GNE-3511 | DLK inhibitor | Probechem Biochemicals

Chemical Structure : GNE-3511

CAS No.: 1496581-76-0

GNE-3511 (GNE3511, GNE 3511)

Catalog No.: PC-43286Not For Human Use, Lab Use Only.

GNE-3511 is a potent, selective, orally bioavailable, brain-penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of <0.5 nM, displays >100-fold selectivity over MKK4/7, JNK1/2/3, MLK1/2/3.

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25 mg	$128	In stock
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Biological Activity

GNE-3511 (GNE3511) is a potent, selective, orally bioavailable, brain-penetrant dual leucine zipper kinase (DLK, MAP3K12) inhibitor with Ki of <0.5 nM, displays >100-fold selectivity over MKK4/7, JNK1/2/3, MLK1/2/3.

GNE-3511 also shows high affinity with Kd of 8.9 nM for leucine zipper-bearing kinase (LZK, MAP3K13).

GNE-3511 inhibits p-JNK with IC50 of 30 nM, displays concentration-dependent protection of neurons from degeneration in vitro (DRG IC50=107 nM).

GNE-3511 demonstrates dose-dependent activity in multiple animal models of neurodegenerative disease.

Physicochemical Properties

M.Wt	440.489
Formula	C23H26F2N6O
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	DMSO: ≥ 32 mg/mL
Chemical Name/SMILES	4-Pyridinecarbonitrile, 2-[[6-(3,3-difluoro-1-pyrrolidinyl)-4-[1-(3-oxetanyl)-4-piperidinyl]-2-pyridinyl]amino]-

References

1. Patel S, et al. J Med Chem. 2015 Jan 8;58(1):401-18.

GNE-3511 (GNE3511, GNE 3511)

Biological Activity

Physicochemical Properties

References

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