GNE-431

Modify Date: 2024-04-12 12:01:40

GNE-431 Structure
GNE-431 structure
Common Name GNE-431
CAS Number 1433820-83-7 Molecular Weight 564.654
Density N/A Boiling Point N/A
Molecular Formula C30H32N10O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GNE-431


GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM and 2.5 nM for WT Btk and C481S mutant, respectively; shows higher selectivity for Btk than any of the covalent inhibitors or non-covalent analogs profiled; does not interact with Cys481 and differs from covalent inhibitors like ibrutinib, potently inhibits the ibrutinib-resistant Btk C481S mutant in vitro and in cells; also shows excellent potency against the C481R, T474I, and T474M mutants (IC50=7.5-10 nM); potently inhibits BCR signaling in stimulated human blood and blocks Btk autophosphorylation in C481S-transfected cells.

 Names

Name GNE-431

 GNE-431 Biological Activity

Description GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM and 2.5 nM for WT Btk and C481S mutant, respectively; shows higher selectivity for Btk than any of the covalent inhibitors or non-covalent analogs profiled; does not interact with Cys481 and differs from covalent inhibitors like ibrutinib, potently inhibits the ibrutinib-resistant Btk C481S mutant in vitro and in cells; also shows excellent potency against the C481R, T474I, and T474M mutants (IC50=7.5-10 nM); potently inhibits BCR signaling in stimulated human blood and blocks Btk autophosphorylation in C481S-transfected cells.
References References 1. Johnson AR, et al. ACS Chem Biol. 2016 Oct 21;11(10):2897-2907. View Related Products by Target BTK

 Chemical & Physical Properties

Molecular Formula C30H32N10O2
Molecular Weight 564.654
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