GSK973

CAT: 0804-HY-138563-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-138563-01Size:5 mg
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Description
GSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5) [1].
CAS Number
[2138473-38-6]
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/gsk973.html
Purity
99.97
Solubility
DMSO : 125 mg/mL (ultrasonic)
Smiles
[H][C@]1([C@@H]2NC(C3=CC(C(NC)=O)=C4C([C@@H]([C@H](O4)CF)C5=CC=CC=C5)=C3)=O)[C@]2([H])COC1
Molecular Formula
C23H23FN2O4
Molecular Weight
410.44
References & Citations
[1]Preston A, et al. GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family. ACS Med Chem Lett. 2020;11 (8) :1581-1587. Published 2020 Jul 6.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
BRD2; BRD3; BRD4; BRDT

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