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Epigenetics
Histone Acetyltransferase inhibitor
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Autophagy activator
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Apoptosis related activator
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Epigenetic Reader Domain inhibitor
C646
僅限科研使用
C646
C646 是一種histone acetyltransferase抑制劑，抑制p300，無細(xì)胞試驗(yàn)中Ki為400 nM，相比于其它乙酰轉(zhuǎn)移酶，優(yōu)先作用于p300。C646 可誘導(dǎo)細(xì)胞周期阻滯、細(xì)胞凋亡與自噬。
C646 Chemical Structure
CAS: 328968-36-1
產(chǎn)品質(zhì)控
批次：
純度：
99.77%
99.77
C646相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | HAT MYST GNAT p300/CBP | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Curcumin Anacardic Acid MG149 A-485 WM-1119 YF-2 CPTH2 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 FDA藥物庫 天然產(chǎn)物庫 已知活性藥物庫-I 生物活性庫Ⅱ | 點(diǎn)擊展開 |
相關(guān)信號通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻(xiàn)信息 |
|---|---|---|---|---|---|
| Kasumi-1 | Growth inhibition assay | 10, 25 and 50 μM | 0, 24, 48, 72 h | cellular growth and colony formation were dramatically suppressed upon C646 treatment. | 23390536 |
| SKNO-1 | Growth inhibition assay | 10, 25 and 50 μM | 0, 24, 48, 72 h | cellular growth and colony formation were dramatically suppressed upon C646 treatment. | 23390536 |
| WM983B | Function assay | 10 μM and 20 μM | 24 h | a dose-dependent decrease in the protein levels of cyclins A and E, accompanied by an increased expression of p53 and its downstream effector p21 | 23698071 |
| WM35 | Function assay | 10 μM and 20 μM | 24 h | a dose-dependent decrease in the protein levels of cyclins A and E, accompanied by an increased expression of p53 and its downstream effector p21 | 23698071 |
| 1205Lu | Function assay | 10 μM and 20 μM | 24 h | a dose-dependent decrease in the protein levels of cyclins A and E, accompanied by an increased expression of p53 and its downstream effector p21 | 23698071 |
| Raw246.7 | Function assay | 1, 5, 10, 15, 20, 25, or 30 μM | 16 h | results in significant inhibition of LPS and IFNγ induced NF-κB promoter activity at 15 μM or higher concentrations | 26718586 |
| KATO III | Function assay | 10 μM | 6 h | C646 treatment significantly reduced the levels of histone H3 acetylation in both GC cells and normal gastric epithelial cells (P<0.05) | 29075795 |
| BGC-823 | Function assay | 10 μM | 6 h | C646 treatment significantly reduced the levels of histone H3 acetylation in both GC cells and normal gastric epithelial cells (P<0.05) | 29075795 |
| MGC-803 | Function assay | 10 μM | 6 h | C646 treatment significantly reduced the levels of histone H3 acetylation in both GC cells and normal gastric epithelial cells (P<0.05) | 29075795 |
| SGC-7901 | Function assay | 10 μM | 6 h | C646 treatment significantly reduced the levels of histone H3 acetylation in both GC cells and normal gastric epithelial cells (P<0.05) | 29075795 |
| MKN45 | Function assay | 10 μM | 6 h | C646 treatment significantly reduced the levels of histone H3 acetylation in both GC cells and normal gastric epithelial cells (P<0.05) | 29075795 |
| GES-1 | Function assay | 10 μM | 6 h | C646 treatment significantly reduced the levels of histone H3 acetylation in both GC cells and normal gastric epithelial cells (P<0.05) | 29075795 |
| SH-SY5Y | Function assay | 20?μM | 24 h | Co-treatment with 20 μM C646 suppressed the effect of TSA treatment on Alox15 mRNA expression by 65.7% | 29235036 |
| NE-4C cells | Function assay | 0-5 μM | high glucose induced increases of H4K5ac and H4K5/8/12/16ac levels in NE-4C cells are inhibited by addition of a selective CBP/p300 inhibitor C646 in a dose-dependent way (from 0 to 5 μM) | 30114346 | |
