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Merck
CN

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:
327036-89-5
Molecular Weight:
222.26
MDL number:
MFCD04973552
UNSPSC Code:
12352200
NACRES:
NA.77

Key Documents

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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

SMILES string

S1N(C(=O)N(C1=O)Cc2ccccc2)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

Related Categories

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

Preparation Note

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

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Certificates of Analysis (COA)

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