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34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 M3THc4N6fG:2b4jpZ4l1gSCjc4PhfS=> NV7QTJNXhjFyMDFOwG0> M3ntVGROW09? NVvjOYxWUUN3ME2yOkBvVQ>? NX6zZVJQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
RS4;11 NXf1UXNz[3m2b4TvfIlkcXS7IHHzd4F6 M37BOJ4yODBizszN NEHSfZBFVVOR NH3TZoJKSzVyPUG5NkBvVQ>? NWK5NGk5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
MOLM13 NHzZNHhkgXSxdH;4bYNqfHliYYPzZZk> NWfscXEzhjFyMDFOwG0> MmLISG1UVw>? NHrIT4ZKSzVyPUGyNEBvVQ>? M4juT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
NOMO1 NVHqcFFT[3m2b4TvfIlkcXS7IHHzd4F6 NFP6cop,OTByIN88US=> NYHkfYNMTE2VTx?= NWL1RVFyUUN3ME2xOUBvVQ>? M3:zTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
HEL NH64OJdkgXSxdH;4bYNqfHliYYPzZZk> NFu3[5R,OTByIN88US=> MkjNSG1UVw>? M3vZbmlEPTB;MTFOwG0> M3rLdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
K562 MnPRZ5l1d3SxeHnjbZR6KGG|c3H5 MVj+NVAxKM7:TR?= M3rrXGROW09? MkPTTWM2OD5zMECg{txO M1noUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
MEG01 M2\2eYN6fG:2b4jpZ4l1gSCjc4PhfS=> NWS3UYluhjFyMDFOwG0> M2PofWROW09? MknJTWM2OD1{NTFOwG0> MlLOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
HL60 NX3XNYE4[3m2b4TvfIlkcXS7IHHzd4F6 NIe1VZl,OTByIN88US=> NHjLbphFVVOR NIXtWmVKSzVyPUi5NEBvVQ>? NXzFd|ZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
MV4;11 MXPBdI9xfG:|aYOgZZN{[Xl? NYfSPY9FhjFyMDFOwG0> M{XacWROW09? NEDq[oNqdmS3Y3XzJIFxd3C2b4Ppdy=> NF65XXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
MOLM13 NVO0SINQSXCxcITvd4l{KGG|c3H5 NFflNHh,OTByIN88US=> NVvBNFY6TE2VTx?= NHLCNY5qdmS3Y3XzJIFxd3C2b4Ppdy=> NFPJ[YE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
MV4;11 NVXTWHUzTnWwY4Tpc44h[XO|YYm= NXzwe2dSTE2VTx?= NFvJb|Nl\WO{ZXHz[ZMhfGinIILlZ5J2cXSvZX70JI9nKEKUREOvOEBidmRiaX3wZYlz\WRicnXjdpVqfG2nboSgc4YhS0SNOTDhcoQhWEGIMTD0c{B1cGVidILhcpNkemmydHnvcoFtKHO2YYL0JJNqfGV? M2DtS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
PBMC MXvGeY5kfGmxbjDhd5NigQ>? M1PNfWROW09? MnfmbY5pcWKrdIOgTWwuPiC5aYToJJBKSzVyIH;mJFYvPw>? M{TuTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEO3NVE2Lz5{MkSzO|EyPTxxYU6=
A2 M2i5eWZ2dmO2aX;uJIF{e2G7 NELEUJJ,OTBizszN M2TtU2ROW09? Mlz3doVi[3SrdnH0[ZMhdGG2ZX70JGhKXi1z NYLWVFJlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOVUzOThpPkKzNlU2OjF6PD;hQi=>
A72 NH;XU4hHfW6ldHnvckBie3OjeR?= MYr+NVAh|ryP MU\EUXNQ M3n6cZJm[WO2aY\heIV{KGyjdHXueEBJUVZvMR?= NFO3cYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K1OVIyQCd-MkOyOVUzOTh:L3G+
BC1 MkXUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWfXWpo5hjFizszN Mlz0SG1UVw>? MlLDTWM2OD1{MkCgcm0> Ml\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
BC3 NFryTIpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NEnObGl,OSEQvF2= NXG1WmdOTE2VTx?= M1nuTGlEPTB;NE[wJI5O NHLpfGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
BCBL1 NIHNWnBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MVH+NUDPxE1? NVLPSFM4TE2VTx?= Mme0TWM2OD1|M{Cgcm0> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BJAB M4THVGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4TkWZ4yKM7:TR?= MkDUSG1UVw>? M{exdWlEPTB;OUewJI5O NIHoSHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
Namalwa NGDpSGhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHvJenV,OSEQvF2= M2D3emROW09? MmXZTWM2OD17N{Cgcm0> M1XpPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
Jurkat M1fVRmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVrqVJZ[hjFizszN Mn75SG1UVw>? Ml3LTWM2OD1zMkKwJI5O MnP5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
MM1S MnfwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXT+NUDPxE1? M4PMeWROW09? MkDFTWM2OD15NkCgcm0> M{fMPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
