| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
HOTAIR-EZH2 interaction. HOTAIR (HOX transcript antisense RNA) is a long non-coding RNA that interacts with EZH2 (enhancer of zeste homolog 2), a histone methyltransferase that catalyzes trimethylation of histone H3 at lysine 27 (H3K27me3), leading to gene silencing. AC1Q3QWB interrupts this interaction, thereby relieving EZH2-mediated gene silencing and upregulating target genes such as CDKN1A (p21) and SOX17.
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| ln Vitro |
AC1Q3QWB upregulates CDKN1A and SOX17 by interrupting the HOTAIR-EZH2 interaction. CDKN1A (p21) is a cyclin-dependent kinase inhibitor that regulates cell cycle progression. SOX17 is a transcription factor that suppresses Wnt signaling and promotes differentiation. By upregulating these genes, AC1Q3QWB may inhibit cell proliferation and promote differentiation.
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| ln Vivo |
AC1Q3QWB enhances the efficacy of Tazemetostat in endometrial cancer. Tazemetostat is an EZH2 inhibitor approved for the treatment of epithelioid sarcoma and follicular lymphoma. By disrupting HOTAIR-EZH2 interaction, AC1Q3QWB may sensitize endometrial cancer cells to Tazemetostat, providing a potential combination therapy strategy.
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| Enzyme Assay |
In vitro binding assays are performed to measure the interaction between HOTAIR and EZH2 in the presence of AC1Q3QWB. RNA immunoprecipitation (RIP) or electrophoretic mobility shift assays (EMSA) can be used to assess the disruption of HOTAIR-EZH2 binding. AC1Q3QWB interrupts the HOTAIR-EZH2 interaction.
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| Cell Assay |
Endometrial cancer cell lines are treated with AC1Q3QWB alone or in combination with Tazemetostat. CDKN1A and SOX17 expression is measured by qPCR and Western blotting to confirm upregulation. Cell proliferation is measured using standard assays. The combination of AC1Q3QWB and Tazemetostat is assessed for synergistic anti-proliferative effects.
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| Animal Protocol |
Mouse xenograft models of endometrial cancer are used to assess the in vivo efficacy of AC1Q3QWB alone and in combination with Tazemetostat. Tumor volume is measured regularly. CDKN1A and SOX17 expression in tumor tissues is measured to confirm target engagement. Tumor growth inhibition is assessed to evaluate the combination therapy.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of AC1Q3QWB have not been extensively characterized. Molecular formula: C12H15Cl2NO. Appearance: colorless to light yellow liquid. Solubility: 100 mg/mL (384.38 mM). Detailed PK data (Cmax, Tmax, AUC, t1/2) are not available in the literature.
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| Toxicity/Toxicokinetics |
Toxicological data for AC1Q3QWB are not available. As an HOTAIR-EZH2 interaction disruptor, its toxicity profile is unknown. Standard laboratory safety practices should be followed when handling the compound. It is not intended for human use.
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| References | |
| Additional Infomation |
AC1Q3QWB (AQB) is a research-grade compound that disrupts HOTAIR-EZH2 interaction. CAS: 46697-00-1. Molecular formula: C12H15Cl2NO. Synonyms: AQB. It upregulates CDKN1A and SOX17 and enhances the efficacy of Tazemetostat in endometrial cancer. For research use only.
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| CAS # |
46697-00-1
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| Appearance |
Colorless to light yellow liquid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO :~100 mg/mL (~384.38 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.61 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 25.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD saline solution and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution. |
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.
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