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Tasquinimod is an oral antiangiogenic and S100A9 inhibitor. Tasquinimod allosteric binding at 10-30 nM Kd in the zinc-regulated domain of HDAC4 inhibits co-localization of N-Cor /HDAC3, thereby inhibiting deacetylation of histones and HDAC4-client transcription factors such as HIF-1α. TAMs secretes angiogenic factors such as VEGF, FGF, TNF- α and TGF-β when bone marrow is derived to inhibit cell differentiation. Tasquinimod inhibits tumor angiogenesis by inhibiting tumor invasion of S100A9/ TLR4-dependent MDSCs and/or by inhibiting HIF-1α deacetylation of HDAC4/ N-COR/HDAC3-dependent MDSCs to TAMs. Tasquinimod is an orally active quinoline-3-carboxylamide that binds with high affinity to HDAC4 and S100A9 in cancer and infiltrates host cells in the impaired tumor microenvironment, inhibiting an adaptive survival pathway required for angiogenic responses.
| Molecular Weight | 406.36 |
| Formula | C20H17F3N2O4 |
| CAS Number | 254964-60-8 |
| Solubility (25°C) | DMSO ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HDAC Products |
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| CM-444
CM-444 is an inhibitor for HDAC and DNA methyltransferases (DNMT) with IC50 values of 6 nM-0.6 μM and 1.8-2.3 μM, respectively. CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models. |
| CM-1758
CM-1758 is a histone deacetylase (HDAC) inhibitor. CM-1758 inhibits tumor growth in vivo. CM-1758 induces acetylation of non-histone proteins in acute myeloid leukemia cells. |
| T-518
T-518 is an orally active, selective, and blood-brain barrier permeable HDAC6 inhibitor with an IC50 value of 36 nM for human HDAC6. |
| SE-7552
SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-hydroxamate HDAC6 inhibitor with an IC50 of 33 nM. |
| BRD9757
BRD9757 is a potent, capless and selective HDAC6 inhibitor with an IC50 of 30 nM. |
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