I-BET151 (GSK1210151A)

Catalog No.S2780

I-BET151 (GSK1210151A) Chemical Structure

Molecular Weight(MW): 415.44

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.

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Cited by 5 Publications

5 Customer Reviews

  • OVTOKO and OVCA420 cells were treated with DMSO, JQ1 (1 μM) or I-BET151 (1 μM). Cell lysates were immunoblotted with indicated antibodies.

    Theranostics, 2016, 6(2):219-30.. I-BET151 (GSK1210151A) purchased from Selleck.

    B. Western blot analysis of pERK and ERK in cells treated with JQ1 or I-BET151.

    Oncotarget, 2016, 7(3):2545-54. I-BET151 (GSK1210151A) purchased from Selleck.

  • C57BL/6 mice were primed with Ad26 (109 vp) and boosted with Ad5 (109 vp) in combination with RMD, IBET151, RMD+IBET151, or PBS/DMSO. (B) Frequency of Gag-specific IFN-γ+ CD8+ T cells in the spleen.

    J Immunol, 2018, 201(9):2744-2752. I-BET151 (GSK1210151A) purchased from Selleck.

    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.

    Front Pharmacol, 2018, 9:1166. I-BET151 (GSK1210151A) purchased from Selleck.

  • The expression levels of p16 and p21 were analyzed by western blotting.

    Cell Tissue Res, 2018, 374(3):577-585. I-BET151 (GSK1210151A) purchased from Selleck.

