I-BET151 (GSK1210151A)

Catalog No.S2780

For research use only.

I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.

I-BET151 (GSK1210151A) Chemical Structure

CAS No. 1300031-49-5

Selleck's I-BET151 (GSK1210151A) has been cited by 35 publications

Purity & Quality Control

Choose Selective Epigenetic Reader Domain Inhibitors

Biological Activity

Description I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.
Features Optimized to retain excellent BET target potency and selectivity while enhancing the in vivo pharmacokinetics and terminal half-life to enable prolonged in vivo studies.
Targets
BRD3 [1]
(Cell-free assay)
BRD2 [1]
(Cell-free assay)
BRD4 [1]
(Cell-free assay)
0.25 μM 0.5 μM 0.79 μM
In vitro

I-BET151 exhibits potent selectivity over an extensive range of diverse protein types such as COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, ion channels, and transporters. Similar to I-BET762 (GSK525762A), I-BET151 displays potent binding affinity to BRD2, BRD3 and BRD4 with KD of 0.02-0.1 μM, and significantly inhibits lipopolysaccharide-stimulated IL-6 cytokine production in human peripheral blood mononuclear cells (PBMC) and whole blood (WB) as well as rat WB with IC50 of 0.16 μM, 1.26 μM, and 1.26 μM, respectively. I-BET151 (0.5 or 5 μM) inhibits the binding of BETs (BRD2, BRD3, BRD4, and BRD9) but not the binding of 23 other bromodomain proteins in HL60 nuclear extract to acetylated histone peptides. I-BET151 has potent efficacy against cell lines harboring different MLL-fusions such as MV4;11, RS4;11, MOLM13, and NOMO1 cells with IC50 of 15-192 nM. Consistently, I-BET151 completely ablates the colony-forming potential of MLL-fusion-driven leukaemias (MOLM13) but not leukaemias driven by tyrosine kinase activation (K562). I-BET151 also displays potent efficacy in both liquid culture and clonogenic assays using primary murine progenitors transformed with either MLL-ENL or MLL-AF9. I-BET151 treatment significantly induces apoptosis and prominent G0/G1 arrest in MLL-fusion cell lines driven by distinct MLL fusions (MOLM13 and MV4;11 containing MLL-AF9 and MLL-AF4, respectively) but not the K562 cells, probably due to the inhibition of transcription of BCL2, C-MYC and CDK6 by blocking the recruitment of BRD3/4, PAFc and SEC components into transcriptional start site (TSS). [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MV4;11 M{DVNYN6fG:2b4jpZ4l1gSCjc4PhfS=> NF\oUll,OTByIN88US=> M{D5eWROW09? MUPJR|UxRTJ4IH7N NWfqdHJ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
RS4;11 MmDpZ5l1d3SxeHnjbZR6KGG|c3H5 NV3IW5hqhjFyMDFOwG0> Ml;MSG1UVw>? M1e3[WlEPTB;MUmyJI5O NH\6SoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
MOLM13 M3\MN4N6fG:2b4jpZ4l1gSCjc4PhfS=> M4HodZ4yODBizszN MYLEUXNQ MlXyTWM2OD1zMkCgcm0> NHnrTGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
NOMO1 NYHHXJA1[3m2b4TvfIlkcXS7IHHzd4F6 MkK1glExOCEQvF2= NXT1WpZXTE2VTx?= Mm\rTWM2OD1zNTDuUS=> NFfCVXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
HEL NIXHV2NkgXSxdH;4bYNqfHliYYPzZZk> MUH+NVAxKM7:TR?= NIr6b|JFVVOR MXPJR|UxRTFizszN M1KwOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
K562 NUjxW29K[3m2b4TvfIlkcXS7IHHzd4F6 NWGzVWdJhjFyMDFOwG0> M3\0SWROW09? NEn3WJNKSzVyPkGwNEDPxE1? MlvqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
MEG01 M2j2NIN6fG:2b4jpZ4l1gSCjc4PhfS=> NHruTZR,OTByIN88US=> MnjhSG1UVw>? NXS1[4lJUUN3ME2yOUDPxE1? M13rSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
HL60 NGOzenlkgXSxdH;4bYNqfHliYYPzZZk> MWf+NVAxKM7:TR?= M1\Tb2ROW09? M3;YdGlEPTB;OEmwJI5O NGTEepo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
