958888-32-9
Chemical Structure
WK88-1
- CAS No.: 958888-32-9
- Formula:C28H42N2O6
- Molecular Weight:502.64
InChIKey: VSRDDIXOACNXNB-SZPRHNSESA-N
SMILES: C/C(C(NC1=CC2=CC=C1)=O)=C/CC[C@H](OC)[C@@H](OC(N)=O)/C(C)=C/[C@H](C)[C@H]([C@@H](OC)C[C@@H](C2)C)O
Biological Activity: WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various EGFR mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases[1][2][3][4][5].
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WK88-1 | WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various EGFR mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases. | |||||||||||||||||||||
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- [1]. Zhao YR, et al. Non-Benzoquinone Geldanamycin Analog, WK-88-1, Induces Apoptosis in Human Breast Cancer Cell Lines. J Microbiol Biotechnol. 2018;28(4):542-550. [Content Brief]
- [2]. Hong YS, et al. Hsp90 inhibition by WK88-1 potently suppresses the growth of gefitinib-resistant H1975 cells harboring the T790M mutation in EGFR. Oncol Rep. 2014;31(6):2619-2624. [Content Brief]
- [3]. Jang WJ, et al. Anti-tumor activity of WK88-1, a novel geldanamycin derivative, in gefitinib-resistant non-small cell lung cancers with Met amplification. Cancer Sci. 2014;105(10):1245-1253. [Content Brief]
- [4]. Choi J, et al. Reblastatins Inhibit Phenotypic Changes of Monocytes/Macrophages in a Milieu Rich in 27-Hydroxycholesterol. Immune Netw. 2020;20(2):e17. Published 2020 Apr 23. [Content Brief]
- [5]. Wan X, et al. GW4869 can inhibit epithelial-mesenchymal transition promoted by extracellular HSP90α in EGFR-mutated NSCLC cells[J]. 2022.
Keywords
