I-BET151 (GSK1210151A)

For research use only.

Catalog No.S2780

34 publications

I-BET151 (GSK1210151A) Chemical Structure

CAS No. 1300031-49-5

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.

Selleck's I-BET151 (GSK1210151A) has been cited by 34 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 NHvX[IhkgXSxdH;4bYNqfHliYYPzZZk> MVr+NVAxKM7:TR?= MYnEUXNQ NFPNdWFKSzVyPUK2JI5O M1TwOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
RS4;11 MUfjfZRwfG:6aXPpeJkh[XO|YYm= Mk[xglExOCEQvF2= NWD0WmJNTE2VTx?= MX3JR|UxRTF7MjDuUS=> M2DjSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
MOLM13 M1nONoN6fG:2b4jpZ4l1gSCjc4PhfS=> M1m0U54yODBizszN M17CcmROW09? MnmxTWM2OD1zMkCgcm0> NF30UW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
NOMO1 NH;GO5NkgXSxdH;4bYNqfHliYYPzZZk> MUD+NVAxKM7:TR?= NYXvepZ5TE2VTx?= MYXJR|UxRTF3IH7N NHzhW2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
HEL NUfI[WFW[3m2b4TvfIlkcXS7IHHzd4F6 MVX+NVAxKM7:TR?= NY\4WlZsTE2VTx?= NWDsdYlbUUN3ME2xJO69VQ>? M{n3WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
K562 MX7jfZRwfG:6aXPpeJkh[XO|YYm= M{\iVZ4yODBizszN NIiyfmJFVVOR Ml3mTWM2OD5zMECg{txO MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl4NEO0NEc,OjF7NkSzOFA9N2F-
MEG01 M{j0WoN6fG:2b4jpZ4l1gSCjc4PhfS=> M2K3XZ4yODBizszN MoPSSG1UVw>? Ml7mTWM2OD1{NTFOwG0> NVu0UXVGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
HL60 NFnTcmRkgXSxdH;4bYNqfHliYYPzZZk> MUH+NVAxKM7:TR?= M336WWROW09? NXv6c3dpUUN3ME24PVAhdk1? NVHIdm4yRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
MV4;11 NHK2bYhCeG:ydH;zbZMh[XO|YYm= MofrglExOCEQvF2= NFT0UWRFVVOR NEDhbG5qdmS3Y3XzJIFxd3C2b4Ppdy=> M1rLWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
MOLM13 M4e3fGFxd3C2b4Ppd{Bie3OjeR?= M1XQUZ4yODBizszN Mk\FSG1UVw>? NULVW5gycW6mdXPld{BieG:ydH;zbZM> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl4NEO0NEc,OjF7NkSzOFA9N2F-
MV4;11 MnL1SpVv[3Srb36gZZN{[Xl? MmjISG1UVw>? NGnPUZVl\WO{ZXHz[ZMhfGinIILlZ5J2cXSvZX70JI9nKEKUREOvOEBidmRiaX3wZYlz\WRicnXjdpVqfG2nboSgc4YhS0SNOTDhcoQhWEGIMTD0c{B1cGVidILhcpNkemmydHnvcoFtKHO2YYL0JJNqfGV? M4TudFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
PBMC NFfS[IpHfW6ldHnvckBie3OjeR?= MmPySG1UVw>? MVnpcohq[mm2czDJUE03KHerdHigdGlEPTBib3[gOk44 M3rHSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NEO3NVE2Lz5{MkSzO|EyPTxxYU6=
A2 NIHVZ5pHfW6ldHnvckBie3OjeR?= Mn3JglExKM7:TR?= M4jJ[GROW09? MV;y[YFkfGm4YYTld{Bt[XSnboSgTGlXNTF? NGnFU3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K1OVIyQCd-MkOyOVUzOTh:L3G+
A72 NIjBZ|RHfW6ldHnvckBie3OjeR?= MX;+NVAh|ryP NESyfWlFVVOR MkXOdoVi[3SrdnH0[ZMhdGG2ZX70JGhKXi1z NIPCVI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K1OVIyQCd-MkOyOVUzOTh:L3G+
BC1 M1K1bWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmD5glEh|ryP MmT3SG1UVw>? MkfTTWM2OD1{MkCgcm0> M1KzT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BC3 MmPuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXT+NUDPxE1? NXOyb2ZwTE2VTx?= M4PNcGlEPTB;NE[wJI5O NI\NcnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
BCBL1 MYrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVnRPZp6hjFizszN NGLwN|dFVVOR NWXwNYJzUUN3ME2zN|Ahdk1? MkPKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
BJAB MojmS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4fPep4yKM7:TR?= M3vPbmROW09? MWTJR|UxRTl5MDDuUS=> MmK4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
Namalwa M4C3T2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml20glEh|ryP NYjmN|FxTE2VTx?= NWrudItsUUN3ME25O|Ahdk1? Mn;BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
Jurkat M4fsXGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIfvSIN,OSEQvF2= MULEUXNQ NHn4V2dKSzVyPUGyNlAhdk1? Mm\PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
MM1S NEDmU4dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYf+NUDPxE1? MnfnSG1UVw>? MWTJR|UxRTd4MDDuUS=> MoDTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
U266 M2PjSWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYH+NUDPxE1? M1G0ZWROW09? NEj0OGhKSzVyPUm1NEBvVQ>? Mlv4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
UM-PEL-1 M3XsdGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MVT+NUDPxE1? Mk\hSG1UVw>? M1zKemlEPTB;MkGwJI5O M{S1TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
