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
• Empirical Formula (Hill Notation): C₁₀H₁₀N₂O₂S
• CAS Number: 327036-89-5
• Molecular Weight: 222.26
• MDL number: MFCD04973552
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• 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

Description

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

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3