MV4;11 MkPsRZBweHSxc3nzJIF{e2G7 NF61Zld,OTByIN88US=> NVfKXmJGTE2VTx?= M4fUR4lv\HWlZYOgZZBweHSxc3nz M{SyZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
MOLM13 MWfBdI9xfG:|aYOgZZN{[Xl? M2\YN54yODBizszN M3Lz[2ROW09? NHzxfGlqdmS3Y3XzJIFxd3C2b4Ppdy=> NF;mVoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
MV4;11 M2fKdWZ2dmO2aX;uJIF{e2G7 MmHpSG1UVw>? MV;k[YNz\WG|ZYOgeIhmKHKnY4L1bZRu\W62IH;mJGJTTDNxNDDhcoQhcW2yYXny[YQhemWlcoXpeI1mdnRib3[gR2RMQSCjbnSgVGFHOSC2bzD0bIUhfHKjboPjdolxfGmxbnHsJJN1[XK2IIPpeIU> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl4NEO0NEc,OjF7NkSzOFA9N2F-
PBMC MXrGeY5kfGmxbjDhd5NigQ>? NYrBd|ZoTE2VTx?= MWHpcohq[mm2czDJUE03KHerdHigdGlEPTBib3[gOk44 NFzH[449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkSzO|EyPSd-MkK0N|cyOTV:L3G+
A2 NHHCWWFHfW6ldHnvckBie3OjeR?= NGDme4d,OTBizszN Mlr5SG1UVw>? NXPPUGlQemWjY4TpeoF1\XNibHH0[Y51KEiLVj2x NWHLe451RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOVUzOThpPkKzNlU2OjF6PD;hQi=>
A72 MWTGeY5kfGmxbjDhd5NigQ>? M{\UfJ4yOCEQvF2= MmHISG1UVw>? MVXy[YFkfGm4YYTld{Bt[XSnboSgTGlXNTF? NIfX[IQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K1OVIyQCd-MkOyOVUzOTh:L3G+
BC1 NXH6d3JOT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mlq5glEh|ryP M1H6TGROW09? M4TVZmlEPTB;MkKwJI5O MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BC3 NYL5bm1HT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWn+NUDPxE1? M1zBWmROW09? NFTvcYtKSzVyPUS2NEBvVQ>? NHjHV4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
BCBL1 M2Dsb2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1fCRp4yKM7:TR?= MkfGSG1UVw>? MXzJR|UxRTN|MDDuUS=> M{O5[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BJAB MorYS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NGjUepV,OSEQvF2= MX3EUXNQ M2DMN2lEPTB;OUewJI5O MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
Namalwa M{K5XWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4LlcJ4yKM7:TR?= NXrFW4dYTE2VTx?= NX3w[oZ1UUN3ME25O|Ahdk1? Mki3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
Jurkat MmW3S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFPhe2l,OSEQvF2= MlzmSG1UVw>? NYHSZ2ZoUUN3ME2xNlIxKG6P NXvuSIJ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVI1PDhpPkKzO|kzPDR6PD;hQi=>
MM1S NXHoSnNWT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmfIglEh|ryP NGn6[WlFVVOR Ml64TWM2OD15NkCgcm0> NEO5WVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
U266 M1\4b2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{HNbZ4yKM7:TR?= NUDuN3ZyTE2VTx?= NH7LXlVKSzVyPUm1NEBvVQ>? M3j3O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
UM-PEL-1 NVrJXIx1T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NHrpO|V,OSEQvF2= M2nKXWROW09? MV\JR|UxRTJzMDDuUS=> NHXxXlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
UM-PEL-3 M{L4[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M{Tkbp4yKM7:TR?= NYnFXGtETE2VTx?= MVLJR|UxRTF6MDDuUS=> M3OyRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BC1 NVvNNlRNTnWwY4Tpc44h[XO|YYm= MlLIOVAxKG6P NGDvUWFFVVOR NX[ye2lzcW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> NFzJOG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
BC3 NULlOYFjTnWwY4Tpc44h[XO|YYm= Ml;COVAxKG6P Ml;WSG1UVw>? NFnIV|RqdmS3Y3XzJINmdGxvY4njcIUh[XK{ZYP0 MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BC1 MYPGeY5kfGmxbjDhd5NigQ>? NITvcnE5ODBibl2= MV;EUXNQ NHXLN2tz\WS3Y3XzJIMuVXmlIIDyc5RmcW5ibHX2[Yx{ MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BC3 M4nBcWZ2dmO2aX;uJIF{e2G7 MoHKPFAxKG6P NGj3UJZFVVOR MlzsdoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
