Product Details
| Product Name:
GNE-049 |
CAS No.:
1936421-41-8 |
| Purity:
98.67% |
Supply Ability:
10g |
| Release date:
2025/10/27 |
Product Introduction
Bioactivity
| Name | GNE-049 |
| Description | GNE-049 is a highly selective and potent inhibitor designed to target the CREB-binding protein (CBP) with high affinity, exhibiting an IC50 of 1.1 nM for the suppression of BRET and BRD4 activity, which consequently blocks prostate cancer cell proliferation in both in vitro and in vivo models. |
| In vitro | GNE-049 performs well in BRET cell assays and, in an orthogonal targeted assay, inhibits MYC expression (MV4-11 cell line) with an EC50 of 14 nM.[1]
CBPD-409 induced strong degradation of CBP/p300 by DC 500.2-0.4 nM and exhibited strong antiproliferative effects with IC50 of 1.2-2.0 nM in VCaP, LNCaP, and 22Rv1 AR+ prostate cancer cell lines. [2] |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 80 mg/mL (156.68 mM), Sonication is recommended.
|
| Keywords | GNE-049 | GNE 049 | EpigeneticReaderDomain | Epigenetic Reader Domain | CBP | BRET | BRD41 |
| Inhibitors Related | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Acetaminophen | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin | GSK1379725A |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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