1314096-68-8
Chemical Structure
Ibulocydine
- CAS No.: 1314096-68-8
- Formula:C16H20BrN5O6
- Molecular Weight:458.26
IUPAC Name: ((2S,3S,4S,5S)-5-(4-amino-6-bromo-5-carbamoyl-1H-pyrrolo[2,3-d]pyrimidin-1-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl isobutyrate
InChIKey: FECJFYFWBIAIIL-IWRVGALASA-N
SMILES: O=C(C(C)C)OC[C@H]1[C@@H](O)[C@H](O)[C@@H](N2C3=NC(Br)=C(C3=C(N)N=C2)C(N)=O)O1
Biological Activity: 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[1][2][3][4].
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Ibulocydine | 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. | |||||||||||||||||||||
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References
- [1]. Cho SJ, et al. Ibulocydine is a novel prodrug Cdk inhibitor that effectively induces apoptosis in hepatocellular carcinoma cells. The Journal of biological chemistry. 2011 Jun 03;286(22):19662-71.
- [2]. Kwon MR, et al. Ibulocydine Inhibits Migration and Invasion of TNBC Cells via MMP-9 Regulation. International journal of molecular sciences. 2024 Jun 01;25(11):6123.
- [3]. Park SS, et al. Ibulocydine sensitizes human hepatocellular carcinoma cells to TRAIL-induced apoptosis via calpain-mediated Bax cleavage. The international journal of biochemistry & cell biology. 2017 Feb;83:47-55.
- [4]. Park SS, et al. Ibulocydine sensitizes human cancers to radiotherapy by induction of mitochondria-mediated apoptosis. Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology. 2014 Aug;112(2):295-301.
