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 9 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 NGTEdmxkgXSxdH;4bYNqfHliYYPzZZk> M{TTZp4yODBizszN MmKxSG1UVw>? M4W4UWlEPTB;Mk[gcm0> M2fBe|IyQTZ2M{Sw
RS4;11 NEDWXmpkgXSxdH;4bYNqfHliYYPzZZk> NGLZS5J,OTByIN88US=> Mo\TSG1UVw>? M1X3WmlEPTB;MUmyJI5O NFLrelAzOTl4NEO0NC=>
MOLM13 NFfJN3FkgXSxdH;4bYNqfHliYYPzZZk> MUf+NVAxKM7:TR?= MYfEUXNQ Mn7BTWM2OD1zMkCgcm0> NVWzbZBZOjF7NkSzOFA>
NOMO1 MX\jfZRwfG:6aXPpeJkh[XO|YYm= MmLLglExOCEQvF2= Mo\TSG1UVw>? NF\EPJRKSzVyPUG1JI5O NInuSJozOTl4NEO0NC=>
HEL Mn\pZ5l1d3SxeHnjbZR6KGG|c3H5 M3zmc54yODBizszN NE\vZ4VFVVOR NHHuTHVKSzVyPUGg{txO MkfwNlE6PjR|NEC=
K562 M1rkSIN6fG:2b4jpZ4l1gSCjc4PhfS=> NVvHfWF7hjFyMDFOwG0> M2PDNmROW09? MmL0TWM2OD5zMECg{txO M3HMbFIyQTZ2M{Sw
MEG01 Ml7OZ5l1d3SxeHnjbZR6KGG|c3H5 NX2zfHRlhjFyMDFOwG0> NWrYWppWTE2VTx?= M4rGfGlEPTB;MkWg{txO MYGyNVk3PDN2MB?=
HL60 MmHhZ5l1d3SxeHnjbZR6KGG|c3H5 MXz+NVAxKM7:TR?= MVLEUXNQ MXnJR|UxRTh7MDDuUS=> NHLESYozOTl4NEO0NC=>
MV4;11 NIO4XW5CeG:ydH;zbZMh[XO|YYm= M1PaWp4yODBizszN NIH6[YxFVVOR Ml\kbY5lfWOnczDhdI9xfG:|aYO= M{S3S|IyQTZ2M{Sw
MOLM13 M2PGXmFxd3C2b4Ppd{Bie3OjeR?= MmfPglExOCEQvF2= MWDEUXNQ NF\ESpJqdmS3Y3XzJIFxd3C2b4Ppdy=> MmDwNlE6PjR|NEC=
MV4;11 M1;nc2Z2dmO2aX;uJIF{e2G7 NEfEepJFVVOR NU\GT2h6\GWlcnXhd4V{KHSqZTDy[YNzfWm2bXXueEBw\iCEUlSzM|Qh[W6mIHntdIFqemWmIILlZ5J2cXSvZX70JI9nKEOGS{mgZY5lKFCDRkGgeI8hfGinIITyZY5{[3KrcITpc45idCC|dHHyeEB{cXSn MmTvNlE6PjR|NEC=
PBMC M3nn[WZ2dmO2aX;uJIF{e2G7 NVHv[o42TE2VTx?= NWXvZld{cW6qaXLpeJMhUUxvNjD3bZRpKHCLQ{WwJI9nKDZwNx?= MUiyNlQ{PzFzNR?=
A2 NYTVcJlSTnWwY4Tpc44h[XO|YYm= MUf+NVAh|ryP MWnEUXNQ NFi5cZZz\WGldHn2ZZRmeyCuYYTlcpQhUEmYLUG= MnfxNlMzPTV{MUi=
A72 Ml;1SpVv[3Srb36gZZN{[Xl? NX:3OVBMhjFyIN88US=> MXTEUXNQ MonndoVi[3SrdnH0[ZMhdGG2ZX70JGhKXi1z NWLOe21sOjN{NUWyNVg>
BC1 MlLMS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXf+NUDPxE1? NIm1[Y1FVVOR NGH2VYhKSzVyPUKyNEBvVQ>? MlvyNlM4QTJ2NEi=
BC3 NX3hVFJ[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXf+NUDPxE1? M1mxSGROW09? MUHJR|UxRTR4MDDuUS=> NFftfW0zOzd7MkS0PC=>
BCBL1 NF\4WmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGfrRXN,OSEQvF2= NEL1cIpFVVOR Ml\VTWM2OD1|M{Cgcm0> MYKyN|c6OjR2OB?=
BJAB NV70fpRyT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXn+NUDPxE1? M2HGcGROW09? NVzhOFlGUUN3ME25O|Ahdk1? MonzNlM4QTJ2NEi=
Namalwa MWjHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NG\EeZd,OSEQvF2= M3;xXmROW09? MWrJR|UxRTl5MDDuUS=> NEjSRW8zOzd7MkS0PC=>
