Art. -Nr.: HY-16706

Remodelin

19 Cited Publications

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Based on 19 publication(s) in Google Scholar

Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model.

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Reinheit: 99.84%
CAS. Nr.: 949912-58-7
Formel: C₁₅H₁₄N₄S
Molecular Weight:282.36

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Remodelin Chemical Structure

CAS. Nr.: 949912-58-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (19)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

NAT10

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BTI-TN-5B1-4	IC₅₀	221 nM Compound: 9	Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay	[PMID: 20579890]
BTI-TN-5B1-4	IC₅₀	644 nM Compound: 9	Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay	[PMID: 20579890]

In Vitro

Remodelin (10-40 μΜ, 1-7 days) inhibits NAT10 activity and cell proliferation with a dose-dependent manner in both AR-positive and AR-negative prostate cancer cells^[2].
Remodelin (20 μΜ, 24 hours) inhibits NAT10 and slows DNA replication in prostate cancer cells^[2].
Remodelin (1 μΜ, 7 days) decreases nuclear shape defects and increase genomic stability in Lmna^G609G/G609G fibroblasts^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:

Prostate cancer cell lines VCaP, PC3, and DU145
Concentration:

0,10,20,40 μM
Incubation Time:

1,2,7 days
Result:

Inhibited NAT10 and suppressed the growth of both AR-positive and AR-negative prostate cancer cells.
Displayed significantly decreased cell proliferation activity over time, compared to the control group.
Decreased colony formation ability with a dose-dependent manner.

Immunofluorescence^[2]

Cell Line:

Prostate cancer cell lines VCaP, PC3, and DU145
Concentration:

0,10,20,40 μM
Incubation Time:

24 hours
Result:

Showed a significant decrease in both the positive labeling rate and the fluorescence intensity compared to the control group.
Significantly reduced both the staining foci of IdU and the staining foci of CldU compared to control group.

Western Blot Analysis^[3]

Cell Line:

Skin fibroblasts from Lmna^G609G/G609G and wildtype (WT) littermates
Concentration:

1 μM
Incubation Time:

7 days
Result:

Decreased the higher level of the DNA double-strand break (DSB) marker gamma H2AX (γH2AX, Ser-139 phosphorylated histone H2AX).

In Vivo

Remodelin (2 or 20 mg/kg, i.p., once every two days for 4 weeks) significantly reduces AR-negative prostate cancer tumor growth in tumor xenograft nude mice model^[2].
Remodelin (100 mg/kg, p.o.) inhibits NAT10 and significantly enhances the healthspan in aLmna^G609G/G609G hutchinson-gilford progeria syndrome (HGPS) mouse model. Remodelin (5 mg/kg, p.o.) shows a T_1/2 of 1.81 hours and oral bioavailability (F%) of 43.5% in mice^[3].
Pharmacokinetic parameters for Remodelin in Mice^[1]
Pharmacokinetic parameters for Remodelin in Mice^[1]

Route	Dose (mg/kg)	T_1/2 (h)	T_max (h)	C_max (ng/mL)	AUC_0-t (ng/h/mL)	AUC_0-Ꝏ (ng/h/mL)	MRT_last (h)	F(%)
p.o.	5	1.81	0.25	409	235	259	0.84	43.5%

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

PC-3 cells tumor xenograft model in nude athymic BALB/c nu/nu mice^[2]
Dosage:

2 or 20 mg/kg
Administration:

Intraperitoneal injection (i.p.), once every two days for 4 weeks
Result:

Significantly reduced 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 Model:

Lmna^G609G/G609G hutchinson-gilford progeria syndrome (HGPS) mouse model^[3]
Dosage:

100 mg/kg
Administration:

Oral gavage (p.o.), daily schedule for 3 weeks of age onward, until the end-point Ameliorated age-dependent weight loss.
Result:

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 Model:

WT Mice (Pharmacokinetic assay)^[3]
Dosage:

5 mg/kg
Administration:

Oral gavage (p.o.)
Result:

Showed a T_1/2 of 1.81 hours and oral bioavailability (F%) of 43.5% in mice^[3].

Chemical Information

CAS. Nr. 949912-58-7
Appearance Solid
Molecular Weight 282.36
Formel C₁₅H₁₄N₄S
Color Off-white to light yellow
SMILES

N#CC1=CC=C(C2=CSC(N/N=C3CCCC/3)=N2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (19)

All Apoptosis AnalysisWBIHC

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Journal Impact Factor

Adv Sci (Weinh)

Trained Immunity Exacerbates Inflammatory Arthritis Progression via Promoting Synovial Fibroblast Ferroptotic Resistance. [Abstract]

2025 Dec;12(46):e04245. PMID: 41255239

Remodelin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Dec;12(46):e04245. [Abstract]

CIA-FLS co-cultured with trained macrophages in a 1:1 ratio for 72 h in the presence of 25.0 μM Remodelin ± 4.5 μg/mL anti-IL-1β, Western blot analysis of FSP1 or Actin expression.

