I-BET151 (GSK1210151A)

For research use only. Not for use in humans.

Catalog No.S2780

20 publications

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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Selleck's I-BET151 (GSK1210151A) has been cited by 20 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 MV\jfZRwfG:6aXPpeJkh[XO|YYm= NYjIVlB4hjFyMDFOwG0> MWrEUXNQ MYrJR|UxRTJ4IH7N NULCbHV6OjF7NkSzOFA>
RS4;11 MlnQZ5l1d3SxeHnjbZR6KGG|c3H5 NVXrXJF1hjFyMDFOwG0> MUTEUXNQ Mn3mTWM2OD1zOUKgcm0> M{\FWlIyQTZ2M{Sw
MOLM13 MVPjfZRwfG:6aXPpeJkh[XO|YYm= MV3+NVAxKM7:TR?= M3TEUWROW09? NHXFdnNKSzVyPUGyNEBvVQ>? Ml3GNlE6PjR|NEC=
NOMO1 M4DibIN6fG:2b4jpZ4l1gSCjc4PhfS=> NFS0OZd,OTByIN88US=> NGrlV5hFVVOR M1P1V2lEPTB;MUWgcm0> MXKyNVk3PDN2MB?=
HEL NUPSV3p6[3m2b4TvfIlkcXS7IHHzd4F6 NHvvepZ,OTByIN88US=> NVXROmlsTE2VTx?= M3\2XGlEPTB;MTFOwG0> NE\FUoEzOTl4NEO0NC=>
K562 NXrIToVN[3m2b4TvfIlkcXS7IHHzd4F6 MorTglExOCEQvF2= MlvOSG1UVw>? M2nwVGlEPTB-MUCwJO69VQ>? NGq5O|IzOTl4NEO0NC=>
MEG01 MYHjfZRwfG:6aXPpeJkh[XO|YYm= MmHWglExOCEQvF2= M3vuSmROW09? MULJR|UxRTJ3IN88US=> NXKwbXhuOjF7NkSzOFA>
HL60 M3m0[IN6fG:2b4jpZ4l1gSCjc4PhfS=> NFrjb2l,OTByIN88US=> MonBSG1UVw>? MnrFTWM2OD16OUCgcm0> M3;Ne|IyQTZ2M{Sw
MV4;11 NV7mTWdGSXCxcITvd4l{KGG|c3H5 NH7SV4R,OTByIN88US=> MVrEUXNQ M1LGXYlv\HWlZYOgZZBweHSxc3nz M{DsdFIyQTZ2M{Sw
MOLM13 NHLDR3lCeG:ydH;zbZMh[XO|YYm= MlL4glExOCEQvF2= NXvnXpQzTE2VTx?= M1rHWYlv\HWlZYOgZZBweHSxc3nz MYCyNVk3PDN2MB?=
MV4;11 NFPUTYlHfW6ldHnvckBie3OjeR?= M3P5bmROW09? NUL2d3Q1\GWlcnXhd4V{KHSqZTDy[YNzfWm2bXXueEBw\iCEUlSzM|Qh[W6mIHntdIFqemWmIILlZ5J2cXSvZX70JI9nKEOGS{mgZY5lKFCDRkGgeI8hfGinIITyZY5{[3KrcITpc45idCC|dHHyeEB{cXSn MkPpNlE6PjR|NEC=
PBMC Moe4SpVv[3Srb36gZZN{[Xl? MV7EUXNQ MoPlbY5pcWKrdIOgTWwuPiC5aYToJJBKSzVyIH;mJFYvPw>? NVLXe5dHOjJ2M{exNVU>
A2 NXTkd2RMTnWwY4Tpc44h[XO|YYm= NY\acopuhjFyIN88US=> NXvaeGpsTE2VTx?= NV\RNYZqemWjY4TpeoF1\XNibHH0[Y51KEiLVj2x MXuyN|I2PTJzOB?=
A72 NG\RcnRHfW6ldHnvckBie3OjeR?= MUX+NVAh|ryP NFHxem5FVVOR M{DHdZJm[WO2aY\heIV{KGyjdHXueEBJUVZvMR?= Mnv5NlMzPTV{MUi=
BC1 M4TwPWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXLscmFUhjFizszN NHi2TopFVVOR MkTZTWM2OD1{MkCgcm0> MVSyN|c6OjR2OB?=
BC3 MkDOS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUn+NUDPxE1? MoDnSG1UVw>? MV\JR|UxRTR4MDDuUS=> NXPSc2lpOjN5OUK0OFg>
BCBL1 MnyxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NWnwb2VGhjFizszN NVzrV3FTTE2VTx?= NF3YVppKSzVyPUOzNEBvVQ>? NGjUWIYzOzd7MkS0PC=>
