Name: GSK1324726A
Brand: BOC Sciences
Price: 599 USD
Availability: MadeToOrder

Size

Price

Stock

Quantity

100 mg

$599

In stock

Purity

>98%

IUPACName

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

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

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.

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

Good morning! Can GSK1324726A be used in vivo?

Oral administration of GSK1324726A to mouse xenograft models of human neuroblastoma results in tumor growth inhibition and down-regulation MYCN and BCL2 expression.

2/5/2018

Do you have any information on its activity in vitro?

A panel of neuroblastoma cell lines are treated with GSK1324726A, and observed potent growth inhibition and cytotoxicity in most cell lines irrespective of MYCN copy number or expression level. All neuroblastoma cell lines tested exhibit potent growth inhibition, with a median growth IC50 value (gIC50; inhibitor concentration resulting in 50% growth inhibition) equal to 75 nM.

11/4/2021

I want to know the solubility of GSK1324726A. Thank you.

Insoluble in water; ≥1.87 mg/mL, ethanol solution, mild heating and ultrasound; ≥17.7 mg/mL in DMSO.

12/10/2022

inhibit neuroblastoma tumor growth

GSK1324726A performed well at inhibiting neuroblastoma tumor growth in my lab.

26/3/2016

downregulate BRD4-regulated proteins

In my research, GSK1324726A not only downregulated BRD4-regulated proteins (c-Myc, Bcl-2, and cyclin D1), but also inhibited sphingosine kinase 1 (SphK1) and Akt signalings in SCC cells. Satisfied with product.

19/9/2019

induce significant apoptosis activation

In our study, GSK1324726A plays key role in inducing significant apoptosis activation in skin squamous cell carcinoma (SCC) cells.

28/10/2022

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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