CPTH2 是有效的组蛋白乙酰基转移酶 (HAT) 抑制剂。CPTH2 选择性地抑制Gcn5对组蛋白 H3 的乙酰化。CPTH2 通过抑制乙酰转移酶p300 (KAT3B)诱导凋亡 (apoptosis) 并降低透明细胞肾癌 (ccRCC) 细胞系的侵袭性。
| 生物活性 | CPTH2 is a potenthistone acetyltransferase(HAT)inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 byGcn5. CPTH2 inducesapoptosisand decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition ofacetyltransferase p300 (KAT3B)[1][2]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | 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[1].
CPTH2 (100 μM; 12 or 48 hours) causes a comparable drop of the activity in both cell lines[1].
CPTH2 (100 μM; 48 hours) produces a drastic increase in apoptotic/dead cell population after 48 h[1].
CPTH2 (100 μM; 12, 24, 48 hours) shows a reduced acetylation of both global AcH3 histone and H3AcK18[1].
CPTH2 (100 μM; 24, 48 hours) is capable to counteract invasion and migration of ccRCC-786-O cells in culture[1].
CPTH2 (0.2, 0.5, 1 mM) inhibits the growth of a GCN5 deleted strain and a single catalytic mutant E173H[2].
CPTH2 (0.6, 0.8 mM; for 24 hours) inhibits histone H3 acetylation in yeast cell cultures[2].
CPTH2 inhibits the Gcn5p dependent functional network[2].
Cell Proliferation Assay[1] | 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[1] | 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[1] | 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[1] | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 16.67 mg/mL(57.13 mM;ultrasonic and warming and heat to 60℃) Ethanol : 1 mg/mL(3.43 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic)(insoluble) 配制储备液 | 1 mM | 3.4270 mL | 17.1350 mL | 34.2701 mL | | 5 mM | 0.6854 mL | 3.4270 mL | 6.8540 mL | | 10 mM | 0.3427 mL | 1.7135 mL | 3.4270 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.67 mg/mL (5.72 mM); Suspended solution
此方案可获得 ≥ 1.67 mg/mL (5.72 mM，饱和度未知) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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