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MedKoo Cat#: 574858 | Name: Remodelin
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Remodelin is an inhibitor of N-acetyltransferase 10 (NAT10), which acetylates both histones and microtubules. It improves nuclear shape in HGPS (Hutchinson-Gilford progeria syndrome) cells and lamin A/C depleted cells. Remodelin improves nuclear architecture, chromatin organization, and survival of both cells lacking lamin A and cells from patients with progeria. reported to reverse the effect of cancer conditions such as epithelial to mesenchymal transition, hypoxia, and drug resistance.

Chemical Structure

Remodelin
Remodelin
CAS#949912-58-7 (free base)

Theoretical Analysis

MedKoo Cat#: 574858

Name: Remodelin

CAS#: 949912-58-7 (free base)

Chemical Formula: C15H14N4S

Exact Mass: 282.0939

Molecular Weight: 282.36

Elemental Analysis: C, 63.81; H, 5.00; N, 19.84; S, 11.35

Price and Availability

Size Price Availability Quantity
10mg USD 600.00 2 Weeks
25mg USD 950.00 2 Weeks
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Related CAS #
949912-58-7 (free base) 1622921-15-6 (HBr)
Synonym
Remodelin
IUPAC/Chemical Name
4-[2-(2-cyclopentylidenehydrazinyl)-4-thiazolyl]-benzonitrile
InChi Key
XAEJIFARBQJLML-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H14N4S/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)
SMILES Code
N#CC1=CC=C(C2=CSC(N/N=C3CCCC\3)=N2)C=C1
Appearance
A crystalline solid
Purity
>95% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, DMF, and ethanol
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO, DMF, and ethanol
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Remodelin is a 2-thiazolylhydrazone derivative that, at 10 µM, improves nuclear architecture, chromatin organization, and survival of both cells lacking lamin A and cells from patients with progeria. Remodelin is an inhibitor of N-acetyltransferase 10 (NAT10), which acetylates both histones and microtubules. Mutation of NAT10 mimics the effects of remodelin on nuclear morphology, suggesting that these effects of remodelin require NAT10.1 Remodelin also has cytotoxic effects against some species of the fungus Candida.
In vitro activity:
This study found a statistically significant decrease in total cholesterol and triglycerides in Remodelin treated cancer cells. The results showed that Remodelin alters mitochondrial fatty acid metabolism and lipid accumulation in cancer cells. Reference: J Cell Biochem. 2021 Dec;122(12):1936-1945. https://pubmed.ncbi.nlm.nih.gov/34605570/
In vivo activity:
This study showed that Remodelin, an inhibitor of NAT10, effectively inhibits the growth of prostate cancer cells under either no castration or castration conditions, likely by impairing DNA replication. Reference: Int J Mol Sci. 2022 Jun 12;23(12):6573. https://pubmed.ncbi.nlm.nih.gov/35743017/
Solvent mg/mL mM
Solubility
DMF 30.0 106.25
DMSO 15.0 53.12
Ethanol 1.0 3.54
