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GNE-049

Cat. No. M13820
GNE-049 Structure
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Quality Control & Documentation
Biological Activity

GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.

Chemical Information
Molecular Weight 510.58
CAS Number 1936421-41-8
Solubility (25°C) DMSO 90 mg/mL
Storage -20°C, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Aaron Waddell, et al. Cancers (Basel). Pharmacological Inhibition of CBP/p300 Blocks Estrogen Receptor Alpha (ERα) Function through Suppressing Enhancer H3K27 Acetylation in Luminal Breast Cancer

[2] Irena Hlushchuk, et al. ACS Chem Neurosci. Domain-Independent Inhibition of CBP/p300 Attenuates α-Synuclein Aggregation

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  Catalog
Abmole Inhibitor Catalog




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