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32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 NX7XPHlS[3m2b4TvfIlkcXS7IHHzd4F6 M4TJNJ4yODBizszN NVXoOIhCTE2VTx?= M{m1ZmlEPTB;Mk[gcm0> NH;SfI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
RS4;11 MmXvZ5l1d3SxeHnjbZR6KGG|c3H5 MlP2glExOCEQvF2= M1frVmROW09? M1i4UmlEPTB;MUmyJI5O NYWzXZdERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
MOLM13 MW\jfZRwfG:6aXPpeJkh[XO|YYm= NF7Eclh,OTByIN88US=> MmDVSG1UVw>? NH3KU4RKSzVyPUGyNEBvVQ>? M{n3dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
NOMO1 NVzBXI1L[3m2b4TvfIlkcXS7IHHzd4F6 MoP5glExOCEQvF2= MnHnSG1UVw>? MlGxTWM2OD1zNTDuUS=> Ml2wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
HEL NVnTVppU[3m2b4TvfIlkcXS7IHHzd4F6 MVT+NVAxKM7:TR?= NHTYR3ZFVVOR M4nvbmlEPTB;MTFOwG0> NFjF[Gc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
K562 NXLjO5po[3m2b4TvfIlkcXS7IHHzd4F6 MU\+NVAxKM7:TR?= M{TISmROW09? NVviS28zUUN3ME6xNFAh|ryP M3jiWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
MEG01 M3PNNIN6fG:2b4jpZ4l1gSCjc4PhfS=> M2XVOp4yODBizszN M{LZfWROW09? M1nBN2lEPTB;MkWg{txO M3jjUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
HL60 NF7ke3hkgXSxdH;4bYNqfHliYYPzZZk> Mkn4glExOCEQvF2= M3nk[GROW09? MnvTTWM2OD16OUCgcm0> MmDlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
MV4;11 NFjXZ|VCeG:ydH;zbZMh[XO|YYm= MXv+NVAxKM7:TR?= NUW4b4tITE2VTx?= NEfqfGRqdmS3Y3XzJIFxd3C2b4Ppdy=> MnXoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
MOLM13 NHjSSmpCeG:ydH;zbZMh[XO|YYm= Mle4glExOCEQvF2= M3;Y[WROW09? NUfYSlhicW6mdXPld{BieG:ydH;zbZM> NV\HWIZjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
MV4;11 M1PQN2Z2dmO2aX;uJIF{e2G7 Mnj5SG1UVw>? M3XjTIRm[3KnYYPld{B1cGVicnXjdpVqfG2nboSgc4YhSlKGMz:0JIFv\CCrbYDhbZJm\CC{ZXPyeYl1dWWwdDDv[kBETEt7IHHu[EBRSUZzIITvJJRp\SC2cnHud4NzcXC2aX;uZYwhe3SjcoSgd4l1\Q>? NXOyXY9uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
PBMC M3;wVWZ2dmO2aX;uJIF{e2G7 MVfEUXNQ MoXIbY5pcWKrdIOgTWwuPiC5aYToJJBKSzVyIH;mJFYvPw>? NFHYO4g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkSzO|EyPSd-MkK0N|cyOTV:L3G+
A2 MoLYSpVv[3Srb36gZZN{[Xl? Ml36glExKM7:TR?= MorQSG1UVw>? NVLv[GNnemWjY4TpeoF1\XNibHH0[Y51KEiLVj2x M2L6cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkW1NlE5Lz5{M{K1OVIyQDxxYU6=
A72 M3PzRWZ2dmO2aX;uJIF{e2G7 MnnyglExKM7:TR?= NVS0[3JtTE2VTx?= Ml73doVi[3SrdnH0[ZMhdGG2ZX70JGhKXi1z M13sU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|MkW1NlE5Lz5{M{K1OVIyQDxxYU6=
BC1 MlXFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M2qw[Z4yKM7:TR?= M4XNNmROW09? MV\JR|UxRTJ{MDDuUS=> M3;aW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BC3 NYrQUWhpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{[4ZZ4yKM7:TR?= MojMSG1UVw>? Mo\jTWM2OD12NkCgcm0> NXXMNmlIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVI1PDhpPkKzO|kzPDR6PD;hQi=>
BCBL1 MW\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkPhglEh|ryP M4[1bWROW09? M{DtcmlEPTB;M{OwJI5O M{\LcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BJAB M1vB[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYTycIhyhjFizszN MV3EUXNQ NWLkZodTUUN3ME25O|Ahdk1? NUHMS4F5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVI1PDhpPkKzO|kzPDR6PD;hQi=>
Namalwa NV\ERVdHT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2XM[54yKM7:TR?= MW\EUXNQ NGP0clRKSzVyPUm3NEBvVQ>? NIXyZ5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
Jurkat Ml;pS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1nhVZ4yKM7:TR?= MYnEUXNQ MVvJR|UxRTF{MkCgcm0> MlHxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
MM1S NUX1Z|d1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{XpbJ4yKM7:TR?= NEDrZlRFVVOR M{fPb2lEPTB;N{[wJI5O MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
U266 NHzzRWJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MlzsglEh|ryP MY\EUXNQ NHXmRlFKSzVyPUm1NEBvVQ>? NHztZ4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
UM-PEL-1 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVr+NUDPxE1? MX;EUXNQ NH\MR5JKSzVyPUKxNEBvVQ>? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
UM-PEL-3 M1Ts[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWjTV49{hjFizszN Ml7uSG1UVw>? NW\UV4g{UUN3ME2xPFAhdk1? MmDVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
