RemodelinNAT10 inhibitor CAS# 1622921-15-6 |
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Quality Control & MSDS
3D structure
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Number of papers citing our products
| Cas No. | 1622921-15-6 | SDF | Download SDF |
| PubChem ID | 86280479 | Appearance | Powder |
| Formula | C15H15BrN4S | M.Wt | 363.28 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 44 mg/mL (121.12 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-[2-(2-cyclopentylidenehydrazinyl)-1,3-thiazol-4-yl]benzonitrile;hydrobromide | ||
| SMILES | C1CCC(=NNC2=NC(=CS2)C3=CC=C(C=C3)C#N)C1.Br | ||
| Standard InChIKey | XNWBCMSPDCSWSD-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C15H14N4S.BrH/c16-9-11-5-7-12(8-6-11)14-10-20-15(17-14)19-18-13-3-1-2-4-13;/h5-8,10H,1-4H2,(H,17,19);1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Remodelin HBr salt is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.
IC50 value:
Target: NAT10 inhibitor
Remodelin can improve nuclear architecture, chromatin organization, and fitness of both human lamin A/C-depleted cells and HGPS-derived patient cells, and decrease markers of DNA damage in these cells. Using a combination of chemical, cellular, and genetic approaches, acetyl-transferase protein NAT10 was identified as the target of Remodelin that mediated nuclear shape rescue in laminopathic cells via microtubule reorganization. Down-regulation and mutations of the nuclear-architecture proteins lamin A and C cause misshapen nuclei and altered chromatin organization associated with cancer and laminopathies, including the premature-aging disease Hutchinson-Gilford progeria syndrome (HGPS). Remodelin is a useful chemical tool to study how NAT10 affects nuclear architecture and suggest alternative strategies for treating laminopathies and aging. References: | |||||
Remodelin Dilution Calculator
Remodelin Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7527 mL | 13.7635 mL | 27.527 mL | 55.054 mL | 68.8174 mL |
| 5 mM | 0.5505 mL | 2.7527 mL | 5.5054 mL | 11.0108 mL | 13.7635 mL |
| 10 mM | 0.2753 mL | 1.3763 mL | 2.7527 mL | 5.5054 mL | 6.8817 mL |
| 50 mM | 0.0551 mL | 0.2753 mL | 0.5505 mL | 1.1011 mL | 1.3763 mL |
| 100 mM | 0.0275 mL | 0.1376 mL | 0.2753 mL | 0.5505 mL | 0.6882 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Remodelin is a potent inhibitor of NAT10 [1].
N-acetyltransferase 10 (NAT10) is the only identified lysine acetyltransferase that acts on microtubules and histones [1]. NAT10 mainly exists in the nucleolus.
Remodelin is a potent NAT10 inhibitor. In lamin A/C depletion (siLMNA) cells, remodelin remodeled nuclear architecture through inhibition of NAT10 lysine acetyltransferase activity. In cells derived from LMNA-mutated HGPS patients and primary MRC5 fibroblasts aged in culture, Remodelin significantly decreased the prevalence of misshapen nuclei. In U2OS cells and normal fibroblasts, remodelin inhibited nuclear shape defects induced by farnesyltransferase inhibitors (FTI). In HGPS cells, remodelin reduced the amount of misshapen nuclei, suggesting that inhibition of NAT10 mediated nuclear shape normalization. Also, remodelin reduced DNA damage signaling, reduced SUN1 accumulation at the nuclear envelope, reduced the levels of autophosphorylated ATM and DNA double-strand break markers γH2AX, and improved chromatin and nucleolar organization. In siLMNA and HGPS cells, remodelin inhibited microtubule anchorage to centrosomes [1].
Reference:
[1]. Larrieu D, Britton S, Demir M, et al. Chemical inhibition of NAT10 corrects defects of laminopathic cells. Science, 2014, 344(6183): 527-532.
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Cell Stem Cell. 2016 Jul 7;19(1):3-4.
Cellular metabolism is a key regulator of cell fate, including fate in pluripotent stem cells. Now in Cell Stem Cell, Zhang et al. (2016) show that Lin28 controls the metabolic transition from naive to primed pluripotency by directly repressing oxidative metabolism genes and metabolic intermediates involved in epigenetic regulation independently of let-7.
