensitive and NCI-H596 non-small cell lung cancer (NSCLC) the most resistant (IC50s = 0.11 and 94 μg/ml, respectively). It increases the number of P388 murine leukemia cells in the G1 phase of the cell cycle in a dose-dependent manner and exerts time-dependent cytotoxicity against HCT116 cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E7070

Compound Identifiers

PubChem CID

216468