Structure
GNE-049, inhibitor
GNE-049
Purity
98.00%
Synonyms
GNE-049; inhibitor
Purity/Purification
98.00%
Form/Format
Solid. Powder
Solubility
DMSO: 100mg/mL (195.86mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C27H32F2N6O2
SMILES
CC(N1CCC(N(C2CCOCC2)N=C3N4CCCC5=C4C=C(C(F)F)C(C6=CN(C)N=C6)=C5)=C3C1)=O
CAS Number
1936421-41-8
Target & IC50
CBP: ic50 1.1nM
BRET: ic50 12nM
BRD41: ic50 4200nM
BRET: ic50 12nM
BRD41: ic50 4200nM
In Vitro
GNE-049 shows acceptable PK in mouse, rat, dog, and monkey. GNE-049 is further evaluated in a rat single dose (30-250mg/kg QD) toxicokinetic study. GNE-049 is selective for CBP/P300 and, importantly, quite selective (3820-fold) over BRD4(1), which revealed from the Determination of potency versus a selection of bromodomains. Furthermore, at the 250mg/kg dose level, the ratio of the unbound drug concentration in the brain to unbound drug concentration in plasma (Kp,uu) 3 hours post-dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity.
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
-80 degree C for 2 years in solvent
Structure
Structure
Related Product Information for GNE-049, inhibitor
GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12nM and 4200nM, respectively).
Product Categories/Family for GNE-049, inhibitor
References
Romero FA, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem. 2017 Nov 22;60(22):9162-9183.
Romero FA, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem. 2017 Nov 22;60(22):9162-9183.
Romero FA, et al. GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP). J Med Chem. 2017 Nov 22;60(22):9162-9183.
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Product Notes
The GNE-049 (Catalog #AAA5754908) is an Inhibitor and is intended for research purposes only. The product is available for immediate purchase. It is sometimes possible for the material contained within the vial of "GNE-049, Inhibitor" to become dispersed throughout the inside of the vial, particularly around the seal of said vial, during shipment and storage. We always suggest centrifuging these vials to consolidate all of the liquid away from the lid and to the bottom of the vial prior to opening. Please be advised that certain products may require dry ice for shipping and that, if this is the case, an additional dry ice fee may also be required.Precautions
All products in the AAA Biotech catalog are strictly for research-use only, and are absolutely not suitable for use in any sort of medical, therapeutic, prophylactic, in-vivo, or diagnostic capacity. By purchasing a product from AAA Biotech, you are explicitly certifying that said products will be properly tested and used in line with industry standard. AAA Biotech and its authorized distribution partners reserve the right to refuse to fulfill any order if we have any indication that a purchaser may be intending to use a product outside of our accepted criteria.Disclaimer
Though we do strive to guarantee the information represented in this datasheet, AAA Biotech cannot be held responsible for any oversights or imprecisions. AAA Biotech reserves the right to adjust any aspect of this datasheet at any time and without notice. It is the responsibility of the customer to inform AAA Biotech of any product performance issues observed or experienced within 30 days of receipt of said product. To see additional details on this or any of our other policies, please see our Terms & Conditions page.Item has been added to Shopping Cart
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