TDZD-8_327036-89-5_DataSheet_MedChemExpress

Product Name:

TDZD-8CAS No.:

327036-89-5Cat. No.:

HY-11012Product Data Sheet

MWt:

222.26Formula:

C10H10N2O2S Purity :>98%

Solubility:

DMSO

Mechanisms:Biological Activity:

TDZD 8(NP 01139)is a selective inhibitor of GSK 3a thiadiazolidinone derivative non ATP

Pathways:PI3K/Akt/mTOR ; Target:GSK-3 Pathways:Wnt/Hedgehog/Notch; Target:GSK-3TDZD-8(NP 01139) is a selective inhibitor of GSK-3, a thiadiazolidinone derivative, non-ATP competitive inhibitor of GSK-3β (IC50 = 2 μM); does not inhibit Cdk-1/cyclin B, CK-II, PKA or PKC at

>100 μM.

IC50 Value: 2 uM (GSK3β)

Target: GSK-3βin vitro: Prophylactic or therapeutic administration of TDZD-8 caused the phosphorylation (Ser(9))and hence inactivation of GSK-3beta. Infarct volume and levels of S100B protein, a marker of cerebral injury, were reduced by TDZD-8. This was associated with a significant reduction in markers of oxidative stress, apoptosis, and the inflammatory response resulting from cerebral I/R References:

[1]. Collino M, et al. Treatment with the glycogen synthase kinase-3beta inhibitor, TDZD-8, affects transient cerebral ischemia/reperfusion injury in the rat hippocampus. Shock. 2008 Sep;30(3):299-307.p p y p g

[1]. Notably, cell death was frequently evident within 2 hours or less of TDZD-8 exposure. Cellular and molecular studies indicate that the mechanism by which TDZD-8 induces cell death involves rapid loss of membrane integrity, depletion of free thiols, a...

[2]. Zhu Q, et al. Suppression of glycogen synthase kinase 3 activity reduces tumor growth of

prostate cancer in vivo. Prostate. 2011 Jun 1;71(8):835-45.[3]. Cuzzocrea S, et al. Effects of glycogen synthase kinase-3beta inhibition on the development of

cerulein-induced acute pancreatitis in mice. Crit Care Med. 2007 Dec;35(12):2811-21.[4]. Guzman ML, 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 Dec

15;110(13):4436-44.Caution: Not fully tested. For research purposes only

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