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 282.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Dalhat MH, Mohammed MRS, Ahmad A, Khan MI, Choudhry H. Remodelin, a N-acetyltransferase 10 (NAT10) inhibitor, alters mitochondrial lipid metabolism in cancer cells. J Cell Biochem. 2021 Dec;122(12):1936-1945. doi: 10.1002/jcb.30155. Epub 2021 Oct 4. PMID: 34605570. 2. Shrimp JH, Jing Y, Gamage ST, Nelson KM, Han J, Bryson KM, Montgomery DC, Thomas JM, Nance KD, Sharma S, Fox SD, Andressen T, Sinclair WR, Wu H, Allali-Hassani A, Senisterra G, Vedadi M, Lafontaine D, Dahlin JL, Marmorstein R, Walters MA, Meier JL. Remodelin Is a Cryptic Assay Interference Chemotype That Does Not Inhibit NAT10-Dependent Cytidine Acetylation. ACS Med Chem Lett. 2020 Jul 27;12(6):887-892. doi: 10.1021/acsmedchemlett.0c00193. PMID: 34141066; PMCID: PMC8201477. 3. Ma N, Liu H, Wu Y, Yao M, Zhang B. 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. doi: 10.3390/ijms23126573. PMID: 35743017; PMCID: PMC9223896. 4. Zhang Z, Zhang Y, Cai Y, Li D, He J, Feng Z, Xu Q. NAT10 regulates the LPS-induced inflammatory response via the NOX2-ROS-NF-κB pathway in macrophages. Biochim Biophys Acta Mol Cell Res. 2023 Jun 10:119521. doi: 10.1016/j.bbamcr.2023.119521. Epub ahead of print. PMID: 37307924.
In vitro protocol:
1. Dalhat MH, Mohammed MRS, Ahmad A, Khan MI, Choudhry H. Remodelin, a N-acetyltransferase 10 (NAT10) inhibitor, alters mitochondrial lipid metabolism in cancer cells. J Cell Biochem. 2021 Dec;122(12):1936-1945. doi: 10.1002/jcb.30155. Epub 2021 Oct 4. PMID: 34605570. 2. Shrimp JH, Jing Y, Gamage ST, Nelson KM, Han J, Bryson KM, Montgomery DC, Thomas JM, Nance KD, Sharma S, Fox SD, Andressen T, Sinclair WR, Wu H, Allali-Hassani A, Senisterra G, Vedadi M, Lafontaine D, Dahlin JL, Marmorstein R, Walters MA, Meier JL. Remodelin Is a Cryptic Assay Interference Chemotype That Does Not Inhibit NAT10-Dependent Cytidine Acetylation. ACS Med Chem Lett. 2020 Jul 27;12(6):887-892. doi: 10.1021/acsmedchemlett.0c00193. PMID: 34141066; PMCID: PMC8201477.
In vivo protocol:
1. Ma N, Liu H, Wu Y, Yao M, Zhang B. 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. doi: 10.3390/ijms23126573. PMID: 35743017; PMCID: PMC9223896. 2. Zhang Z, Zhang Y, Cai Y, Li D, He J, Feng Z, Xu Q. NAT10 regulates the LPS-induced inflammatory response via the NOX2-ROS-NF-κB pathway in macrophages. Biochim Biophys Acta Mol Cell Res. 2023 Jun 10:119521. doi: 10.1016/j.bbamcr.2023.119521. Epub ahead of print. PMID: 37307924.
