Remodelin

Alias: Remodelin
Cat No.:V2042 Purity: ≥98%
Remodelin is a novel, selective and potent acetyl-transferase NAT10 inhibitor that is cell-permeable and stable analog of CPTH2.
Remodelin Chemical Structure CAS No.: 949912-58-7
Product category: Histone Acetyltransferase
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
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Other Forms of Remodelin:

  • Remodelin HBr
Official Supplier of:
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Top Publications Citing lnvivochem Products
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Remodelin is a novel, selective and potent acetyl-transferase NAT10 inhibitor that is cell-permeable and stable analog of CPTH2. Remodelin inhibits acetyl-transferase NAT10, a nuclear N-acetyltransferase involved in stabilization of microtubules. Remodelin was found to correct cell defects associated with progeria, restoring and improving nuclear shape and reducing the DNA damage believed to be associated with mutations in the gene for laminin A. 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. Remodelin is a useful chemical tool to study how NAT10 affects nuclear architecture and suggest alternative strategies for treating laminopathies and aging.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Both AR-positive and AR-negative prostate cancer cells exhibit dose-dependent inhibition of NAT10 function and cell proliferation when exposed to remodelin (10–40 μM) for 1–7 days [2]. In prostate cancer cells, remodelin (20 μM, 24 hours) inhibits NAT10 and slows down DNA replication [2]. In LmnaG609G/G609G fibroblasts, remodelin (1 μM, 7 days) decreases nuclear morphological abnormalities and promotes genome stability [3].
ln Vivo
In a tumor xenograft nude mouse model, remodelin (2 or 20 mg/kg, intraperitoneally, once every two days for 4 weeks) dramatically slows the growth of AR-negative prostate cancer [2]. Remodelin (100 mg/kg, oral) prolongs healthspan in the LmnaG609G/G609G mouse model of premature aging syndrome (HGPS) by a significant amount and suppresses NAT10 [3]. In mice, remodelin (5 mg/kg, oral) had an oral bioavailability (F%) of 43.5% and a T1/2 of 1.81 hours [3]. Mouse remodelin pharmacokinetic parameters: route dose (mg/kg), T1/2 (h), Tmax (h), Cmax (ng/mL), AUC0-t (ng/h/mL), AUC0-Ɲ (ng/h/mL), MRT_last (h), F(%) po 5 1.81 0.25 409 235 259 0.84 43.5%
Cell Assay
Cell Proliferation Assay[2]
Cell Types: Prostate cancer cell lines VCaP, PC3, and DU145
Tested Concentrations: 0,10,20,40 μM
Incubation Duration: 1,2,7 days
Experimental Results: Inhibited NAT10 and suppressed the growth of both AR- positive and AR-negative prostate cancer cells. Displayed Dramatically diminished cell proliferation activity over time, compared to the control group. diminished colony formation ability with a dose-dependent manner.

Immunofluorescence[2]
Cell Types: Prostate cancer cell lines VCaP, PC3, and DU145
Tested Concentrations: 0,10,20,40 μM
Incubation Duration: 24 hrs (hours)
Experimental Results: demonstrated a significant decrease in both the positive labeling rate and the fluorescence intensity compared to the control group. Dramatically decreased both the staining foci of IdU and the staining foci of CldU compared to control group.

Western Blot Analysis[3]
Cell Types: Skin fibroblasts from LmnaG609G/G609G and wildtype (WT) littermates
Tested Concentrations: 1 μM
Incubation Duration: 7 days
Experimental Results: diminished the higher level of the DNA dou
Animal Protocol
Animal/Disease Models: PC-3 cells tumor xenograft model in nude athymic BALB/c nu/nu (nude) mice[2]
Doses: 2 or 20 mg/ kg
Route of Administration: intraperitoneal (ip)injection, once every two days for 4 weeks
Experimental Results: Dramatically decreased AR-negative prostate cancer tumor growth. In the high-dose group, xenograft tumor weight at the endpoint was much smaller than that in the low- dose group.

Animal/Disease Models: LmnaG609G/G609G hutchinson-gilford progeria syndrome (HGPS) mouse model[3]
Doses: 100 mg/kg
Route of Administration: po (oral gavage), daily schedule for 3 weeks of age onward, until the end-point Ameliorated age-dependent weight loss.
Experimental Results: Ameliorated cardiac pathology. Led to the dramatic amelioration of HGPS cardiac pathologies, including reduction of adventitial fibrosis of the aorta, rescue of vascular smooth muscle cell loss, and salvage of smooth muscle actin (SMA) loss , both in the aorta and the coronary arteries.

Animal/Disease Models: WT Mice (pharmacokinetic/PK assay)[3]
Doses: 5 mg/kg
Route of Administration: Oral gav
References
[1]. Larrieu D, et al. Chemical inhibition of NAT10 corrects defects of laminopathic cells. Science. 2014 May 2;344(6183):527-32.
[2]. Ma N, et.al. Inhibition of N-Acetyltransferase 10 Suppresses the Progression of Prostate Cancer through Regulation of DNA Replication. Int J Mol Sci. 2022 Jun 12;23(12):6573.
[3]. Balmus G, et.al. Targeting of NAT10 enhances healthspan in a mouse model of human accelerated aging syndrome. Nat Commun. 2018 Apr 27;9(1):1700.
[4]. Zhang X, et.al. N-Acetyltransferase 10 Enhances Doxorubicin Resistance in Human Hepatocellular Carcinoma Cell Lines by Promoting the Epithelial-to-Mesenchymal Transition. Oxid Med Cell Longev. 2019 Jul 1;2019:7561879.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H14N4S
Molecular Weight
282.36
CAS #
949912-58-7
SMILES
N#CC1=CC=C(C2=CSC(N/N=C3CCCC/3)=N2)C=C1
Synonyms
Remodelin
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)
Solubility Data
Solubility (In Vitro)
DMSO: 72 mg/mL
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.5416 mL 17.7079 mL 35.4158 mL
5 mM 0.7083 mL 3.5416 mL 7.0832 mL
10 mM 0.3542 mL 1.7708 mL 3.5416 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.

Calculator

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.
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Biological Data
  • Remodelin

    Inhibiting NAT10 activity by Remodelin mediates nuclear shape rescue of LMNA depleted cells. Science. 2014 May 2;344(6183):527-32.

  • Remodelin

    Remodelin targets NAT10 to improve nuclear shape and fitness of HGPS cells. Science. 2014 May 2;344(6183):527-32.

  • Remodelin

    Inhibiting NAT10 acetyltransferase activity modifies microtubule organisation to rescue nuclear shape defects. Science. 2014 May 2;344(6183):527-32.

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