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| | GSK 525762A Basic information |
| Product Name: | GSK 525762A | | Synonyms: | I-BET-762;GSK 525762A (I-BET-762);GSK525762 (I-BET-762);GSK525762;4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4S)-;(4S)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide GSK 525762A I-BET-762;GSK 525762A (4S)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide;IBET762(GSK525762A) | | CAS: | 1260907-17-2 | | MF: | C22H22ClN5O2 | | MW: | 423.9 | | EINECS: | | | Product Categories: | Inhibitors;Apis | | Mol File: | 1260907-17-2.mol |  |
| | GSK 525762A Chemical Properties |
| Melting point | >132°C (dec.) | | density | 1.35 | | storage temp. | 2-8°C | | solubility | Soluble in DMSO (up to at least 25 mg/ml) or in Ethanol (up to at least 25 mg/ml) | | pka | 15.71±0.46(Predicted) | | form | powder | | color | white to beige | | optical activity | [α]/D +80 to +90°, c = 0.3 in methanol | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| | GSK 525762A Usage And Synthesis |
| Description | The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, affect inflammatory gene expression by controlling the assembly of histone acetylation-dependent chromatin complexes. I-BET762 is a synthetic compound which interacts with BET proteins with high-affinity (Kd = 32.5-42.5 nM). It blocks binding of BET proteins with acetylated histones, disrupting the formation of chromatin complexes involved in the expression of specific inflammatory genes in activated macrophages. Through these actions, I-BET762 provides protection against bacteria-induced sepsis and lipopolysaccharide-triggered endotoxic shock. | | Uses | GSK 525762A, is a BET Bromodomain Inhibitor, which is now in clinical development. BET bromodomains have emerged as promising drug targets for treatment of cancers, inflammatory diseases, and other medical conditions. | | Definition | ChEBI: 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide is a benzodiazepine. | | Biochem/physiol Actions | I-BET762 possesses anti-inflammatory property by controlling the pro-inflammatory gene expression. I-BET762 hinders the MYC (proto-oncogene) expression in cellular models. This action of I-BET762 might serve as an effective therapy in treating prostate cancer. | | target | BET | | storage | Store at -20°C | | References | 1) Nicodeme?et al.?(2010),?Suppression of inflammation by a synthetic histone mimic; Nature?468?1119
2) Mirguet?et al.?(2013),?Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains; J. Med. Chem.,?56?7501
3) Bandukwala?et al.?(2012),?Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors; Proc. Natl. Acad. Sci. USA,?109?14532
4) Delmore?et al.?(2011),?BET Bromodomain as a Therapeutic Strategy to Target c-Myc; Cell?146?904 |
| | GSK 525762A Preparation Products And Raw materials |
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