I-BET151 (GSK1210151A)

For research use only. Not for use in humans.

目录号：S2780

I-BET151 (GSK1210151A) Chemical Structure

CAS No. 1300031-49-5

I-BET151 (GSK1210151A)是一种新型，选择性的BET抑制剂，作用于BRD2，无细胞试验中BRD3和BRD4，IC50分别为0.5 μM， 0.25 μM和0.79 μM。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2121.21 现货
RMB 1382.25 现货
RMB 2231.18 现货
RMB 7130.63 现货
RMB 10401.3 现货
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客户使用Selleck生产的I-BET151 (GSK1210151A)发表文献33篇：

产品安全说明书

Epigenetic Reader Domain抑制剂选择性比较

生物活性

产品描述 I-BET151 (GSK1210151A)是一种新型，选择性的BET抑制剂，作用于BRD2，无细胞试验中BRD3和BRD4，IC50分别为0.5 μM， 0.25 μM和0.79 μM。
特性 优化I-BET151，使其有效及选择性靶向作用于BET，同时增强体内药代动力学和终末半衰期，以使延长体内研究。
靶点
BRD3 [1]
(Cell-free assay)		 BRD2 [1]
(Cell-free assay)		 BRD4 [1]
(Cell-free assay)
0.25 μM 0.5 μM 0.79 μM
体外研究

