TDZD-8 是抑制GSK-3β的抑制剂，其 IC50=2 μM。它对 CDK-1/cyclin?B，CK-II，PKA 和 PKC 的作用较弱，IC50值均 >100 μM。

TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; minimal inhibitory effect observed on CDK1, casein kinase II, PKA and PKC.

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]

327036-89-5

C10H10N2O2S

222.26

NP 01139;GSK-3β Inhibitor I

H2O:<1 mgml
DMSO:44.5 mg/mL (200.21 mM)
Ethanol:44.5 mg/mL (200.21 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years