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BRD3BRD4IC50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BRD3BRD4IC50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 NUnFNm9X[3m2b4TvfIlkcXS7IHHzd4F6 NULBeo1QhjFyMDFOwG0> NYLWWm4zTE2VTx?= NYfEfGpQUUN3ME2yOkBvVQ>? NH3lN4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
RS4;11 M1rJOIN6fG:2b4jpZ4l1gSCjc4PhfS=> MXP+NVAxKM7:TR?= NETNSo9FVVOR M2jk[mlEPTB;MUmyJI5O NHfRRlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
MOLM13 MYLjfZRwfG:6aXPpeJkh[XO|YYm= MoHhglExOCEQvF2= NXfobHhpTE2VTx?= NILicIhKSzVyPUGyNEBvVQ>? NWq3SJYzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
NOMO1 NWnyfJZz[3m2b4TvfIlkcXS7IHHzd4F6 MnPOglExOCEQvF2= NXrSRlM4TE2VTx?= M17C[WlEPTB;MUWgcm0> M3fWV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
HEL MnHTZ5l1d3SxeHnjbZR6KGG|c3H5 Mn;YglExOCEQvF2= MV\EUXNQ M1XXcmlEPTB;MTFOwG0> MmDRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
K562 MlXyZ5l1d3SxeHnjbZR6KGG|c3H5 NITORXZ,OTByIN88US=> NVzXUXRVTE2VTx?= M4TUeWlEPTB-MUCwJO69VQ>? Mn\tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
MEG01 Mkf6Z5l1d3SxeHnjbZR6KGG|c3H5 NYTFRohZhjFyMDFOwG0> NWDWd2xkTE2VTx?= NY\rUpRrUUN3ME2yOUDPxE1? NEjRXYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
HL60 MVrjfZRwfG:6aXPpeJkh[XO|YYm= NIWweXd,OTByIN88US=> MkHPSG1UVw>? Ml;sTWM2OD16OUCgcm0> NVfqbGQ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
MV4;11 M{O3Z2Fxd3C2b4Ppd{Bie3OjeR?= MnHTglExOCEQvF2= MVvEUXNQ NXjicFlmcW6mdXPld{BieG:ydH;zbZM> NGDxUJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
MOLM13 M36wbmFxd3C2b4Ppd{Bie3OjeR?= MkXaglExOCEQvF2= MVLEUXNQ MWDpcoR2[2W|IHHwc5B1d3Orcx?= NULpSGtRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
MV4;11 M4nQNmZ2dmO2aX;uJIF{e2G7 M3XoT2ROW09? NXjwRXZT\GWlcnXhd4V{KHSqZTDy[YNzfWm2bXXueEBw\iCEUlSzM|Qh[W6mIHntdIFqemWmIILlZ5J2cXSvZX70JI9nKEOGS{mgZY5lKFCDRkGgeI8hfGinIITyZY5{[3KrcITpc45idCC|dHHyeEB{cXSn NH7iRpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
PBMC MkTCSpVv[3Srb36gZZN{[Xl? NF;lWGRFVVOR NWfGUoU5cW6qaXLpeJMhUUxvNjD3bZRpKHCLQ{WwJI9nKDZwNx?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjR|N{GxOUc,OjJ2M{exNVU9N2F-
A2 NVHtU29lTnWwY4Tpc44h[XO|YYm= NFTUV2N,OTBizszN NHuyNI5FVVOR NHjhVIJz\WGldHn2ZZRmeyCuYYTlcpQhUEmYLUG= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ3NUKxPEc,OjN{NUWyNVg9N2F-
A72 NITROZZHfW6ldHnvckBie3OjeR?= M1Gycp4yOCEQvF2= M2[0bGROW09? NIe4PJVz\WGldHn2ZZRmeyCuYYTlcpQhUEmYLUG= NXTJN5RkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOVUzOThpPkKzNlU2OjF6PD;hQi=>
BC1 MXnHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MnK3glEh|ryP M2LHPGROW09? MWHJR|UxRTJ{MDDuUS=> NGfs[mE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
BC3 NHfvS41Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoPaglEh|ryP NWPKcYszTE2VTx?= M1KzWGlEPTB;NE[wJI5O NH;zZYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
BCBL1 NEWz[JRIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYLYTXY4hjFizszN MnXJSG1UVw>? NYOwWIczUUN3ME2zN|Ahdk1? MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BJAB NEO5[G9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGTFS5l,OSEQvF2= MYLEUXNQ M1L5SmlEPTB;OUewJI5O NULrUmd7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVI1PDhpPkKzO|kzPDR6PD;hQi=>
Namalwa MVfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MX;+NUDPxE1? MV7EUXNQ NUPTR3JnUUN3ME25O|Ahdk1? MknPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
Jurkat NF\6O5JIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXK1NFh4hjFizszN M3S1UGROW09? M3HuNGlEPTB;MUKyNEBvVQ>? MnzXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
MM1S NWjQVlZ1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHzsSpB,OSEQvF2= MoL4SG1UVw>? Mn\MTWM2OD15NkCgcm0> NGTyN2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
U266 MVjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmPNglEh|ryP MXrEUXNQ MlXuTWM2OD17NUCgcm0> M2Sy[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
UM-PEL-1 MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NFvXbGl,OSEQvF2= NUn6TZlRTE2VTx?= NHLzRXZKSzVyPUKxNEBvVQ>? MnzSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
