BIX-01294 trihydrochloride

目錄號(hào)：S8006 Purity: 99.08%

BIX-01294 trihydrochloride 是一種G9a histone methyltransferase抑制劑，無(wú)細(xì)胞試驗(yàn)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(duì)其他組蛋白甲基轉(zhuǎn)移酶沒(méi)有顯著的抑制活性。BIX01294 可誘導(dǎo)自噬。BIX01294 還可通過(guò)癌蛋白 NSD1、NSD2 和 NSD3 來(lái)抑制H3K36甲基化。

BIX-01294 trihydrochloride Chemical Structure

CAS: 1392399-03-9

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1566.17	現(xiàn)貨
10mg	1222.94	現(xiàn)貨
50mg	3415.23	現(xiàn)貨
1g	17772.3	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 info@selleck.cn

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)靶點(diǎn)	Menin-MLL interaction WDR5-MLL interaction	點(diǎn)擊展開(kāi)
相關(guān)產(chǎn)品	GSK126 DZNeP (3-deazaneplanocin A) HCl GSK343 Pinometostat (EPZ5676) EPZ004777 EPZ015666 (GSK3235025) UNC1999 Chaetocin EPZ005687 Pemrametostat (GSK3326595) SGC 0946 MM-102 UNC0638 EPZ011989 UNC0642 OICR-9429 UNC0379 GSK591 Lirametostat (CPI-1205) MI-2 (Menin-MLL Inhibitor) CPI-169 MI-503 MS023 A-196 GSK503 AMI-1 PFI-2 HCl SGC707 A-366 MI-3 (Menin-MLL Inhibitor) BRD4770 LLY-507 Onametostat (JNJ-64619178) WDR5-0103 EI1 UNC3866 EPZ020411 2HCl MI-463 HLCL-61 HCL MAK683 MI-136 MS049 SAH (S-Adenosyl-L-homocysteine) PF-06726304 CPI-360 JQ-EZ-05 (JQEZ5) SGC2085 UNC0631	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 已知活性藥物庫(kù)-I 高選擇性抑制劑庫(kù)	點(diǎn)擊展開(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類(lèi)型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
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

靶點(diǎn)

G9a ^[1]
(Cell-free assay)

2.7 μM

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(shí)驗(yàn)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(jìng)爭(zhēng)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(jià)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(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)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

參考文獻(xiàn)
[1] Kubicek S, et al. Mol Cell, 2007, 25(3), 473-481. [2] Imai K, et al. J Biol Chem, 2010, 285(22), 16538-16545. [3] Mabe NW, et al. Cell Rep. 2020 Nov 3;33(5):108341.

參考文獻(xiàn)

[1] Kubicek S, et al. Mol Cell, 2007, 25(3), 473-481.
[2] Imai K, et al. J Biol Chem, 2010, 285(22), 16538-16545.
[3] Mabe NW, et al. Cell Rep. 2020 Nov 3;33(5):108341.

化學(xué)信息&溶解度

分子量	600.02	分子式	C₂₈H₃₈N₆O₂.3HCl
CAS號(hào)	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(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 100 mg/mL ( (166.66 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : 100 mg/mL (166.66 mM)

Ethanol : 100 mg/mL (166.66 mM)

DMSO : 100 mg/mL ( (166.66 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : 100 mg/mL (166.66 mM)

Ethanol : 25 mg/mL (41.66 mM)

摩爾濃度計(jì)算器

體內(nèi)溶解配方批次：現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑				動(dòng)物體內(nèi)配方計(jì)算器
澄清溶液	saline	100.000mg/ml (166.66mM)	以 1 mL 工作液為例，取 100 mg該產(chǎn)品加到1ml生理鹽水（0.9% NaCL溶液）中，混合均勻使其澄清，請(qǐng)現(xiàn)配現(xiàn)用！
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	saline	100.000mg/ml (166.66mM)	以 1 mL 工作液為例，取 100 mg該產(chǎn)品加到1ml生理鹽水（0.9% NaCL溶液）中，混合均勻使其澄清，請(qǐng)現(xiàn)配現(xiàn)用！
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)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(qǐng)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(guò)該批次藥物DMSO溶解度，請(qǐng)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。

技術(shù)支持

在訂購(gòu)、運(yùn)輸、儲(chǔ)存和使用我們的產(chǎn)品的任何階段，您遇到的任何問(wèn)題，均可以通過(guò)撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱tech@selleck.cn，直接聯(lián)系到我們。我們會(huì)在24小時(shí)內(nèi)盡快聯(lián)系您。

操作手冊(cè)

如果有其他問(wèn)題，請(qǐng)給我們留言。

* 必填項(xiàng)

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

天堂网亚洲,天天操天天搞,91视频高清,菠萝蜜视频在线观看入口,美女视频性感美女视频,95丝袜美女视频国产,超高清美女视频图片