2. MAPK/ERK Pathway
  3. JNK
  4. DN-1289

DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability.

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DN-1289 Chemical Structure

DN-1289 Chemical Structure

CAS No. : 3026597-15-6

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Based on 1 publication(s) in Google Scholar

DN-1289 Related Antibodies

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Description

DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability[1].

IC50 & Target

IC50: 17 nM (DLK), 40 nM (LZK)[1]
In Vitro

DN-1289 (compound 14) (0.1, 0.3, and 1 μM; 0-20 h) can block axon degeneration in dorsal root ganglion (DRG) neurons induced by nerve growth factor (NGF) withdrawal[1].
DN-1289 (0.1, 0.3, and 1 μM; 0-20 h) inhibits the activation of caspases in DRG neurons over time induced by NGF withdrawal[1].

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

DN-1289 Related Antibodies
In Vivo

DN-1289 (compound 14) (100 mg/kg and 150 mg/kg; i.p.; once daily for 10-15 d) is well-tolerated in mice model[1].
DN-1289 (150 mg/kg; p.o.; b.i.d. for 10 d) inhibits phosphorylation of c-Jun in an acute injury model with optic nerve crush (ONC) application[1].

Pharmacokinetic Analysis[1]

Species Route Dose (mg/kg) plasma Cmax (μM) plasma AUC0-24 h (μM·h) CLp (mL/min/kg) CLu (mL/min/kg) Vd (L/kg) t1/2 (h) F (%) Kpuu (AUC) brain AUC0-2 h (μM·h)
rat IV 1 1.09 2.42 14.7 150 6.7 6.5 / 0.6 4.05
PO 3 0.58 3.9 / / / 4.6 52 / /
mouse IV 1 1.06 4.06 8.6 200 4.7 6.8 / / /
PO 10 2.32 21.9 / / / 7.9 56 0.4 6.91
PO 150 24.9 324 / / / 23.7 53 / /
IP 100 15.4 280 / / / 23.7 53 / /
cyno IV 0.5 0.746 2.79 6.1 64 3.4 7.9 / / /

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

441.38

Formula

C18H19F4N7O2
CAS No.
SMILES

NC1=C(OC(F)F)N=C(C2=NC(N3[C@@H](C4)CO[C@@H]4C3)=NC(N5CCC(F)(F)C5)=C2)C=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DN-1289 Related Classifications

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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.

Keywords:

DN-12893026597-15-6DN1289DN 1289JNKc-Jun N-terminal kinaseInhibitorinhibitorinhibit

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