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I-BET762

SIGMA/SML1272 - ≥98% (HPLC)

Synonym: (4S)- 6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide; GSK525762; GSK525762A; I-BET

CAS Number: 1260907-17-2
Empirical Formula (Hill Notation): C22H22ClN5O2
Molecular Weight: 423.90
MDL Number: MFCD22417091
Linear Formula: C22H22ClN5O2
Product Type: Chemical
Catalog Number PKG Qty. Price Quantity
45-SML1272-5MG 5 mg
 $150.00
1/EA		 Add To Favorites
45-SML1272-25MG 25 mg
 $594.00
1/EA		 Add To Favorites

 

assay ≥98% (HPLC)
color white to beige
drug control regulated under CDSA - not available from Sigma-Aldrich Canada
form powder
InChI 1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1
InChI key AAAQFGUYHFJNHI-SFHVURJKSA-N
optical activity [α]/D +80 to +90°, c = 0.3 in methanol
Quality Level 100 
SMILES string CCNC(C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C3=CC(OC)=CC=C3N4C1=NN=C4C)=O
solubility DMSO: 10 mg/mL, clear
storage temp. 2-8°C
Biochem/physiol Actions: I-BET762 (GSK525762) is a selective inhibitor of bromodomain and extra terminal (BET) domain proteins BRD2, BRD3 and BRD4 with IC50 values of 32.5–42.5 nM and no interaction with other bromodomain-containing proteins. I-BET mimicks acetylated histone, preventing the protein-protein interaction between acetyl-lysines and the BET reader protein. This was shown to block expression of inflammatory genes in activated macrophages and confer protection against endotoxic shock and bacterial sepsis. I-BET762 also showed potent anti-myeloma activity in vitro and in vivo.
Biochem/physiol Actions: I-BET762 is a selective inhibitor of bromodomain and extra terminal (BET) domain proteins; synthetic histone mimic.
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.
Packaging: 5, 25 mg in glass bottle
RIDADR NONH for all modes of transport
WGK Germany WGK 3
Flash Point(F) Not applicable
Flash Point(C) Not applicable
Purity ≥98% (HPLC)
Storage Temp. 2-8°C
UNSPSC 12352200

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