BJAB M4\Uc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mo\QglEh|ryP M{H4PWROW09? NX6yXY9SUUN3ME25O|Ahdk1? NW\DSXNlOjN5OUK0OFg>
Namalwa NFXVUJFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGHuO5J,OSEQvF2= MWTEUXNQ M{DYXWlEPTB;OUewJI5O NE\2cJYzOzd7MkS0PC=>
Jurkat NXn4[4JvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEfTU4N,OSEQvF2= NVzGNnRxTE2VTx?= Ml\ETWM2OD1zMkKwJI5O NHGzOpgzOzd7MkS0PC=>
MM1S NVniTGhRT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWr+NUDPxE1? MlG2SG1UVw>? NFW5emtKSzVyPUe2NEBvVQ>? NX;uUW1oOjN5OUK0OFg>
U266 M1X1fmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mmi4glEh|ryP NHLTV4JFVVOR NGnrXmtKSzVyPUm1NEBvVQ>? NEDaPIIzOzd7MkS0PC=>
UM-PEL-1 MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NWrpeFFPhjFizszN M1q0cGROW09? NIPvfphKSzVyPUKxNEBvVQ>? M2TDRlI{Pzl{NES4
UM-PEL-3 M4rZNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml\VglEh|ryP NHThSVRFVVOR NITFU2xKSzVyPUG4NEBvVQ>? MVmyN|c6OjR2OB?=
BC1 Ml\rSpVv[3Srb36gZZN{[Xl? M3;GWVUxOCCwTR?= M4PXVGROW09? M{S1XIlv\HWlZYOgZ4VtdC2leXPs[UBienKnc4S= MXOyN|c6OjR2OB?=
BC3 NGe0eGJHfW6ldHnvckBie3OjeR?= MnWyOVAxKG6P M4fXN2ROW09? NUTucJN7cW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> NXTENIs{OjN5OUK0OFg>
BC1 NYHERWV{TnWwY4Tpc44h[XO|YYm= M3\PNlgxOCCwTR?= MXvEUXNQ NXX4cXhEemWmdXPld{BkNU27YzDwdo91\WmwIHzleoVtew>? NUXiXI42OjN5OUK0OFg>
BC3 NHXGdm5HfW6ldHnvckBie3OjeR?= MmC1PFAxKG6P NU\5bJVRTE2VTx?= M1XuVpJm\HWlZYOgZ{1OgWNicILveIVqdiCuZY\lcJM> NX7FfXAzOjN5OUK0OFg>
H929 MUfGeY5kfGmxbjDhd5NigQ>? NWnnenNLhjFizszN M1HVWWROW09? MnvzbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NIPpWpIzPDN|NUS5PS=>
KMS12PE NYfuXoptTnWwY4Tpc44h[XO|YYm= M4rXc54yKM7:TR?= NUnt[pUzTE2VTx?= NGnXcYVqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MmnhNlQ{OzV2OUm=
KMS12BM MkDhSpVv[3Srb36gZZN{[Xl? NH[yVll,OSEQvF2= NFXX[IpFVVOR MW\pcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 M{HaVlI1OzN3NEm5
KMS18 NX\3SoFGTnWwY4Tpc44h[XO|YYm= NWWyTGJFhjFizszN MWLEUXNQ Ml7obY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M4C3cFI1OzN3NEm5
KMS11 NYjmRnNqTnWwY4Tpc44h[XO|YYm= MmK1glEh|ryP NXizbmZ4TE2VTx?= NET3NFNqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MlW4NlQ{OzV2OUm=
RPMI8226 M1;uU2Z2dmO2aX;uJIF{e2G7 NF\aNJV,OSEQvF2= NWL2V4x3TE2VTx?= MV7pcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MUSyOFM{PTR7OR?=
H929 Mn34RZBweHSxc3nzJIF{e2G7 Mm\SglEh|ryP M3rBb2ROW09? MnvvbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MUOyOFM{PTR7OR?=
