Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | 8-10 weeks | $ 523.00 | |
25 mg | 8-10 weeks | $ 1,750.00 | |
50 mg | 8-10 weeks | $ 2,280.00 | |
100 mg | 8-10 weeks | $ 3,270.00 |
Description | GNE-049 is a highly potent and selective inhibitor of CBP (IC50: 1.1 nM in TR-FRET assay). GNE-049 also inhibits BRET and BRD4(1) (IC50s: 12 nM and 4200 nM, respectively). |
Targets&IC50 | BRD41:4200 nM, CBP:1.1 nM, BRET:12 nM |
In vitro | GNE-049 inhibits the expression of MYC (EC50: 14 nM). GNE-049 has excellent potency in the BRET cellular assay and, in an orthogonal measure of the target engagement. GNE-049 is selected for further profiling as it has the best balance of liver microsomes (LM) stability, selectivity, and cellular potency. |
In vivo | GNE-049 shows acceptable PK in mouse, rat, dog, and monkey. GNE-049 is further evaluated in a rat single dose (30-250 mg/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 250 mg/kg dose level, the ratio of the unbound drug concentration in the brain to unbound drug concentration in plasma (Kp,uu) 3 h post-dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity. |
Molecular Weight | 510.58 |
Formula | C27H32F2N6O2 |
CAS No. | 1936421-41-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (195.86 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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GNE-049 1936421-41-8 Chromatin/Epigenetic Epigenetic Reader Domain GNE 049 GNE049 inhibitor inhibit