71294-60-5
Chemical Structure
Rohitukine
- CAS No.: 71294-60-5
- Formula:C16H19NO5
- Molecular Weight:305.33
IUPAC Name: 5,7-dihydroxy-8-((3S,4R)-3-hydroxy-1-methylpiperidin-4-yl)-2-methyl-4H-chromen-4-one
InChIKey: MOCVYVBNJQIVOV-TVQRCGJNSA-N
SMILES: O=C1C=C(OC2=C1C(O)=CC(O)=C2[C@@H]3[C@@H](CN(CC3)C)O)C
Biological Activity: Rohitukine is an orally active CDK9/T1 inhibitor with an IC50 of 0.3 μM. Rohitukine blocks ATP binding sites of CDK2/A and CDK9/T1, suppresses PPARγ, AKT, mTOR, C/EBPα, SREBP-2, and NF-κB signaling, and increases hepatic LXRα expression. Rohitukine induces S-phase cell cycle arrest, ROS generation, apoptosis, and exhibits anti-inflammatory activity. Rohitukine can be used for the research of leukemia, pancreatic cancer, prostate cancer, breast cancer, CNS cancer, ovarian cancer, lung cancer, dyslipidemia, inflammatory diseases, inflammatory bowel disease, and arthritis[1][2][3][4].
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Rohitukine | Rohitukine is an orally active CDK9/T1 inhibitor with an IC50 of 0.3 μM. Rohitukine blocks ATP binding sites of CDK2/A and CDK9/T1, suppresses PPARγ, AKT, mTOR, C/EBPα, SREBP-2, and NF-κB signaling, and increases hepatic LXRα expression. Rohitukine induces S-phase cell cycle arrest, ROS generation, apoptosis, and exhibits anti-inflammatory activity. Rohitukine can be used for the research of leukemia, pancreatic cancer, prostate cancer, breast cancer, CNS cancer, ovarian cancer, lung cancer, dyslipidemia, inflammatory diseases, inflammatory bowel disease, and arthritis. | |||||||||||||||||||||
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- [1]. Kumar V, et al. A chromatography-free isolation of rohitukine from leaves of Dysoxylum binectariferum: Evaluation for in vitro cytotoxicity, Cdk inhibition and physicochemical properties. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3457-63. [Content Brief]
- [2]. Varshney S, et al. Rohitukine inhibits in vitro adipogenesis arresting mitotic clonal expansion and improves dyslipidemia in vivo. J Lipid Res. 2014 Jun;55(6):1019-32. [Content Brief]
- [3]. Singh A, et al. Rohitukine inhibits NF-κB activation induced by LPS and other inflammatory agents. Int Immunopharmacol. 2019 Apr;69:34-49. [Content Brief]
- [4]. Ahmed S, et al. Exogenously Applied Rohitukine Inhibits Photosynthetic Processes, Growth and Induces Antioxidant Defense System in Arabidopsis thaliana. Antioxidants (Basel). 2022 Aug 3;11(8):1512. [Content Brief]
Keywords
