Chemical Name: 1,2-dihydro-4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethyl)phenyl]-3-quinolinecarboxamide
Biological ActivityTasquinimod is a high affinity negative allosteric modulator of HDAC4 (Kd = 10 - 30 nM). Binds the regulatory Zn2+ binding domain of HDAC4. Suppresses hypoxia-induced decrease in histone acetylation in human prostate cancer cells in vitro. Also binds S100A9. Antiangiogenic. Inhibits endothelial sprouting in vitro and growth of prostate tumor xenografts in nude mice. Orally bioavailable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Tasquinimod Is an Allosteric Modulator of HDAC4 survival signaling within the compromised cancer microenvironment.
Isaacs JT, Antony L, Dalrymple SL et al.
Anti-cancer potency of Tasquinimod is enhanced via albumin-binding facilitating increased uptake in the tumor microenvironment.
Isaacs et al.
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