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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
 $161.00
1/EA		 Add To Favorites
45-SML1272-25MG 25 mg
 $637.00
1/EA		 Add To Favorites
This picture is provided solely for illustration purposes, it may have been created or edited with AI. Optical properties of the actual product may deviate. Relevant product information is printed on labeled products and other accompanying or available information material.
This image depicts SML1272-5MG.

 

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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