H929 M2jES2Z2dmO2aX;uJIF{e2G7 MVH+NUDPxE1? NXrQbIo4TE2VTx?= MnP6bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NFfOUXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS12PE NYn6SXJQTnWwY4Tpc44h[XO|YYm= M4XvW54yKM7:TR?= M3jnO2ROW09? NFHXSndqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
KMS12BM MVjGeY5kfGmxbjDhd5NigQ>? MWn+NUDPxE1? NEP6e5VFVVOR Ml21bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NHX6OVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS18 NFS0[nRHfW6ldHnvckBie3OjeR?= MVf+NUDPxE1? MUnEUXNQ MXTpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 M4fQWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS11 MUnGeY5kfGmxbjDhd5NigQ>? Mmm5glEh|ryP MXTEUXNQ MWnpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NGKwbXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
RPMI8226 MkjFSpVv[3Srb36gZZN{[Xl? M33iS54yKM7:TR?= NGPQOXhFVVOR NEPPPZhqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
H929 NGTKUZJCeG:ydH;zbZMh[XO|YYm= MWf+NUDPxE1? MlL6SG1UVw>? M{DLWIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M3WxfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS12PE NHjkSIRCeG:ydH;zbZMh[XO|YYm= MnSyglEh|ryP NYfScW1ZTE2VTx?= MlfubY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M1\VclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS12BM M2nkTGFxd3C2b4Ppd{Bie3OjeR?= MkP4glEh|ryP MYPEUXNQ NHTENlBqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NWjCVnk5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
KMS18 NHL0U2FCeG:ydH;zbZMh[XO|YYm= MYP+NUDPxE1? M4DPfWROW09? NF7RN4ZqdmS3Y3XzJINmdGxiYYDvdJRwe2m| M4f2VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS11 NFzqUJJCeG:ydH;zbZMh[XO|YYm= MlXOglEh|ryP NUDqPGNHTE2VTx?= NHrHdlBqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NYSz[FdHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
RPMI8226 M3\aVGFxd3C2b4Ppd{Bie3OjeR?= MWL+NUDPxE1? NH;L[oZFVVOR MmnHbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
U87MG NX3OTJRnTnWwY4Tpc44h[XO|YYm= Mnv4glExKM7:TR?= Mlf6SG1UVw>? MVLy[YR2[2W|IGW4O21IKGOnbHz1cIFzKEGWUDD3bZRpKEmFNUCgc4YhOS5yNTFOwG0> Mn\zQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2OU[zPFEoRjJ2NEm2N|gyRC:jPh?=
A172 MWXGeY5kfGmxbjDhd5NigQ>? MXH+NVAh|ryP NYixUYh6TE2VTx?= MVfy[YR2[2W|IHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMT6yPEDPxE1? M{G3[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEm2N|gyLz5{NES5OlM5OTxxYU6=
SW1783 NHLSWWRHfW6ldHnvckBie3OjeR?= M1PzS54yOCEQvF2= NVvldFRVTE2VTx?= NGG5RoZz\WS3Y3XzJINmdGy3bHHyJGFVWCC5aYToJGlEPTBib3[gNk43QCEQvF2= MmjZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2OU[zPFEoRjJ2NEm2N|gyRC:jPh?=
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RAW267.4 NXH5S5ZSTnWwY4Tpc44h[XO|YYm= NX3QN2NmOSEQvF2= NGLZeI1FVVOR MlrodoVlfWOnczDJUE03KHC{b3T1Z5Rqd25iaX7keYNm\CCkeTDMVHM> NUKxS5hTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4OVkxODhpPkK0PFU6ODB6PD;hQi=>
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HepG2 MYHGeY5kfGmxbjDhd5NigQ>? NW[2Z5FIOThiaILz NGr5Z4JWeHKnZ4XsZZRqd25ib3[gRZBwSTFiZYjwdoV{e2mxbjDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyClb37j[Y51emG2aX;uJJJmeXWrcnXkJJRwKGmwY4LlZZNmKDdyJTDv[kBtfWOrZnXyZZNmKGGldHn2bZR6KGGodHXyJFE5KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDNVcxKD1iMD6wPUDPxE1w NImxTY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkO4OlUzQSd-MkKzPFY2Ojl:L3G+
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MV4-11 MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{\BNVczKGi{cx?= NFrwbnZIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOXjRvMUGgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDBwMUG5JO69VS5? M2nYUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUW5OFI5Lz5{NUW1PVQzQDxxYU6=