UM-PEL-3 M1Lkdmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVLySHN4hjFizszN MnnlSG1UVw>? MWfJR|UxRTF6MDDuUS=> MlvQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
BC1 NXr4cGFUTnWwY4Tpc44h[XO|YYm= NEHENnU2ODBibl2= M1fL[GROW09? NFPXdI5qdmS3Y3XzJINmdGxvY4njcIUh[XK{ZYP0 MlmzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
BC3 NVvC[XdSTnWwY4Tpc44h[XO|YYm= MnjIOVAxKG6P M3nRRWROW09? MXPpcoR2[2W|IHPlcIwu[3mlbHWgZZJz\XO2 MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BC1 MYTGeY5kfGmxbjDhd5NigQ>? MlrCPFAxKG6P MlnGSG1UVw>? MmLTdoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BC3 MWnGeY5kfGmxbjDhd5NigQ>? NVvhPVZtQDByIH7N MYPEUXNQ MYny[YR2[2W|IHOtUZlkKHC{b4TlbY4hdGW4ZXzz NFzHN489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
H929 Mn22SpVv[3Srb36gZZN{[Xl? M{HSRZ4yKM7:TR?= MXfEUXNQ MUXpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
KMS12PE M3HPRmZ2dmO2aX;uJIF{e2G7 NFrZNGt,OSEQvF2= Mne1SG1UVw>? MojtbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= Mm[wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
KMS12BM MmLmSpVv[3Srb36gZZN{[Xl? NV\QRnhThjFizszN MnfqSG1UVw>? NV3jdnNWcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M3rrWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS18 NUfVRXRFTnWwY4Tpc44h[XO|YYm= MlvxglEh|ryP MoD4SG1UVw>? NWLMN3o5cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NIXoNVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS11 MnnaSpVv[3Srb36gZZN{[Xl? MWL+NUDPxE1? NEDFOW5FVVOR Mm[wbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NX7BfXJYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
RPMI8226 NYHjVlBYTnWwY4Tpc44h[XO|YYm= MUD+NUDPxE1? NVS5[WhmTE2VTx?= MWDpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MkjHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
H929 NGTTfZhCeG:ydH;zbZMh[XO|YYm= NXfLcmRHhjFizszN NGPyOoZFVVOR MWjpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NFjjOYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS12PE NWjsUII6SXCxcITvd4l{KGG|c3H5 MljOglEh|ryP NF[ze3BFVVOR NY\LSHJQcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NWnX[HBbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
KMS12BM M3HvXWFxd3C2b4Ppd{Bie3OjeR?= M2nTcp4yKM7:TR?= NVuwNlZCTE2VTx?= MVTpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NV[xOpBxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
KMS18 NFPoXZhCeG:ydH;zbZMh[XO|YYm= MV\+NUDPxE1? NYPvSVZOTE2VTx?= NWDRVG5PcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NHzSNFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
KMS11 M1rpTmFxd3C2b4Ppd{Bie3OjeR?= M3zIPZ4yKM7:TR?= MXvEUXNQ M3eyN4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M2nKclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
RPMI8226 M3LUWGFxd3C2b4Ppd{Bie3OjeR?= NF[0[pV,OSEQvF2= Mmf3SG1UVw>? NWfZO4wxcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= Ml\mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
U87MG NV;XPJgxTnWwY4Tpc44h[XO|YYm= NXfyWmxshjFyIN88US=> NYfCeph3TE2VTx?= MUny[YR2[2W|IGW4O21IKGOnbHz1cIFzKEGWUDD3bZRpKEmFNUCgc4YhOS5yNTFOwG0> Mki2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2OU[zPFEoRjJ2NEm2N|gyRC:jPh?=
A172 NH3mVWNHfW6ldHnvckBie3OjeR?= MnG1glExKM7:TR?= NHHCNnlFVVOR NEjKUnVz\WS3Y3XzJINmdGy3bHHyJGFVWCC5aYToJGlEPTBib3[gNU4zQCEQvF2= M4jiZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEm2N|gyLz5{NES5OlM5OTxxYU6=
SW1783 NHLvZ2ZHfW6ldHnvckBie3OjeR?= MlnVglExKM7:TR?= NXjWc45zTE2VTx?= M2nIcJJm\HWlZYOgZ4VtdHWuYYKgRXRRKHerdHigTWM2OCCxZjCyMlY5KM7:TR?= NHnKZWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES5OlM5OSd-MkS0PVY{QDF:L3G+
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RAW267.4 M13oc2Z2dmO2aX;uJIF{e2G7 NVHmdpoyOSEQvF2= MlXQSG1UVw>? M1HxVpJm\HWlZYOgTWwuPiCycn;keYN1cW:wIHnu[JVk\WRiYomgUHBU NVfTfpR{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4OVkxODhpPkK0PFU6ODB6PD;hQi=>
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SK-Mel-28 NIrD[npHfW6ldHnvckBie3OjeR?= MY[xNEDPxE1? NFyyeVNFVVOR M1LVTJVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= M4\HPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC2NVM4Lz5{NEmwOlE{PzxxYU6=
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Mel-JD MkLNSpVv[3Srb36gZZN{[Xl? MXGxNEDPxE1? MlvZSG1UVw>? MYT1dJJm\3WuYYTld{Bxem:jcH;weI91cWNiYX7kJINmdGxiY4njcIUh[XK{ZYP0JIdmdmW| M4jiO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC2NVM4Lz5{NEmwOlE{PzxxYU6=
