Chemical Structure : class I HDACs inhibitor JT86
CAS No.:
2708136-83-6
class I HDACs inhibitor JT86
Catalog No.: PC-25167Not For Human Use, Lab Use Only.
class I HDACs inhibitor JT86 is a potent class I HDACs inhibitor with IC50 of 0.72/8.0/2.0 nM for HDAC1/2/3 respectively, 61-fold selectivity over HDAC8 (IC50 44 nM) and 11-fold over HDAC2.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
class I HDACs inhibitor JT86 is a potent class I HDACs inhibitor with IC50 of 0.72/8.0/2.0 nM for HDAC1/2/3 respectively, 61-fold selectivity over HDAC8 (IC50 44 nM) and 11-fold over HDAC2.
JT86 is much less active against the class IIa enzyme HDAC7.
JT86 shows potent cytotoxic effect (IC50= 0.02-0.1 μM) across the five cancer cell lines with 15- to 23-fold increased potency over AR-42.
JT86 induces concentration-dependent accumulation of acetylated histone H4 in MM96L melanoma cells, indicating inhibition of endogenous HDAC1.
Physicochemical Properties
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M.Wt
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390.44
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Formula
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C23H22N2O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(4-(Hydroxycarbamoyl)phenyl)-4-(naphthalen-2-yl)tetrahydro-2H-pyran-4-carboxamide
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References
1. Jiahui Tng, et al. J Med Chem. 2020 Jun 11;63(11):5956-5971.
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