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Chemical Structure : HDAC3 inhibitor 4i
Catalog No.: PC-21115Not For Human Use, Lab Use Only.
HDAC3 inhibitor 4i is a potent, selective HDAC3 inhibitor with IC50 of 14 nM, shows 121-fold selectivity over HDAC1 (IC50=1983 nM) and HDAC2 (IC50=1696 nM).
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HDAC3 inhibitor 4i is a potent, selective HDAC3 inhibitor with IC50 of 14 nM, shows 121-fold selectivity over HDAC1 (IC50=1983 nM) and HDAC2 (IC50=1696 nM).
HDAC3 inhibitor 4i shows no activity against other HDACs such as HDAC8 (IC50 = 10,744 nM), HDAC6 (IC50 = 25,930 nM), HDAC4 (IC50 > 20,000 nM) and HDAC5 (IC50 > 20,000 nM).
HDAC3 inhibitor 4i exhibits a minimum of 17.5-fold HDAC3 inhibitory potency than the reference HDAC3 inhibitor UF010 (IC50=256.7 nM).
HDAC3 inhibitor 4i exhibits selectivity toward different subtypes of breast cancer cell lines (4T1, IC50=0.55 uM) over normal human cell lines including normal breast cell line MCF-10A (IC50>200 uM).
HDAC3 inhibitor 4i induced significant apoptosis and causes G2/M phase cell cycle arrest in TNBC cells.
HDAC3 inhibitor 4i demonstrates potential in overcoming the oxaliplatin resistance in the TNBC cell line MDA-MB-231.
HDAC3 inhibitor 4i (5 mg/kg, and 15 mg/kg) inhibits tumor growth in the 4T1-Luc tumor-bearing mouse model.
| M.Wt | 315.38 | |
| Formula | C16H21N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Sravani Pulya, et al. J Med Chem. 2023 Sep 3. doi: 10.1021/acs.jmedchem.3c00614.
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