1041469-97-9
Chemical Structure
RKS262
- CAS No.: 1041469-97-9
- Formula:C15H14BrClN2O4S
- Molecular Weight:433.70
IUPAC Name: (E)-6-bromo-4-chloro-3-(((3-methyl-1,1-dioxidothiomorpholino)imino)methyl)-2H-chromen-2-one
InChIKey: RPUHUUBAOXLODQ-CNHKJKLMSA-N
SMILES: O=C1OC2=C(C(Cl)=C1/C=N/N3CCS(=O)(CC3C)=O)C=C(Br)C=C2
Biological Activity: RKS262 is an orally active cyclin/CDK inhibitor. RKS262 is also an apoptosis inducer and cell cycle regulator, exhibiting cytotoxic activity against cancer cells. RKS262 induces caspase-3 cleavage, ROS generation, SAPK/JNK activation, and upregulates the expression of p53, Bid, Bad, Bok, and p27. RKS262 inhibits the expression of Bcl-2, Mcl-1, Bcl-xL, p21, cyclin D1, cyclin B1, cdc-2, cyclin D4, and DNA-pk KU-80 subunit. RKS262 suppresses the phosphorylation of the IGF-1R/PI3K/PKC pathway, ras oncogene activity, and Cdk-6, while increasing total Akt expression. RKS262 induces G2/M or S phase cell cycle arrest, disrupts mitochondrial transmembrane potential, and reduces tumor burden in xenograft models. RKS262 is used in research on neuroblastoma and ovarian cancer[1][2][3].
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RKS262 | RKS262 is an orally active cyclin/CDK inhibitor. RKS262 is also an apoptosis inducer and cell cycle regulator, exhibiting cytotoxic activity against cancer cells. RKS262 induces caspase-3 cleavage, ROS generation, SAPK/JNK activation, and upregulates the expression of p53, Bid, Bad, Bok, and p27. RKS262 inhibits the expression of Bcl-2, Mcl-1, Bcl-xL, p21, cyclin D1, cyclin B1, cdc-2, cyclin D4, and DNA-pk KU-80 subunit. RKS262 suppresses the phosphorylation of the IGF-1R/PI3K/PKC pathway, ras oncogene activity, and Cdk-6, while increasing total Akt expression. RKS262 induces G2/M or S phase cell cycle arrest, disrupts mitochondrial transmembrane potential, and reduces tumor burden in xenograft models. RKS262 is used in research on neuroblastoma and ovarian cancer. | |||||||||||||||||||||
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References
- [1]. Singh RK, et al. Oral RKS262 reduces tumor burden in a neuroblastoma xenograft animal model and mediates cytotoxicity through SAPK/JNK and ROS activation in vitro. Cancer biology & therapy. 2011 Jun 15;11(12):1036-45.
- [2]. Singh RK, et al. A coumarin derivative (RKS262) inhibits cell-cycle progression, causes pro-apoptotic signaling and cytotoxicity in ovarian cancer cells. Investigational new drugs. 2011 Feb;29(1):63-72.
- [3]. Şeker Karatoprak G, et al. A comprehensive review on the potential of coumarin and related derivatives as multi-target therapeutic agents in the management of gynecological cancers. Frontiers in pharmacology. 2024;15:1423480.
