4-Benzyl-2-methyl-[1,2,4]thiadiazolidine-3,5-dione TDZD-8
TDZD-8
CAS: 327036-89-5
Molecular Formula: C10H10N2O2S
4-Benzyl-2-methyl-[1,2,4]thiadiazolidine-3,5-dione TDZD-8 - Names and Identifiers
4-Benzyl-2-methyl-[1,2,4]thiadiazolidine-3,5-dione TDZD-8 - Physico-chemical Properties
| Molecular Formula | C10H10N2O2S |
| Molar Mass | 222.26 |
| Density | 1.375±0.06 g/cm3(Predicted) |
| Melting Point | 63-64.4°C |
| Boling Point | 335.5±35.0 °C(Predicted) |
| Solubility | DMSO: 18mg/mL |
| Appearance | needles |
| Color | white |
| pKa | -2.08±0.20(Predicted) |
| Storage Condition | 2-8°C |
| MDL | MFCD04973552 |
| Use | TDZD-8 |
| In vitro study | TDZD-8 as non-ATP competitive inhibitors or in combination with GS-1. In the kinase assay, TDZD-8 had no inhibitory effect on PKA, PKC, Cdk-1/cyclin B and CK-II. TDZD-8 specific induction of cell death in primary leukemia cell samples. TDZD-8 can remove leukemia progenitor cells and stem cells. TDZD-8 induces cell death with extremely rapid kinetics of cell death and complete loss of cell membrane. TDZD-8 act on primary AML cell samples and inhibit PKC and FLT3. |
| In vivo study | 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. |
4-Benzyl-2-methyl-[1,2,4]thiadiazolidine-3,5-dione TDZD-8 - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 43 - May cause sensitization by skin contact |
| Safety Description | 36/37 - Wear suitable protective clothing and gloves. |
| WGK Germany | 3 |
4-Benzyl-2-methyl-[1,2,4]thiadiazolidine-3,5-dione TDZD-8 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 4.499 ml | 22.496 ml | 44.992 ml |
| 5 mM | 0.9 ml | 4.499 ml | 8.998 ml |
| 10 mM | 0.45 ml | 2.25 ml | 4.499 ml |
| 5 mM | 0.09 ml | 0.45 ml | 0.9 ml |
Last Update：2024-01-02 23:10:35
4-Benzyl-2-methyl-[1,2,4]thiadiazolidine-3,5-dione TDZD-8 - Reference Information
| biological activity | TDZD-8 (NP 01139) is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; It has minimal inhibitory effect on CDK1, casein kinase II, PKA and PKC. |
| target | TargetValue GSK-3β 2 μM |
| Target | Value |
| GSK-3β | 2 μM |
| in vitro study | TDZD-8 as a non-ATP competitive inhibitor or binding to GS-1. In the kinase experiment, TDZD-8 had no inhibitory effect on PKA, PKC, Cdk-1/cyclin B and CK-II. TDZD-8 specifically induced cell death in primary leukemia cell samples. TDZD-8 can remove leukemia progenitor cells and stem cells. TDZD-8 induces cell death with extremely rapid cell death kinetics and complete cell membrane loss. TDZD-8 acts on primary AML cell samples to inhibit PKC and FLT3. |
| in vivo research | 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 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. |
| use | Glycogen Synthase Kinase-3β is a highly conserved ubiquitously expressed serine/threonine protein kinase involved in signal transduction cascades of multiple cellular processes. TDZD-8 is a thiadiazo lidinone (TDZD) analog that acts as a highly selective, non-ATP competitive inhibitor of GSK-3β ( IC50 = 2nM). binds to the active site of GSK-3β. does not significantly affect the activities of Cd k-1/cyclin B, CK-II, PKA, and PKC (IC50 >100nM). |
Last Update：2024-04-09 15:16:35
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Product Name: TDZD-8 Visit Supplier Webpage Request for quotationCAS: 327036-89-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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