GSK620 | BD2 selective BET inhibitor

CAS:
 2088410-46-0
Catalog Number:
 10-4180

Available Options

SizePriceQuantity 
5mg$60.00
25mg$225.00

GSK620 (2088410-46-0) is a BET inhibitor 220-fold more selective for BD2 over BD1 (pIC50 BD2 = 7.1; BD1 = 4.8).1 It ameliorated collagen-induced arthritis in a rat model and imiquimod-induced psoriasis in a mouse model.GSK620 was also able to reduce hepatic fibrosis, steatosis, and inflammation in a mouse model of non-alcoholic steatohepatitis (NASH).

References/Citations:

  1. Seal et al. (2020), The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor; J. Med. Chem., 63 9093
  2. Gilan et al. (2020), Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation; Science, 368 387
CAS:
2088410-46-0
Catalog Number:
10-4180
Activity:
BD2 selective BET inhibitor
Chemical Names:
1-Benzyl-5-N-cyclopropyl-3-N-methyl-2-oxopyridine-3,5-dicarboxamide
Molecular Weight:
325.37
Molecular Formula:

C18H19N3O3

Solubility:
Soluble in DMSO (25 mg/ml)
Physical Properties:
White solid
Purity:

>98% HPLC
NMR (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee