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Chemical Structure : DUAL946
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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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.
| M.Wt | 552.67 | |
| Formula | C30H40N4O6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Stephen J. Atkinson, et al. MedChemComm (2014), 5 (3), 342-351.
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