BIX 01294

For research use only. Not for use in humans.

目录号:S8006

BIX 01294 Chemical Structure

CAS No. 1392399-03-9

BIX01294 是一种G9a histone methyltransferase抑制剂,无细胞试验中IC50为2.7 μM,降低大部分组蛋白H3K9me2,也微弱抑制GLP(主要是H3K9me3),对其他组蛋白甲基转移酶没有显著的抑制活性。BIX01294 可诱导自噬。BIX01294 还可通过癌蛋白 NSD1NSD2NSD3 来抑制H3K36甲基化。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1566.17 现货
RMB 1222.94 现货
RMB 3415.23 现货
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客户使用Selleck生产的BIX 01294发表文献26篇:

产品安全说明书

Histone Methyltransferase抑制剂选择性比较

生物活性

产品描述 BIX01294 是一种G9a histone methyltransferase抑制剂,无细胞试验中IC50为2.7 μM,降低大部分组蛋白H3K9me2,也微弱抑制GLP(主要是H3K9me3),对其他组蛋白甲基转移酶没有显著的抑制活性。BIX01294 可诱导自噬。BIX01294 还可通过癌蛋白 NSD1NSD2NSD3 来抑制H3K36甲基化。
靶点
G9a [1]
(Cell-free assay)
2.7 μM
体外研究

BIX01294是选择性的G9a组蛋白甲基转移酶抑制剂,在实验浓度范围内不影响SUV39H1(H320R)和PRMT1。BIX-01294特异性抑制G9a (H3K9me2),并在较小程度上抑制密切相关的GLP酶(主要是H3K9me3),作用于G9a 和GLP,IC50分别为1.7 μM 和 38 μM。BIX-01294抑制G9a,与SAM按非竞争性的方式。BIX-01294 (4.1μM) 作用于野生型ES细胞,小鼠胚胎成纤维细胞和HeLa细胞,而非缺乏G9a的干细胞,降低H3K9me2水平。BIX-01294是抑制有价值的染色体H3K9me2瞬态调制的抑制剂。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病毒从潜伏感染的细胞,如ACH-2和 OM10.1中重新表达。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells MlW3SpVv[3Srb36gZZN{[Xl? NYqxe5RCUW6qaXLpeIlwdiCxZjDFVms2KHCqb4PwbI9zgWyjdHnvckBqdiC|b4LibZRwdC2|dHnteYxifGWmIHj1cYFvKEinTHGgZ4VtdHNuIFnDOVA:OC5yNUmg{txO NVTBPI1jRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2OVY1ODdpPkKzOlU3PDB5PD;hQi=>
HeLa M4LLUWZ2dmO2aX;uJIF{e2G7 M3T3R|QvPSCqcoO= NV2zU3I5UW6qaXLpeIlwdiCxZjDFZo9t[X[rcoXzJIdtgWOxcILveIVqdi:vYYTybZgheHKxdHXpckBXWDRyIHXueJJ6KGmwIHj1cYFvKEinTHGgZ4VtdHNiYX\0[ZIhPC53IHjyd{Bj\XSjLXzhZ5RidWG|ZTDy[ZBwenSncjDhd5NigSxiSVO1NEA:KDBwOU[2JO69VS5? M3TxelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NkK0N|g4Lz5{OU[yOFM5PzxxYU6=
BL21 (DE3)-Gold MoXNSpVv[3Srb36gZZN{[Xl? MXKyNEBucW6| MVvJcohq[mm2aX;uJI9nKE5vdHXycYlv[WxiaHX4ZYhqe3SrZHnu[U11[WepZXSgbJVu[W5iR{nhJEg6OTNidH:gNVE6OyC{ZYPp[JVmeyliZYjwdoV{e2WmIHnuJGV{[2incnnjbIliKGOxbHmgRmwzOSBqRFWzLU1Id2ymIHPlcIx{KHW|aX7nJIhqe3SxbnWgTFMhMDFidH:gNVUhemW|aXT1[ZMqKGG|IIP1ZpN1emG2ZTDwdoVqdmO3YnH0[YQh\m:{IEKwJI1qdnNiZn;scI94\WRiYomgd5Vje3S{YYTlJIFl\Gm2aX;uJIJ6KG2jc4Ogd5Bm[3S{b33leJItKEmFNUCgQUAyNjlizszNMi=> MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzd{MEW1O{c,Ojd5MkC1OVc9N2F-
HL60 Ml20RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NYX1fmp5PDhiaILz MnuzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFQ1u4JIF{e2G7LDDJR|UxKD1iMj6yJO69VS5? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzN7M{m0PEc,Ojd|OUO5OFg9N2F-
A549 MYPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MWK0PEBpenN? M{nNT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB2ODDodpMh[nliQ1PLPEBie3OjeTygTWM2OCB;IEKuPEDPxE1w MljtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd|OUO5OFgoRjJ5M{mzPVQ5RC:jPh?=
HepG2 MVLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MUO0PEBpenN? NI\Yd3NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyIE2gN{44KM7:TT6= NV3BfXZJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkezPVM6PDhpPkK3N|k{QTR6PD;hQi=>
K562 MmjiRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NH;ySmk1QCCqcoO= MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEt3NkKgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOFS{igZZN{[XluIFnDOVAhRSB|Lkmg{txONg>? NFWxXHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{O5N|k1QCd-MkezPVM6PDh:L3G+
MDA-MB-231 MXLGeY5kfGmxbjDhd5NigQ>? MkTJNkBl[Xm| MV3Jcohq[mm2aX;uJI9nKEd7YTDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCKM1u5cYUzKGyndnXsJIFnfGW{IEKg[IF6eyCkeTDpcY12dm:obIXvdoV{[2WwY3WgbY4u[2WubDD3[ZN1\XKwIHHuZYx6e2m|LDDJR|UxKD1iND61OlMh|ryPLh?= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTV2MUO1N{c,Ojl3NEGzOVM9N2F-
K562 NHrkOmRHfW6ldHnvckBie3OjeR?= MViwMlUhfG9iMjD1US=> NGPoNWM4OiCqcoO= NUHCWphJUW6qaXLpeIlwdiCxZjDobZN1d26nIH3leIh6dHS{YX7z[oVz[XOnIFe5ZUBqdiCqdX3hckBMPTZ{IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBpcXO2b37lJGg{UzmvZUKgcIV3\Wy|IHH0JFAvPSC2bzCyJJVOKGGodHXyJFczKGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzN7M{m0PEc,Ojd|OUO5OFg9N2F-
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A673 MUjxTHRUKGG|c3H5 Mny3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? M170bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC NF76PVByUFSVIHHzd4F6 M1u1c5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz M1XB[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 NF3YZ|RyUFSVIHHzd4F6 NHXKW5dyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= NHL0OFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 M1HGVJFJXFNiYYPzZZk> MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= M1\zVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 MY\xTHRUKGG|c3H5 M4f4VpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH Ml7OdWhVWyCjc4PhfS=> MnTTdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= NGS1Wmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 NWK1OpNneUiWUzDhd5NigQ>? NF:3eFlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz NG\5fnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 M3zBfZFJXFNiYYPzZZk> MkfEdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| NEDQfJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 MYPxTHRUKGG|c3H5 NVnt[ZNveUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz NHrHT5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh18 NGj1PWdyUFSVIHHzd4F6 M3nEe5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy| MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 Mk[zdWhVWyCjc4PhfS=> NX3RWWhleUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> NVfmNohvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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MG 63 (6-TG R) NWXEWG1oeUiWUzDhd5NigQ>? MoX3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| MlqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
wild type fibroblast cells NETBOJdyUFSVIHHzd4F6 MYjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5Ih[2:wdILvcEBJcCC5aXzkJJR6eGViZnnido9jdGG|dDDj[Yxtew>? M1;TXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cyclin D1 / CDK2 / CDK4 / CDK 6 / Cyclin E ; 

