1. Epigenetics
  2. Histone Acetyltransferase
  3. Remodelin hydrobromide

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

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Remodelin hydrobromide Chemical Structure

Remodelin hydrobromide Chemical Structure

CAS No. : 1622921-15-6

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10 mM * 1 mL in DMSO
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Remodelin hydrobromide:

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Remodelin hydrobromide is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin hydrobromide inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin hydrobromide inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin hydrobromide enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model[1][2][3][4].

In Vitro

Remodelin hydrobromide (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 hydrobromide (20 μΜ, 24 hours) inhibits NAT10 and slows DNA replication in prostate cancer cells[2].
Remodelin hydrobromide (1 μΜ, 7 days) decreases nuclear shape defects and increase genomic stability in LmnaG609G/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: 20 μM
Incubation Time: 24 h
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 LmnaG609G/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 hydrobromide (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 hydrobromide (100 mg/kg, p.o.) inhibits NAT10 and significantly enhances the healthspan in aLmnaG609G/G609G hutchinson-gilford progeria syndrome (HGPS) mouse model. Remodelin hydrobromide (5 mg/kg, p.o.) shows a T1/2 of 1.81 hours and oral bioavailability (F%) of 43.5% in mice[3].
Pharmacokinetic parameters for Remodelin hydrobromide in Mice[1]

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

Route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng/h/mL) AUC0-Ꝏ (ng/h/mL) MRT_last (h) F(%)
p.o. 5 1.81 0.25 409 235 259 0.84 43.5%
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: LmnaG609G/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
Result: Ameliorated age-dependent weight loss.
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 T1/2 of 1.81 hours and oral bioavailability (F%) of 43.5% in mice[3].
Molecular Weight

363.28

Formula

C15H15BrN4S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

N#CC1=CC=C(C2=CSC(N/N=C3CCCC/3)=N2)C=C1.[H]Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 44 mg/mL (121.12 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7527 mL 13.7635 mL 27.5270 mL
5 mM 0.5505 mL 2.7527 mL 5.5054 mL
View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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

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:  15% Cremophor EL    85% Saline

    Solubility: 10 mg/mL (27.53 mM); Suspended solution; Need ultrasonic

  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (6.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.49%

References

Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7527 mL 13.7635 mL 27.5270 mL 68.8174 mL
5 mM 0.5505 mL 2.7527 mL 5.5054 mL 13.7635 mL
10 mM 0.2753 mL 1.3763 mL 2.7527 mL 6.8817 mL
15 mM 0.1835 mL 0.9176 mL 1.8351 mL 4.5878 mL
20 mM 0.1376 mL 0.6882 mL 1.3763 mL 3.4409 mL
25 mM 0.1101 mL 0.5505 mL 1.1011 mL 2.7527 mL
30 mM 0.0918 mL 0.4588 mL 0.9176 mL 2.2939 mL
40 mM 0.0688 mL 0.3441 mL 0.6882 mL 1.7204 mL
50 mM 0.0551 mL 0.2753 mL 0.5505 mL 1.3763 mL
60 mM 0.0459 mL 0.2294 mL 0.4588 mL 1.1470 mL
80 mM 0.0344 mL 0.1720 mL 0.3441 mL 0.8602 mL
100 mM 0.0275 mL 0.1376 mL 0.2753 mL 0.6882 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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