1: Dalhat MH, Mohammed MRS, Ahmad A, Khan MI, Choudhry H. Remodelin, a N-acetyltransferase 10 (NAT10) inhibitor, alters mitochondrial lipid metabolism in cancer cells. J Cell Biochem. 2021 Dec;122(12):1936-1945. doi: 10.1002/jcb.30155. Epub 2021 Oct 4. PMID: 34605570. 2: Shrimp JH, Jing Y, Gamage ST, Nelson KM, Han J, Bryson KM, Montgomery DC, Thomas JM, Nance KD, Sharma S, Fox SD, Andressen T, Sinclair WR, Wu H, Allali- Hassani A, Senisterra G, Vedadi M, Lafontaine D, Dahlin JL, Marmorstein R, Walters MA, Meier JL. Remodelin Is a Cryptic Assay Interference Chemotype That Does Not Inhibit NAT10-Dependent Cytidine Acetylation. ACS Med Chem Lett. 2020 Jul 27;12(6):887-892. doi: 10.1021/acsmedchemlett.0c00193. PMID: 34141066; PMCID: PMC8201477. 3: Xie R, Cheng L, Huang M, Huang L, Chen Z, Zhang Q, Li H, Lu J, Wang H, Zhou Q, Huang J, Chen X, Lin T. NAT10 Drives Cisplatin Chemoresistance by Enhancing ac4C-Associated DNA Repair in Bladder Cancer. Cancer Res. 2023 May 15;83(10):1666-1683. doi: 10.1158/0008-5472.CAN-22-2233. PMID: 36939377. 4: Wu Y, Cao Y, Liu H, Yao M, Ma N, Zhang B. Remodelin, an inhibitor of NAT10, could suppress hypoxia-induced or constitutional expression of HIFs in cells. Mol Cell Biochem. 2020 Sep;472(1-2):19-31. doi: 10.1007/s11010-020-03776-w. Epub 2020 Jun 11. Erratum in: Mol Cell Biochem. 2020 Sep;472(1-2):33. doi: 10.1007/s11010-020-03822-7. PMID: 32529496. 5: Shi J, Yang C, Zhang J, Zhao K, Li P, Kong C, Wu X, Sun H, Zheng R, Sun W, Chen L, Kong X. NAT10 Is Involved in Cardiac Remodeling Through ac4C-Mediated Transcriptomic Regulation. Circ Res. 2023 Dec 8;133(12):989-1002. doi: 10.1161/CIRCRESAHA.122.322244. Epub 2023 Nov 13. PMID: 37955115. 6: Guo Q, Yu W, Tan J, Zhang J, Chen J, Rao S, Guo X, Cai K. Remodelin delays non-small cell lung cancer progression by inhibiting NAT10 via the EMT pathway. Cancer Med. 2024 Jun;13(11):e7283. doi: 10.1002/cam4.7283. PMID: 38826095; PMCID: PMC11145023. 7: Mathieu J, Ruohola-Baker H. Metabolic RemodeLIN of Pluripotency. Cell Stem Cell. 2016 Jul 7;19(1):3-4. doi: 10.1016/j.stem.2016.06.016. PMID: 27392218. 8: Wang C, Liu Y, Zhang Y, Wang D, Xu L, Li Z, Bai X, Wang Y. Targeting NAT10 protects against sepsis-induced skeletal muscle atrophy by inhibiting ROS/NLRP3. Life Sci. 2023 Oct 1;330:121948. doi: 10.1016/j.lfs.2023.121948. Epub 2023 Jul 17. PMID: 37467885. 9: Jin C, Wang T, Zhang D, Yang P, Zhang C, Peng W, Jin K, Wang L, Zhou J, Peng C, Tan Y, Ji J, Chen Z, Sun Q, Yang S, Tang J, Feng Y, Sun Y. Acetyltransferase NAT10 regulates the Wnt/β-catenin signaling pathway to promote colorectal cancer progression via ac4C acetylation of KIF23 mRNA. J Exp Clin Cancer Res. 2022 Dec 15;41(1):345. doi: 10.1186/s13046-022-02551-7. PMID: 36522719; PMCID: PMC9753290. 10: Zhang Z, Zhang Y, Cai Y, Li D, He J, Feng Z, Xu Q. NAT10 regulates the LPS- induced inflammatory response via the NOX2-ROS-NF-κB pathway in macrophages. Biochim Biophys Acta Mol Cell Res. 2023 Oct;1870(7):119521. doi: 10.1016/j.bbamcr.2023.119521. Epub 2023 Jun 10. PMID: 37307924. 11: Larrieu D, Britton S, Demir M, Rodriguez R, Jackson SP. Chemical inhibition of NAT10 corrects defects of laminopathic cells. Science. 2014 May 2;344(6183):527-32. doi: 10.1126/science.1252651. PMID: 24786082; PMCID: PMC4246063. 