CPTH2

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CPTH2  纯度: 99.79%

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。

CPTH2

CPTH2 Chemical Structure

CAS No. : 357649-93-5

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10 mM * 1 mL in DMSO ￥1540 In-stock
10 mg ￥1400 In-stock
50 mg ￥3500 In-stock
100 mg ￥5500 In-stock
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CPTH2 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Targeted Diversity Library

生物活性

CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B)[1][2].

IC50 & Target[1]

GCN5

 

p300

 

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

291.80

Formula

C14H14ClN3S
CAS 号

357649-93-5
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 : 25 mg/mL (85.68 mM; Need ultrasonic)

H2O : 1 mg/mL (3.43 mM; Need ultrasonic)

Ethanol : 1 mg/mL (3.43 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 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: ≥ 2.5 mg/mL (8.57 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.57 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Cocco E, et al. KAT3B-p300 and H3AcK18/H3AcK14 levels are prognostic markers for kidney ccRCC tumoraggressiveness and target of KAT inhibitor CPTH2. Clin Epigenetics. 2018 Apr 4;10:44.

    [2]. Chimenti F, et al. 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.

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