LW6

Based on 62 publications in PubMed 9 10 62

Axon 2480

CAS [934593-90-5]

MF C26H29NO5
MW 435.51

Purity: 99%
Soluble in DMSO

LW6

Description

Novel HIF-1 inhibitor (IC50 value 2.44 μM) that promotes proteasomal degradation of HIF-1α via upregulation of von-Hippel-Lindau (VHL), without affecting the activity of prolyl hydroxylase (PHD). Evidence was found that identified MDH2 as a target protein of LW-6.?Moreover, LW6 suppresses angiogenesis by inhibition of HIF-1α stability via direct binding with calcineurin b homologous protein 1 (CHP1) in a Ca2+ dependent manner.

K. Lee et al. LW6, a novel HIF-1 inhibitor, promotes proteasomal degradation of HIF-1alpha via upregulation of VHL in a colon cancer cell line. Biochem Pharmacol. 2010 Oct 1;80(7):982-9.

B.S. Kim et al. HIF-1α suppressing small molecule, LW6, inhibits cancer cell growth by binding to calcineurin b homologous protein 1. Biochem Biophys Res Commun. 2015 Feb 27;458(1):14-20.

R. Naik et al. Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as hypoxia-inducible factor (HIF) 1α inhibitors. J Med Chem. 2012 Dec 13;55(23):10564-71.

K. Lee et al. Identification of malate dehydrogenase 2 as a target protein of the HIF-1 inhibitor LW6 using chemical probes. Angew Chem Int Ed Engl. 2013 Sep 23;52(39):10286-9.

Certificate of Analysis
Material Safety Data Sheet

Angiogenesis Cell Signaling & Oncology Epigenetics Transcription Factors MAPK Calcineurin TF class 1.2.5 MDH HIF

Inhibitor of HIF-1α stability via MDH2 inhibition and/or binding with CHP1

Chemical name

methyl 3-[[2-[4-(1-adamantyl)phenoxy]acetyl]amino]-4-hydroxybenzoate

Parent CAS No.

[934593-90-5]

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