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 NIPVSHdkgXSxdH;4bYNqfHliYYPzZZk> M2HQS54yODBizszN MX3EUXNQ MkHhTWM2OD1{NjDuUS=> MnvVNlE6PjR|NEC=
RS4;11 MVHjfZRwfG:6aXPpeJkh[XO|YYm= NWLEVIJPhjFyMDFOwG0> MV3EUXNQ MX7JR|UxRTF7MjDuUS=> MVeyNVk3PDN2MB?=
MOLM13 M1P3eIN6fG:2b4jpZ4l1gSCjc4PhfS=> M{\pcJ4yODBizszN MX7EUXNQ MkOxTWM2OD1zMkCgcm0> MonWNlE6PjR|NEC=
NOMO1 M{fvToN6fG:2b4jpZ4l1gSCjc4PhfS=> NVXyUlRNhjFyMDFOwG0> NEKycXFFVVOR NInYRW5KSzVyPUG1JI5O M{nWNVIyQTZ2M{Sw
HEL MWTjfZRwfG:6aXPpeJkh[XO|YYm= MmTnglExOCEQvF2= Mon0SG1UVw>? NH\5doFKSzVyPUGg{txO M2\POVIyQTZ2M{Sw
K562 NEjiTVNkgXSxdH;4bYNqfHliYYPzZZk> MmTrglExOCEQvF2= Mnq0SG1UVw>? M1X6XWlEPTB-MUCwJO69VQ>? NWDoV2lpOjF7NkSzOFA>
MEG01 M2HWXYN6fG:2b4jpZ4l1gSCjc4PhfS=> M4qyTp4yODBizszN M3\nfWROW09? M4Dn[mlEPTB;MkWg{txO NXW5RnNVOjF7NkSzOFA>
HL60 M17rWoN6fG:2b4jpZ4l1gSCjc4PhfS=> NVLJS5VQhjFyMDFOwG0> NEHXZoNFVVOR M1X1NWlEPTB;OEmwJI5O NXS3U|IzOjF7NkSzOFA>
MV4;11 Mm\kRZBweHSxc3nzJIF{e2G7 MnnUglExOCEQvF2= NFzsPXBFVVOR NGPwS4RqdmS3Y3XzJIFxd3C2b4Ppdy=> MXWyNVk3PDN2MB?=
MOLM13 MX7BdI9xfG:|aYOgZZN{[Xl? M4fFRp4yODBizszN NFzHdW9FVVOR M2nCOYlv\HWlZYOgZZBweHSxc3nz MYKyNVk3PDN2MB?=
MV4;11 MmHwSpVv[3Srb36gZZN{[Xl? MUTEUXNQ MUfk[YNz\WG|ZYOgeIhmKHKnY4L1bZRu\W62IH;mJGJTTDNxNDDhcoQhcW2yYXny[YQhemWlcoXpeI1mdnRib3[gR2RMQSCjbnSgVGFHOSC2bzD0bIUhfHKjboPjdolxfGmxbnHsJJN1[XK2IIPpeIU> MVuyNVk3PDN2MB?=
PBMC MXrGeY5kfGmxbjDhd5NigQ>? MmXRSG1UVw>? NVzBVmNycW6qaXLpeJMhUUxvNjD3bZRpKHCLQ{WwJI9nKDZwNx?= NEXJbmYzOjR|N{GxOS=>
A2 NWi4TIx4TnWwY4Tpc44h[XO|YYm= M2XrV54yOCEQvF2= NGTkbpJFVVOR MV3y[YFkfGm4YYTld{Bt[XSnboSgTGlXNTF? NXLSSJhEOjN{NUWyNVg>
A72 NHLWXGFHfW6ldHnvckBie3OjeR?= NXXZeGNrhjFyIN88US=> M33XcGROW09? NG\U[YVz\WGldHn2ZZRmeyCuYYTlcpQhUEmYLUG= MmLBNlMzPTV{MUi=
BC1 NXHVbWpQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MkjhglEh|ryP M1;uRmROW09? MmrjTWM2OD1{MkCgcm0> M{T2S|I{Pzl{NES4
BC3 MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWT2boZVhjFizszN MkPpSG1UVw>? MWrJR|UxRTR4MDDuUS=> M2S1fVI{Pzl{NES4
BCBL1 MnLFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MYL+NUDPxE1? M4LYZmROW09? NYPkbGhzUUN3ME2zN|Ahdk1? MlTSNlM4QTJ2NEi=
BJAB MYHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYDMcXNOhjFizszN NGfVe2pFVVOR NYHNfZE2UUN3ME25O|Ahdk1? M4LuS|I{Pzl{NES4
Namalwa M4PTUWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVPFPJVZhjFizszN MmHBSG1UVw>? MWjJR|UxRTl5MDDuUS=> NHK4OJczOzd7MkS0PC=>
Jurkat M3LPfGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnjaglEh|ryP NHnTdXpFVVOR NF3MemRKSzVyPUGyNlAhdk1? M3HkTVI{Pzl{NES4
MM1S MoHNS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NETEOZV,OSEQvF2= MXLEUXNQ MXHJR|UxRTd4MDDuUS=> NYTsZZVNOjN5OUK0OFg>
U266 MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWL+NUDPxE1? NVf4WJZoTE2VTx?= MUTJR|UxRTl3MDDuUS=> MXyyN|c6OjR2OB?=
UM-PEL-1 M3vsZ2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHnCfWh,OSEQvF2= M2nBUGROW09? M1ru[GlEPTB;MkGwJI5O M3PE[lI{Pzl{NES4
UM-PEL-3 M4PqUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWL+NUDPxE1? MY\EUXNQ M1\hfWlEPTB;MUiwJI5O NVrGdXdiOjN5OUK0OFg>
BC1 MVLGeY5kfGmxbjDhd5NigQ>? NXS1TnJ4PTByIH7N MkT2SG1UVw>? NUGzNIE4cW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> NFHXSnAzOzd7MkS0PC=>
BC3 M17ofmZ2dmO2aX;uJIF{e2G7 Mnz2OVAxKG6P NFf5UpJFVVOR NYnpOXF5cW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> MnOyNlM4QTJ2NEi=
