TDZD-8

製品コードS2926 バッチS292601

化学情報

	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
* <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. TDZD-8 shows no inhibition of PKA, PKC, Cdk-1/cyclin B or CK-II in kinase assays. ^[1] 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. ^[2]

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. TDZD-8 shows no inhibition of PKA, PKC, Cdk-1/cyclin B or CK-II in kinase assays. ^[1] 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. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	GSK-3β inhibition
キナーゼアッセイ	GSK-3β enzyme isincubated 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 isassayed 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 ismeasured in a liquid scintillation counter. Blank values are subtracted, and the GSK-3β activity isexpressed in picomoles of phosphate incorporated in GS-1 per 20 min or in percentage of maximal activity.

参考

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：

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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