GSK620|CAS 2088410-46-0|DC Chemicals

Cas No.:	2088410-46-0
Chemical Name:	GSK620
Synonyms:	GSK620;GSK-620;GSK 620
SMILES:	O=C(C1=CC(C(NC2CC2)=O)=CN(CC3=CC=CC=C3)C1=O)NC
Formula:	C₁₈H₁₉N₃O₃
M.Wt:	325.36
Sotrage:	Please store the product under the recommended conditions in the Certificate of Analysis.
Publication:	[1]. Seal JT, et al. 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. 2020;63(17):9093-9126.

Description:

GSK620 is a potent and orally active pan-BD2 with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.

MSDS

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MSDS_25907_DC42300_2088410-46-0

COA

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Cat. No.	Product name	Field of application
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DC47977	I-BET567	I-BET567 is a potent and oral active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.
DC47894	SR-0813	SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia.
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DC42491	GSK778（iBET-BD1 dihydrochloride）	GSK778 (iBET-BD1) is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.
DC42300	GSK620	GSK620 is a potent and orally active pan-BD2 with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620
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