IQ-1

SKU: orb1225281

Description

A small molecule, specific inhibitor of p300/β-catenin interaction that binds to PR72/130 subunit of PP2A; decreases phosphorylation of p300 at Ser-89 and disrupts β-catenin/p300 interaction, prevents β-catenin coactivator switching from CBP to p300, maintains the pluripotency of murine ESCs in long-term culture in a Wnt-dependent manner.

Key Properties

• CAS Number: 331001-62-8
• MW: 362.42498
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₂N₄O₂
• SMILES: CC(=O)C1=CC=C(C=C1)NN=C(C2=NC(CC3=CC=CC=C32)(C)C)C(=O)N
• Target: Beta-catenin
• Solubility: DMSO: ≥ 33 mg/mL

Bioactivity

• In Vitro:
  IQ-1 (1.10, 3.48, 11.04 mM; 7 days) maintains the undifferentiated state of ESCs. IQ-1 (0.28, 1.10, 2.76, 11.04 mM; 21 h) maintains murine ESC self-renewal independently of LIF. IQ-1 Binds the PR72/130 Subunit of the Serine/ Threonine Phosphatase PP2A in P19 cells. IQ-1 (10 μM; 24 h) modulates Wnt signaling via interaction with PR72/130 in P19 cells. IQ-1 (10 μM; 24 h) indirectly decreases the phosphorylation of p300 Ser-89 and Thereby the β-Catenin/p300 interaction. Cell Viability Assay Cell line: Embryonic stem cells (ESCs). Concentration: 1.10, 3.48, 11.04 mM Incubation time: 7 days. Result: Dose dependently increased alkaline phosphatase activity, in media containing 15% FCS without the addition of exogenous leukemia inhibitory factor (LIF). Maintained SSEA-1 (undifferentiated ESC marker) expression dose-dependently. RT-PCR Cell line: Embryonic stem cells (ESCs). Concentration: 0.28, 1.10, 2.76, 11.04 mM Incubation time: 21 h. Result: Significantly increased and maintained Nanog expression in culture. (Nanog: a divergent homeoprotein pluripotency sustaining factor for ESCs that drives ESC self-renewal). Exhibited the maintenance of murine ESC pluripotency were independent of the LIF/Stat3 pathway. Western blot analysis. Cell line: P19 cells. Concentration: 10 μM. Incubation time: 24 h. Result: Significantly reduced coimmuno precipitation of PR72/130 with both PP2A and Nkd. Binded to PR72/130 subunit of PP2A, and disrupted the PP2A/Nkd complex. Decreased the affinity of the β-catenin/p300 interaction and increases β-catenin/CBP usage by negatively regulating the phosphorylation of p300 Ser-89.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IQ 1 | IQ1

Quick Database Links

Gene Symbol

Beta-catenin