U266 NUP3eWJRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmSwglEh|ryP MVXEUXNQ MWPJR|UxRTl3MDDuUS=> NWLDWopZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVI1PDhpPkKzO|kzPDR6PD;hQi=>
UM-PEL-1 NYryXIFvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWf+NUDPxE1? NIG3fVlFVVOR MYfJR|UxRTJzMDDuUS=> NVHkSmpQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVI1PDhpPkKzO|kzPDR6PD;hQi=>
UM-PEL-3 M{HzOmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3j2dZ4yKM7:TR?= M1LaOWROW09? M3Llb2lEPTB;MUiwJI5O M2DQOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BC1 MkX0SpVv[3Srb36gZZN{[Xl? M1XHS|UxOCCwTR?= NFLwcI9FVVOR NV7Yb5g{cW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> NVvZPIZ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVI1PDhpPkKzO|kzPDR6PD;hQi=>
BC3 NGWzW3VHfW6ldHnvckBie3OjeR?= NVrVfppQPTByIH7N NEXqO2JFVVOR NW\oblJMcW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BC1 MXfGeY5kfGmxbjDhd5NigQ>? NH;ZeoM5ODBibl2= M1HLSmROW09? M4nrdZJm\HWlZYOgZ{1OgWNicILveIVqdiCuZY\lcJM> NFm5dHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
BC3 M1HjUGZ2dmO2aX;uJIF{e2G7 MlnnPFAxKG6P NIfybWRFVVOR NXmxfJhYemWmdXPld{BkNU27YzDwdo91\WmwIHzleoVtew>? MnLMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
H929 NYfEbmVETnWwY4Tpc44h[XO|YYm= NX7JVFUyhjFizszN NXvRXVc2TE2VTx?= NFLKVYVqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NYD1fWpNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
KMS12PE MkT5SpVv[3Srb36gZZN{[Xl? NX62VHZzhjFizszN NIS2b2pFVVOR M33vcIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
KMS12BM M4fnUmZ2dmO2aX;uJIF{e2G7 NVzsXYg4hjFizszN MVvEUXNQ MknGbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= Mnf3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
KMS18 NFG3UJhHfW6ldHnvckBie3OjeR?= MX\+NUDPxE1? M4P6[2ROW09? MUPpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
KMS11 NUXXSXd3TnWwY4Tpc44h[XO|YYm= NIPIbnB,OSEQvF2= NFvab|dFVVOR M1\XPIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
RPMI8226 M2r3O2Z2dmO2aX;uJIF{e2G7 NV;4ZXlEhjFizszN M1v5PWROW09? NIewU2FqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NYTMdohqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
H929 MmTWRZBweHSxc3nzJIF{e2G7 M3HIWJ4yKM7:TR?= NInGN|NFVVOR NWPtW|VJcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NHLwS|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS12PE NEj6dmVCeG:ydH;zbZMh[XO|YYm= MXj+NUDPxE1? NHuzdoVFVVOR MlW0bY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NHXBRZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS12BM NHrhV5RCeG:ydH;zbZMh[XO|YYm= MnPvglEh|ryP Mn\tSG1UVw>? MlLXbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MmXQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
KMS18 MofaRZBweHSxc3nzJIF{e2G7 MX7+NUDPxE1? MlrhSG1UVw>? M4\Xcolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M4[4PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS11 NXrkdmNpSXCxcITvd4l{KGG|c3H5 NI\hR|J,OSEQvF2= NGDm[plFVVOR NGrTWnBqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MkXxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
RPMI8226 NXzaTlh{SXCxcITvd4l{KGG|c3H5 MnjNglEh|ryP Mk\JSG1UVw>? NYrEOHp[cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
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A172 NG[wRZFHfW6ldHnvckBie3OjeR?= MlTYglExKM7:TR?= MmnoSG1UVw>? MX7y[YR2[2W|IHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMT6yPEDPxE1? NIDNXXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES5OlM5OSd-MkS0PVY{QDF:L3G+
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Rosetta2 DE3 NHzpNHdHfW6ldHnvckBie3OjeR?= MoPZRolv\GmwZzDh[oZqdmm2eTD0c{BjcW:2aX75cIF1\WRiQmLEN{BDTDFiKEK0JJRwKDF2NDDhcYlvdyCjY3nkJJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYomgZolwNWyjeXXyJIlvfGW{ZnXyc41mfHK7IH3leIhw\CxiS3SgQUAxNjB{OUig{txONg>? NVzZWGlDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