| BL21-CodonPlus(DE3)-RIL | Function assay | 10 mins | Inhibition of FLAG-tagged p300 (1195 to 1673 residues) (unknown origin) expressed in competent Escherichia coli BL21-CodonPlus(DE3)-RIL cells using histone H4 substrate incubated for 10 mins by scintillation counting method in presence of [14C]acetyl-CoA, IC50 = 9 μM. | 26701186 | |
| BL21(RIL)-DE3 | Function assay | 10 mins | Inhibition of synthetic VMA-tagged p300 (1287 to 1652 residues) (unknown origin) expressed in Escherichia coli BL21(RIL)-DE3 cells using H4-15 peptide substrate incubated for 10 mins by radiometric filter binding assay in presence of [14C]acetyl-CoA, IC50 = 1.6 μM. | 26701186 | |
| BL21(RIL)-DE3 | Function assay | 10 mins | Inhibition of synthetic VMA-tagged p300 (1287 to 1652 residues) (unknown origin) expressed in Escherichia coli BL21(RIL)-DE3 cells using H4-15 peptide substrate incubated for 10 mins by radiometric filter binding assay in presence of [14C]acetyl-CoA, Ki = 0.4 μM. | 26701186 | |
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | C646 是一種histone acetyltransferase抑制劑，抑制p300，無細(xì)胞試驗(yàn)中Ki為400 nM，相比于其它乙酰轉(zhuǎn)移酶，優(yōu)先作用于p300。C646 可誘導(dǎo)細(xì)胞周期阻滯、細(xì)胞凋亡與自噬。 | ||
|---|---|---|---|
| 靶點(diǎn) |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | C646是一種組蛋白乙酰轉(zhuǎn)移酶抑制劑，抑制p300，Ki為400 nM，選擇性作用于其他乙酰轉(zhuǎn)移酶。10 μM C646在體外抑制86% p300。C646是傳統(tǒng)的，可逆p300抑制劑。C646(25μM)作用于細(xì)胞，降低組蛋白 H3 和 H4 乙酰化水平，且廢除TSA誘導(dǎo)的乙?；?。[1]C646(20μM)作用于對雄激素敏感的閹割性前列腺癌細(xì)胞系，通過干擾AR和NF-kB通路，而誘導(dǎo)細(xì)胞凋亡。[2]C646作用于小鼠細(xì)胞，抑制全部H3K4me3動態(tài)乙?；揖植繖M跨啟動子和誘導(dǎo)基因的起始位點(diǎn)，從而干擾RNA聚合酶II相互作用和這些基因的激活。[3] | |||
|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | 放射性檢測 | |||
| 使用直接放射性測定法測定對假定的p300 HAT抑制劑的IC50值。反應(yīng)在20 mM HEPES (pH 7.9)中進(jìn)行，包含5 mM DTT, 80μM EDTA, 40μg/ml BSA, 100μM H4-15, 和 5 nM p300。加入在一個濃度范圍內(nèi)的假定抑制劑，DMSO 濃度保持不變(<5%)。反應(yīng)在30°C 下溫育10分鐘, 然后加入1:1 12C-acetyl-CoA 和 14C-acetyl-CoA 的混合物到 20 mM，開始反應(yīng)。在30°C下進(jìn)行10分鐘后，使用14% SDS (w/v) 淬火。所有濃度按一式兩份篩選。跑膠，洗滌，干燥，暴露于PhosphorImager板上，對產(chǎn)生的Ac-H4-15進(jìn)行量化，得到IC50值。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | C3H10T1/2 | ||
| 濃度 | ~25 μM | |||
| 孵育時間 | 1 到3小時 | |||
| 方法 | 在小鼠細(xì)胞中測定組蛋白乙?；?。C3H10T1/2小鼠成纖維細(xì)胞在含10% FCS的DMEM 培養(yǎng)基中 在37°C下含6% CO2的環(huán)境中生長。鋪滿培養(yǎng)物在含0.5% FCS 的DMEM 培養(yǎng)基中靜置18-20小時，然后再處理。使用如下化合物處理細(xì)胞：TSA (10 ng/ml [33 nM]), C646 (25 μM), C37 (25 μM)。使用如下濃度的抗體: 總H3 (1:10000); H4K12ac (1:2500)。兔anti-H3K9ac(1:10000)抗體內(nèi)部產(chǎn)生。通過酸提取從細(xì)胞中分離組蛋白，經(jīng)SDS和酸-尿素聚丙烯酰胺凝膠電泳分離，并通過免疫印跡分析。 | |||
| 實(shí)驗(yàn)圖片 | 檢測方法 | 檢測指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | α-c-Myc Cyclin A1/2 / Cyclin E2 / p53 / p21 H3K27Ac |
|
28630312 | |
| Immunofluorescence | BRD4 / p300 |
|
28630312 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 弱滅絕訓(xùn)練后，C646立即注入到ILPFC，增強(qiáng)恐懼消退記憶的整合。[4]C646處理脊髓，衰減機(jī)械痛和熱痛覺過敏，伴隨著抑制COX-2表達(dá)。[5] | |
|---|---|---|
| 動物實(shí)驗(yàn) | Animal Models | 小鼠 |
| Dosages | 每種情況下2×0.75 μl 注射體積, 1.5 μg, 處理 超過2分鐘 | |
| Administration | 注入 ILPFC | |
化學(xué)信息&溶解度
| 分子量 | 445.42 | 分子式 | C24H19N3O6 |
| CAS號 | 328968-36-1 | SDF | Download C646 SDF |
| Smiles | CC1=CC(=C(C=C1C)[N+](=O)[O-])C2=CC=C(O2)C=C3C(=NN(C3=O)C4=CC=C(C=C4)C(=O)O)C | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 11 mg/mL ( (24.69 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
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體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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常見問題及建議解決方法
問題 1:
I am planning to conduct IP studies in mice, any specific vehicle that you can recommend to me?
回答：
We found it can be dissolved in 5% DMSO+30% PEG 300+ddH2O at 1 mg/ml as a clear solution. It should be ok for i.p. injection.
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