KMS12PE NF21RoZCeG:ydH;zbZMh[XO|YYm= M3;rbp4yKM7:TR?= MYPEUXNQ MWfpcoR2[2W|IHPlcIwh[XCxcITvd4l{ MWKyOFM{PTR7OR?=
KMS12BM MkfsRZBweHSxc3nzJIF{e2G7 NEK5[Y1,OSEQvF2= MVXEUXNQ NVPvV2docW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MoXTNlQ{OzV2OUm=
KMS18 NVvYd3lkSXCxcITvd4l{KGG|c3H5 MXT+NUDPxE1? NHfTTHBFVVOR NGPhR|VqdmS3Y3XzJINmdGxiYYDvdJRwe2m| M4O0NlI1OzN3NEm5
KMS11 NWfDSFNUSXCxcITvd4l{KGG|c3H5 NV7iNo9ihjFizszN NX\OTot[TE2VTx?= NVjQVIVzcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MmeyNlQ{OzV2OUm=
RPMI8226 MXvBdI9xfG:|aYOgZZN{[Xl? MVn+NUDPxE1? Mo[3SG1UVw>? MmrzbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NWjLemNSOjR|M{W0PVk>
U87MG MYDGeY5kfGmxbjDhd5NigQ>? MXn+NVAh|ryP Mny5SG1UVw>? NHXk[HFz\WS3Y3XzJHU5P02JIHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMT6wOUDPxE1? MWiyOFQ6PjN6MR?=
A172 MojISpVv[3Srb36gZZN{[Xl? NYfpV|dQhjFyIN88US=> M2HMW2ROW09? NI[yVlVz\WS3Y3XzJINmdGy3bHHyJGFVWCC5aYToJGlEPTBib3[gNU4zQCEQvF2= M{jqTlI1PDl4M{ix
SW1783 NHP1fWtHfW6ldHnvckBie3OjeR?= NG\KU4J,OTBizszN NF;ac45FVVOR MoTtdoVlfWOnczDj[YxtfWyjcjDBWHAhf2m2aDDJR|UxKG:oIEKuOlgh|ryP MnvLNlQ1QTZ|OEG=
U87MG NXLBSoRlTnWwY4Tpc44h[XO|YYm= MmO3glExKM7:TR?= MU\EUXNQ NXjzUVg1cW6lcnXhd4V{KHC{b4DvdpRqd25ib3[gZ4VtdHNiaX6geIhmKEdzL2OgeJJidnOrdHnvci=> NIi2fJEzPDR7NkO4NS=>
RAW267.4 MmLTSpVv[3Srb36gZZN{[Xl? NYfDU5dQOSEQvF2= NILrPYVFVVOR MYfy[YR2[2W|IFnMMVYheHKxZIXjeIlwdiCrbnT1Z4VlKGK7IFzQVy=> MV:yOFg2QTByOB?=
RAW267.4 MmiwSpVv[3Srb36gZZN{[Xl? M4LtfFEh|ryP NWLEelljTE2VTx?= NXSzNplOemWmdXPld{B1cGViYYPzc4Nq[XSrb36gZoV1f2WnbjDCVmQ1KGGwZDDhZ4V1gWyjdHXkJJA3PQ>? NXy1S|VpOjR6NUmwNFg>
Me007 NEezfJJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGjobVV,OTByIN88US=> MUHEUXNQ MmrPbY5pcWKrdIOgeIhmKGe{b4f0bC=> MkPvNlQ6ODZzM{e=
SK-Mel-28 NXLVfZVxT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn73glExOCEQvF2= MULEUXNQ M3PRVIlvcGmkaYTzJJRp\SCpcn;3eIg> MoS0NlQ6ODZzM{e=
Mel-RMU M{HJXWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1TQUZ4yODBizszN MmXqSG1UVw>? MX3pcohq[mm2czD0bIUh\3Kxd4To MoHONlQ6ODZzM{e=
Mel-JD NVjvOHl[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MW\+NVAxKM7:TR?= MmXMSG1UVw>? M2PSU4lvcGmkaYTzJJRp\SCpcn;3eIg> NInHOpAzPDlyNkGzOy=>
Mel-RM MnvzS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1zGTp4yODBizszN MoTqSG1UVw>? M1nJVIlvcGmkaYTzJJRp\SCpcn;3eIg> M{exWFI1QTB4MUO3