Remodelin purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Dec;12(46):e04245. [Abstract]

The levels of 4-HNE and 8-OHDG in VCAM+ FLS were elevated in the hyperplastic synovium of β-glu/CIA rats treated with both iFSP1 and Remodelin (40.0 mg/kg daily).
J Hazard Mater

Nanoplastic-induced NAT10/ac4C axis drives both oxidative stress and chemoresistance. [Abstract]

2025 Oct 19:499:140193. PMID: 41124733
Cell Death Dis

N4-acetylcytidine-dependent GLMP mRNA stabilization by NAT10 promotes head and neck squamous cell carcinoma metastasis and remodels tumor microenvironment through MAPK/ERK signaling pathway. [Abstract]

2023 Nov 1;14(11):712. PMID: 37914704

Remodelin purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Nov 1;14(11):712. [Abstract]

Representative of IHC (H) were displayed in randomly selected tumor and quantification of the relative intensities of IHC staining (I–M) was performed. Data are shown as mean ± SEM at least three independent experiments. P-values were calculated by two-sided Student’s t-test in (F) and two-sided log-rank test in (G). (Remodelin 5 mg/kg).
Acta Pharmacol Sin

Activated SIRT1 contributes to DPT-induced glioma cell parthanatos by upregulation of NOX2 and NAT10. [Abstract]

2023 Oct;44(10):2125-2138. PMID: 37277492
Oncogene

BRD4 inhibition sensitizes cervical cancer to radiotherapy by attenuating DNA repair. [Abstract]

2021 Apr;40(15):2711-2724. PMID: 33712705
Cell Rep

NAT10-dependent N4-acetylcytidine reprograms R-loops and promotes cancer stem cell growth. [Abstract]

2026 Jun 23;45(6):117408. PMID: 42228575
Cell Rep

NAT10-mediated ac4C tRNA modification promotes EGFR mRNA translation and gefitinib resistance in cancer. [Abstract]

2023 Jul 17;42(7):112810. PMID: 37463108

Remodelin purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Jul 17;42(7):112810. [Abstract]

Remodelin (0-50 μM) treatment reduced the protein level of NAT10 and inhibited ESCA cell proliferation in a dose-dependent manner

Remodelin purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Jul 17;42(7):112810. [Abstract]

Remodelin (25 μM) treatment can significantly increase the apoptosis of both TE9 and ECA109 ESCA cells.
J Agric Food Chem

Antimicrobial Peptide BCp12 Inhibits Staphylococcus aureus Growth by Altering Lysine Malonylation Levels in the Arginine Synthesis Pathway. [Abstract]

2022 Jan 12;70(1):403-414. PMID: 34942069
Life Sci

Targeting NAT10 protects against sepsis-induced skeletal muscle atrophy by inhibiting ROS/NLRP3. [Abstract]

2023 Oct 1:330:121948. PMID: 37467885
J Mol Med (Berl)

Combination of PARP inhibitor and temozolomide to suppress chordoma progression. [Abstract]

2019 Aug;97(8):1183-1193. PMID: 31201471
iScience

Mechanistic study of N-acetyltransferase 10 deficiency enhancing olaparib sensitivity in triple negative breast cancer by inhibiting RAD51 N4-acetylcytidine modification. [Abstract]

2025 Jun 9;28(7):112860. PMID: 40606759
J Virol

N-acetyltransferase 10 regulates alphavirus replication via N4-acetylcytidine (ac4C) modiﬁcation of the lymphocyte antigen six family member E (LY6E) mRNA. [Abstract]

2024 Jan 23;98(1):e0135023. PMID: 38169284
Heliyon

ac4C acetylation regulates mRNA stability and translation efficiency in osteosarcoma. [Abstract]

2023 Jun 8;9(6):e17103. PMID: 37484432
Epigenetics

MK-801-exposure induces increased translation efficiency and mRNA hyperacetylation of Grin2a in the mouse prefrontal cortex. [Abstract]

2024 Dec;19(1):2417158. PMID: 39460980
bioRxiv

2026 Jun 19.
bioRxiv

2026 Jan 14.
bioRxiv

NAT10 Suppresses RNA Sensing Induced IFN-β Transactivation to Promote Viral Infection via Interfering with IRF3 Activities. [Abstract]

2025 Sep 1:2025.09.01.673489. PMID: 40949982
SSRN

2025 Jul 28.
bioRxiv

2023 Feb 11.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 116.67 mg/mL (413.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (17.71 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (17.71 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 10 mg/mL (35.42 mM); Suspended solution; Need ultrasonic

Protocol 2

Add each solvent one by one: 0.5% CMC/saline water

Solubility: 5 mg/mL (17.71 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (394 KB)
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- Español - ES (394 KB)
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- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Larrieu D, et al. Chemical inhibition of NAT10 corrects defects of laminopathic cells. Science. 2014 May 2;344(6183):527-32. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Route	Dose (mg/kg)	T_1/2 (h)	T_max (h)	C_max (ng/mL)	AUC_0-t (ng/h/mL)	AUC_0-Ꝏ (ng/h/mL)	MRT_last (h)	F(%)
p.o.	5	1.81	0.25	409	235	259	0.84	43.5%

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.5416 mL	17.7079 mL	35.4158 mL	88.5395 mL
	5 mM	0.7083 mL	3.5416 mL	7.0832 mL	17.7079 mL
	10 mM	0.3542 mL	1.7708 mL	3.5416 mL	8.8539 mL
	15 mM	0.2361 mL	1.1805 mL	2.3611 mL	5.9026 mL
	20 mM	0.1771 mL	0.8854 mL	1.7708 mL	4.4270 mL
	25 mM	0.1417 mL	0.7083 mL	1.4166 mL	3.5416 mL
	30 mM	0.1181 mL	0.5903 mL	1.1805 mL	2.9513 mL
	40 mM	0.0885 mL	0.4427 mL	0.8854 mL	2.2135 mL
	50 mM	0.0708 mL	0.3542 mL	0.7083 mL	1.7708 mL
	60 mM	0.0590 mL	0.2951 mL	0.5903 mL	1.4757 mL
	80 mM	0.0443 mL	0.2213 mL	0.4427 mL	1.1067 mL
	100 mM	0.0354 mL	0.1771 mL	0.3542 mL	0.8854 mL

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Remodelin

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Remodelin

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Remodelin

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Remodelin

Alle Histone Acetyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Remodelin Related Classifications

Art. -Nr.: HY-16706