ChemicalBook > CAS DataBase List > GSK 525762A

GSK 525762A

Product Name: GSK 525762A
CAS No.: 1260907-17-2
Chemical Name: GSK 525762A
Synonyms: I-BET-762;GSK525762;Molibresib;GSK 525762A;IBET762(GSK525762A);Molibresib (I-BET762;GSK525762 (I-BET-762);GSK 525762A USP/EP/BP;GSK 525762A (I-BET-762);Molibresib (GSK 525762A)
CBNumber: CB42627926
Molecular Formula: C22H22ClN5O2
Formula Weight: 423.9
MOL File: 1260907-17-2.mol

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GSK 525762A Property

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.

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1272
Product name: I-BET762
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $142.5
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML1272
Product name: I-BET762
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $297
Updated: 2025/07/31

Sigma-Aldrich

Product number: 5.06071
Product name: I-BET
Purity: InSolution<tmsymbol></tmsymbol>, ≥98%, 50 mM in DMSO, A cell-permeable benzodiazepine compound
Packaging: 5 mg
Price: $123
Updated: 2025/07/31

Sigma-Aldrich

Product number: 401010
Product name: I-BET - CAS 1260907-17-2 - Calbiochem
Packaging: 5MG
Price: $159
Updated: 2025/07/31

Cayman Chemical

Product number: 10676
Product name: I-BET762
Purity: ≥98%
Packaging: 1mg
Price: $32
Updated: 2024/03/01

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GSK 525762A Chemical Properties,Usage,Production

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 (K_d = 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.

Synthesis

1300019-38-8

75-04-7

1260907-17-2

Example 1: (S)-2-(6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)acetic acid (16.0 g, 40 mmol) was dissolved in THF, N,N-diisopropylethylamine (DIEA, 14 mL, 80 mmol) was added followed by 1-[bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxide hexafluorophosphate (HATU, 30.4 g, 80 mmol) was added. The reaction mixture was stirred at room temperature for 3 h. Then THF solution of ethylamine (40 mL, 2 M, 80 mmol) was added. Stirring was continued for 48 h. The reaction mixture was concentrated under reduced pressure. The crude product was suspended in water and extracted with dichloromethane (DCM). The organic layer was dried with anhydrous sodium sulfate (Na2SO4), filtered and concentrated under reduced pressure. The crude product was purified by silica gel column chromatography (DCM/MeOH, 95:5) and the resulting solid was recrystallized in acetonitrile (MeCN). Subsequently, the solid was dissolved in DCM and precipitated with diisopropyl ether (1-Pr2O) to afford (S)-2-(6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide (8 g, 47% yield) as a white solid. rf = 0.48 (DCM/MeOH, 90:10). Melting point >140°C (viscosity change).1H NMR (300 MHz, CDCl3) δ 7.53-7.47 (m, 2H), 7.39 (d, J = 8.9 Hz, 1H), 7.37-7.31 (m, 2H), 7.20 (dd, J = 2.9, 8.9 Hz, 1H), 6.86 (d, J = 2.9 Hz, 1H). 6.40 (m, 1H), 4.62 (m, 1H), 3.80 (s, 3H), 3.51 (dd, J = 7.3, 14.1 Hz, 1H), 3.46-3.21 (m, 3H), 2.62 (s, 3H), 1.19 (t, J = 7.3 Hz, 3H). lc/ms: m/z 424 [M(35Cl)+H]+. Retention time 2.33 min.

target

BET

storage

Store at -20°C

References

[1] EDWIGE NICODEME. Suppression of inflammation by a synthetic histone mimic[J]. Nature, 2010, 468 7327: 1119-1123. DOI:10.1038/nature09589
[2] OLIVIER MIRGUET*. Discovery of Epigenetic Regulator I-BET762: Lead Optimization to Afford a Clinical Candidate Inhibitor of the BET Bromodomains[J]. Journal of Medicinal Chemistry, 2013, 56 19: 7501-7515. DOI:10.1021/jm401088k
[3] HOZEFA S BANDUKWALA. Selective inhibition of CD4+ T-cell cytokine production and autoimmunity by BET protein and c-Myc inhibitors.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2012, 109 36: 14532-14537. DOI:10.1073/pnas.1212264109
[4] JAKE E DELMORE. BET bromodomain inhibition as a therapeutic strategy to target c-Myc.[J]. Journal of Chemical Theory and Computation, 2011: 904-917. DOI:10.1016/j.cell.2011.08.017

GSK 525762A Preparation Products And Raw materials

Raw materials

Preparation Products

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1260907-17-2, GSK 525762ARelated Search:

(+)-JQ-1 TRICHOSTATIN A GSK J1 2-N-HEXYL-4-PENTYNOIC ACID APICIDIN I-BET151 (GSK1210151A) RVX-208 OTX015 (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol BI 2536 PFI-1

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)

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

(S)-2-(6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo-[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4

Molibresib (GSK 525762A)

2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide

Molibresib

Molibresib (GSK525762) (I-BET762)

Molibresib (Synonyms: GSK 525762A

GSK 525762A USP/EP/BP

GSK525762A(Molibresib I-BET762)

Molibresib (I-BET762

I-BET762 I-BET-762 GSK-525762A

2-((4S)-6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide

I-BET762 (MOLIBRESIB) (GSK525762)

GSK 525762A|||GSK525762|||I-BET 762

Molibresib, 10 mM in DMSO

Molibresib (GSK 525762A, I-BET-762)

Molibresib (I-BET-762) ，S7189

(4S)-6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]-triazolo[4,3-a][1,4]benzodiazepin-4-acetamide

1260907-17-2

Inhibitors

Apis