Dehydrocrenatidine
Dehydrocrenatidine Basic information
- Product Name:
- Dehydrocrenatidine
- Synonyms:
-
- Dehydrocrenatidine
- 9H-Pyrido[3,4-b]indole, 1-ethenyl-4,8-dimethoxy-
- 1-ethenyl-4,8-dimethoxy-9H-pyrido[3,4-b]indole
- TOP 3
- TOP3
- TOP-3
- O-Methylpicrasidine I
- CAS:
- 65236-62-6
- MF:
- C15H14N2O2
- MW:
- 254.28
- Mol File:
- 65236-62-6.mol
Dehydrocrenatidine Chemical Properties
- form
- Solid
- color
- Off-white to light yellow
Dehydrocrenatidine Usage And Synthesis
Uses
Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain[1][2].
in vivo
Dehydrocrenatidine inhibits JAK-STAT3 dependent DU145 and MDA-MB-468 cell survival and induces cell apoptosis. Dehydrocrenatidine inhibits JAKs-JH1 domain over-expression induced STAT3 and STAT1 phosphorylations[1].
Dehydrocrenatidine diminishes IL-6, IFNα and IFNγ stimulated STAT3 phosphorylation as well as constitutive STAT3 phosphorylation[1].
DHCT suppresses both tetrodotoxin-resistant (TTX-R) and sensitive (TTX-S) voltage-gated sodium channel (VGSC) currents with IC50 values of 12.36 μM and 4.87 μM, respectively[2].
References
[1] Jing Zhang, et al. Dehydrocrenatidine is a novel janus kinase inhibitor. Mol Pharmacol. 2015 Apr;87(4):572-81. DOI:10.1124/mol.114.095208
[2] Fang Zhao, et al. Dehydrocrenatidine Inhibits Voltage-Gated Sodium Channels and Ameliorates Mechanic Allodia in a Rat Model of Neuropathic Pain. Toxins (Basel). 2019 Apr 18;11(4):229. DOI:10.3390/toxins11040229
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