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    TDZD-8 (NP-01139)
    TDZD-8 (NP-01139)

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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 #: V0222
    CAS #: 327036-89-5Purity ≥98%

    Description: TDZD-8 (NP01139; GSK3 Inhibitor I) is a novel, potent and non-ATP competitive GSK-3β (glycogen synthase kinase-3beta) inhibitor with the potential for treating neurodegenerative diseases such as PD (parkinson disease). In inhibits GSK-3β with an IC50 of 2 μM; and has little effects against CDK1, casein kinase II, PKA and PKC. TDZD-8 protects the brain against I/R injury by inhibiting GSK-3beta activity. TDZD-8 also has potential antitumor activity, showed potent antiproliferative activity in vitro and high antitumor efficacy in vivo. TDZD-8 decreased proliferation and induced apoptosis of GL261 glioblastoma cells in vitro, delayed tumor growth in vivo, and augmented animal survival. These effects were associated with an early activation of extracellular signal-regulated kinase (ERK) pathway and increased expression of EGR-1 and p21 genes. 

    References: J Med Chem. 2002 Mar 14;45(6):1292-9; Blood. 2007 Dec 15;110(13):4436-44.

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    Molecular Weight (MW)

    222.26

    Formula

    C10H10N2O2S

    CAS No.

    327036-89-5

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 44.5 mg/mL (200.2 mM)

    Water: <1 mg/mL

    Ethanol: 44.5 mg/mL (200.2 mM)

    SMILES

     O=C(N1CC2=CC=CC=C2)N(C)SC1=O

    Synonyms

     NP 01139; NP01139; NP-01139; NP 01139; TDZD-8; TDZD8; TDZD 8. GSK3 Inhibitor I


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    In Vitro

    In vitro activity: TDZD-8 acts as a noncompetitive inhibitor of ATP or GS-1 binding. TDZD-8 shows no inhibition of PKA, PKC, Cdk-1/cyclin B or CK-II in kinase assays. TDZD-8 specifically induces cell death of primary leukemia specimens. TDZD-8 ablates leukemia progenitor and stem cells. TDZD-8 treatment induces oxidative stress. TDZD-8 induces cell death with extremely rapid cell death kinetics showing loss of membrane integrity. TDZD-8 inhibits PKC and FLT3 in primary AML specimens.

     

    Kinase Assay: GSK-3 activity is assayed in 50 mM Tris-HCl, pH 7.5, 10 mM MgCl2, 1 mM EGTA, and 1 mM EDTA buffer, at 37°C, in the presence of 15 μM GS-1 (substrate), 15 μM [γ-32P]ATP in a final volume of 12 μL. After 20 min incubation at 37°C, 4 μL aliquots of the supernatant are spotted onto 2×2 cm pieces of Whatman P81 phosphocellulose paper, and 20 s later, the filters are washed four times (for at least 10 min each time) in 1% phosphoric acid. The dried filters are transferred into scintillation vials, and the radioactivity is measured in a liquid scintillation counter. Blank values are subtracted, and the GSK-3β activity is expressed in picomoles of phosphate incorporated in GS-1 per 20 min or in percentage of maximal activity.

     

    Cell Assay: TDZD8 results in a significant decline of cellular ATP levels in PC-3 cells. TDZD8 (10 μM) treatment also triggers a drastic autophagy response and AMPK activation in PC-3 cells. Furthermore, TDZD8 (10 μM) reduces mTOR phosphorylation levels at the S2448 site. In addition, TDZD8 (10 μM) induces LKB1 nuclear-cytoplasm translocation

    In Vivo

    TDZD-8 (TDZD8, 1 or 2 mg/kg, i.p.) both reduces the induction of p-DARPP32 following chronic L-dopa treatment in parkinsonian animals. TDZD8 treatment of 21 days induces a significant reduction in PKA expression in rats with established dyskinesia. Moreover, TDZD8 reduces FosB mRNA level in the striatum and lowers the expression of PPEB mRNA to similar levels as in 6-OHDA-lesioned rats without treated with L-dopa. The decrease in dyskinesia induced by TDZD8 is overcome by dopamine rceptor-1 agonist. 

    Animal model

     NOD/SCID mouse 

    Formulation & Dosage

     1 or 2 mg/kg, i.p.

    References

    J Med Chem. 2002 Mar 14;45(6):1292-9; Blood. 2007 Dec 15;110(13):4436-44.


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

    TDZD-8

    TDZD-8 induces cell death with extremely rapid cell death kinetics showing loss of membrane integrity. Blood. 2007 Dec 15;110(13):4436-44.

    TDZD-8

    TDZD-8 inhibits PKC and FLT3 in primary AML specimens.


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