纯度:>98% by HPLC ,;NMR (Conforms)
分子式:C14H12ClN3O4S2
分子量:385.84
溶剂:DMSO (>25 mg/ml)
性状:Off-white solid
存储:-20°C
Activity (short version):RBM39 Molecular glue
Function / Pharmacology:Indisulam was originally described as a potent antitumor agent that targeted the G1 phase of cell cycle via suppression of activation of CDK2 and cyclin E expression.1 More recently it has been found to act as a molecular glue promoting the recruitment of RNA binding motif protein 39 (RBM39) to the CUL4-DCAF15 E3 ubiquitin ligase leading to proteasomal degradation.2 Removal of splicing factor RBM39 leads to altered RNA splicing and death in multiple cancer cell lines – Indisulam alters the expression of more than 3000 genes and causes widespread intron retention and exon skipping.3 It induced metabolome perturbations and mitochondrial dysfunction in neuroblastoma models leading to complete tumor regression without relapse.4 Arginine has been found to bind to RBM39 causing reprogramming of metabolic genes to promote tumor growth – indisulam treatment leading to RBM39 degradation mimics arginine depletion resulting in reduced growth in patient-derived hepatocellular carcinoma organoids.5