| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| 250mg | |||
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| Targets |
TIQ-A targets tankyrase 2 (TNKS2), an enzyme that is part of the poly(ADP-ribose) polymerase (PARP) family. It also inhibits PARP1. TNKS2 is involved in various cellular processes, including Wnt signaling, telomere maintenance, and mitosis. By inhibiting TNKS2, TIQ-A modulates these pathways. Its role as a PARP1 inhibitor implicates it in DNA repair mechanisms, as PARP1 is activated by DNA damage and facilitates repair through the base excision repair pathway. Overactivation of PARP1 has been implicated in ischemia-reperfusion injury, asthma-related inflammation, and atherosclerosis.
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| ln Vitro |
In vitro, TIQ-A is a potent inhibitor of TNKS2 with an IC₅₀ of 24 nM. It also inhibits PARP1. The compound's activity has been demonstrated in cell-free enzymatic assays. Its potential as an anti-ischemic agent is based on its ability to inhibit PARP1, thereby reducing the excessive DNA repair activity that can lead to cell death in ischemic conditions. Specific cellular assay data, such as effects on cell viability or signaling pathways, are not detailed in the available sources.
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| ln Vivo |
In vivo, TIQ-A has been used to inhibit eosinophilic infiltration into the airways of ovalbumin (OVA)-challenged mice. It has also been used to study the regression of atherosclerotic plaques in high-fat diet-fed apolipoprotein E-deficient (ApoE⁻/⁻) mice. These studies suggest that TIQ-A has anti-inflammatory and anti-atherosclerotic effects in vivo. However, specific dosing regimens, routes of administration, and detailed results are not provided in the available sources.
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| Enzyme Assay |
A cell-free assay for TIQ-A involves measuring its inhibition of TNKS2 or PARP1 enzymatic activity. In such assays, the enzyme is incubated with a substrate (e.g., NAD⁺) and the compound, and the rate of poly(ADP-ribosylation) is measured. The compound's potency is expressed as an IC₅₀ value. For TIQ-A, the IC₅₀ for TNKS2 is 24 nM. This type of assay confirms the compound's direct inhibition of the target enzyme. Specific assay conditions are not detailed in the available sources.
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| Cell Assay |
Cellular assays for TIQ-A are not extensively described in the available sources. As a PARP inhibitor, its effects could be evaluated in cells treated with DNA-damaging agents to assess its impact on DNA repair and cell survival. However, specific protocols, cell lines, or concentrations are not provided. The compound's activity has been characterized primarily in cell-free enzymatic assays and in vivo models.
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| Animal Protocol |
In vivo animal experiments with TIQ-A have been conducted in mouse models. One study used OVA-challenged mice to evaluate the compound's effect on eosinophilic infiltration into the airways. Another study used high-fat diet-fed ApoE⁻/⁻ mice to assess its role in the regression of atherosclerotic plaques. Specific details such as dosage, route of administration, treatment duration, and outcome measures are not provided in the available sources. The compound was used as a PARP-1 inhibitor in these studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of TIQ-A are not reported in the available sources. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) profiles have not been characterized. The compound is available from chemical suppliers with a purity of ≥98%. Its molecular weight is 201.24, and it is a solid at room temperature. Standard storage conditions for research compounds apply.
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| Toxicity/Toxicokinetics |
Toxicity data for TIQ-A are not provided in the available sources. The compound is intended for research use only and is not for human consumption. While it has been used in animal models, specific toxicological information, such as LD₅₀ values or adverse effects, is not available. Standard laboratory safety precautions should be observed when handling this compound.
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| References | |
| Additional Infomation |
TIQ-A (CAS: 420849-22-5) is a research compound that functions as a potent inhibitor of TNKS2 and PARP1. It is also known as Thieno[2,3-c]isoquinolin-5(4H)-one. The compound has been investigated for its potential as an anti-ischemic agent and for its effects on inflammation and atherosclerosis. It is not an approved drug and has not undergone clinical trials. Its primary value lies in its use as a tool compound for studying PARP biology and evaluating the therapeutic potential of PARP inhibition in various diseases. The compound is available from research chemical suppliers for non-clinical research purposes only.
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| Molecular Formula |
C11H7NOS
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|---|---|
| Molecular Weight |
201.244381189346
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| Exact Mass |
201.024
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| CAS # |
420849-22-5
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| PubChem CID |
9899130
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| Appearance |
Light green to green solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
282.2±9.0 °C at 760 mmHg
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| Flash Point |
124.5±18.7 °C
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| Vapour Pressure |
0.0±0.6 mmHg at 25°C
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| Index of Refraction |
1.675
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| LogP |
3.16
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
14
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| Complexity |
256
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LQJVOLSLAFIXSV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H7NOS/c13-10-8-4-2-1-3-7(8)9-5-6-14-11(9)12-10/h1-6H,(H,12,13)
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| Chemical Name |
4H-thieno[2,3-c]isoquinolin-5-one
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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 : ~125 mg/mL (~621.15 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9692 mL | 24.8460 mL | 49.6919 mL | |
| 5 mM | 0.9938 mL | 4.9692 mL | 9.9384 mL | |
| 10 mM | 0.4969 mL | 2.4846 mL | 4.9692 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.
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