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Rosetta2 DE3 MlH1SpVv[3Srb36gZZN{[Xl? NVPhNGs2OzBibXnudy=> MUfEbZNxdGGlZX3lcpQhd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IH\yc40hSlKGNDDCSFEhMDR2IITvJFE3QCCjbXnuc{Bi[2mmIILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBTd3OndIThNkBFTTNiY3XscJMh[W[2ZYKgN|AhdWmwczDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7LDDJR|UxKD1iMD6wN|E4KM7:TT6= NV;He4tCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
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MOLM13 M3\2N2N6fG:2b4jpZ4l1gSCjc4PhfS=> NV;KUJN{PCCmYYnz M3S0VmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1QVE1zMzDj[YxteyCqYYLic5JqdmdiTVzMNUBnfXOrb36g[4Vv\SCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB2IHThfZMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCCjc4PhfUwhUUN3MDC9JFAvOjJ6IN88UU4> NXPT[HpCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
Rosetta2 DE3 M2Lkc2Z2dmO2aX;uJIF{e2G7 NXTPSFVuOzBibXnudy=> NXnoT4c3UW6qaXLpeIlwdiCxZjDGRW0udGGkZXzl[EBbSkF{NEigZolv\GmwZzD0c{Bz\WOxbXLpcoFvfCCqdX3hckBPNXSncn3pcoFtKEirc{[teIFo\2WmIFLSSFQh[nKxbX;kc41icW5iMTCoOFQhfG9iMU[4JJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy|IHHmeIVzKDNyIH3pcpMh[nliRnzveZJme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhUUN3MDC9JFAvODNzNzFOwG0v MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
MV4-11 MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{\QeVQh\GG7cx?= NVjodnR3T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVVZ2LUGxJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCZU2StPEBie3OjeTygTWM2OCB;IECuNVYzKM7:TT6= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
Rosetta2 DE3 NHXYT2dHfW6ldHnvckBie3OjeR?= NYr5OnNHOzBibXnudy=> NETSe4dKdmirYnn0bY9vKG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDibY5lcW6pIITvJJJm[2:vYnnuZY51KGi3bXHuJG4ufGW{bXnuZYwhUGm|Nj30ZYdo\WRiQmLEOEBjem:vb3TvcYFqdiB{IDizN|MhfG9iNE[wJJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy|IHHmeIVzKDNyIH3pcpMh[nliRnzveZJme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhUUN3MDC9JFAvOjJ4IN88UU4> NVXuV5ZnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0OlM1QDdpPkK4OFY{PDh5PD;hQi=>
MOLM13 NXHjV2JoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M17FOFQh\GG7cx?= NWewWXRjT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OTUGzJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCZU2StPEBie3OjeTygTWM2OCB;IECuNlI5KM7:TT6= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
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MV4-11 NV;QUVM2TnWwY4Tpc44h[XO|YYm= M1fWZ2lvcGmkaYTpc44hd2ZiQmLEOEBqdiCqdX3hckBOXjRvMUGgZ4VtdHNiYYPz[ZN{\WRiYYOg[I94dnKnZ4XsZZRqd25ib3[gRmNNOiCUTlGg[ZhxemW|c3nvckBjgSCUTlGtd4VyKGGwYXz5d4l{ NEj1ZXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK1PVc2OSd-MkmyOVk4PTF:L3G+
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SJ-GBM2 MUnxTHRUKGG|c3H5 MVzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MlzDdWhVWyCjc4PhfS=> M3r3c5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz NH7vfIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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Rh18 MWrxTHRUKGG|c3H5 MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index PMID
Western blot α-SMA / Fibronectin / Collagen-1 ; FoxM1 / AURKB / Survivin / cyclin B / PLK1 ; HP1α / HP1β / HP1γ 27732564 26877780 30386240
In vivo Administration of I-BET151 at 30 mg/kg/day significantly inhibits tumor growth of murine MLL-AF9 and human MLL-AF4 leukaemia in mice, and provides marked survival benefit. [1]