12: Deng M, Zhang L, Zheng W, Chen J, Du N, Li M, Chen W, Huang Y, Zeng N, Song Y, Chen Y. Helicobacter pylori-induced NAT10 stabilizes MDM2 mRNA via RNA acetylation to facilitate gastric cancer progression. J Exp Clin Cancer Res. 2023 Jan 6;42(1):9. doi: 10.1186/s13046-022-02586-w. Erratum in: J Exp Clin Cancer Res. 2023 Apr 24;42(1):98. doi: 10.1186/s13046-023-02676-3. PMID: 36609449; PMCID: PMC9817303. 13: Wei R, Cui X, Min J, Lin Z, Zhou Y, Guo M, An X, Liu H, Janz S, Gu C, Wang H, Yang Y. NAT10 promotes cell proliferation by acetylating CEP170 mRNA to enhance translation efficiency in multiple myeloma. Acta Pharm Sin B. 2022 Aug;12(8):3313-3325. doi: 10.1016/j.apsb.2022.01.015. Epub 2022 Jan 29. PMID: 35967285; PMCID: PMC9366180. 14: Yang W, Li HY, Wu YF, Mi RJ, Liu WZ, Shen X, Lu YX, Jiang YH, Ma MJ, Shen HY. ac4C acetylation of RUNX2 catalyzed by NAT10 spurs osteogenesis of BMSCs and prevents ovariectomy-induced bone loss. Mol Ther Nucleic Acids. 2021 Jul 2;26:135-147. doi: 10.1016/j.omtn.2021.06.022. PMID: 34513300; PMCID: PMC8413676. 15: Wu Y, Cao Y, Liu H, Yao M, Ma N, Zhang B. Correction to: Remodelin, an inhibitor of NAT10, could suppress hypoxia-induced or constitutional expression of HIFs in cells. Mol Cell Biochem. 2020 Sep;472(1-2):33. doi: 10.1007/s11010-020-03822-7. Erratum for: Mol Cell Biochem. 2020 Sep;472(1-2):19-31. doi: 10.1007/s11010-020-03776-w. PMID: 32638257. 16: Ma W, Tian Y, Shi L, Liang J, Ouyang Q, Li J, Chen H, Sun H, Ji H, Liu X, Huang W, Gao X, Jin X, Wang X, Liu Y, Yu Y, Guo X, Tian Y, Yang F, Li F, Wang N, Cai B. N-Acetyltransferase 10 represses Uqcr11 and Uqcrb independently of ac4C modification to promote heart regeneration. Nat Commun. 2024 Mar 8;15(1):2137. doi: 10.1038/s41467-024-46458-7. PMID: 38459019; PMCID: PMC10923914. 17: Gao J, Xu P, Wang F, Zhang W, Min M, Urba R, Fan L. Revealing the pharmacological effects of Remodelin against osteosarcoma based on network pharmacology, acRIP-seq and experimental validation. Sci Rep. 2024 Feb 13;14(1):3577. doi: 10.1038/s41598-024-54197-4. PMID: 38347067; PMCID: PMC10861577. 18: Wu J, Zhu H, Wu J, Chen W, Guan X. Inhibition of N-acetyltransferase 10 using remodelin attenuates doxorubicin resistance by reversing the epithelial- mesenchymal transition in breast cancer. Am J Transl Res. 2018 Jan 15;10(1):256-264. PMID: 29423010; PMCID: PMC5801363. 19: Zhang W, Gao J, Fan L, Wang J, He B, Wang Y, Zhang X, Mao H. ac4C acetylation regulates mRNA stability and translation efficiency in osteosarcoma. Heliyon. 2023 Jun 8;9(6):e17103. doi: 10.1016/j.heliyon.2023.e17103. PMID: 37484432; PMCID: PMC10361233. 20: Balmus G, Larrieu D, Barros AC, Collins C, Abrudan M, Demir M, Geisler NJ, Lelliott CJ, White JK, Karp NA, Atkinson J, Kirton A, Jacobsen M, Clift D, Rodriguez R; Sanger Mouse Genetics Project; Adams DJ, Jackson SP. Targeting of NAT10 enhances healthspan in a mouse model of human accelerated aging syndrome. Nat Commun. 2018 Apr 27;9(1):1700. doi: 10.1038/s41467-018-03770-3. PMID: 29703891; PMCID: PMC5923383.