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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
Lin281632 targets the RNA binding protein Lin28. Lin28 is a key regulator of stem cell pluripotency and development. It normally blocks the biogenesis of the lethal-7 (let-7) microRNA family and directly binds to messenger RNA (mRNA) targets, such as IGF-2 mRNA, altering downstream splicing and translation events. By inhibiting Lin28, Lin281632 promotes the processing of let-7 miRNAs and releases its repression of mRNA targets. This leads to the promotion of differentiation.
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| ln Vitro |
In vitro, Lin281632 inhibits or disrupts the binding of Lin28A to pre-let-7a-2 with an IC50 of 8 μM. This activity confirms its role as a potent antagonist of the Lin28/pre-let-7 interaction. By inhibiting Lin28, it promotes the differentiation of mouse embryonic stem cells (mESC). These in vitro activities confirm its mechanism of action.
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| ln Vivo |
Detailed in vivo activity data for Lin281632 are not extensively provided in the search results. However, its ability to promote mESC differentiation suggests potential for in vivo applications in regenerative medicine and developmental biology. Its role as a Lin28 inhibitor also makes it a potential tool for studying Lin28-driven cancers.
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| Enzyme Assay |
Non-cell-based assays for Lin281632 would typically involve measuring its ability to disrupt the Lin28/pre-let-7 interaction in a cell-free system. This can be done using a fluorescence polarization or AlphaScreen assay with purified Lin28A protein and a labeled pre-let-7 RNA probe. The compound's ability to displace the RNA probe is measured, and an IC50 value is determined.
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| Cell Assay |
Cellular assays for Lin281632 are performed using mouse embryonic stem cells (mESC). The cells are treated with the compound, and the levels of mature let-7 miRNAs are measured by qPCR. The expression of Lin28 target genes, such as IGF-2, is also measured. The compound's ability to promote differentiation is assessed by measuring the expression of differentiation markers.
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| Animal Protocol |
In vivo animal models for Lin281632 would likely involve the use of mice to study its effects on development or tumorigenesis. For example, in a cancer model, the compound could be administered to inhibit Lin28 and potentially reduce tumor growth. These studies are crucial for evaluating the compound's therapeutic potential. Detailed protocols are not provided in the search results.
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| ADME/Pharmacokinetics |
Lin281632 has a molecular weight of 295.34 g/mol and a molecular formula of C15H13N5O. It is a small molecule that is soluble in DMSO. Detailed PK parameters such as half-life and bioavailability are not extensively detailed in the provided search results.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for Lin281632 are not provided in the search results. As a research compound, its safety profile would need to be established through standard preclinical toxicity assessments. The compound is intended for research use only and is not for human consumption.
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| Additional Infomation |
Lin281632 is also known as Lin28-let-7 antagonist 1 and compound 1632. It is a potent antagonist of the Lin28/pre-let-7 interaction, with an IC50 of 8 μM. It is an inhibitor of the RNA binding protein Lin28 and bromodomain and promotes mESC differentiation. It has the CAS number 108825-65-6 and is supplied for research purposes.
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| Molecular Formula |
C15H15N5O
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|---|---|
| Molecular Weight |
281.319
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| Exact Mass |
281.128
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| CAS # |
108825-65-6
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| PubChem CID |
2737312
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.28g/cm3
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| Melting Point |
200ºC
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| Index of Refraction |
1.665
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| LogP |
2.082
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
390
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C1C=CC=C(C2=NN3C(C)=NN=C3C=C2)C=1)C(=O)C
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| InChi Key |
WPAQLESUVYGUJZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H15N5O/c1-10-16-17-15-8-7-14(18-20(10)15)12-5-4-6-13(9-12)19(3)11(2)21/h4-9H,1-3H3
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| Chemical Name |
N-methyl-N-[3-(3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)phenyl]acetamide
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| Synonyms |
Lin 28 163; Lin-28 1632; Lin28 1632
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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 : ~50 mg/mL (~177.74 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 | 3.5547 mL | 17.7734 mL | 35.5467 mL | |
| 5 mM | 0.7109 mL | 3.5547 mL | 7.1093 mL | |
| 10 mM | 0.3555 mL | 1.7773 mL | 3.5547 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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