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Purity: ≥98%
AS8351 is a potent inhibitor of KDM5B (lysine-specific histone demethylase 5B) which plays an important role in maintaining cancer stem cells and justifies the rationale for studying the effects of continuous inhibition of this epigenetic factor in cancer. AS8351 can induce and sustain active chromatin marks to facilitate the induction of cardiomyocyte-like cells.It induces reprogramming of human fetal lung fibroblasts into functional cardiomyocytes, in combination with CHIR 99021, A83-01, BIX 01294, SC1, Y-27632, OAC2, SU 16f and JNJ 10198409. Reprogramming somatic fibroblasts into alternative lineages would provide a promising source of cells for regenerative therapy. However, transdifferentiating human cells into specific homogeneous, functional cell types is challenging.
| ln Vitro |
By competing with α-ketoglutarate (α-KG) to chelate iron [Fe(II)] in specific epigenetic enzymes, like the JmjC-containing structure that needs α-KG and iron domain-based histone demethylase (JmjC-KDM) as a cofactor, AS8351 influences epigenetic modifications [2].
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| ln Vivo |
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| References |
[1]. Liu K, et al. Chemical Modulation of Cell Fate in Stem Cell Therapeutics and Regenerative Medicine. Cell Chem Biol. 2016 Aug 18;23(8):893-916.
[2]. Cao N, et al. Conversion of human fibroblasts into functional cardiomyocytes by small molecules. Science. 2016 Jun 3;352(6290):1216-20. |
| Molecular Formula |
C17H13N3O2
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| Molecular Weight |
291.3
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| CAS # |
796-42-9
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| SMILES |
OC1=CC=C2C=CC=CC2=C1/C=N/NC(C3=CC=NC=C3)=O
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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: ≥ 2.5 mg/mL (8.58 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 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 | 3.4329 mL | 17.1644 mL | 34.3289 mL | |
| 5 mM | 0.6866 mL | 3.4329 mL | 6.8658 mL | |
| 10 mM | 0.3433 mL | 1.7164 mL | 3.4329 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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