Protocol (from reference)

Kinase Assay:

[1]

  • Fluorescence anisotropy (FP) ligand displacement assay:

    All components are dissolved in buffer of composition 50 mM HEPES pH 7.4, 150 mM NaCl and 0.5 mM CHAPS with final concentrations of BRD 2/3/4 75 nM, fluorescent ligand 5 nM. 10 μL of this reaction mixture is added using a micro multidrop to wells containing 100 nL of various concentrations of I-BET151 or DMSO vehicle (1% final) in Greiner 384 well Black low volume microtitre plate and equilibrated in the dark for 60 minutes at room temperature. Fluorescence anisotropy is read in Envision (lex = 485 nm, lEM = 530 nm; Dichroic = 505 nM).

Cell Research:

[1]

  • Cell lines: MV4;11, MOLM13, NOMO1, RS4;11, HEL, HL60 and K562
  • Concentrations: Dissolved in DMSO, final concentrations ~100 μM
  • Incubation Time: 24, or 72 hours
  • Method:

    Cells are exposed to various concentrations of I-BET151 for 24 or 72 hours in 384-well or 96-well plates. For cell growth inhibition assays, plates are added with CellTiter-Glo reagent using a volume equivalent to the cell culture volume in the wells, shaken for approximately 2 minutes and chemiluminescent signal is read on the Analyst GT or EnVision Plate Reader. For cell proliferation assays, CellTiter-Aqueous One is added to each well and plates are incubated for 4 hours at 37 °C. Absorbance is read at 490 nm on a SpectraMax Gemini reader

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: NOD-SCID mice injected intravenously with MV4;11 cells, and C57BL/6 mice injected intravenously with MLL-AF9 cells
  • Dosages: ~30 mg/kg/day
  • Administration: Intraperitoneal injection
  • (Only for Reference)

Solubility (25°C)

In vitro

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 415.44
Formula

C23H21N5O3

CAS No. 1300031-49-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)C(C)C5=CC=CC=N5)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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