Tasisulam Chemical Properties

Density 

1.812

storage temp. 

Store at -20° C

solubility 

DMF: 20 mg/ml; DMSO: 20 mg/ml; Ethanol: 10 mg/ml; PBS (pH 7.2): 0.2 mg/ml

form 

A crystalline solid

pka

3.45±0.10(Predicted)

color 

Light yellow to yellow

Tasisulam Usage And Synthesis

Uses

The sodium salt of Tasisulam has potential antineoplastic activity. Selectively toxic towards tumor cells, tasisulam appears to induce tumor cell apoptosis by a mitochondrial-targeted mechanism involving the loss of mitochondrial membrane potential and induction of reactive oxygen species (ROS).

Biological Activity

Tasisulam (LY573636) is a SPLAM (SPLicing inhibitor sulfonAMide) th at bridges RNA binding motif protein 39 (RBM39; CAPERα, HCC1) and DCAF15 for interaction, thereby promoting (CUL4-DDB1-DDA1-DCAF15) E3 ubiquitin ligase complex-mediated RBM39 ubiquitination and subsequent proteasomal degradation. Tasisulam exerts selective toxicity in parental HCT116 cancer cultures (IC50 = 6.5 μM), but not those harboring non-CUL4-DCAF15-associating RBM39 G268V mutant even at a high concentration of 50 μM.

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