IQ-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种 p300/β-连环蛋白相互作用的小分子特异性抑制剂，可与 PP2A 的 PR72/130 亚基结合。

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.

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 hResult: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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IQ 1 | IQ1

Wnt/Notch/Hedgehog

Beta-catenin

Others

Cancer

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331001-62-8

362.42498

C21H22N4O2

>98% (HPLC)

DMSO: ≥ 33 mg/mL

CC(=O)C1=CC=C(C=C1)NN=C(C2=NC(CC3=CC=CC=C32)(C)C)C(=O)N

Acetamide, 2-[2-(4-acetylphenyl)diazenyl]-2-(3,4-dihydro-3,3-dimethyl-1(2H)-isoquinolinylidene)

(-20℃)

With Ice Pack

≥ 2 years