TDZD-8

製品コードS2926 バッチS292601

印刷

化学情報

Chemical Structure Synonyms NP 01139 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C10H10N2O2S
分子量 222.26 CAS No. 327036-89-5
Solubility (25°C)* 体外 DMSO 44.5 mg/mL (200.21 mM)
Ethanol 44.5 mg/mL (200.21 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 TDZD-8 (NP 01139) is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.
in vitro TDZD-8 acts as a noncompetitive inhibitor of ATP or GS-1 binding. This compound shows no inhibition of PKA, PKC, Cdk-1/cyclin B or CK-II in kinase assays. [1] It specifically induces cell death of primary leukemia specimens. This chemical ablates leukemia progenitor and stem cells. Its treatment induces oxidative stress. It induces cell death with extremely rapid cell death kinetics showing loss of membrane integrity. This compound inhibits PKC and FLT3 in primary AML specimens. [2]

プロトコル(参考用のみ)

キナーゼアッセイ GSK-3β inhibition
GSK-3β enzyme is incubated with 15 μM of ATP, 0.2μCi of [γ- 32 P]ATP, GS-1 as substrate and different concentrations of the test compound. 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 ℃, 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 ℃, 4 μL aliquots of the supernatant are spotted onto 2 × 2 cm pieces of Whatman P81 phosphocellulose paper, and 20s 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.

参考

  • http://www.ncbi.nlm.nih.gov/pubmed/?term=11881998
  • http://www.ncbi.nlm.nih.gov/pubmed/?term=17785584

カスタマーフィードバック

Data from [Data independently produced by , , Int Immunopharmacol. 2017, 43:164-171.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Emodin promotes GSK-3β-mediated PD-L1 proteasomal degradation and enhances anti-tumor immunity in hepatocellular carcinoma [ Chin Med, 2025, 20(1):126] PubMed: 40804393
β-Catenin and SOX2 Interaction Regulate Visual Experience-Dependent Cell Homeostasis in the Developing Xenopus Thalamus [ Int J Mol Sci, 2023, 24(17)13593] PubMed: 37686400
β-Catenin and SOX2 Interaction Regulate Visual Experience-Dependent Cell Homeostasis in the Developing Xenopus Thalamus [ Int J Mol Sci, 2023, 24(17)13593] PubMed: 37686400
GSK-3β inhibition alleviates arthritis pain via reducing spinal mitochondrial reactive oxygen species level and inflammation [ PLoS One, 2023, 18(4):e0284332] PubMed: 37058473
Glycogen synthase kinase-3β inhibition decreases inflammation and relieves cancer induced bone pain via reducing Drp1-mediated mitochondrial damage [ J Cell Mol Med, 2022, 26(14):3965-3976] PubMed: 35689386
The VRK1 chromatin kinase regulates the acetyltransferase activity of Tip60/KAT5 by sequential phosphorylations in response to DNA damage [ Biochim Biophys Acta Gene Regul Mech, 2022, 1865(8):194887] PubMed: 36280132
Activation of NRF2 ameliorates oxidative stress and cystogenesis in autosomal dominant polycystic kidney disease [ Sci Transl Med, 2020, 12(554):eaba3613] PubMed: 32727915
AMPK/GSK3β/β-catenin cascade–triggered overexpression of CEMIP promotes migration and invasion in anoikis-resistant prostate cancer cells by enhancing metabolic reprogramming [Zhang P FASEB J, 2018, 32(7):3924-3935] PubMed: 29505302
Identifying Host Regulators and Inhibitors of Liver Stage Malaria Infection Using Kinase Activity Profiles [ Nat Commun, 2017, 1;8(1):1232] PubMed: 29089541
Purinergic P2X7 receptor mediates acetaldehyde-induced hepatic stellate cells activation via PKC-dependent GSK3β pathway [Wu X Int Immunopharmacol, 2017, 43:164-171] PubMed: 28061416

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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