BRD0209

SKU: orb1700967

Description

BRD0209

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1597439-87-6
• MW: 347.45
• Purity: 99.92% (May vary between batches)
• Formula: C₂₂H₂₅N₃O
• SMILES: C[C@@]1(C2=C(NN=C2NC3=C1C(=O)CC(C)(C)C3)C4CC4)C5=CC=CC=C5
• Target: GSK-3
• Solubility: DMSO:3.48 mg/mL (10.02 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.88 mM)

Bioactivity

• Target IC50:
  GSK-3β:5 nM|GSK-3α:19 nM
• In Vitro:
  BRD0209 showed concentration-dependent inhibition of Tau with cellular EC50s of 1.76 μM, respectively, in SH-SY5Y cells using ELISA. Treatment of SH-SY5Y cells with BRD0209 (10 μM) significantly inhibited GSK3 kinase activity within 30 min, as seen in the decrease in phospho-CRMP2 and phospho-β-catenin. BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively).BRD0209 treatment caused a dramatic decrease in autophosphorylation at Tyr279 (pGSK3α) and Tyr216 (pGSK3β) with longer exposure (24 h) .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BRD0209, BRD-0209, BRD 0209, GSK3, GSK-3α, GSK-3β

Compound Identifiers

PubChem CID

135567204