| Identification | Back Directory | [Name]
GSK 525762A | [CAS]
1260907-17-2 | [Synonyms]
GSK525762
I-BET-762
Cibinetide
Molibresib
GSK 525762A
IBET762(GSK525762A)
Molibresib (I-BET762
GSK 525762A USP/EP/BP
GSK525762 (I-BET-762)
GSK 525762A (I-BET-762)
Molibresib (GSK 525762A)
GSK525762A(Molibresib I-BET762)
Molibresib (GSK525762) (I-BET762)
Molibresib (Synonyms: GSK 525762A
(S)-2-(6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo-[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4
(4S)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide
4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4S)-
2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide
(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 | [Molecular Formula]
C22H22ClN5O2 | [MDL Number]
MFCD22417091 | [MOL File]
1260907-17-2.mol | [Molecular Weight]
423.895 |
| Chemical Properties | Back Directory | [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) | [form ]
powder | [pka]
15.71±0.46(Predicted) | [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. |
| Hazard Information | Back Directory | [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.1,2 I-BET762 is a synthetic compound which interacts with BET proteins with high-affinity (Kd = 32.5-42.5 nM).3,4 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.3 Through these actions, I-BET762 provides protection against bacteria-induced sepsis and lipopolysaccharide-triggered endotoxic shock.3 | [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 |
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