Remodelin HBr
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MedKoo CAT#: 317135

CAS#: 1622921-15-6 (HBr)

Description: Remodelin is a cell-permeable, potent, and stable analog of CPTH2. Remodelin inhibits acetyl-transferase NAT10, a nucleolar N-acetyltransferase involved in stabilization of microtubules. Remodelin is a cell-permeable, potent, and stable analog of CPTH2. 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.

Chemical Structure

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Remodelin HBr
CAS# 1622921-15-6 (HBr)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 317135
Name: Remodelin HBr
CAS#: 1622921-15-6 (HBr)
Chemical Formula: C15H15BrN4S
Exact Mass: 0.00
Molecular Weight: 363.280
Elemental Analysis: C, 49.59; H, 4.16; Br, 22.00; N, 15.42; S, 8.83

Price and Availability

Size Price Availability Quantity
10mg USD 90 Ready to ship
25mg USD 150 Ready to ship
50mg USD 250 Ready to ship
100mg USD 450 Ready to ship
200mg USD 550 Ready to ship
500mg USD 750 Ready to ship
1g USD 950 Ready to ship
2g USD 1650 Ready to ship
5g USD 2650 Ready to ship
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Related CAS #: 949912-58-7 (free base)   1622921-15-6 (HBr)  

Synonym: Remodelin HBr; Remodelin Hydrobromide

IUPAC/Chemical Name: 4-[2-(2-Cyclopentylidenehydrazinyl)-4-thiazolyl]benzonitrile Hydrobromide

InChi Key: XNWBCMSPDCSWSD-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H14N4S.BrH/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);1H

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

Appearance: Solid powder

Purity: >98% (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: >2 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:

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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 25.0 68.82
DMF 25.0 68.82
Ethanol 0.5 1.38

Preparing Stock Solutions

The following data is based on the product molecular weight 363.28 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.

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1: de Carlo TE, Chin AT, Bonini Filho MA, Adhi M, Branchini L, Salz DA, Baumal CR, Crawford C, Reichel E, Witkin AJ, Duker JS, Waheed NK. DETECTION OF MICROVASCULAR CHANGES IN EYES OF PATIENTS WITH DIABETES BUT NOT CLINICAL DIABETIC RETINOPATHY USING OPTICAL COHERENCE TOMOGRAPHY ANGIOGRAPHY. Retina. 2015 Oct 14. [Epub ahead of print] PubMed PMID: 26469537.

2: Lacruz RS, Bromage TG, O'Higgins P, Toro-Ibacache V, Warshaw J, Berger LR. Distinct growth of the nasomaxillary complex in Au. sediba. Sci Rep. 2015 Oct 15;5:15175. doi: 10.1038/srep15175. PubMed PMID: 26469387.

3: Ock S, Lee WS, Ahn J, Kim HM, Kang H, Kim HS, Jo D, Abel ED, Lee TJ, Kim J. Deletion of IGF-1 Receptors in Cardiomyocytes Attenuates Cardiac Aging in Male Mice. Endocrinology. 2015 Oct 15:en20151709. [Epub ahead of print] PubMed PMID: 26469138.

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5: Kim SY, Sim CK, Tang H, Han W, Zhang K, Xu F. Acetylome Analysis Identifies SIRT1 Targets in mRNA-Processing and Chromatin-Remodeling in Mouse Liver. PLoS One. 2015 Oct 15;10(10):e0140619. doi: 10.1371/journal.pone.0140619. eCollection 2015. PubMed PMID: 26468954.

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7: Kokoszka P, Markuszewski J, Łapaj Ł, Wierusz-Kozłowska M. Remodeling of bone tissue around the distal part of Zweymüller stem. Ortop Traumatol Rehabil. 2015 Sep 7;17(4):371-80. doi: 10.5604/15093492.1173379. PubMed PMID: 26468174.

8: Kuzubova NA, Lebedeva ES, Dvorakovskaya IV, Surkova EA, Platonova IS, Titova ON. Modulating Effect of Peptide Therapy on the Morphofunctional State of Bronchial Epithelium in Rats with Obstructive Lung Pathology. Bull Exp Biol Med. 2015 Oct 15. [Epub ahead of print] PubMed PMID: 26468022.

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12: Dey D, Diaz Zamudio M, Schuhbaeck A, Juarez Orozco LE, Otaki Y, Gransar H, Li D, Germano G, Achenbach S, Berman DS, Meave A, Alexanderson E, Slomka PJ. Relationship Between Quantitative Adverse Plaque Features From Coronary Computed Tomography Angiography and Downstream Impaired Myocardial Flow Reserve by 13N-Ammonia Positron Emission Tomography: A Pilot Study. Circ Cardiovasc Imaging. 2015 Oct;8(10). pii: e003255. doi: 10.1161/CIRCIMAGING.115.003255. PubMed PMID: 26467104.

13: Sannegowda KM, Venkatesha SH, Moudgil KD. Tinospora cordifolia inhibits autoimmune arthritis by regulating key immune mediators of inflammation and bone damage. Int J Immunopathol Pharmacol. 2015 Oct 14. pii: 0394632015608248. [Epub ahead of print] PubMed PMID: 26467057.

14: Knorr RL, Lipowsky R, Dimova R. Autophagosome closure requires membrane scission. Autophagy. 2015 Oct 14:0. [Epub ahead of print] PubMed PMID: 26466816.

15: Hankins HM, Sere YY, Diab NS, Menon AK, Graham TR. Phosphatidylserine translocation at the yeast trans-Golgi network regulates protein sorting into exocytic vesicles. Mol Biol Cell. 2015 Oct 14. pii: mbc.E15-07-0487. [Epub ahead of print] PubMed PMID: 26466678.

16: Han S, Li YY, Chan BP. Protease inhibitors enhance extracellular collagen fibril deposition in human mesenchymal stem cells. Stem Cell Res Ther. 2015 Oct 15;6(1):197. doi: 10.1186/s13287-015-0191-1. PubMed PMID: 26466582.

17: Engelholm LH, Melander MC, Hald A, Persson M, Madsen DH, Jürgensen HJ, Johansson K, Nielsen C, Nørregaard KS, Ingvarsen SZ, Kjaer A, Trovik CS, Laerum OD, Bugge TH, Eide J, Behrendt N. Targeting a novel bone degradation pathway in primary bone cancer by inactivation of the collagen receptor uPARAP/Endo180. J Pathol. 2015 Oct 15. doi: 10.1002/path.4661. [Epub ahead of print] PubMed PMID: 26466547.

18: El-Najjar N, Orsó E, Wallner S, Liebisch G, Schmitz G. Increased Levels of Sphingosylphosphorylcholine (SPC) in Plasma of Metabolic Syndrome Patients. PLoS One. 2015 Oct 14;10(10):e0140683. doi: 10.1371/journal.pone.0140683. eCollection 2015. PubMed PMID: 26466367.

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