BC1 NVn3Woh[TnWwY4Tpc44h[XO|YYm= M2fVflUxOCCwTR?= M3nkPWROW09? MnXBbY5lfWOnczDj[YxtNWO7Y3zlJIFzemW|dB?= M2TFO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BC3 M4LaOWZ2dmO2aX;uJIF{e2G7 M1mwPFUxOCCwTR?= MVTEUXNQ NVnlSoh{cW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> M3zFcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BC1 NYDJPWtsTnWwY4Tpc44h[XO|YYm= NIjGbHA5ODBibl2= MXzEUXNQ NWe2UoU2emWmdXPld{BkNU27YzDwdo91\WmwIHzleoVtew>? M4LDfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BC3 M13IVmZ2dmO2aX;uJIF{e2G7 MYW4NFAhdk1? NEf2dIpFVVOR M3G0[ZJm\HWlZYOgZ{1OgWNicILveIVqdiCuZY\lcJM> NWLuVldMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVI1PDhpPkKzO|kzPDR6PD;hQi=>
H929 NVHZS4tTTnWwY4Tpc44h[XO|YYm= NGfKVmF,OSEQvF2= MX\EUXNQ MUDpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 Mlv3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
KMS12PE Mn;nSpVv[3Srb36gZZN{[Xl? NVn1OGRPhjFizszN M2HpeWROW09? MnLRbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
KMS12BM MnrzSpVv[3Srb36gZZN{[Xl? NFnnOZN,OSEQvF2= Ml7tSG1UVw>? M2SwSYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NYrHS3FwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
KMS18 M1;ZbmZ2dmO2aX;uJIF{e2G7 MUL+NUDPxE1? MVXEUXNQ M1TSb4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= M2DENVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS11 MnLJSpVv[3Srb36gZZN{[Xl? Ml7mglEh|ryP M2XMRmROW09? NFq3XFZqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
RPMI8226 NWTFeVVxTnWwY4Tpc44h[XO|YYm= M{frU54yKM7:TR?= M4rmWWROW09? NWrqe|ZNcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
H929 NWK3UldvSXCxcITvd4l{KGG|c3H5 NEfjeoZ,OSEQvF2= NWmxRllSTE2VTx?= MnXJbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NX7Kb4Q{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
KMS12PE MVfBdI9xfG:|aYOgZZN{[Xl? NHfvR49,OSEQvF2= M33LeWROW09? MlX6bY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NGe0O2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS12BM NXXKSFd5SXCxcITvd4l{KGG|c3H5 NIrCXGd,OSEQvF2= NHHEU2VFVVOR NWf2SG5vcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NHLYPFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS18 MVrBdI9xfG:|aYOgZZN{[Xl? MlSxglEh|ryP Mn;USG1UVw>? M{Dme4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M1vYZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS11 NGnBUGtCeG:ydH;zbZMh[XO|YYm= NHf6dXJ,OSEQvF2= NHjPTZdFVVOR M1PVZ4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NED3d3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
RPMI8226 MonLRZBweHSxc3nzJIF{e2G7 M3W3UZ4yKM7:TR?= M3;od2ROW09? MlzvbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NV7XSoJHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
U87MG M{XPSGZ2dmO2aX;uJIF{e2G7 MXz+NVAh|ryP M{\l[GROW09? NYTtRmxyemWmdXPld{BWQDePRzDj[YxtfWyjcjDBWHAhf2m2aDDJR|UxKG:oIEGuNFUh|ryP NHuzb2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES5OlM5OSd-MkS0PVY{QDF:L3G+
A172 NXHKVItCTnWwY4Tpc44h[XO|YYm= NYi5fmNChjFyIN88US=> M1S1OGROW09? M2HybJJm\HWlZYOgZ4VtdHWuYYKgRXRRKHerdHigTWM2OCCxZjCxMlI5KM7:TR?= NVz6XZc3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0PVY{QDFpPkK0OFk3OzhzPD;hQi=>
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Rosetta2 DE3 NInHOnpHfW6ldHnvckBie3OjeR?= MWPCbY5lcW6pIHHm[olvcXS7IITvJIJqd3SrbonsZZRm\CCEUlSzJGJFOSBqMkSgeI8hOTR2IHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCkeTDibY8udGG7ZYKgbY51\XKoZYLvcYV1enlibXX0bI9lNCCNZDC9JFAvODJ7ODFOwG0v NUHtOVhNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3 M{XwPWZ2dmO2aX;uJIF{e2G7 MnLZRolv\GmwZzDh[oZqdmm2eTD0c{BjcW:2aX75cIF1\WRiQmLEN{BDTDJiKEOwOkB1dyB2MUegZY1qdm9iYXPp[EBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy|IHL5JIJqdy2uYYnldkBqdnSncn\ldo9u\XS{eTDt[ZRpd2RuIFvkJF0hOC5yNEC1JO69VS5? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
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Rosetta2 DE3 NUXRT5ExTnWwY4Tpc44h[XO|YYm= NUXGbXdNSmmwZHnu[{Bi\m[rbnn0fUB1dyCkaX;0bY56dGG2ZXSgRnJFPCCEREKgLFM{OyC2bzC0OlAh[W2rbn:gZYNq\CC{ZYPp[JVmeyliKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gVo9{\XS2YUKgSGU{KGOnbHzzJIJ6KGKrbz3sZZlmeiCrboTldoZmem:vZYTyfUBu\XSqb3SsJGtlKD1iMD6yNVUh|ryPLh?= M2C0dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
