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ZM 39923 HCl
本半岛bd体育手机客户端 不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ZM 39923 HCl图片
CAS NO:1021868-92-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

半岛bd体育手机客户端 介绍
理化性质和储存条件
Molecular Weight (MW)367.91
FormulaC23H25NO.HCl
CAS No.1021868-92-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 30 mg/mL (81.5 mM)
Water: <1 mg/mL
Ethanol: 8 mg/mL (21.7 mM)
Solubility (In vivo)

Chemical Name: 3-[Benzyl(propan-2-yl)amino]-1-naphthalen-2-ylpropan-1-one hydrochloride

InChi Key: NJTUORMLOPXPBY-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H25NO.ClH/c1-18(2)24(17-19-8-4-3-5-9-19)15-14-23(25)22-13-12-20-10-6-7-11-21(20)16-22;/h3-13,16,18H,14-15,17H2,1-2H3;1H

SMILES Code: O=C(C1=CC=C2C=CC=CC2=C1)CCN(CC3=CC=CC=C3)C(C)C.[H]Cl

Synonyms

Synonym: ZM 39923; ZM-39923; ZM39923 HCl; ZM39923; ZM 39923 Hydrochloride;

实验参考方法
In Vitro

In vitro activity: ZM39923 breaks down to form the JAK3 inhibitor ZM449829 which exhibit similar IC50 values. ZM39923 decomposes in neutral buffer to afford potent inhibition of the Janus kinase 3, and could be used as a standard Jak3 inhibitor in assays where breakdown could occur. ZM39923 is reduced by 300-fold in the presence of DTT (10 mM) in inhibiting TGM2. ZM39923 is reversible inhibitors when TGM2 is incubated with inhibitors in the absence of Ca2+. ZM39923 shows significant inhibition of crosslinking activity with IC50 of 25 nM in the absence of DTT and IC50 of 10 μM in the presence of DTT. ZM39923 prevents early death in a Drosophila Melanogaster model of a polyQ repeat disorder called Machado-Joseph Disease. ZM39923 inhibits the generation of AICD-FLAG and both Aβ40 and Aβ42 by purified γ-secretase in a concentration-dependent fashion with an approximate IC50 of 20 μM. ZM39923 decreases photoaffinity-labeled PS1-CTF in the presense of γ-secretase.


Kinase Assay: ZM39923 hydrochloride is a JAK3 inhibitor, with a pIC50 of 7.1. ZM39923 (Compound 7) shows weak inhibitory effect on EGF-R and JAK1 (pIC50, 5.6, 4.4, respectively), and insignificantly inhibits tyrosine kinases Lck and CDK4 (pIC50 <5.0)


Cell Assay: ZM39923 is a JAK3 inhibitor. ZM39923 is also a potent inhibitor of TGM2 with IC50 of 10 nM. ZM39923 is reversible inhibitors when TGM2 is incubated with inhibitors in the absence of Ca2+. ZM39923 shows significant inhibition of crosslinking activity with IC50 of 25 nM in the absence of DTT and IC50 of 10 μM in the presence of DTT. ZM39923 prevents early death in a Drosophila Melanogaster model of a polyQ repeat disorder called Machado-Joseph Disease. ZM39923 inhibits the generation of AICD-FLAG and both Aβ40 and Aβ42 by purified γ-secretase in a concentration-dependent fashion with an approximate IC50 of 20 μM. ZM39923 decreases photoaffinity-labeled PS1-CTF in the presense of γ-secretase.

In Vivo
Animal model
Formulation & Dosage
References

Chem Biol. 2008 Sep 22;15(9):969-78; J Biol Chem. 2005 Dec 23;280(51):41987-96.

生物活性


Ca+2-dependent Inhibition of TGase/TGM2 by chemical inhibitors. Chem Biol. 2008 Sep 22;15(9):969-78.


Fluorescent GTP Binding Assay. Chem Biol.2008 Sep 22;15(9):969-78.


Effects of chemical inhibitors in rescuing Drosophila in HD model of neurodegeneration. Chem Biol. 2008 Sep 22;15(9):969-78.

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