SML3635
AGX51
≥98% (HPLC)
Sinónimos:
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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About This Item
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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).
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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
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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