I-BET151有效，选择性作用于多种不同蛋白类型，如COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, 离子通道，转运体。与I-BET762 (GSK525762A)类似, I-BET151 对BRD2, BRD3 和BRD4具有高的结合亲和力，Kd为0.02-0.1 μM,作用于人类外周血单核细胞（PBMC）和全血（WB）以及大鼠WB，显著抑制脂多糖刺激的IL-6细胞因子产生，IC50分别为0.16 μM, 1.26 μM, 和 1.26 μM。I-BET151(0.5 or 5 μM)作用于HL60核提取物，抑制BETs(BRD2, BRD3, BRD4, 和 BRD9)而非23种其他溴区蛋白结合到乙酰化的组蛋白肽。I-BET151有效作用于含不同 MLL融合的细胞系，如MV4;11, RS4;11, MOLM13, 和NOMO1 细胞， IC50为15-192 nM。一致的是，I-BET151完全消除MLL融合驱动的白血病（MOLM13）而非酪氨酸激酶激活（K562）驱动的白血病的菌落形成潜力。I-BET151也有效作用于液体培养和转化MLL-ENL或MLL-AF9的原代小鼠祖细胞的克隆形成实验。I-BET151作用于由不同的MLL融合（分别含MLL-AF9和MLL-AF4的MOLM13和MV4;11）而非K562细胞驱动的MLL融合细胞系，显著诱导细胞凋亡和G0/G1期停滞，可能是由于通过抑制BRD3/4，PAFc和SEC组分招募到转录起始位点（TSS），而抑制BCL-2，C-MYC和CDK6的转录。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV4;11 MX\jfZRwfG:6aXPpeJkh[XO|YYm= NFPkeGR,OTByIN88US=> NYD0RWFYTE2VTx?= NHjVXndKSzVyPUK2JI5O M2rrSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
RS4;11 NVPwXVhU[3m2b4TvfIlkcXS7IHHzd4F6 MUT+NVAxKM7:TR?= NU\DXYJFTE2VTx?= M3zmUWlEPTB;MUmyJI5O NF;idnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
MOLM13 MkXUZ5l1d3SxeHnjbZR6KGG|c3H5 NUL3UWdXhjFyMDFOwG0> M3zmVmROW09? MlzNTWM2OD1zMkCgcm0> NV7EelVPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
NOMO1 MnfOZ5l1d3SxeHnjbZR6KGG|c3H5 MoPYglExOCEQvF2= NYfYdoJjTE2VTx?= NFG1WolKSzVyPUG1JI5O MkfWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
HEL NUPnRmpi[3m2b4TvfIlkcXS7IHHzd4F6 M4PGdZ4yODBizszN NWTNRZdJTE2VTx?= NIPJSGxKSzVyPUGg{txO NHPt[lU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
K562 NWixVpNk[3m2b4TvfIlkcXS7IHHzd4F6 NHHneHV,OTByIN88US=> NHrPVmRFVVOR M3vWfmlEPTB-MUCwJO69VQ>? MoTaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
MEG01 NFjidXRkgXSxdH;4bYNqfHliYYPzZZk> NGnQO|l,OTByIN88US=> MnHTSG1UVw>? NWPHbow4UUN3ME2yOUDPxE1? NGTuXpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
HL60 Mni4Z5l1d3SxeHnjbZR6KGG|c3H5 MW\+NVAxKM7:TR?= M3jkUWROW09? M3rOcGlEPTB;OEmwJI5O MofuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
MV4;11 MW\BdI9xfG:|aYOgZZN{[Xl? MljyglExOCEQvF2= Mmf1SG1UVw>? NEPqSHpqdmS3Y3XzJIFxd3C2b4Ppdy=> M{[xflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
MOLM13 NWq0SlQ3SXCxcITvd4l{KGG|c3H5 M2q2OZ4yODBizszN M1T6VmROW09? NEn2cIlqdmS3Y3XzJIFxd3C2b4Ppdy=> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl4NEO0NEc,OjF7NkSzOFA9N2F-
MV4;11 Ml74SpVv[3Srb36gZZN{[Xl? MWrEUXNQ NGi4dmJl\WO{ZXHz[ZMhfGinIILlZ5J2cXSvZX70JI9nKEKUREOvOEBidmRiaX3wZYlz\WRicnXjdpVqfG2nboSgc4YhS0SNOTDhcoQhWEGIMTD0c{B1cGVidILhcpNkemmydHnvcoFtKHO2YYL0JJNqfGV? NVLDSnZGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
PBMC NGnnPHBHfW6ldHnvckBie3OjeR?= MW\EUXNQ M1Lkb4lvcGmkaYTzJGlNNTZid3n0bEBxUUN3MDDv[kA3Njd? NXnmPXZiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK0N|cyOTVpPkKyOFM4OTF3PD;hQi=>
A2 NUT3fWx7TnWwY4Tpc44h[XO|YYm= NF\3ZmJ,OTBizszN M1\5XWROW09? NI\6WZJz\WGldHn2ZZRmeyCuYYTlcpQhUEmYLUG= M1;xfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkW1NlE5Lz5{M{K1OVIyQDxxYU6=
A72 NEWwd|VHfW6ldHnvckBie3OjeR?= MkT1glExKM7:TR?= MlnjSG1UVw>? M2\JTJJm[WO2aY\heIV{KGyjdHXueEBJUVZvMR?= Mmf1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{NUWyNVgoRjJ|MkW1NlE5RC:jPh?=
BC1 NFq0d45Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWL3PYpihjFizszN MlT0SG1UVw>? MWDJR|UxRTJ{MDDuUS=> NHfa[W09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
BC3 MU\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVLPR441hjFizszN Mn7HSG1UVw>? NX7aXm9mUUN3ME20OlAhdk1? M{XOU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BCBL1 NFvYenBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MkHPglEh|ryP M3\vRmROW09? MmjCTWM2OD1|M{Cgcm0> NIS0cpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
BJAB NVr4dmFOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVjUN3AzhjFizszN NX3CUoozTE2VTx?= NWe3R3dmUUN3ME25O|Ahdk1? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
Namalwa NF;JWXNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWP+NUDPxE1? NFrTT49FVVOR MWHJR|UxRTl5MDDuUS=> NHX6dHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
