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    ZM 39923 HCl
    ZM 39923 HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0329
    CAS #: 1021868-92-7Purity ≥98%

    Description: ZM 39923 HCl, the hydrochloride salt of ZM-39923, is a novel and potent inhibitor of Janus kinase-JAK1/3 with potential anti-inflammatory activity. It inhibits JAK1/3 with pIC50s of 4.4/7.1, and shows little/no activity against JAK2 and modestly potency to EGFR; also found to be sensitive to transglutaminase. 

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

    Related CAS #: 273727-89-2; 58753-54-1

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    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;


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    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.

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    References

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


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    ZM 39923 HCl

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

    ZM 39923 HCl

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

    ZM 39923 HCl

    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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