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GSK8814

CAT: 0804-HY-114204-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-114204-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
GSK8814 is a potent and selective ATAD2 bromodomain chemical probe and inhibitor (IC50 = 0.059 μM), 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. GSK8814 can be researched for cancer associated with ATAD2 bromodomain[1][2][3].
CAS Number
1997369-78-4
Product Name Alternative
RU-42932
UNSPSC
12352005
Target
Epigenetic Reader Domain
Type
Reference compound
Related Pathways
Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/gsk8814.html
Purity
99.80
Solubility
DMSO : 100 mg/mL (ultrasonic)
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
Molecular Formula
C28H35F2N5O3
Molecular Weight
527.61
References & Citations
[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.|[3]Yao, D., et al., (2023) . Fragment-based design, synthesis and biological evaluation of theophylline derivatives as ATAD2 inhibitors in BT-549 cells. Journal of enzyme inhibition and medicinal chemistry, 38 (1), 2242601.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
BRD4

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