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DDO-5936

  Cat. No.:  DC57011   Featured
Chemical Structure
2355377-13-6
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More than 5000 active chemicals with high quality for research!
Field of application
DDO-5936 is a potent PPI inhibitor targeting Hsp90-Cdc37 protein-protein interaction (PPI) as Orally Active Inhibitors for the Treatment of Colorectal Cancer. DDO-5936 disrupted the Hsp90-Cdc37 PPI both in vitro and in vivo via binding to a previously unknown site on Hsp90 involving Glu47, one of the binding determinants for the Hsp90-Cdc37 PPI, leading to selective down-regulation of Hsp90 kinase clients in HCT116 cells. In addition, inhibition of Hsp90-Cdc37 complex formation by DDO-5936 resulted in a remarkable cyclin-dependent kinase 4 decrease and consequent inhibition of cell proliferation through Cdc37-dependent cell cycle arrest.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2355377-13-6
Chemical Name: DDO-5936
Synonyms: N-[4-[[2-(1-Pyrrolidinyl)-4-pyrimidinyl]amino]phenyl]-N-[(2,4,6-trimethylphenyl)sulfonyl]glycine
SMILES: C1CCCN1C1N=C(C=CN=1)NC1=CC=C(C=C1)N(S(=O)(=O)C1C(=CC(=CC=1C)C)C)CC(=O)O
Formula: C25H29N5O4S
M.Wt: 495.59
Purity: >98%
Sotrage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Description: DDO-5936 is a potent and specific Hsp90-Cdc37 PPI inhibitor. DDO-5936 can be used for the research of colorectal cancer[1].
Target: Hsp90-Cdc37 PPI[1]
In Vivo: DDO-5936 (0~80 mg/kg; p.o.) shows effect at the high dose group[1]. DDO-5936 is well tolerated for the absence of serious weight loss. DDO-5936 high dose groups show that tumor cells in the xenografts decreased significantly. DDO-5936 shows limited oral efficiency[1]. Animal Model: Mice[1] Dosage: 0~80 mg/kg Administration: P.o. Result: Showed a moderate effect at the high dose group.
In Vitro: DDO-5936 is a Hsp90-Cdc37 PPI inhibitor with potency and specificity through binding to a critical site on Hsp90 involving Glu47[1].
References: [1]. Wang L, et al. Discovery and Optimization of Small Molecules Targeting the Protein-Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer. J Med Chem. 2020;63(3):1281-1297.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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