2. Epigenetics
  3. Histone Acetyltransferase
  4. Remodelin

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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Remodelin Chemical Structure

Remodelin Chemical Structure

CAS No. : 949912-58-7

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Customer Review

Based on 10 publication(s) in Google Scholar

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Remodelin Related Antibodies

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Description

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[1][2][3][4].

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 LmnaG609G/G609G fibroblasts[3].

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

Remodelin Related Antibodies

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 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 (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 aLmnaG609G/G609G hutchinson-gilford progeria syndrome (HGPS) mouse model. Remodelin (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 in Mice[1]

Pharmacokinetic parameters for Remodelin in Mice[1]
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%

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 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 T1/2 of 1.81 hours and oral bioavailability (F%) of 43.5% in mice[3].
Molecular Weight

282.36

Formula

C15H14N4S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (442.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
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, 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.

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In Vivo Dissolution Calculator
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Purity & Documentation

Purity: 99.92%

COA (246 KB) HNMR (261 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
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, 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.

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 Related Classifications

Help & FAQs
  • 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.

Keywords:

Remodelin949912-58-7Histone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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