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Rosetta2 DE3 NXe4T49KTnWwY4Tpc44h[XO|YYm= MVmzNEBucW6| NFnSVZVFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLENkBDTDFiKEeyJJRwKDJyNTDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5MEBMcSB;IECuNFA6KM7:TT6= M4ToflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3 M2GzWWZ2dmO2aX;uJIF{e2G7 MWezNEBucW6| M3TXTmRqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlSzJGJFOiBqM{C2JJRwKDRzNzDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5MEBMcSB;IECuNFIzOyEQvF2u M17jRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3 NU\BdWlqTnWwY4Tpc44h[XO|YYm= MW[zNEBucW6| M{f0VmRqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlSyJGJFOiBqM{S5JJRwKDR4MDDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCobIXvdoV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5MEBMcSB;IECuNFQ6PiEQvF2u MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
Rosetta2 DE3 NIHvclRHfW6ldHnvckBie3OjeR?= MkjaN|AhdWmwcx?= NHHy[VdFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLEOEBDTDJiKEOzN{B1dyB2NkCgZY1qdm9iYXPp[EBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy|IHHmeIVzKDNyIH3pcpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhU2liPTCwMlA4PDhizszNMi=> NWGxUZViRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
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Rosetta2 DE3 NVW2XVRrTnWwY4Tpc44h[XO|YYm= NV;EU2t{OzBibXnudy=> M1[zW2lvcGmkaYTpc44hd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IHLpcoRqdmdidH:gdoVkd22kaX7hcpQhcHWvYX6gUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCEUlS0JIJzd22xZH;tZYlvKDJiKEOzN{B1dyB2NkCgdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCIbH;1doV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5MEBMcSB;IECuNFc1QCEQvF2u MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
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MV4-11 MmL2SpVv[3Srb36gZZN{[Xl? M37OOGlvcGmkaYTpc44hd2ZiQmLEOEBqdiCqdX3hckBOXjRvMUGgZ4VtdHNiYYPz[ZN{\WRiYYOg[I94dnKnZ4XsZZRqd25ib3[gRmNNOiCUTlGg[ZhxemW|c3nvckBjgSCUTlGtd4VyKGGwYXz5d4l{ MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTJ3OUe1NUc,Ojl{NUm3OVE9N2F-
MV4-11 NXi0NItqTnWwY4Tpc44h[XO|YYm= M3HhV2lvcGmkaYTpc44hd2ZiQmLEOEBqdiCqdX3hckBOXjRvMUGgZ4VtdHNiYYPz[ZN{\WRiYYOg[I94dnKnZ4XsZZRqd25ib3[gZ21[SyCUTlGg[ZhxemW|c3nvckBjgSCUTlGtd4VyKGGwYXz5d4l{ NGfydVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK1PVc2OSd-MkmyOVk4PTF:L3G+
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BT-37 NX7m[Wl{eUiWUzDhd5NigQ>? M2TKVJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD MoPDdWhVWyCjc4PhfS=> M3zNXJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>? Mle3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH MmjLdWhVWyCjc4PhfS=> NH\YXlNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=> M{Tk[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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OHS-50 NHLHNGFyUFSVIHHzd4F6 NFrCcHdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
fibroblast cells MUDxTHRUKGG|c3H5 NGHLXmZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiY3;ueJJwdCCKaDD3bYxlKHS7cHWg[oljem:kbHHzeEBk\Wyucx?= M13EZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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SK-N-MC MV;xTHRUKGG|c3H5 M{\wdZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz MnTFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 Mmi0dWhVWyCjc4PhfS=> M{XxNpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz M4W3[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 Ml;0dWhVWyCjc4PhfS=> MnjEdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| M1m1XVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18 M3WwTpFJXFNiYYPzZZk> M2rwcZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy| NIK4d3I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+

... 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

  • 选择性强的BET抑制剂

    PFI-1 (PF-6405761) : BRD4-selective, IC50=0.22 μM.

  • 活性最高的BET抑制剂

    I-BET-762 : BET proteins, IC50=~35 nM.

  • 用于临床的BET抑制剂

    RVX-208 New : Phase II for Dyslipidemia.

  • 最新的BET抑制剂

    Bromosporine : Broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID