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CPTH2
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CPTH2图片
CAS NO:357649-93-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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]

GCN5

 

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.
分子量

291.80

性状

Solid

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 : 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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.4270 mL17.1350 mL34.2701 mL
5 mM0.6854 mL3.4270 mL6.8540 mL
10 mM0.3427 mL1.7135 mL3.4270 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℃, 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。

    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本网站选购。