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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
IQ-1 (IQ1) is a cell-permeable tetrahydroisoquinolinylidene small molecule compound that modulates Wnt/beta-catenin signaling. IQ-1 was identified from a high-throughput cell-based assay and has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on. IQ-1 binds to serine/threonine phosphatase PP2A and prevents PP2A/Nkd interaction. IQ-1 allows for the Wnt/beta-catenin-driven long-term expansion of mouse ESCs and prevents spontaneous differentiation. IQ-1, by targeting the PR72/130 subunit of the serine/threonine phosphatase PP2A, prevents beta-catenin from switching coactivator usage from CBP to p300. The increase in beta-catenin/CBP-mediated transcription at the expense of beta-catenin/p300-mediated transcription is critical for the maintenance of murine stem cell pluripotency.
ln Vitro |
For seven days, IQ-1 (1.10, 3.48, 11.04 mM) keeps ESCs in their undifferentiated state[1]. Independent of LIF, IQ-1 (0.28, 1.10, 2.76, 11.04 mM; 21 h) sustains the self-renewal of murine ESCs[1]. In P19 cells, IQ-1 Binds the Serine/Threonine Phosphatase PP2A PR72/130 Subunit[1]. In P19 cells, IQ-1 (10 µM; 24 h) modifies Wnt signaling by interaction with PR72/130[1]. IQ-1 (10 µM; 24 h) reduces p300 Ser-89 phosphorylation indirectly, which in turn reduces the β-Catenin/p300 interaction[1].
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ln Vivo |
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Cell Assay |
Cell Viability Assay[1]
Cell Types: Embryonic stem cells (ESCs) Tested Concentrations: 1.10, 3.48, 11.04 mM Incubation Duration: 7 days Experimental Results: 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[1] Cell Types: Embryonic stem cells (ESCs) Tested Concentrations: 0.28, 1.10, 2.76, 11.04 mM Incubation Duration: 21 h Experimental Results: Dramatically increased and maintained Nanog expression in culture. (Nanog: a divergent homeoprotein pluripotency sustaining factor for ESCs that drives ESC self-renewal). demonstrated the maintenance of murine ESC pluripotency were independent of the LIF/Stat3 pathway. Western Blot Analysis[1] Cell Types: P19 cells Tested Concentrations: 10 µM Incubation Duration: 24 h Experimental Results: Dramatically decreased coimmunoprecipitation of PR72/130 with both PP2A and Nkd. Binded to PR72/130 subunit of PP2A, and disrupted the PP2A/Nkd complex. |
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Animal Protocol |
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References |
[1]. Miyabayashi T, et al. Wnt/beta-catenin/CBP signaling maintains long-term murine embryonic stem cell pluripotency. Proc Natl Acad Sci U S A. 2007 Mar 27;104(13):5668-73.
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Molecular Formula |
C21H22N4O2
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Molecular Weight |
362.42
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CAS # |
331001-62-8
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Related CAS # |
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SMILES |
CC(C1=CC=C(/N=N/C(C(N)=O)=C2NC(C)(C)CC3=CC=CC=C3/2)C=C1)=O
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.7592 mL | 13.7961 mL | 27.5923 mL | |
5 mM | 0.5518 mL | 2.7592 mL | 5.5185 mL | |
10 mM | 0.2759 mL | 1.3796 mL | 2.7592 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
IQ-1 maintains undifferentiated state of ESCs.Proc Natl Acad Sci U S A.2007 Mar 27;104(13):5668-73. th> |
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IQ-1 modulates Wnt signaling via interaction with PR72/130.Proc Natl Acad Sci U S A.2007 Mar 27;104(13):5668-73. td> |
IQ-1 Maintenance of ESCs is Wnt/β-catenin/CBP-dependent. Pluripotency of long-term-cultured ESCs.Proc Natl Acad Sci U S A.2007 Mar 27;104(13):5668-73. td> |