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Histone Methyltransferase inhibitor
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BIX-01294 trihydrochloride
僅限科研使用
BIX-01294 trihydrochloride
BIX-01294 trihydrochloride 是一種G9a histone methyltransferase抑制劑，無細(xì)胞試驗中IC50為2.7 μM，降低大部分組蛋白H3K9me2，也微弱抑制GLP（主要是H3K9me3），對其他組蛋白甲基轉(zhuǎn)移酶沒有顯著的抑制活性。BIX01294 可誘導(dǎo)自噬。BIX01294 還可通過癌蛋白 NSD1、NSD2 和 NSD3 來抑制H3K36甲基化。
BIX-01294 trihydrochloride Chemical Structure
CAS: 1392399-03-9
產(chǎn)品質(zhì)控
批次：
純度：
99.08%
99.08
BIX-01294 trihydrochloride相關(guān)產(chǎn)品
相關(guān)信號通路圖
細(xì)胞實驗數(shù)據(jù)示例
| 細(xì)胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| K562 | Function assay | 0.5 to 2 uM | 72 hrs | Inhibition of histone methyltransferase G9a in human K562 cells assessed as reduction in histone H3K9me2 levels at 0.5 to 2 uM after 72 hrs by Western blot analysis | 27393948 |
| HeLa | Function assay | 4.5 hrs | Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay, IC50 = 0.966 μM. | 29624387 | |
| BL21 (DE3)-Gold | Function assay | 20 mins | Inhibition of N-terminal hexahistidine-tagged human G9a (913 to 1193 residues) expressed in Escherichia coli BL21 (DE3)-Gold cells using histone H3 (1 to 15 residues) as substrate preincubated for 20 mins followed by substrate addition by mass spectrometr, IC50 = 1.9 μM. | 27720557 | |
| HL60 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay, IC50 = 2.2 μM. | 27393948 | |
| A549 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay, IC50 = 2.8 μM. | 27393948 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay, IC50 = 3.7 μM. | 27393948 | |
| K562 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay, IC50 = 3.9 μM. | 27393948 | |
| MDA-MB-231 | Function assay | 2 days | Inhibition of G9a in human MDA-MB-231 cells assessed as reduction in H3K9me2 level after 2 days by immunofluorescence in-cell western analysis, IC50 = 4.563 μM. | 29541353 | |
| HeLa cells | Function assay | Inhibition of ERK5 phosphorylation in sorbitol-stimulated human HeLa cells, IC50=0.059 μM | 23656407 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| wild type fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | BIX-01294 trihydrochloride 是一種G9a histone methyltransferase抑制劑，無細(xì)胞試驗中IC50為2.7 μM，降低大部分組蛋白H3K9me2，也微弱抑制GLP（主要是H3K9me3），對其他組蛋白甲基轉(zhuǎn)移酶沒有顯著的抑制活性。BIX01294 可誘導(dǎo)自噬。BIX01294 還可通過癌蛋白 NSD1、NSD2 和 NSD3 來抑制H3K36甲基化。 | ||
|---|---|---|---|
| 靶點(diǎn) |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | BIX01294是選擇性的G9a組蛋白甲基轉(zhuǎn)移酶抑制劑，在實驗濃度范圍內(nèi)不影響SUV39H1(H320R)和PRMT1。BIX-01294特異性抑制G9a (H3K9me2)，并在較小程度上抑制密切相關(guān)的GLP酶（主要是H3K9me3），作用于G9a 和GLP，IC50分別為1.7 μM 和 38 μM。BIX-01294抑制G9a，與SAM按非競爭性的方式。BIX-01294 (4.1μM) 作用于野生型ES細(xì)胞，小鼠胚胎成纖維細(xì)胞和HeLa細(xì)胞，而非缺乏G9a的干細(xì)胞，降低H3K9me2水平。BIX-01294是抑制有價值的染色體H3K9me2瞬態(tài)調(diào)制的抑制劑。BIX-01294在一些G9a靶向基因上，包括Bim1 和Serac1，降低H3K9me2。[1] BIX01294可使HIV-1病毒從潛伏感染的細(xì)胞，如ACH-2和 OM10.1中重新表達(dá)。[2] |
|||
|---|---|---|---|---|
| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
| Western blot | Cyclin D1 / CDK2 / CDK4 / CDK 6 / Cyclin E G9a / H3K9me2 Atg7 / Atg5 / Atg5-Atg12 / Atg3 / Atg12 / LC3B |
|
25198515 | |
| Immunofluorescence | Ran / H3K9me3 |
|
30565836 | |
| Growth inhibition assay | Cell viability |
|
26013382 | |
|
化學(xué)信息&溶解度
| 分子量 | 600.02 | 分子式 | C28H38N6O2.3HCl |
| CAS號 | 1392399-03-9 | SDF | Download BIX-01294 trihydrochloride SDF |
| Smiles | CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)CC5=CC=CC=C5)OC)OC.Cl.Cl.Cl | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 100 mg/mL ( (166.66 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : 100 mg/mL (166.66 mM) Ethanol : 100 mg/mL (166.66 mM) |
摩爾濃度計算器 |
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體內(nèi)溶解配方 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)配方計算器 | |||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，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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