WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H527671
CAS#: 357649-93-5
Description: CPTH2 is a novel histone acetyltransferase inhibitor modulating Gcn5 network.
Hodoodo Cat#: H527671
Name: CPTH2
CAS#: 357649-93-5
Chemical Formula: C14H14ClN3S
Exact Mass: 291.06
Molecular Weight: 291.797
Elemental Analysis: C, 57.63; H, 4.84; Cl, 12.15; N, 14.40; S, 10.99
Synonym: CPTH2; CPTH 2; CPTH-2
IUPAC/Chemical Name: N-[4-(4-Chloro-phenyl)-thiazol-2-yl]-N'-cyclopentylidene-hydrazine
InChi Key: YYTHPXHGWSAKIZ-UHFFFAOYSA-N
InChi Code: InChI=1S/C14H14ClN3S/c15-11-7-5-10(6-8-11)13-9-19-14(16-13)18-17-12-3-1-2-4-12/h5-9H,1-4H2,(H,16,18)
SMILES Code: ClC1=CC=C(C2=CSC(N/N=C3CCCC/3)=N2)C=C1
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
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
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: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 291.80 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.
| 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: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Wu Y, Ma S, Xia Y, Lu Y, Xiao S, Cao Y, Zhuang S, Tan X, Fu Q, Xie L, Li Z, Yuan Z. Loss of GCN5 leads to increased neuronal apoptosis by upregulating E2F1- and Egr-1-dependent BH3-only protein Bim. Cell Death Dis. 2017 Jan 26;8(1):e2570. doi: 10.1038/cddis.2016.465. PubMed PMID: 28125090; PubMed Central PMCID: PMC5386373.
2: Canzonetta C, Leo M, Guarino SR, Montanari A, Francisci S, Filetici P. SAGA complex and Gcn5 are necessary for respiration in budding yeast. Biochim Biophys Acta. 2016 Dec;1863(12):3160-3168. doi: 10.1016/j.bbamcr.2016.10.002. Epub 2016 Oct 11. PubMed PMID: 27741413.
3: Hu N, Ren J, Zhang Y. Mitochondrial aldehyde dehydrogenase obliterates insulin resistance-induced cardiac dysfunction through deacetylation of PGC-1α. Oncotarget. 2016 Nov 22;7(47):76398-76414. doi: 10.18632/oncotarget.11977. PubMed PMID: 27634872; PubMed Central PMCID: PMC5363518.
4: Thevis M, Schänzer W. Emerging drugs affecting skeletal muscle function and mitochondrial biogenesis - Potential implications for sports drug testing programs. Rapid Commun Mass Spectrom. 2016 Mar 15;30(5):635-51. doi: 10.1002/rcm.7470. PubMed PMID: 26842585.
5: Yin YW, Jin HJ, Zhao W, Gao B, Fang J, Wei J, Zhang DD, Zhang J, Fang D. The Histone Acetyltransferase GCN5 Expression Is Elevated and Regulated by c-Myc and E2F1 Transcription Factors in Human Colon Cancer. Gene Expr. 2015;16(4):187-96. doi: 10.3727/105221615X14399878166230. PubMed PMID: 26637399; PubMed Central PMCID: PMC5584536.
6: Lin S, Nazif K, Smith A, Baas PW, Smith GM. Histone acetylation inhibitors promote axon growth in adult dorsal root ganglia neurons. J Neurosci Res. 2015 Aug;93(8):1215-28. doi: 10.1002/jnr.23573. Epub 2015 Feb 20. PubMed PMID: 25702820; PubMed Central PMCID: PMC4502923.
7: Shibuya M, Hatano M, Kawamura K. Interactive histone acetylation and methylation in regulating transdifferentiation-related genes during tunicate budding and regeneration. Dev Dyn. 2015 Jan;244(1):10-20. doi: 10.1002/dvdy.24212. Epub 2014 Oct 24. PubMed PMID: 25298085.
8: Carradori S, Rotili D, De Monte C, Lenoci A, D'Ascenzio M, Rodriguez V, Filetici P, Miceli M, Nebbioso A, Altucci L, Secci D, Mai A. Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: enzyme and cellular studies. Eur J Med Chem. 2014 Jun 10;80:569-78. doi: 10.1016/j.ejmech.2014.04.042. Epub 2014 Apr 15. PubMed PMID: 24835815.
9: Kamiya T, Machiura M, Makino J, Hara H, Hozumi I, Adachi T. Epigenetic regulation of extracellular-superoxide dismutase in human monocytes. Free Radic Biol Med. 2013 Aug;61:197-205. doi: 10.1016/j.freeradbiomed.2013.04.013. Epub 2013 Apr 18. PubMed PMID: 23602908.
10: Ablack JN, Cohen M, Thillainadesan G, Fonseca GJ, Pelka P, Torchia J, Mymryk JS. Cellular GCN5 is a novel regulator of human adenovirus E1A-conserved region 3 transactivation. J Virol. 2012 Aug;86(15):8198-209. doi: 10.1128/JVI.00289-12. Epub 2012 May 23. PubMed PMID: 22623781; PubMed Central PMCID: PMC3421684.
11: Chimenti F, Bizzarri B, Maccioni E, Secci D, Bolasco A, Chimenti P, Fioravanti R, Granese A, Carradori S, Tosi F, Ballario P, Vernarecci S, Filetici P. A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl)hydrazone. J Med Chem. 2009 Jan 22;52(2):530-6. doi: 10.1021/jm800885d. PubMed PMID: 19099397.
