Calpain Activator

Diatrizoate meglumine (N-Methyl-D-glucamine diatrizoate) is an orally active, water-soluble, poorly absorbable iodinated contrast agent. Diatrizoate meglumine is widely used as an adjuvant for radiological diagnosis and can also be applied to studies of small bowel obstruction in non-malignant conditions.

Diatrizoic acid dihydrate (Diatrizoate dihydrate) is an iodinated contrast agent. Diatrizoic acid dihydrate induces intracellular calcium homeostasis dysregulation, activates calpain and caspase-12, and activates the executor caspase-3, inducing cell apoptosis. Diatrizoic acid dihydrate induces mitophagy, oxidative stress, and TNFα secretion/inflammatory responses, while inhibiting mitochondrial respiratory function. Diatrizoic acid dihydrate can be used for research on contrast-induced acute kidney injury (ci-aki).

Ibulocydine is an isobutyrate prodrug of the Cdk inhibitor BMK-Y101 (HY-188159), with oral activity, and exhibits IC₅₀ values of approximately 50 nM against CDK1/CDK2, 530 nM against CDK7/cyclin H/Mat1, and 85 nM against CDK9/cyclin T. Ibulocydine reduces the phosphorylation levels of Rb, nucleolin, and RNA polymerase II CTD Ser-5 and Ser-2, downregulates the expression of Mcl-1, survivin, and XIAP, decreases MMP-9 expression, and lowers the Bcl-2/Bax ratio, activates calpain-mediated Bax cleavage, cytochrome c release, and caspase activation. Ibulocydine induces apoptosis, inhibits the growth of cancer cells and xenografts, enhances the sensitivity of cancer cells to TRAIL and radiotherapy, and blocks cancer cell metastasis. Ibulocydine can be used in research related to various cancers, including hepatocellular carcinoma, triple-negative breast cancer, lung cancer, and colon cancer.