| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 250mg | |||
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| Targets |
Epiblastin A selectively inhibits casein kinase 1 (CK1) isoforms α, δ, and ε. It is an ATP-competitive inhibitor that binds to the ATP-binding site of the enzyme. It has IC₅₀ values of 8.9 µM for CK1α, 0.5 µM for CK1δ, and 4.7 µM for CK1ε. By inhibiting CK1, epiblastin A induces the reprogramming of EpiSCs into ESCs.
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| ln Vitro |
In vitro, epiblastin A is an ATP-competitive inhibitor of CK1α, CK1δ, and CK1ε with IC₅₀ values of 8.9, 0.5, and 4.7 µM, respectively. It engages CK1 isoenzymes in cell lysates and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs). Its activity has been characterized in biochemical and cellular assays.
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| ln Vivo |
In vivo, epiblastin A is primarily used as a research tool to study CK1 function and stem cell reprogramming. Its role in inducing the conversion of EpiSCs to ESCs suggests potential applications in regenerative medicine and developmental biology.
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| Enzyme Assay |
Non-cellular enzyme assays for epiblastin A involve assessing its inhibition of casein kinase 1 (CK1) isoforms using purified recombinant CK1 enzymes (α, δ, ε). The enzyme is incubated with a peptide substrate and ATP in the presence of varying concentrations of epiblastin A. The phosphorylation of the substrate is measured using a radioactive (³³P-ATP) or luminescence-based assay. IC₅₀ values for each CK1 isoform are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for epiblastin A involve treating epiblast stem cells (EpiSCs) with the compound and assessing its effects on cell reprogramming. EpiSCs are treated with varying concentrations of epiblastin A for a defined period. The conversion to embryonic stem cells (ESCs) is assessed by measuring the expression of ESC-specific markers (e.g., Nanog, Oct4) by qPCR or immunofluorescence. The efficiency of reprogramming is quantified.
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| Animal Protocol |
In vivo animal experiments for epiblastin A are not extensively documented in the available literature. As a research tool for studying stem cell biology, its primary applications are in vitro. However, it could be used in animal models to study the effects of CK1 inhibition on stem cell populations and tissue regeneration.
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| ADME/Pharmacokinetics |
Epiblastin A has a molecular weight of 287.71 and a molecular formula of C₁₂H₁₀ClN₇. It is a solid powder with a purity of ≥98%. The compound is soluble in DMSO. For storage, it should be kept at +4°C. It is stable under recommended storage conditions. Its CAS number is 16470-02-3.
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| Toxicity/Toxicokinetics |
Epiblastin A is a research compound for laboratory use only and is not intended for human therapeutic or diagnostic use. In preclinical studies, it has been generally well-tolerated at the concentrations used for cell reprogramming. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation.
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| References | |
| Additional Infomation |
Epiblastin A (CAS 16470-02-3) is a triamterene derivative and a potent, reversible, ATP-competitive inhibitor of casein kinase 1 (CK1) isoforms α, δ, and ε. It has IC₅₀ values of 8.9, 0.5, and 4.7 µM for CK1α, CK1δ, and CK1ε, respectively. Epiblastin A potently induces the reprogramming of epiblast stem cells (EpiSCs) into embryonic stem cells (ESCs) and is available from various commercial suppliers for research applications.
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| Molecular Formula |
C12H10CLN7
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|---|---|
| Molecular Weight |
287.71
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| Exact Mass |
287.068
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| Elemental Analysis |
C, 50.10; H, 3.50; Cl, 12.32; N, 34.08
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| CAS # |
16470-02-3
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| PubChem CID |
118987042
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| Appearance |
Light yellow to green yellow solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
596.1±60.0 °C at 760 mmHg
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| Flash Point |
314.3±32.9 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.821
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
344
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1=C2C(N=C(C3=CC=CC(Cl)=C3)C(N)=N2)=C(N)N=C1N
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| InChi Key |
ZWNKKZSRANLVEW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H10ClN7/c13-6-3-1-2-5(4-6)7-9(14)18-11-8(17-7)10(15)19-12(16)20-11/h1-4H,(H6,14,15,16,18,19,20)
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| Chemical Name |
6-(3-chlorophenyl)pteridine-2,4,7-triamine
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| Synonyms |
AUE; Epiblastin A
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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 : ~4.55 mg/mL (~15.81 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 | 3.4757 mL | 17.3786 mL | 34.7572 mL | |
| 5 mM | 0.6951 mL | 3.4757 mL | 6.9514 mL | |
| 10 mM | 0.3476 mL | 1.7379 mL | 3.4757 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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