Me007 NHvSTpFCeG:ydH;zbZMh[XO|YYm= NUTnfGh6hjFyMDFOwG0> MULEUXNQ MUDpcoR2[2W|IHHwc5B1d3Orcx?= MYCyOFkxPjF|Nx?=
SK-Mel-28 NHXKeGVCeG:ydH;zbZMh[XO|YYm= MYD+NVAxKM7:TR?= MmDsSG1UVw>? MlfwbY5lfWOnczDhdI9xfG:|aYO= MlXpNlQ6ODZzM{e=
Mel-RMU M2TjVWFxd3C2b4Ppd{Bie3OjeR?= NVv0dmhlhjFyMDFOwG0> MXnEUXNQ MUDpcoR2[2W|IHHwc5B1d3Orcx?= NWHoNJM1OjR7ME[xN|c>
Mel-JD MlfaRZBweHSxc3nzJIF{e2G7 MV3+NVAxKM7:TR?= MXHEUXNQ NHvk[W9qdmS3Y3XzJIFxd3C2b4Ppdy=> MnvKNlQ6ODZzM{e=
Mel-RM MWrBdI9xfG:|aYOgZZN{[Xl? M1P4VJ4yODBizszN MkTYSG1UVw>? NYHSPVRFcW6mdXPld{BieG:ydH;zbZM> NVrGPIM6OjR7ME[xN|c>
Me007 MX3GeY5kfGmxbjDhd5NigQ>? NWnsXGdxOTBizszN NYnSZodmTE2VTx?= NGnEXZZqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF? M4XPflI1QTB4MUO3
SK-Mel-28 NITGR|dHfW6ldHnvckBie3OjeR?= M1fIbFExKM7:TR?= M{DR[WROW09? NXrYRVVbcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBjgSC3cILl[5Vt[XSrb36gc4YheDJz NFHzUmwzPDlyNkGzOy=>
Mel-RMU NWf1b29lTnWwY4Tpc44h[XO|YYm= NIjIbo8yOCEQvF2= NHjpU2JFVVOR MojEbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDifUB2eHKnZ4XsZZRqd25ib3[gdFIy NYjMN2JuOjR7ME[xN|c>
Mel-JD MW\GeY5kfGmxbjDhd5NigQ>? Mly0NVAh|ryP NFTTN5JFVVOR NIfQ[YFqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF? NGPRW|EzPDlyNkGzOy=>
Mel-RM NIro[ZdHfW6ldHnvckBie3OjeR?= NX2yVpBKOTBizszN NV;oW5BTTE2VTx?= M3\mOolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZpkhfXC{ZXf1cIF1cW:wIH;mJJAzOQ>? MUCyOFkxPjF|Nx?=
Me007 MnXHSpVv[3Srb36gZZN{[Xl? NHfMdJkyOCEQvF2= NELyempFVVOR M3rKXpVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= NHnyd4UzPDlyNkGzOy=>
SK-Mel-28 MkTNSpVv[3Srb36gZZN{[Xl? MmfQNVAh|ryP M1zKfWROW09? NInneJV2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz NFnZcFEzPDlyNkGzOy=>
Mel-RMU NYnveXhqTnWwY4Tpc44h[XO|YYm= NWjMZ2MxOTBizszN NWnVN3p6TE2VTx?= NI\oV4R2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz NW\FVYRMOjR7ME[xN|c>
Mel-JD M321R2Z2dmO2aX;uJIF{e2G7 NIraRYUyOCEQvF2= Ml3wSG1UVw>? M2jHWZVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= NVLjd3BXOjR7ME[xN|c>
Mel-RM M4TwVWZ2dmO2aX;uJIF{e2G7 M3XxN|ExKM7:TR?= MlTMSG1UVw>? NGj5WWx2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz NIf3NGozPDlyNkGzOy=>

... 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
  • 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
Smiles COC1=C(C=C2N=CC3=C(N(C(C)C4=CC=CC=N4)C(=O)N3)C2=C1)C5=C(C)ON=C5C

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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