1429054-64-7

Basic information

• Product Name: 2-(4-(adamantan-1-yl)phenoxy)-1-(piperazin-1-yl)ethanone
• Synonyms: 2-(4-(adamantan-1-yl)phenoxy)-1-(piperazin-1-yl)ethanone
• CAS NO: 1429054-64-7
• Molecular Weight: 354.492
• Mol File: 1429054-64-7.mol

Chemical Properties

• CAS DataBase Reference: 2-(4-(adamantan-1-yl)phenoxy)-1-(piperazin-1-yl)ethanone(CAS DataBase Reference)
• NIST Chemistry Reference: 2-(4-(adamantan-1-yl)phenoxy)-1-(piperazin-1-yl)ethanone(1429054-64-7)
• EPA Substance Registry System: 2-(4-(adamantan-1-yl)phenoxy)-1-(piperazin-1-yl)ethanone(1429054-64-7)

Safety Data

• Hazardous Substances Data: 1429054-64-7(Hazardous Substances Data)

Upstream product

• 52804-26-9 (4-adamantan-1-yl-phenoxy)acetic acid 
• 1429054-63-6 tert-butyl 4-(2-(4-(adamantan-1-yl)phenoxy)acetyl)piperazine-1-carboxylate 

Relevant articles and documents

Probe for detecting HSP70 and manufacturing method thereof

The present invention relates to a probe for detecting heat shock protein (HSP) 70 as a target protein of IDF-11774, a compound capable of inhibiting activities of hypoxia inducible factor-1 (HIF-1). The present invention further relates to a production method thereof. By using the probe of the present invention, it is possible to know that the IDF-11774 binds to an allosteric site of HSP70 and inhibits chaperone activities of HSP70 by reducing refolding, thereby inhibiting activities of HIF-1. The probe can also be used to develop drugs to suppress proliferation and metastasis of cancer in an investigation on the target protein of IDF-11774.(AA) Probe 1: R=H(BB) Probe 2: R=Adamantyl(CC) Probe 3: R=H(DD) Probe 4: R=AdamantylCOPYRIGHT KIPO 2018

Identification of Targets of the HIF-1 Inhibitor IDF-11774 Using Alkyne-Conjugated Photoaffinity Probes

We developed a hypoxia-inducible factor-1 (HIF-1) inhibitor, IDF-11774, as a clinical candidate for cancer therapy. To understand the mechanism of action of IDF-11774, we attempted to isolate target proteins of IDF-11774 using bioconjugated probes. Multifunctional chemical probes containing sites for click conjugation and photoaffinity labeling were designed and synthesized. After fluorescence and photoaffinity labeling of proteins, two-dimensional electrophoresis (2DE) was performed to isolate specific molecular targets of IDF-11774. Heat shock protein (HSP) 70 was identified as a target protein of IDF-11774. We revealed that IDF-11774 inhibited HSP70 chaperone activity by binding to its allosteric pocket, rather than the ATP-binding site in its nucleotide-binding domain (NBD). Moreover, IDF-11774 reduced the oxygen consumption rate (OCR) and ATP production, thereby increasing intracellular oxygen tension. This result suggests that the inhibition of HSP70 chaperone activity by IDF-11774 suppresses HIF-1α refolding and stimulates HIF-1α degradation. Taken together, these findings indicate that IDF-11774-derived chemical probes successfully identified IDF-11774's target molecule, HSP70, and elucidated the mode of action of IDF-11774 in inhibiting HSP70 chaperone activity and stimulating HIF-1α degradation in cancer cells.

NOVEL COMPOUNDS AS HIF-1ALPHAINHIBITORS AND MANUFACTURING PROCESS THEREOF

The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.

NOVEL COMPOUNDS AS HIF-1αINHIBITORS AND MANUFACTURING PROCESS THEREOF

The present invention relates to novel compounds as HIF-1α inhibitors, manufacturing process thereof, and a pharmaceutical compositions. The compounds according to the present invention having inhibition activity against HIF-1α, can be used as a therapeutic prevention and/or treatment for various solid cancers such as colon cancer, liver cancer, stomach cancer and breast cancer. Also, the compounds according to the present invention are useful in the treatment of diabetic retinopathy and rheumatoid arthritis, which are aggravated by HIF-1α-mediated VEGFA expression.