UM-PEL-3 NETYVG9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWLPR4RmhjFizszN NILuS4JFVVOR MXrJR|UxRTF6MDDuUS=> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BC1 NX36XZQxTnWwY4Tpc44h[XO|YYm= MX:1NFAhdk1? M2XaXGROW09? NXrhe5VJcW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BC3 NYrpbplWTnWwY4Tpc44h[XO|YYm= MXu1NFAhdk1? MnrhSG1UVw>? MUTpcoR2[2W|IHPlcIwu[3mlbHWgZZJz\XO2 MlPYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
BC1 MUXGeY5kfGmxbjDhd5NigQ>? MXi4NFAhdk1? MVPEUXNQ MWry[YR2[2W|IHOtUZlkKHC{b4TlbY4hdGW4ZXzz MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BC3 NIm4fXZHfW6ldHnvckBie3OjeR?= NYriS|JYQDByIH7N NGTGdWtFVVOR MknOdoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> NYSwXHgxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVI1PDhpPkKzO|kzPDR6PD;hQi=>
H929 NHTad25HfW6ldHnvckBie3OjeR?= Mlr6glEh|ryP MnjVSG1UVw>? NHTGO3lqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M1XBW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS12PE M1X4eGZ2dmO2aX;uJIF{e2G7 NUfve3drhjFizszN NWr6TolTTE2VTx?= M1n2Nolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NGO5S|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS12BM MYLGeY5kfGmxbjDhd5NigQ>? MojXglEh|ryP MVrEUXNQ MXLpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NXXUPXRORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
KMS18 MXfGeY5kfGmxbjDhd5NigQ>? NFfhNnZ,OSEQvF2= MkXPSG1UVw>? M2DFeYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M1;kcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS11 NEOwU2RHfW6ldHnvckBie3OjeR?= NVzVd4xIhjFizszN NXPERlR1TE2VTx?= M1S3eYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NFTyd4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
RPMI8226 NE\EPI9HfW6ldHnvckBie3OjeR?= MYf+NUDPxE1? MnvOSG1UVw>? NXfFfoRGcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NWrsZpBURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
H929 MVfBdI9xfG:|aYOgZZN{[Xl? NWjXOpNVhjFizszN MX;EUXNQ NGXSPVZqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NG[4XIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS12PE NXHUPGpUSXCxcITvd4l{KGG|c3H5 MXX+NUDPxE1? M33WTmROW09? MnvKbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
KMS12BM NVLKTFNqSXCxcITvd4l{KGG|c3H5 NHPmZol,OSEQvF2= MoD2SG1UVw>? NXrtellzcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= Ml\4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
KMS18 NGXkXIdCeG:ydH;zbZMh[XO|YYm= NXXkTZBxhjFizszN NVi4N4RLTE2VTx?= M2LJNIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
KMS11 NV7xZXlXSXCxcITvd4l{KGG|c3H5 NFTkRZd,OSEQvF2= NWfjO5dpTE2VTx?= MnHlbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M3zhblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
RPMI8226 NIjxe4xCeG:ydH;zbZMh[XO|YYm= NVeyOVVQhjFizszN M{\uWWROW09? NYLrSVZbcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
U87MG NWHZRWEyTnWwY4Tpc44h[XO|YYm= NWfDTItnhjFyIN88US=> NF\CfnFFVVOR NIfJT4Zz\WS3Y3XzJHU5P02JIHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMT6wOUDPxE1? NWLRXIZ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0PVY{QDFpPkK0OFk3OzhzPD;hQi=>
A172 M2nR[GZ2dmO2aX;uJIF{e2G7 MVr+NVAh|ryP NGD6OWJFVVOR M1r3[ZJm\HWlZYOgZ4VtdHWuYYKgRXRRKHerdHigTWM2OCCxZjCxMlI5KM7:TR?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR7NkO4NUc,OjR2OU[zPFE9N2F-
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Mel-RM MXrGeY5kfGmxbjDhd5NigQ>? M3G0TVExKM7:TR?= MUnEUXNQ NUDU[5l{fXC{ZXf1cIF1\XNicILvZZBweHSxdHnjJIFv\CClZXzsJIN6[2ynIHHydoV{fCCpZX7ldy=> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyNkGzO{c,OjR7ME[xN|c9N2F-
HepG2 MkXhSpVv[3Srb36gZZN{[Xl? MYixPEBpenN? M3q2fXVxemWpdXzheIlwdiCxZjDBdI9COSCneIDy[ZN{cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGOxbnPlcpRz[XSrb36gdoVyfWm{ZXSgeI8hcW6lcnXhd4UhPzBnIH;mJIx2[2moZYLhd4Uh[WO2aY\peJkh[W[2ZYKgNVghcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVOxO|AhRSByLkC5JO69VS5? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjN6NkWyPUc,OjJ|OE[1Nlk9N2F-
Raji NFu1dWFHfW6ldHnvckBie3OjeR?= MV60JIhzew>? NEPNcm9KdmirYnn0bY9vKG:oIFLSSFQhcW5iaIXtZY4hWmGsaTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhVVmFIHX4dJJme3Orb36gZYZ1\XJiNDDodpMtKEmFNUCgQUAxNjF|IN88UU4> NXzkW2ExRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA4PThpPkK0PVAxPzV6PD;hQi=>
