Chemical Structure : DUAL946
CAS No.:
1868180-45-3
DUAL946
(DUAL 946)
Catalog No.: PC-21726Not For Human Use, Lab Use Only.
DUAL946 is a sub-micromolar inhibitor of both BET and class I & IIb HDAC proteins with IC50 of 0.05/0.25/0.42/14.13/34.89 uM for BRD4/HDAC1/HDAC2/HDAC5/HDAC7/HDAC9, respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
DUAL946 is a sub-micromolar inhibitor of both BET and class I & IIb HDAC proteins with IC50 of 0.05/0.25/0.42/14.13/34.89 uM for BRD4/HDAC1/HDAC2/HDAC5/HDAC7/HDAC9, respectively.
DUAL946 shows an equilibrium binding constant of 57 nM against the BRD4 WT tandem bromodomains and 53 nM versus BRD4-BD2.
DUAL946 engaged BET and HDAC dependent mechanisms in an NMC cell line, as demonstrated by down regulation of c-myc expression levels and an increase on acetylation of histone H4, respectively.
DUAL946 also inhibited growth in NMC and AML cells.
Physicochemical Properties
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M.Wt
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552.67
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Formula
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C30H40N4O6
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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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isopropyl ((2S,4R)-1-acetyl-6-(4-(8-(hydroxyamino)-8-oxooctanamido)phenyl)-2-methyl-1,2,3,4-tetrahydroquinolin-4-yl)carbamate
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References
1. Stephen J. Atkinson, et al. MedChemComm (2014), 5 (3), 342-351.
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