AS8351 (Synonyms: NCI 51355, NSC 51355) |
| رقم الكتالوجGC17820 |
AS8351 (NSC51355) هو مثبط KDM5B ، والذي يمكن أن يحفز ويحافظ على علامات الكروماتين النشطة لتسهيل تحريض الخلايا الشبيهة بخلايا عضلة القلب
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Cas No.: 796-42-9
Sample solution is provided at 25 µL, 10mM.
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IC50: N/A
AS8351 is a histone demethylase inhibitor.
Histone methylation is considered as a more dynamic modification with the discovery of Histone demethylases. Removal of methyl groups is mediated by LSD1, PAD14 and JmjC domain containing proteins.
In vitro: In a previous study, in order to identify indispensable factors for human fibroblasts, the authors removed combined compounds one by one and treated cells with the remaining compounds. Results showed that the number of beating clusters was significantly reduced by removal of seven compounds including AS8351. Moreover, these seven compounds inlcuding AS8351 were sufficient and necessary to induce cardiac reprogramming efficiently. The authors then investigated the role of the reprogramming compound of AS8351 and the results showed that AS8351 and its functional analogs could affect epigenetic modifications by competing with α- ketoglutarate for chelating iron/Fe(II) in some epigenetic enzymes, including the JmjC-domain-containing histone demethylases that require α-KG and iron as co-factors. In addition, the authors abrogated each of the 22 genes in the JmjC-KDM family by small hairpin RNAs and found that only with KDM5B knockdown, or using a KDM5B inhibitor, PBIT could phenocopy AS8351 in generating ciCMs, indicating that it might be a target of AS8351 [1].
In vivo: Currently, there is no animal in vivo data reported.
Clinical trial: Up to now, AS8351 is still in the preclinical development stage.
Reference:
[1] N. Cao, Y. Huang, J. Zheng,et al.Conversion of human fibroblasts into functional cardiomyocytes by small molecules.Science 352(6290),1216-1220(2016).
| Cas No. | 796-42-9 | SDF | |
| المرادفات | NCI 51355, NSC 51355 | ||
| Chemical Name | (E)-N'-((2-hydroxynaphthalen-1-yl)methylene)isonicotinohydrazide | ||
| Canonical SMILES | OC(C=CC1=CC=CC=C12)=C2/C([H])=N/NC(C3=CC=NC=C3)=O | ||
| Formula | C17H13N3O2 | M.Wt | 291.3 |
| الذوبان | ≥ 29.1mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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- Purity: >99.50%
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