361540
GSK-3β Inhibitor I
The GSK-3β Inhibitor I, also referenced under CAS 327036-89-5, controls the biological activity of GSK-3β. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
GSK-3β Inhibitor I, TDZD-8, 4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
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About This Item
Empirical Formula (Hill Notation):
C10H10N2O2S
CAS Number:
Molecular Weight:
222.26
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Quality Level
Assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white to off-white
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
2-8°C
InChI
1S/C10H10N2O2S/c1-11-9(13)12(10(14)15-11)7-8-5-3-2-4-6-8/h2-6H,7H2,1H3
InChI key
JDSJDASOXWCHPN-UHFFFAOYSA-N
General description
A cell-permeable, thiadiazolidinone (TDZD) analog that acts as a highly selective, non-ATP-competitive inhibitor of GSK-3β (IC50 = 2 µM). Inhibits Flt-3 and PKC activities (IC50 = 673 nM and 1.4-5.5 µM, respectively). Does not significantly affect the activities of Cdk1/cyclin B, CK-II, PKA, or PKC (IC50 >100 µM). Shown to inhibit collagen- and thrombin-induced platelet aggregation.
A thiadiazolidinone (TDZD) analog that acts as a highly selective, non-ATP competitive inhibitor of GSK-3β (IC50 = 2 µM). Inhibits Flt-3 and PKC activities (IC50 = 673 nM and 1.4-5.5 µM, respectively). Does not significantly affect the activities of Cdk-1/cyclin B, CK-II, and PKA, (IC50 >100 µM). Binds to the active site of GSK-3β.
Biochem/physiol Actions
Cell permeable: no
Primary Target
Gsk-3β
Gsk-3β
Product does not compete with ATP.
Reversible: no
Target IC50: 2 µM, 673 nM, 1.4-5.5 µM, against GSK-3β, Flt-3, and PKC activities, respectively
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Guzman, M.L., et al. 2007. Blood110, 4436.
Barry, F.A., et al. 2003. FEBS Lett.553, 173.
Martinez, A., et al. 2002. J. Med. Chem.45, 1292.
Barry, F.A., et al. 2003. FEBS Lett.553, 173.
Martinez, A., et al. 2002. J. Med. Chem.45, 1292.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
Certificates of Analysis (COA)
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