Jurkat NInlbmVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NF7tOYt,OSEQvF2= MVjEUXNQ Mnn5TWM2OD1zMkKwJI5O M3P4eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
MM1S MVXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYf3NXZQhjFizszN MXfEUXNQ M2LtfmlEPTB;N{[wJI5O Mn[4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
U266 M1zicmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYD+NUDPxE1? NWHwc5RJTE2VTx?= M2HhTmlEPTB;OUWwJI5O MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
UM-PEL-1 NHP4OHZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NX\aZXg4hjFizszN M1m4bWROW09? MmfMTWM2OD1{MUCgcm0> M1y3N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
UM-PEL-3 NEGzcWlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2DZT54yKM7:TR?= NF\vcHFFVVOR M4XoR2lEPTB;MUiwJI5O MoD4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
BC1 NYTrV4JoTnWwY4Tpc44h[XO|YYm= NUf4c3I1PTByIH7N M1zaXWROW09? MVfpcoR2[2W|IHPlcIwu[3mlbHWgZZJz\XO2 M3nQ[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BC3 MX\GeY5kfGmxbjDhd5NigQ>? NVjoW5VXPTByIH7N NIP0[5ZFVVOR Ml7kbY5lfWOnczDj[YxtNWO7Y3zlJIFzemW|dB?= Mm\3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
BC1 MUjGeY5kfGmxbjDhd5NigQ>? NGr0cJM5ODBibl2= NGPOOFFFVVOR MmfvdoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> NELqb3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
BC3 NWG0cI5zTnWwY4Tpc44h[XO|YYm= MlHOPFAxKG6P MVHEUXNQ NYO4fWtzemWmdXPld{BkNU27YzDwdo91\WmwIHzleoVtew>? MkCwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
H929 NF;LVVJHfW6ldHnvckBie3OjeR?= NIfFe2d,OSEQvF2= M3PvXGROW09? NX3vRlE2cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M33te|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS12PE MkD1SpVv[3Srb36gZZN{[Xl? M{LNNp4yKM7:TR?= MnG1SG1UVw>? NH\WRlVqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NW\YOndsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
KMS12BM M{LkZ2Z2dmO2aX;uJIF{e2G7 MkDSglEh|ryP MlrBSG1UVw>? M4rteolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M{G2UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS18 MV;GeY5kfGmxbjDhd5NigQ>? M3W2Vp4yKM7:TR?= MnzjSG1UVw>? NF;IfY1qdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M3O4TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS11 NWrHUmZCTnWwY4Tpc44h[XO|YYm= NYXTfXhwhjFizszN M{K1SGROW09? MmXSbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MnXrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
RPMI8226 MofMSpVv[3Srb36gZZN{[Xl? NH7nW4p,OSEQvF2= MVfEUXNQ MYXpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NGjQO3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
H929 M{T2UmFxd3C2b4Ppd{Bie3OjeR?= MXz+NUDPxE1? MY\EUXNQ M4rLR4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
KMS12PE MnjHRZBweHSxc3nzJIF{e2G7 MYj+NUDPxE1? MYTEUXNQ NVvr[3E6cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NFW0Nok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS12BM NWTqdndkSXCxcITvd4l{KGG|c3H5 NWPGeWJUhjFizszN NXTGNndSTE2VTx?= NEP0Z4hqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MoDDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
KMS18 NYjLPGx7SXCxcITvd4l{KGG|c3H5 NEWxTmV,OSEQvF2= NWPlUnYxTE2VTx?= NInZNopqdmS3Y3XzJINmdGxiYYDvdJRwe2m| M4TTd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS11 NIT4c3FCeG:ydH;zbZMh[XO|YYm= NXTOdYI2hjFizszN NGj1SXhFVVOR NIOyXotqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NUP4[|RnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
RPMI8226 NWXNdmpiSXCxcITvd4l{KGG|c3H5 NGTQT2F,OSEQvF2= MmDWSG1UVw>? NHTaWIVqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NX3lO4tQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
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A172 NVPwOIJSTnWwY4Tpc44h[XO|YYm= MY\+NVAh|ryP NIO0S5FFVVOR MVny[YR2[2W|IHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMT6yPEDPxE1? NV7P[YhYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0PVY{QDFpPkK0OFk3OzhzPD;hQi=>