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Raji MmDySpVv[3Srb36gZZN{[Xl? M4T1d|QhcHK| NHnQcohKdmirYnn0bY9vKG:oIFLSSFQhcW5iaIXtZY4hWmGsaTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhVVmFIHX4dJJme3Orb36gZYZ1\XJiNDDodpMtKEmFNUCgQUAxNjF|IN88UU4> MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyMEe1PEc,OjR7MEC3OVg9N2F-
MV4-11 M3\Mcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH3YZ5U4OiCqcoO= NGPjbYJIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOXjRvMUGgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDBwMUG5JO69VS5? NV7PTG9IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1OVk1OjhpPkK1OVU6PDJ6PD;hQi=>
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Rosetta2 DE3 M37VbmZ2dmO2aX;uJIF{e2G7 MYezNEBucW6| M3jTVWRqe3CuYXPlcYVvfCCxZjDGRW0udGGkZXzl[EBbSkF{NEig[pJwdSCEUlS0JGJFOSBqNESgeI8hOTZ6IHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO|YYmsJGlEPTBiPTCwMlA{OTdizszNMi=> NH;TW3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
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Rosetta2 DE3 NFTW[4ZHfW6ldHnvckBie3OjeR?= NEDCd2o{OCCvaX7z NEe3PVNFcXOybHHj[Y1mdnRib3[gSmFONWyjYnXs[YQhYkKDMkS4JIZzd21iQmLEOEBDTDJiKEOzN{B1dyB2NkCgZY1qdm9iYXPp[EBz\XOrZIXld{khMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy|IHHmeIVzKDNyIH3pcpMh[nliZnz1c5Jme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhUUN3MDC9JFAvOjJ4IN88UU4> MlnCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
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MV4-11 M4PuWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIXsZZA1KGSjeYO= MXrHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JHdUXC16IHHzd4F6NCCLQ{WwJF0hOC5zNkKg{txONg>? M1W2[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NE[zOFg4Lz5{OES2N|Q5PzxxYU6=
Rosetta2 DE3 NVnHc3RYTnWwY4Tpc44h[XO|YYm= M{HWW|MxKG2rboO= NUC0U4J[UW6qaXLpeIlwdiCxZjDGRW0udGGkZXzl[EBbSkF{NEigZolv\GmwZzD0c{Bz\WOxbXLpcoFvfCCqdX3hckBPNXSncn3pcoFtKEirc{[teIFo\2WmIFLSSFQh[nKxbX;kc41icW5iMjCoN|M{KHSxIES2NEBz\XOrZIXld{kh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDh[pRmeiB|MDDtbY5{KGK7IF\sc5Vz\XOlZX7j[UBxd2yjcnn6ZZRqd25iYYPzZZktKEmFNUCgQUAxNjJ{NjFOwG0v MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
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OHS-50 MYfxTHRUKGG|c3H5 NHzhSJJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz M1jqeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
fibroblast cells M3f2NZFJXFNiYYPzZZk> NGLtVWJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiY3;ueJJwdCCKaDD3bYxlKHS7cHWg[oljem:kbHHzeEBk\Wyucx?= NHPDV4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 M1nlXZFJXFNiYYPzZZk> M4nWeJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy| M{XafVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh30 MnnxdWhVWyCjc4PhfS=> M17aRpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEOwJINmdGy| NWD0VpZMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 NUDwNlNveUiWUzDhd5NigQ>? M3PYdJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC M{nlepFJXFNiYYPzZZk> NXjyVo92eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> NFqyZ2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 NUjvT2N3eUiWUzDhd5NigQ>? MYjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= M{[4NlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 M4TmeZFJXFNiYYPzZZk> MlnZdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| M3nhOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18 MUjxTHRUKGG|c3H5 NInBZnNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?= MlHIQIEhfGG{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
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

Kinase Assay:

[1]

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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]

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  • 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]

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  • 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 powder
in solvent
Synonyms N/A
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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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