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GNE-3511 

Cat. No.: HY-12947 Purity: 99.85%
COA Handling Instructions

GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases.

For research use only. We do not sell to patients.

GNE-3511 Chemical Structure

GNE-3511 Chemical Structure

CAS No. : 1496581-76-0

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10 mM * 1 mL in DMSO USD 109 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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25 mg USD 165 In-stock
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50 mg USD 275 In-stock
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100 mg USD 495 In-stock
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Based on 5 publication(s) in Google Scholar

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Description

GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases[1].

IC50 & Target

Ki: 0.5 nM (DLK); IC50: 30 nM (p-JNK), 107 nM (DRG); >5000 nM (MKK4), >5000 nM (MKK7), 129 nM (JNK1),514 nM (JNK2), 364 nM (JNK3), 67.8 nM (MLK1), 767 nM (MLK2) and 602 nM (MLK3)[1]

In Vitro

GNE-3511 has inhibitory activity for p-JNK and DRG with IC50 values of 30 nM and 107 nM, respectively[1].
GNE-3511 has kinase selectivity for MKK4, MKK7, JNK1, JNK2, JNK3, MLK1, MLK2 and MLK3 with IC50 values of >5000 nM, >5000 nM, 129 nM, 514 nM, 364 nM, 67.8 nM, 767 nM and 602 nM, respectively[1].
GNE-3511 displays concentration-dependent protection of neurons from degeneration in vitro[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced nociceptive behavior by inhibiting DLK in mice[2].
GNE-3511 (oral gavage; 75 mg/kg; single) suppresses CYP-induced edema and hemorrhage in mouse bladder[2].
GNE-3511 (iv.; 1 mg/kg or po.; 5 mg/kg) exhibits moderate in vivo plasma clearances, moderate volumes of distribution, short half-lives, and brain penetration[2].
Pharmacokinetic Parameters of GNE-3511 (iv.; 1 mg/kg or po.; 5 mg/kg)[2].

species CLp (mL/min/kg Vdss (L/kg t1/2 (h) F (%) Bu/Pu CSF/Pu
mouse 56 2.5 0.6 45 0.24 at 6 h
rat 30 3.7 1.8 63 0.7 0.4
dog 41 6.5 4 32 0.4
cynomolgous 16 3.1 2.4 19 0.6

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Cystitis mouse model[1]
Dosage: 75 mg/kg
Administration: oral gavage;75 mg/kg; single
Result: Significantly reduced the number of nociceptive behavior as well as nociceptive score.
Had no impact on bladder weight, did not induce bladder edema or hemorrhage and significantly suppressed CYP-induced increase in bladder weight, bladder edema, and hemorrhage.
Animal Model: mouse, rat, cynomolgus and dog[2]
Dosage: 1 mg/k, 5 mg/kg
Administration: iv.; 1 mg/kg or po.; 5 mg/kg
Result: Exhibited moderate in vivo plasma clearances, moderate volumes of distribution, short half-lives and brain penetration.
Molecular Weight

440.49

Formula

C23H26F2N6O

CAS No.
SMILES

N#CC1=CC=NC(NC2=NC(N3CC(F)(F)CC3)=CC(C4CCN(C5COC5)CC4)=C2)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 31.25 mg/mL (70.94 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2702 mL 11.3510 mL 22.7020 mL
5 mM 0.4540 mL 2.2702 mL 4.5404 mL
10 mM 0.2270 mL 1.1351 mL 2.2702 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.85%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GNE-3511
Cat. No.:
HY-12947
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