357649-93-5
357649-93-5 結(jié)構(gòu)式
基本信息
Histone Acetyltransferase Inhibitor IV, CPTH2
Cyclopentylidene-[4-(4-chlorophenyl)thiazol-2-yl)hydrazone
Cyclopentanone, 2-[4-(4-chlorophenyl)-2-thiazolyl]hydrazone
物理化學(xué)性質(zhì)
制備方法
7283-39-8
536-38-9
357649-93-5
以2-亞環(huán)戊基肼-1-硫代甲酰胺和α-溴代-4-氯苯乙酮為原料合成4-(4-氯苯基)-2-(2-環(huán)戊基亞基肼基)噻唑的一般步驟：準(zhǔn)確稱取0.157 g環(huán)戊酮縮氨基硫脲席夫堿和0.234 g對(duì)氯-α-溴苯乙酮，置于反應(yīng)瓶中，加入15 mL異丙醇作為溶劑。在室溫下攪拌反應(yīng)混合物，并通過薄層色譜（TLC，展開劑比例為乙酸乙酯：石油醚=1：2）監(jiān)測(cè)反應(yīng)進(jìn)程。反應(yīng)4小時(shí)后，觀察到反應(yīng)體系無明顯變化，遂終止反應(yīng)。將反應(yīng)混合物過濾，所得濾餅用乙醇洗滌，最終獲得0.271 g白色固體產(chǎn)物。
參考文獻(xiàn)：
[1] Patent: CN108409683, 2018, A. Location in patent: Paragraph 0010; 0011
[2] Bioorganic and Medicinal Chemistry Letters, 2007, vol. 17, # 16, p. 4635 - 4640
[3] Bioorganic and Medicinal Chemistry, 2010, vol. 18, # 14, p. 5063 - 5070
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2026/06/05 | HY-W013274 | CPTH2 CPTH2 | 357649-93-5 | 1 mg | 371元 |
| 2026/06/05 | HY-W013274 | CPTH2 | 357649-93-5 | 5 mg | 875元 |
| 2026/06/05 | HY-W013274 | CPTH2 CPTH2 | 357649-93-5 | 10mM * 1mLin DMSO | 962元 |
常見問題列表
| Target | Value |
|
HAT
() | |
|
Gcn5p
() | |
|
KAT3B
() |
CPTH2 (100 μM; 12, 24, 48 hours) causes a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation.
CPTH2 (100 μM; 12 or 48 hours) causes a comparable drop of the activity in both cell lines.
CPTH2 (100 μM; 48 hours) produces a drastic increase in apoptotic/dead cell population after 48 h.
CPTH2 (100 μM; 12, 24, 48 hours) shows a reduced acetylation of both global AcH3 histone and H3AcK18.
CPTH2 (100 μM; 24, 48 hours) is capable to counteract invasion and migration of ccRCC-786-O cells in culture.
CPTH2 (0.2, 0.5, 1 mM) inhibits the growth of a GCN5 deleted strain and a single catalytic mutant E173H.
CPTH2 (0.6, 0.8 mM; for 24 hours) inhibits histone H3 acetylation in yeast cell cultures.
CPTH2 inhibits the Gcn5p dependent functional network.
Cell Proliferation Assay
| Cell Line: | Papillary thyroid (K1) and clear cell Renal Cell Carcinoma (ccRCC-786-O) cell lines |
| Concentration: | 100 μM |
| Incubation Time: | 12, 24, 48 hours |
| Result: | Caused a decrease in cell proliferation after as early as 12 h with a further significant reduction after 48 h stimulation. |
Cell Viability Assay
| Cell Line: | K1 and ccRCC-786-O cell lines |
| Concentration: | 100 μM |
| Incubation Time: | 24 hours (K1 cell) and 48 hours (ccRCC-786-O cell) |
| Result: | Caused a comparable drop of the activity in both cell lines. |
Apoptosis Analysis
| Cell Line: | ccRCC-786-O cells |
| Concentration: | 100 μM |
| Incubation Time: | 48 hours |
| Result: | Produced a drastic increase in apoptotic/dead cell population after 48 h. |
Western Blot Analysis
| Cell Line: | ccRCC-786-O cells |
| Concentration: | 100 μM |
| Incubation Time: | 12, 24, 48 hours |
| Result: | Showed a reduced acetylation of both global AcH3 histone and H3AcK18. |