BC1 M{HLXmZ2dmO2aX;uJIF{e2G7 NHflO4Q5ODBibl2= NFH1XnNFVVOR MYTy[YR2[2W|IHOtUZlkKHC{b4TlbY4hdGW4ZXzz NUfRXGRnOjN5OUK0OFg>
BC3 NEewcXhHfW6ldHnvckBie3OjeR?= MknUPFAxKG6P M2\1T2ROW09? MnH6doVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> M2e0b|I{Pzl{NES4
H929 NGLwR2tHfW6ldHnvckBie3OjeR?= M2PDfp4yKM7:TR?= NUPMeW9UTE2VTx?= NHzXOJRqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MYqyOFM{PTR7OR?=
KMS12PE NXHJXodFTnWwY4Tpc44h[XO|YYm= MXz+NUDPxE1? MmTGSG1UVw>? NWjqSWFXcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M1ezNlI1OzN3NEm5
KMS12BM NYnHco81TnWwY4Tpc44h[XO|YYm= MnL4glEh|ryP MUXEUXNQ NHzOS5JqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MnfRNlQ{OzV2OUm=
KMS18 NVHqTYFnTnWwY4Tpc44h[XO|YYm= NFew[Zp,OSEQvF2= MVTEUXNQ M4S3UIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NXnRdIh2OjR|M{W0PVk>
KMS11 M4XuNGZ2dmO2aX;uJIF{e2G7 M2XVPZ4yKM7:TR?= MWLEUXNQ MljMbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NYPZcnYxOjR|M{W0PVk>
RPMI8226 NVfDVnIxTnWwY4Tpc44h[XO|YYm= MVH+NUDPxE1? NIjxUlNFVVOR NWTT[Hg3cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M1XsVlI1OzN3NEm5
H929 M4XyS2Fxd3C2b4Ppd{Bie3OjeR?= M2rNdp4yKM7:TR?= MknRSG1UVw>? M3XlfYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M1nLSFI1OzN3NEm5
KMS12PE NI\6SYhCeG:ydH;zbZMh[XO|YYm= MmfLglEh|ryP NVfDRWZ3TE2VTx?= M{nkPIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M4HKSlI1OzN3NEm5
KMS12BM NHryRlVCeG:ydH;zbZMh[XO|YYm= M4Pwe54yKM7:TR?= MVnEUXNQ NETxT2hqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MV2yOFM{PTR7OR?=
KMS18 MmXvRZBweHSxc3nzJIF{e2G7 NUD0WmVPhjFizszN MULEUXNQ NITTR4xqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MkWzNlQ{OzV2OUm=
KMS11 Mm\2RZBweHSxc3nzJIF{e2G7 MW\+NUDPxE1? MUXEUXNQ M3jZSolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MXyyOFM{PTR7OR?=
RPMI8226 NHfGboFCeG:ydH;zbZMh[XO|YYm= NX7DfYc5hjFizszN MXTEUXNQ NUHOSWxkcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NV\T[|k2OjR|M{W0PVk>
U87MG MUPGeY5kfGmxbjDhd5NigQ>? NIDSfHh,OTBizszN NGKx[|FFVVOR NGjOZnFz\WS3Y3XzJHU5P02JIHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMT6wOUDPxE1? NWPrU3ZlOjR2OU[zPFE>
A172 M3iwcGZ2dmO2aX;uJIF{e2G7 MX;+NVAh|ryP MVzEUXNQ NVjIcmJRemWmdXPld{Bk\WyudXzhdkBCXFBid3n0bEBKSzVyIH;mJFEvOjhizszN MVKyOFQ6PjN6MR?=
SW1783 NVPXU4VkTnWwY4Tpc44h[XO|YYm= MlztglExKM7:TR?= NX3NZVQxTE2VTx?= NVPnfJd{emWmdXPld{Bk\WyudXzhdkBCXFBid3n0bEBKSzVyIH;mJFIvPjhizszN NHvrWXAzPDR7NkO4NS=>
U87MG MlLQSpVv[3Srb36gZZN{[Xl? Mn3wglExKM7:TR?= NX[4dJJ{TE2VTx?= Mn34bY5kemWjc3XzJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5idHjlJGcyN1NidILhcpNqfGmxbh?= M3H3e|I1PDl4M{ix
RAW267.4 NFHBTYNHfW6ldHnvckBie3OjeR?= NWXj[mxGOSEQvF2= NIjZXoZFVVOR NVfKXINLemWmdXPld{BKVC14IIDyc4R2[3Srb36gbY5lfWOnZDDifUBNWFN? MVyyOFg2QTByOB?=
RAW267.4 NXTwepRYTnWwY4Tpc44h[XO|YYm= MV6xJO69VQ>? MYjEUXNQ MWXy[YR2[2W|IITo[UBie3OxY3nheIlwdiCkZYT3[YVvKEKURESgZY5lKGGlZYT5cIF1\WRicE[1 MkjxNlQ5PTlyMEi=
Me007 NHGwfJBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MmPmglExOCEQvF2= NX;BVmM{TE2VTx?= NVXFb5BFcW6qaXLpeJMhfGinIHfyc5d1cA>? NELue3UzPDlyNkGzOy=>
SK-Mel-28 NWjkNlc2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NVnxeZJ5hjFyMDFOwG0> MULEUXNQ MWHpcohq[mm2czD0bIUh\3Kxd4To NW\QVpZqOjR7ME[xN|c>
Mel-RMU NIr6VVZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M2WybJ4yODBizszN MV7EUXNQ M3;UbYlvcGmkaYTzJJRp\SCpcn;3eIg> NUexZmZpOjR7ME[xN|c>