MV4-11 M{\4SWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2XUWFczKGi{cx?= NWfjbJdyT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVVZ2LUGxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSByLkGxPUDPxE1w M2G0PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUW5OFI5Lz5{NUW1PVQzQDxxYU6=
MM1S MnrvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXHtfmdKPzJiaILz M330ZWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1OOVNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFAvOjl7IN88UU4> NGLnNFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW1PVQzQCd-MkW1OVk1Ojh:L3G+
HT-29 M1rwdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn\QO|IhcHK| MUHHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNE46PDVizszNMi=> M1fO[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUW5OFI5Lz5{NUW1PVQzQDxxYU6=
Rosetta2 DE3 Mnf2SpVv[3Srb36gZZN{[Xl? MWSzNEBucW6| MoflSIl{eGyjY3Xt[Y51KG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDmdo9uKEKURESgRmQyKCh2NDD0c{AyPjhiYX3pco8h[WOrZDDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hWm:|ZYT0ZVIhTEV|IHPlcIx{KGGodHXyJFMxKG2rboOgZpkh\my3b4Lld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeTygTWM2OCB;IECuNFMyPyEQvF2u MnPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
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Rosetta2 DE3 MV;GeY5kfGmxbjDhd5NigQ>? NXH6c2FGOzBibXnudy=> NEn3b49FcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLENkBDTDFiKEeyJJRwKDJyNTDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5MEBMcSB;IECuNFA6KM7:TT6= NYixdoFQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
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Rosetta2 DE3 MVLGeY5kfGmxbjDhd5NigQ>? NY\0XGc6OzBibXnudy=> M335OGRqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlSyJGJFOiBqM{S5JJRwKDR4MDDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5MEBMcSB;IECuNFQ6PiEQvF2u NHW5flU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
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Rosetta2 DE3 M3nUO2Z2dmO2aX;uJIF{e2G7 NHjpfGg{OCCvaX7z M1mzPGlvcGmkaYTpc44hd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IHLpcoRqdmdidH:gdoVkd22kaX7hcpQhcHWvYX6gUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCEUlS0JIJzd22xZH;tZYlvKDJiKEOzN{B1dyB2NkCgdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCIbH;1doV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5MEBMcSB;IECuNFc1QCEQvF2u MljUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2NkO0PFcoRjJ6NE[zOFg4RC:jPh?=
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BT-12 NU\4NJNQeUiWUzDhd5NigQ>? MkHhdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| M3;QPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) NG\zU5VyUFSVIHHzd4F6 Mn3ldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 MVrxTHRUKGG|c3H5 MnjidWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= NY\6[WhiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 M{e2O5FJXFNiYYPzZZk> MVLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| M4HCPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
fibroblast cells M2HiXZFJXFNiYYPzZZk> NIO5XGZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiY3;ueJJwdCCKaDD3bYxlKHS7cHWg[oljem:kbHHzeEBk\Wyucx?= M3fFXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 NIHufHJyUFSVIHHzd4F6 MWTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? NH74NJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh30 MXzxTHRUKGG|c3H5 NXTF[VAzeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoN|Ah[2WubIO= NXrjWFdiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 MmTBdWhVWyCjc4PhfS=> NFLLfm5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> NVrkVmxORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC M2[z[pFJXFNiYYPzZZk> M3vHV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz NE[z[po9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 MYjxTHRUKGG|c3H5 MYnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 NHTiUWhyUFSVIHHzd4F6 M3jUU5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 Ml33dWhVWyCjc4PhfS=> NUTz[pBteUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO= Mnn3QIEhfGG{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
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

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