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Rosetta2 DE3 M3XLe2Z2dmO2aX;uJIF{e2G7 NHm2e3A{OCCvaX7z NWL5SnEyTGm|cHzhZ4Vu\W62IH;mJGZCVS2uYXLlcIVlKFqEQUK0PEBnem:vIFLSSFIhSkR{IDizOFkhfG9iNE[wJIFucW6xIHHjbYQhemW|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDh[pRmeiB|MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBxd2yjcnn6ZZRqd25iYYPzZZktKEurIE2gNE4xPDl4IN88UU4> MoPEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3 NI\wUHhHfW6ldHnvckBie3OjeR?= MUezNEBucW6| NYTVdJZ{TGm|cHzhZ4Vu\W62IH;mJGZCVS2uYXLlcIVlKFqEQUK0PEBnem:vIFLSSFQhSkR{IDizN|MhfG9iNE[wJIFucW6xIHHjbYQhemW|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDh[pRmeiB|MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBxd2yjcnn6ZZRqd25iYYPzZZktKEurIE2gNE4xPzR6IN88UU4> MmfmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3 MX\GeY5kfGmxbjDhd5NigQ>? M1\nTFMxKG2rboO= NYXYU3NTUW6qaXLpeIlwdiCxZjDGRW0udGGkZXzl[EBbSkF{NEigZolv\GmwZzD0c{Bz\WOxbXLpcoFvfCCqdX3hckBPNXSncn3pcoFtKEirc{[teIFo\2WmIFLSSFQh[nKxbX;kc41icW5iMTCoOFQhfG9iMU[4JJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy|IHHmeIVzKDNyIH3pcpMh[nliRnzveZJme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhU2liPTCwMlAxQSEQvF2u NFnyRok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OES2N|Q5Pyd-Mki0OlM1QDd:L3G+
Rosetta2 DE3 NXXwPYp[TnWwY4Tpc44h[XO|YYm= MUOzNEBucW6| NFfGbZRKdmirYnn0bY9vKG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDibY5lcW6pIITvJJJm[2:vYnnuZY51KGi3bXHuJG4ufGW{bXnuZYwhUGm|Nj30ZYdo\WRiQmLEOEBjem:vb3TvcYFqdiB{IDizN|MhfG9iNE[wJJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy|IHHmeIVzKDNyIH3pcpMh[nliRnzveZJme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhU2liPTCwMlA4PDhizszNMi=> M4\2OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NE[zOFg4Lz5{OES2N|Q5PzxxYU6=
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HT-29 MkftSpVv[3Srb36gZZN{[Xl? NVTGc2hUOC5|MUK1JJVOKHSxIEWgeW0> M1m4dlI1KGi{cx?= NYjvdJJUUW6qaXLpeIlwdiCxZjDCVmQ1KGmwIHj1cYFvKEiWLUK5JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClLV35Z{Bxem:2ZXnuJIV5eHKnc4Ppc44h[XRiMD6zNVI2KHWPIITvJFUhfU1idV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdibXX0bI9l M4K0bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUW5OFI5Lz5{NUW1PVQzQDxxYU6=
MV4-11 M4PyR2Z2dmO2aX;uJIF{e2G7 M2nYbWlvcGmkaYTpc44hd2ZiQmLEOEBqdiCqdX3hckBOXjRvMUGgZ4VtdHNiYYPz[ZN{\WRiYYOg[I94dnKnZ4XsZZRqd25ib3[gRmNNOiCUTlGg[ZhxemW|c3nvckBjgSCUTlGtd4VyKGGwYXz5d4l{ MkW1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{NUm3OVEoRjJ7MkW5O|UyRC:jPh?=
MV4-11 NUPVNHo3TnWwY4Tpc44h[XO|YYm= MYnJcohq[mm2aX;uJI9nKEKURESgbY4hcHWvYX6gUXY1NTFzIHPlcIx{KGG|c3Xzd4VlKGG|IHTve45z\We3bHH0bY9vKG:oIHPNXWMhWk6DIHX4dJJme3Orb36gZpkhWk6DLYPldUBidmGueYPpdy=> MlHpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl{NUm3OVEoRjJ7MkW5O|UyRC:jPh?=
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BT-37 NF;jUVRyUFSVIHHzd4F6 NYLONGxbeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz M4PibFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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OHS-50 MV7xTHRUKGG|c3H5 NH7mT21yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
fibroblast cells M1vDcpFJXFNiYYPzZZk> NF30XYNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiY3;ueJJwdCCKaDD3bYxlKHS7cHWg[oljem:kbHHzeEBk\Wyucx?= NFqxRmI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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SJ-GBM2 M2TqZpFJXFNiYYPzZZk> MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= NUSxd297RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC Ml25dWhVWyCjc4PhfS=> MljFdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= M17JcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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LAN-5 NFvMeXByUFSVIHHzd4F6 MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NWfo[VZWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 M{XiZ5FJXFNiYYPzZZk> MmHpdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? MmO2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
α-SMA / Fibronectin / Collagen-1; 

