CPTH2 - CAS:357649-93-5

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CPTH2

目录号 : KM15899 CAS No. : 357649-93-5 纯度 : ≥95%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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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).

体外研究

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.

分子式

C₁₄H₁₄N₃Scl

分子量

291.80

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)

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

H₂O : < 0.1 mg/mL (insoluble)

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。