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Chemical Structure| 327036-89-5 Chemical Structure| 327036-89-5
Chemical Structure| 327036-89-5

TDZD-8

CAS No.: 327036-89-5

TDZD-8, the derivative of thiadiazolidinone, is a selective inhibitor of GSK-3. It inhibits GSK-3β with IC50 of 2 μM.

Synonyms: NP 01139; GSK-3β Inhibitor I; TDZD 8. GSK3 Inhibitor I

4.5 *For Research Use Only !

Cat. No.: A251413 Purity: 98%

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Product Details of TDZD-8

CAS No. :327036-89-5
Formula : C10H10N2O2S
M.W : 222.26
SMILES Code : CN1SC(=O)N(CC2=CC=CC=C2)C1=O
Synonyms :
NP 01139; GSK-3β Inhibitor I; TDZD 8. GSK3 Inhibitor I
MDL No. :MFCD04973552
InChI Key :JDSJDASOXWCHPN-UHFFFAOYSA-N
Pubchem ID :4124851

Safety of TDZD-8

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of TDZD-8

PI3K-AKT
Hedgehog

Isoform Comparison

Biological Activity

Target
  • GSK-3β

    GSK-3β, IC50:2 μM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
Murine podocytes 5µM 24 h TDZD-8 inhibited GSK3 β, reduced LPS-induced RelA/p65 phosphorylation at serine 467, ameliorated podocyte injury, but did not affect Bcl-xL expression or sensitize apoptosis. PMC4449834
Tubular epithelial cells (TKPT) 5, 10, 20 μM 24 h TDZD-8 significantly improved the survival rate of DCLF-stimulated TKPT cells, suppressed apoptosis and necrosis, and prevented the mitochondrial permeability transition (MPT). PMC3305839
Microglia 5 μM 6 h Inhibited GSK3β phosphorylation, promoted Nrf2 nuclear accumulation, and reduced oxidative stress and inflammation PMC9951499

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice LPS-induced proteinuria and podocytopathy model Intraperitoneal injection 5mg/Kg Single injection, lasting 24 hours TDZD-8 therapy improved LPS-induced podocyte injury and proteinuria, suppressed podocytopathic mediators, but retained Bcl-xL in the glomerulus. PMC4449834
Mice DCLF-induced nephrotoxicity model Intravenous injection 1 mg/kg, 5 mg/kg Single dose, lasting 6 hours TDZD-8 significantly improved kidney function, attenuated tubular necrosis and apoptosis, and inhibited the mitochondrial permeability transition (MPT) in DCLF-injured mice. PMC3305839
Mice MRL/ lpr mice and (NZB × NZW)F1 mice Intraperitoneal injection 5 mg/kg Once daily for 8 weeks or 12 weeks TDZD-8 treatment significantly attenuated severe proteinuria and renal inflammation in both mouse models, with a significant reduction in anti-dsDNA antibody production, renal immune complex deposition, and circulating proinflammatory cytokine levels. PMC4731039
Mice HgCl2-induced acute kidney injury model Intraperitoneal injection 1 mg/kg and 0.5 mg/kg Once on day 2 and day 3 TDZD-8 treatment accelerated the recovery of renal structure and function and increased cell proliferation. PMC3472082
Mice RCDP models Subcutaneous injection 5 mg/kg Daily for 4 days TDZD-8 restored Schwann cell differentiation and axonal sorting defects. PMC4038568
Mice Middle cerebral artery occlusion model Intraperitoneal injection 5 mg/kg Once daily for 3 days Inhibited GSK3β phosphorylation, promoted Nrf2 nuclear accumulation, reduced oxidative stress and inflammation, and improved neurological function PMC9951499
Mice Prolonged learned helplessness model Intraperitoneal injection 5mg/kg Once daily for three days Treatment with the GSK3 inhibitor TDZD-8 reduced inflammatory cytokine levels, increased tight junction protein levels, and reversed impaired recovery from learned helplessness, demonstrating that prolonged learned helplessness is reversible and is maintained by abnormally active GSK3. PMC5963697

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.50mL

0.90mL

0.45mL

22.50mL

4.50mL

2.25mL

44.99mL

9.00mL

4.50mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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