PubMed: 27732564     


Normally cultured NRK-49F cells were treated with I-BET151 (0-5μM) for 36 h. Then, cell lysates were prepared and subjected to immunoblot analysis with antibodies against α-SMA, collagen-1, fibronectin, and GAPDH.

FoxM1 / AURKB / Survivin / cyclin B / PLK1; 

PubMed: 26877780     


OVTOKO and OVCA420 cells were treated with DMSO, JQ1 (1 μM) or I-BET151 (1 μM). Cell lysates were immunoblotted with indicated antibodies. 

HP1α / HP1β / HP1γ; 

PubMed: 30386240     


Protein expression levels of HP1α, β, and γ in U937, R-U937, HL-60, and R-HL-60 cells after incubation with I-BET151 at indicated dose for 48 h. Typical blots from a representative experiment are shown. The experiments were repeated three times.

27732564 26877780 30386240
体内研究 I-BET151每天按30 mg/kg剂量处理小鼠，显著抑制鼠类MLL-AF9和人类MLL-AF4白血病肿瘤生长，显著延长寿命。[1]

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)

激酶实验：

[1]
- 合并

荧光各向异性（FP）的配体位移检测:

所有组分溶解在50 mM HEPES pH 7.4, 150 mM NaCl和 0.5 mM CHAPS组成的Buffer中，BRD 2/3/4终浓度为75 nM，荧光配体为5 nM。在Greiner 384孔黑色的低量微孔板中，使用Micro Multidrop 将10 μL反应混合物加入到含100 nL各种浓度I-BET151或DMSO空白对照（1%最终）的孔中，并在黑暗中室温下平衡60分钟。使用 Envision (lex=485 nm，lEM=530 nm；Dichroic=505 nM)读取荧光各向异性。
细胞实验：

[1]
- 合并
  • Cell lines: MV4;11, MOLM13, NOMO1, RS4;11, HEL, HL60 和 K562
  • Concentrations: 溶于DMSO, 终浓度为~100 μM
  • Incubation Time: 24,或72小时
  • Method:

    使用多种不同浓度I-BET151在384孔或96孔板中处理细胞24或72小时。细胞生长抑制实验中，实验板每孔中加入与细胞培养基同等体积的CellTiter-Glo试剂，震荡约2分钟，然后在Analyst GT 或EnVision酶标仪上读取化学发光信号。细胞增殖实验中，每孔加入CellTiter-Aqueous One，然后实验板在37°C下温育4小时。在SpectraMax Gemini酶标仪上490 nm处读取吸光度。


    (Only for Reference)
动物实验：

[1]
- 合并
  • Animal Models: 静脉注射MV4;11细胞的NOD-SCID小鼠,静脉注射MLL-AF9细胞的C57BL/6小鼠
  • Dosages: ~30 mg/kg/day
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 Ethanol 27 mg/mL (64.99 mM)
DMSO Insoluble
Water Insoluble

* 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 415.44
化学式

C23H21N5O3
CAS号 1300031-49-5
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 只
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
Selleck产品目录册

Epigenetic Reader Domain Signaling Pathway Map

Epigenetic Reader Domain Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID