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Chemical Structure : GNE-431
Catalog No.: PC-62888Not For Human Use, Lab Use Only.
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.
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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.
GNE-431 shows higher selectivity for Btk than any of the covalent inhibitors or non-covalent analogs profiled.
GNE-431 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.
GNE-431 also shows excellent potency against the C481R, T474I, and T474M mutants (IC50=7.5-10 nM).
GNE-431 potently inhibits BCR signaling in stimulated human blood and blocks Btk autophosphorylation in C481S-transfected cells.
| M.Wt | 564.654 | |
| Formula | C30H32N10O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Johnson AR, et al. ACS Chem Biol. 2016 Oct 21;11(10):2897-2907.
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