ChemicalBook >> CAS DataBase List >>4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE

4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE

CAS No.
327036-89-5
Chemical Name:
4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE
Synonyms
CS-568;NP 01139;TDZD-8/TDZD8;TDZD-8, >=98%;TDZD-8 (NP-01139);GSK-3β Inhibitor I;GSK-3InhibitorI,TDZD-8;TDZD-8;TDZD 8;TDZD8;NP 01139;TDZD8; TDZD 8;GSK-3Β) INHIBITOR I; NP 01139;GSK-3β Inhibitor I - CAS 327036-89-5 - Calbiochem
CBNumber:
CB7501586
Molecular Formula:
C10H10N2O2S
Molecular Weight:
222.26
MDL Number:
MFCD04973552
MOL File:
327036-89-5.mol
MSDS File:
SDS
Last updated:2023-06-30 15:45:59

4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE Properties

Melting point 63-64.4 °C
Boiling point 335.5±35.0 °C(Predicted)
Density 1.375±0.06 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: 18 mg/mL
pka -2.08±0.20(Predicted)
form needles
color white

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS08
Signal word  Danger
Hazard statements  H334
Precautionary statements  P261-P342+P311
Hazard Codes  Xi
Risk Statements  43
Safety Statements  36/37
WGK Germany  3
HS Code  2934999090
NFPA 704
0
2 0

4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE price More Price(50)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich T8325 TDZD-8 ≥98% (HPLC), needles 327036-89-5 5mg $179 2024-03-01 Buy
Sigma-Aldrich 361540 GSK-3β Inhibitor I 327036-89-5 5mg $144 2024-03-01 Buy
TCI Chemical B4436 4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione >98.0%(HPLC) 327036-89-5 5mg $98 2024-03-01 Buy
TCI Chemical B4436 4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione >98.0%(HPLC) 327036-89-5 25mg $294 2024-03-01 Buy
Cayman Chemical 16287 TDZD-8 ≥98% 327036-89-5 5mg $61 2024-03-01 Buy
Product number Packaging Price Buy
T8325 5mg $179 Buy
361540 5mg $144 Buy
B4436 5mg $98 Buy
B4436 25mg $294 Buy
16287 5mg $61 Buy

4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE Chemical Properties,Uses,Production

Chemical Properties

White Solid

Uses

TDZD-8 has been used to study the role of GSK-3 in maintaining MLL leukemia stem cell transcriptional program. TDZD-8 has also been used to analyze its effect on neural functions of the mouse olfactory bulb.

Uses

Glycogen Synthase Kinase-3? is a highly conserved ubiquitously expressed serine/threonine protein kinase involved in signal transduction cascades of multiple cellular processes. TDZD-8 is a thiadiazolidinone (TDZD) analogue that acts as a highly selectiv

Definition

ChEBI: TDZD-8 is a member of the class of thiadiazolidines that is 1,2,4-thiadiazolidine-3,5-dione which is substituted by a methyl group at position 2 and by a benzyl group at position 4. It is a non-ATP competitive inhibitor of glycogen synthase kinase 3beta (GSK3beta). An experimental compound which was being developed for the potential treatment of Alzheimer's disease. It has a role as an EC 2.7.11.26 (tau-protein kinase) inhibitor, an apoptosis inducer, an antineoplastic agent, a neuroprotective agent and an anti-inflammatory agent. It is a thiadiazolidine and a member of benzenes.

General Description

A cell-permeable, thiadiazolidinone (TDZD) analog that acts as a highly selective, non-ATP-competitive inhibitor of GSK-3β (IC50 = 2 μM). Inhibits Flt-3 and PKC activities (IC50 = 673 nM and 1.4-5.5 μM, respectively). Does not significantly affect the activities of Cdk1/cyclin B, CK-II, PKA, or PKC (IC50 >100 μM). Shown to inhibit collagen- and thrombin-induced platelet aggregation.

Biological Activity

tdzd-8 is an inhibitor of glycogen synthase kinase-3β (gsk-3β) with ic50 value of 1.4μm [1].tdzd-8 is a potent inhibitor of gsk-3β. it is found to act as a noncompetitive inhibitor of atp binding. tdzd-8 is selective against gsk-3β over other protein kinases including pka, casein kinase ii and cyclin dependent kinase 1 (cdk-1/cyclin b). however, it is also reported that tdzd-8 can inhibit the protein kinase c isoforms pkcβi and pkcδ with ic50 values of 1.4μm and 1.1μm, respectively [1, 2].in cellular assay, tdzd-8 is found to decrease pdt-induced necrosis of neurons and decrease pdt-induced apoptosis of glial cells through inhibiting gsk-3β as well as pkc. besides that, tdzd-8 also has anti-leukemia activity in many primary human leukemia cells. it is probably due to its inhibition of pkc and flt3 [3].

Biochem/physiol Actions

Primary TargetGsk-3β

storage

Store at -20°C

References

[1] komandirov m a, knyazeva e a, fedorenko y p, et al. on the role of phosphatidylinositol 3-kinase, protein kinase b/akt, and glycogen synthase kinase-3β in photodynamic injury of crayfish neurons and glial cells. journal of molecular neuroscience, 2011, 45(2): 229-235.
[2] martinez a, alonso m, castro a, et al. first non-atp competitive glycogen synthase kinase 3 β (gsk-3β) inhibitors: thiadiazolidinones (tdzd) as potential drugs for the treatment of alzheimer's disease. journal of medicinal chemistry, 2002, 45(6): 1292-1299.
[3] guzman m l, li x, corbett c a, et al. rapid and selective death of leukemia stem and progenitor cells induced by the compound 4-benzyl, 2-methyl, 1, 2, 4-thiadiazolidine, 3, 5 dione (tdzd-8). blood, 2007, 110(13): 4436-4444.

4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 131)Suppliers
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Capot Chemical Co.,Ltd.
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SHANGHAI T&W PHARMACEUTICAL CO., LTD.
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Guangzhou Yuheng Pharmaceutical Technology Co., Ltd
+8613580539051 joe@yuhengpharm.com CHINA 21149 58

View Lastest Price from 4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE pictures 2019-07-06 4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE
327036-89-5
US $2.00 / kg 1kg 99% 100kg Career Henan Chemical Co

4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE Spectrum

GSK-3InhibitorI,TDZD-8 NP 01139 1,2,4-Thiadiazolidine-3,5-dione,2-Methyl-4-(phenylMethyl)- TDZD-8/TDZD8 4-Benzyl-2-methyl-[1,2,4]thiadiazolidine-3,5-dione TDZD-8 TDZD-8, >=98% TDZD-8;TDZD 8;TDZD8;NP 01139 2-Methyl-4-(phenylmethyl)-1,2,4-thiadiazolidine-3,5-dione GSK-3β Inhibitor I - CAS 327036-89-5 - Calbiochem CS-568 TDZD8; TDZD 8;GSK-3Β) INHIBITOR I; NP 01139 TDZD-8 (NP-01139) GSK-3β Inhibitor I inhibit,TDZD8,Inhibitor,TDZD 8,NP01139,GSK-3,TDZD-8,Glycogen synthase kinase 3,NP-01139,Glycogen synthase kinase-3 327036-89-5 Amines Aromatics Sulfur & Selenium Compounds Other Enzyme Inhibitors and Activators. Inhibitors Akt mTOR PI3K