product name TDZD-8
Description: TDZD-8 is a non-ATP competitive GSK-3β inhibitor with IC50 of 2 μM;, it shows minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC. TDZD-8 protects the brain against I/R injury by inhibiting GSK-3beta activity. TDZD-8 decreased proliferation and induced apoptosis of GL261 glioblastoma cells in vitro, delayed tumor growth in vivo, and augmented animal survival. These effects were associated with an early activation of extracellular signal-regulated kinase (ERK) pathway and increased expression of EGR-1 and p21 genes.
References: J Med Chem. 2002 Mar 14;45(6):1292-9; Blood. 2007 Dec 15;110(13):4436-44.
222.26
Formula
C10H10N2O2S
CAS No.
327036-89-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 44.5 mg/mL (200.2 mM)
Water: <1 mg/mL
Ethanol: 44.5 mg/mL (200.2 mM)
Solubility (In vivo)
Synonyms
NP 01139
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19423996
| In Vitro |
In vitro activity: 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. 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. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | |
| Animal model | NOD/SCID mouse |
| Formulation & Dosage | |
| References | J Med Chem. 2002 Mar 14;45(6):1292-9; Blood. 2007 Dec 15;110(13):4436-44. |
