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SynKinase
I-BET762
114
CHF
CHF 114.00
In stock
SYN-3033-M0011 mgCHF 114.00
SYN-3033-M0055 mgCHF 170.00
SYN-3033-M01010 mgCHF 227.00
SYN-3033-M05050 mgCHF 639.00
SYN-3033-M100100 mgCHF 1'022.00
| Product Details | |
|---|---|
| Synonyms | GSK-525762A |
| Product Type | Chemical |
| Properties | |
| Formula | C22H22ClN5O2 |
| MW | 423.9 |
| CAS | 1260907-17-2 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data | Target: BRD2, BRD3, and BRD4 | Kinase Group: N/A | Substrate: N/A |
| InChi Key | AAAQFGUYHFJNHI-SFHVURJKSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS | Inquire |
| Product Specification Sheet | |
| Datasheet |
 Download PDF |
Description
I-BET762 (GSK525762A) is an inhibitor for BET (bromodomain and extra terminal domain) proteins, BRD2, BRD3 and BRD4. It binds to the tandem bromodomains of BET with a Kd of 50.5-61.3nM, displaces a tetra-acetylated H4 peptide prebound to tandem bromodomains of BET with IC50 of 32.5-42.5nM in FRET analysis. I-BET762 disrupts the formation of the chromatin complexes essential for expression of inflammatory genes.
Product References
- Suppression of inflammation by a synthetic histone mimic: E. Nicodeme, et al.; Nature 468, 1119 (2010)
- Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors: H.S. Bandukwala, et al.; PNAS 109, 14532 (2012)