GNA002
- CAS No.
- 1385035-79-9
- Chemical Name:
- GNA002
- Synonyms
- G002;GNA002;GNA002,GNA-002;2-Butenamide, 4-[(1R,3aS,5S,12aS)-9-[(2E)-3,7-dimethyl-2,6-octadien-1-yl]-3a,4,5,7-tetrahydro-8,10-dihydroxy-3,3-dimethyl-11-(3-methyl-2-buten-1-yl)-7,13-dioxo-1,5-methano-1H,3H-furo[3,4-d]xanthen-1-yl]-N-(2-ethoxyethyl)-2-methyl-, (2Z)-
- CBNumber:
- CB44667948
- Molecular Formula:
- C42H55NO8
- Molecular Weight:
- 701.9
- MDL Number:
- MFCD32174245
- MOL File:
- 1385035-79-9.mol
- MSDS File:
- SDS
- TDS File:
- TDS
GNA002 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Biosynth | KFC03579 | GNA002 | 1385035-79-9 | 1mg | $540.72 | 2026-06-04 | Buy |
| Biosynth | KFC03579 | GNA002 | 1385035-79-9 | 2mg | $831.88 | 2026-06-04 | Buy |
| Biosynth | KFC03579 | GNA002 | 1385035-79-9 | 5mg | $1247.8 | 2026-06-04 | Buy |
| ChemScene | CS-0021611 | GNA002 98.02% | 1385035-79-9 | 1mg | $412 | 2026-06-04 | Buy |
| ChemScene | CS-0021611 | GNA002 98.02% | 1385035-79-9 | 5mg | $1029 | 2026-06-04 | Buy |
GNA002 Chemical Properties, Uses, Production
Description
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor. It can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination.
Uses
GNA002 is a highly potent, specific and covalent EZH2 (Enhancer of zeste homolog 2) inhibitor with an IC50 of 1.1 μM. GNA002 can specifically and covalently bind to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination. GNA002 efficiently reduces EZH2-mediated H3K27 trimethylation, reactivates polycomb repressor complex 2 (PRC2)-silenced tumor suppressor genes[1].
in vivo
GNA002 (oral administration; 100 mg/kg; daily) significantly decreases the volumes of Cal-27-derived tumors and reduces H3K27Me3 levels in tumor tissues. GNA002 also significantly suppresses the in vivo tumor growth derived from the xenografted A549 lung cancer cells, Daudi and Pfeiffer cells. GNA002 inhibits the aberrant oncogenic functions of EZH2, thus inhibiting tumor growth in vivo, at least in the xenograft experimental model[1].
| Animal Model: | Male BALB/C Nude mice aged 30-35 days and weighing 18-22 g, bearing Cal-27 xenograft tumors[1] |
| Dosage: | 100 mg/kg |
| Administration: | Oral administration; daily |
| Result: | Decreased the size and weight of tumors formed by Cal-27 cells. |
IC 50
EZH2: 1.1 μM (IC50)
References
[1] Wang X, et al. A covalently bound inhibitor triggers EZH2 degradation through CHIP-mediated ubiquitination. EMBO J. 2017 May, 36(9):1243-1260. DOI:10.15252/embj.201694058
GNA002 Preparation Products And Raw materials
Raw materials
Preparation Products
GNA002 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| BOC Sciences | 1-631-485-4226; 16314854226 | info@bocsci.com | United States | 9920 | 65 |
| Sichuan Wei Keqi Biological Technology Co., Ltd. | 028-81700200 18116577057 | 3003855609@qq.com | China | 7717 | 56 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32431 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6288 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11123 | 58 |
| TargetMol Chemicals Inc. | 4008200310 15002144251 | marketing@tsbiochem.com | China | 24951 | 58 |
| Nanjing Shizhou Biology Technology Co.,Ltd | 025-85560043 15850508050 | cindy.huang@synzest.com | China | 11975 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9831 | 58 |
| TargetMol Chemicals Inc. | 13564774135 | marketing@targetmol.com | United States | 19950 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 38999 | 58 |