Mel-JD MlfiS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NV73SVlVhjFyMDFOwG0> M{TZ[GROW09? MnPYbY5pcWKrdIOgeIhmKGe{b4f0bC=> MnXoNlQ6ODZzM{e=
Mel-RM NGrxS2lIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NIXReJJ,OTByIN88US=> M2i2emROW09? M2\3VYlvcGmkaYTzJJRp\SCpcn;3eIg> NG\OdJAzPDlyNkGzOy=>
Me007 M{TkdmFxd3C2b4Ppd{Bie3OjeR?= MmnxglExOCEQvF2= NXnXb2VTTE2VTx?= M4fDfIlv\HWlZYOgZZBweHSxc3nz NHTsVnczPDlyNkGzOy=>
SK-Mel-28 MkfCRZBweHSxc3nzJIF{e2G7 M{XQfp4yODBizszN MnT2SG1UVw>? M4jwUIlv\HWlZYOgZZBweHSxc3nz MWiyOFkxPjF|Nx?=
Mel-RMU MlLDRZBweHSxc3nzJIF{e2G7 NEW4UZp,OTByIN88US=> NVnkWG83TE2VTx?= M2LNNolv\HWlZYOgZZBweHSxc3nz NW[3e5I{OjR7ME[xN|c>
Mel-JD NWDDN5IzSXCxcITvd4l{KGG|c3H5 M{HNbJ4yODBizszN NXfme3o3TE2VTx?= MY\pcoR2[2W|IHHwc5B1d3Orcx?= MkPBNlQ6ODZzM{e=
Mel-RM NEP2VFRCeG:ydH;zbZMh[XO|YYm= MkDOglExOCEQvF2= NGey[YxFVVOR NV3tb3gzcW6mdXPld{BieG:ydH;zbZM> MV[yOFkxPjF|Nx?=
Me007 NV\KUpZ4TnWwY4Tpc44h[XO|YYm= NH;2RmwyOCEQvF2= MkPkSG1UVw>? MWDpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHL5JJVxemWpdXzheIlwdiCxZjDwNlE> NE\3cXgzPDlyNkGzOy=>
SK-Mel-28 NFLxcZRHfW6ldHnvckBie3OjeR?= MkfpNVAh|ryP MkTQSG1UVw>? MmXEbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDifUB2eHKnZ4XsZZRqd25ib3[gdFIy M3niU|I1QTB4MUO3
Mel-RMU M37TWWZ2dmO2aX;uJIF{e2G7 MYGxNEDPxE1? NVjPfJVHTE2VTx?= Mn3BbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDifUB2eHKnZ4XsZZRqd25ib3[gdFIy MWeyOFkxPjF|Nx?=
Mel-JD MVfGeY5kfGmxbjDhd5NigQ>? NX;HUFB1OTBizszN NYrTNpU3TE2VTx?= Mn3BbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDifUB2eHKnZ4XsZZRqd25ib3[gdFIy M2\ad|I1QTB4MUO3
Mel-RM NH\GWFdHfW6ldHnvckBie3OjeR?= M2nNR|ExKM7:TR?= MUfEUXNQ MYfpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHL5JJVxemWpdXzheIlwdiCxZjDwNlE> M4Ll[VI1QTB4MUO3
Me007 M2\ZUmZ2dmO2aX;uJIF{e2G7 MYixNEDPxE1? M2H1T2ROW09? NX;XcZlvfXC{ZXf1cIF1\XNicILvZZBweHSxdHnjJIFv\CClZXzsJIN6[2ynIHHydoV{fCCpZX7ldy=> Mk\xNlQ6ODZzM{e=
SK-Mel-28 MmD2SpVv[3Srb36gZZN{[Xl? MXGxNEDPxE1? NYPtVXBpTE2VTx?= NECwRpZ2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz MmXzNlQ6ODZzM{e=
Mel-RMU NFzFcmtHfW6ldHnvckBie3OjeR?= NIrpSXAyOCEQvF2= M{T6[GROW09? MleweZBz\We3bHH0[ZMheHKxYYDvdJRwfGmlIHHu[EBk\WyuIHP5Z4xmKGG{cnXzeEBo\W6ncx?= NWjJemJpOjR7ME[xN|c>
Mel-JD NFnSXGVHfW6ldHnvckBie3OjeR?= M{\D[lExKM7:TR?= NYnjSnJKTE2VTx?= NIrYPHF2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz NVjtRYJmOjR7ME[xN|c>
Mel-RM NU[1WZZ1TnWwY4Tpc44h[XO|YYm= MkDpNVAh|ryP NGLVdnZFVVOR NIXEd4p2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz NYDEeFFnOjR7ME[xN|c>

... Click to View More Cell Line Experimental Data

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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • Animal Models: NOD-SCID mice injected intravenously with MV4;11 cells, and C57BL/6 mice injected intravenously with MLL-AF9 cells
  • Formulation: Dissolved in normal saline containing 5% (v/v) DMSO and 10% (w/v) Kleptose HPB
  • 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

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    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / 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 MSDS / 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.

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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