PubMed: 25198515     


Western blot analysis of cyclins and CDKs associated with G1 phase in neuroblastoma cells treated with BIX01294 or water for 2 days. α-Tubulin levels are shown as the loading control.

G9a / H3K9me2 ; 

PubMed: 25198515     


Western blot analysis of G9a function in neuroblastoma cells treated with BIX01294 or water for 2 days. 

Atg7 / Atg5 / Atg5-Atg12 / Atg3 / Atg12 / LC3B ; 

PubMed: 25198515     


Western blot analysis of autophagy-related genes in neuroblastoma cells treated with BIX01294 or water for 2 days. α-Tubulin levels are shown as the loading control.

25198515
Immunofluorescence
Ran / H3K9me3 ; 

PubMed: 30565836     


Effects of histone methyltransferase G9a inhibitors on the Ran gradient and H3K9me3 levels in human fibroblasts. Chemical inhibitors (Bix01294, UNC0638, A‐366) were applied to human fibroblasts and endogenous Ran and Histone H3K9me3 levels examined by IF microscopy. Scale bar 20 μm.

30565836
Growth inhibition assay
Cell viability; 

PubMed: 26013382     


HepG2 cells were treated with different concentrations of BIX01294. After 24 h, cell viability was measured by the MTT assay.

26013382

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 98 mg/mL (163.32 mM)
Water 98 mg/mL (163.32 mM)
Ethanol '8 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 600.02
化学式

C28H38N6O2.3HCl

CAS号 1392399-03-9
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID