GNE-431
Modify Date: 2025-08-22 11:02:27
GNE-431 structure
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Common Name | GNE-431 | ||
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| 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-431GNE-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. |
| Name | GNE-431 |
|---|
| 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. |
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| References | References 1. Johnson AR, et al. ACS Chem Biol. 2016 Oct 21;11(10):2897-2907. View Related Products by Target BTK |
| Molecular Formula | C30H32N10O2 |
|---|---|
| Molecular Weight | 564.654 |
| InChIKey | XCTHZVUJRUQEGV-UHFFFAOYSA-N |
| SMILES | CN1CCn2nc(Nc3cc(-c4ccnc(N5CCn6c(cc7c6CCCC7)C5=O)c4CO)nn4ccnc34)cc2C1 |