Tasquinimod
Chemical Name: 1,2-dihydro-4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethyl)phenyl]-3-quinolinecarboxamide
Purity: ≥98%
Biological Activity
Tasquinimod 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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Tasquinimod Is an Allosteric Modulator of HDAC4 survival signaling within the compromised cancer microenvironment.
Isaacs JT, Antony L, Dalrymple SL et al.
Cancer Res. -
Anti-cancer potency of Tasquinimod is enhanced via albumin-binding facilitating increased uptake in the tumor microenvironment.
Isaacs et al.
Oncotarget, 2014;5:8093
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