GSK8814

SKU HY-114204-10 mg Category Tags , ,

$460$780

Products Details

Product Description

– GSK8814 is a potent, selective, and ATAD2/2B bromodomain chemical probe and inhibitor, with a binding constant pKd=8.1 and a pKi=8.9 in BROMOscan. GSK8814 binds to ATAD2 and BRD4 BD1 with pIC50s of 7.3 and 4.6, respectively. GSK8814 shows 500-fold selectivity for ATAD2 over BRD4 BD1[1].

Web ID

– HY-114204

Storage Temperature

– -20°C, 3 years (Powder)

Shipping

– Blue Ice

Applications

– Cancer-programmed cell death

Molecular Formula

– C28H35F2N5O3

References

– [1]Bamborough P, et al. A Chemical Probe for the ATAD2 Bromodomain. Angew Chem Int Ed Engl. 2016 Sep 12;55(38):11382-6.|[2]Bamborough P, et al. Aiming to Miss a Moving Target: Bromo and Extra Terminal Domain (BET) Selectivity in Constrained ATAD2 Inhibitors. J Med Chem. 2018 Sep 27;61(18):8321-8336.

CAS Number

– 1997369-78-4

Molecular Weight

– 527.61

Compound Purity

– 99.60

SMILES

– O=C1NC2=C(N[C@H]3[C@H](OCC4CCC(F)(F)CC4)CNC[C@@H]3OC)N=CC(C5=CC(C)=CN=C5)=C2C=C1C

Clinical Information

– No Development Reported

Research Area

– Cancer

Solubility

– DMSO : 100 mg/mL (ultrasonic)

Target

– Epigenetic Reader Domain

Isoform

– BRD4

Pathway

– Epigenetics

Product type

– Reference compound

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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