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Rosetta2 DE3 MlPMSpVv[3Srb36gZZN{[Xl? M{jlS2JqdmSrbnegZYZncW6rdImgeI8h[mmxdHnufYxifGWmIFLSSFQhSkRzIDi0OEB1dyBzNkigZY1qdm9iYXPp[EBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy|IHL5JIJqdy2uYYnldkBqdnSncn\ldo9u\XS{eTDt[ZRpd2RuIFvkJF0hOC5yNUK4JO69VS5? MnnuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
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Rosetta2 DE3 MnzjSpVv[3Srb36gZZN{[Xl? MnXJN|AhdWmwcx?= MWfEbZNxdGGlZX3lcpQhd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IH\yc40hSlKGMzDCSFIhMDNyNjD0c{A1OTdiYX3pco8h[WOrZDDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hWm:|ZYT0ZVIhTEV|IHPlcIx{KGGodHXyJFMxKG2rboOgZpkh\my3b4Lld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeTygT4khRSByLkCyNlMh|ryPLh?= M2nZU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
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Rosetta2 DE3 NH:zUVhHfW6ldHnvckBie3OjeR?= M37jNlMxKG2rboO= NFn2NXhFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLEOEBDTDJiKEOzN{B1dyB2NkCgZY1qdm9iYXPp[EBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy|IHHmeIVzKDNyIH3pcpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhU2liPTCwMlA4PDhizszNMi=> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
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Rosetta2 DE3 MVzGeY5kfGmxbjDhd5NigQ>? MYKzNEBucW6| M4TwUWlvcGmkaYTpc44hd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IHLpcoRqdmdidH:gdoVkd22kaX7hcpQhcHWvYX6gUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCEUlS0JIJzd22xZH;tZYlvKDJiKEOzN{B1dyB2NkCgdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiCUb4PleJRiOiCGRUOgZ4VtdHNiYX\0[ZIhOzBibXnud{BjgSCIbH;1doV{[2WwY3WgdI9t[XKrenH0bY9vKGG|c3H5MEBMcSB;IECuNFc1QCEQvF2u MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
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BT-12 Mn3xdWhVWyCjc4PhfS=> M3fZV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= NWTlVVNJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) M1;0d5FJXFNiYYPzZZk> MnO4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| M1T0OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 MYfxTHRUKGG|c3H5 M2\iNJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 NFi3O2JyUFSVIHHzd4F6 NYHld3ZoeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> NXW3eYdbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
fibroblast cells MX\xTHRUKGG|c3H5 M3Lme5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiClb370do9tKEiqIIfpcIQhfHmyZTDmbYJzd2KuYYP0JINmdGy| MnqyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 MW\xTHRUKGG|c3H5 MXXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? Ml7lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh30 MVvxTHRUKGG|c3H5 NUTiW4ZGeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoN|Ah[2WubIO= NFrIVYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MnzqdWhVWyCjc4PhfS=> MoeydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NIHieHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NFHyd5pyUFSVIHHzd4F6 NECwR3dyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> M3zlOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NFr3[G5yUFSVIHHzd4F6 NWXGPJRTeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> NE\Me209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 NYP3OJRbeUiWUzDhd5NigQ>? NFvTcpFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTFHOMVUh[2WubIO= M1zhbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18 NFTRXWRyUFSVIHHzd4F6 MojIdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? NILh[Jg9[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
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、SDS / 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、SDS / 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