SML3635
AGX51
≥98% (HPLC)
别名:
AGX 51, AGX-51, N-[3-(1,3-Benzodioxol-5-yl)-3-(2-methoxyphenyl)propyl]-N-(phenylmethyl)propenamide, N-[3-(1,3-Benzodioxol-5-yl)-3-(2-methoxyphenyl)propyl]-N-benzylpropanamide
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关于此项目
经验公式（希尔记法）:
C27H29NO4
化学文摘社编号:
分子量:
431.52
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Biochem/physiol Actions
AGX51 is an antagonist that blocks transcriptional regulators ID1-4 from binding basic helix-loop-helix (bHLH) transcription factor E47, causing ubiquitin-mediated degradation of IDs (10-40 μM for 2-48h; HCT116). AGX51 reduces cell viability, G0/G1 growth arrest, and a reduction in cyclin D1 levels in cultures (5-40 μM for 4-24h; HUVEC and HCT116) and suppresses ocular neovascularization in mouse models of age-related macular degeneration (AMD) and retinopathy of prematurity (ROP) in vivo (500 μg/mouse via twice daily i.p. or 1-30 μg/eye via intravitreal injection immediately and 7 days after rupture of Bruch’s membrane).
Antagonist that blocks transcriptional regulators ID1-4 from binding basic helix-loop-helix (bHLH) transcription factor E47, causing ubiquitin-mediated ID degradation.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
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NFkB-signaling promotes glial reactivity and suppresses Muller glia-mediated neuron regeneration in the mammalian retina
Glia, 70(7), 1380-1401 (2022)
Paulina M Wojnarowicz et al.
NPJ breast cancer, 7(1), 58-58 (2021-05-26)
ID proteins are helix-loop-helix (HLH) transcriptional regulators frequently overexpressed in cancer. ID proteins inhibit basic-HLH transcription factors often blocking differentiation and sustaining proliferation. A small-molecule, AGX51, targets ID proteins for degradation and impairs ocular neovascularization in mouse models. Here we
Paulina M Wojnarowicz et al.
Cell reports, 29(1), 62-75 (2019-10-03)
Id helix-loop-helix (HLH) proteins (Id1-4) bind E protein bHLH transcription factors, preventing them from forming active transcription complexes that drive changes in cell states. Id proteins are primarily expressed during development to inhibit differentiation, but they become re-expressed in adult
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