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GSK1324726A - CAS 1300031-52-0

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Catalog Number	Size	Price	Stock	Quantity
BP-300137	100 mg	$599	In stock

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GSK1324726A is a novel, potent and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50 = 41 nM), BRD3 (IC50 = 31 nM), and BRD4 (IC50 = 22 nM).

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Molecular Formula

C25H23ClN2O3

Molecular Weight

434.91

GSK1324726A

- Specification
  - Purity
    
    >98%
    
    IUPAC Name
    
    4-[(2S,4R)-1-acetyl-4-(4-chloroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoic acid
    
    Synonyms
    
    I-BET-726; I-BET 726; I-BET726; GSK-1324726A; GSK 1324726A
- Properties
  - InChI Key
    
    FAWSUKOIROHXAP-NPMXOYFQSA-N
    
    InChI
    
    InChI=1S/C25H23ClN2O3/c1-15-13-23(27-21-10-8-20(26)9-11-21)22-14-19(7-12-24(22)28(15)16(2)29)17-3-5-18(6-4-17)25(30)31/h3-12,14-15,23,27H,13H2,1-2H3,(H,30,31)/t15-,23+/m0/s1
    
    Canonical SMILES
    
    CC1CC(C2=C(N1C(=O)C)C=CC(=C2)C3=CC=C(C=C3)C(=O)O)NC4=CC=C(C=C4)Cl
- Reference Reading
  - 1.The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
    
    Gosmini R1, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicod J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24.
    
    Through their function as epigenetic readers of the histone code, the BET family of bromodomain-containing proteins regulate expression of multiple genes of therapeutic relevance, including those involved in tumor cell growth and inflammation. BET bromodomain inhibitors have profound antiproliferative and anti-inflammatory effects which translate into efficacy in oncology and inflammation models, and the first compounds have now progressed into clinical trials. The exciting biology of the BETs has led to great interest in the discovery of novel inhibitor classes. Here we describe the identification of a novel tetrahydroquinoline series through up-regulation of apolipoprotein A1 and the optimization into potent compounds active in murine models of septic shock and neuroblastoma. At the molecular level, these effects are produced by inhibition of BET bromodomains. X-ray crystallography reveals the interactions explaining the structure-activity relationships of binding.
- Preparing Stock Solutions
  - ConcentrationVolumeMass 1 mg 5 mg 10 mg
    
    1 mM 2.2993 mL 11.4966 mL 22.9933 mL
    
    5 mM 0.4599 mL 2.2993 mL 4.5987 mL
    
    10 mM 0.2299 mL 1.1497 mL 2.2993 mL
    
    50 mM 0.0460 mL 0.2299 mL 0.4599 mL

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	2.2993 mL	11.4966 mL	22.9933 mL
5 mM	0.4599 mL	2.2993 mL	4.5987 mL
10 mM	0.2299 mL	1.1497 mL	2.2993 mL
50 mM	0.0460 mL	0.2299 mL	0.4599 mL

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