Jurkat NFPZT3hIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXj+NUDPxE1? MnznSG1UVw>? MUTJR|UxRTF{MkCgcm0> MUWyN|c6OjR2OB?=
MM1S NWLwO2RET3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXX+NUDPxE1? NXPuUYRRTE2VTx?= MVrJR|UxRTd4MDDuUS=> NFuxT|kzOzd7MkS0PC=>
U266 NUjkVpdNT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmHVglEh|ryP MUjEUXNQ MnTNTWM2OD17NUCgcm0> MnfSNlM4QTJ2NEi=
UM-PEL-1 M{DjWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MmPDglEh|ryP NFzQdW5FVVOR MUHJR|UxRTJzMDDuUS=> Mk\XNlM4QTJ2NEi=
UM-PEL-3 MoThS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHmyXVV,OSEQvF2= MYLEUXNQ MVPJR|UxRTF6MDDuUS=> NXHnWJhqOjN5OUK0OFg>
BC1 MV3GeY5kfGmxbjDhd5NigQ>? MoDaOVAxKG6P NWXINWo5TE2VTx?= M32zdYlv\HWlZYOgZ4VtdC2leXPs[UBienKnc4S= NHLMcIozOzd7MkS0PC=>
BC3 NVPJ[ZZrTnWwY4Tpc44h[XO|YYm= M2rZTFUxOCCwTR?= MVnEUXNQ NVrpfZFjcW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> M{f0TVI{Pzl{NES4
BC1 NG\LU5RHfW6ldHnvckBie3OjeR?= M2fXRlgxOCCwTR?= MmW4SG1UVw>? MX\y[YR2[2W|IHOtUZlkKHC{b4TlbY4hdGW4ZXzz NUXCbIVtOjN5OUK0OFg>
BC3 MVzGeY5kfGmxbjDhd5NigQ>? MYq4NFAhdk1? M3W0ZmROW09? MkHadoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> NHrXZ5czOzd7MkS0PC=>
H929 MX3GeY5kfGmxbjDhd5NigQ>? NH;yR|h,OSEQvF2= NIjhZ|lFVVOR MoDqbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= Mnv0NlQ{OzV2OUm=
KMS12PE NX\GcHVtTnWwY4Tpc44h[XO|YYm= NITkbpR,OSEQvF2= M4D2WGROW09? NGfjXm5qdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NITJUIYzPDN|NUS5PS=>
KMS12BM NHTpVXVHfW6ldHnvckBie3OjeR?= NXXMfYd[hjFizszN NUXQVmJ6TE2VTx?= Moj5bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MVqyOFM{PTR7OR?=
KMS18 Mkj4SpVv[3Srb36gZZN{[Xl? MX3+NUDPxE1? MnfsSG1UVw>? MoXlbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NFLlXlAzPDN|NUS5PS=>
KMS11 NXqw[lJjTnWwY4Tpc44h[XO|YYm= MlHGglEh|ryP NGD6dZNFVVOR MoHvbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MnrENlQ{OzV2OUm=
RPMI8226 MmnsSpVv[3Srb36gZZN{[Xl? MmD2glEh|ryP MX\EUXNQ M{\UfYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NXzveYhZOjR|M{W0PVk>
H929 M{XXSmFxd3C2b4Ppd{Bie3OjeR?= M2rHUp4yKM7:TR?= NXrEdmU{TE2VTx?= MnP4bY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M1zRS|I1OzN3NEm5
KMS12PE MkC3RZBweHSxc3nzJIF{e2G7 MWL+NUDPxE1? NX3UO4VtTE2VTx?= NFn2To5qdmS3Y3XzJINmdGxiYYDvdJRwe2m| NFPZfFEzPDN|NUS5PS=>
KMS12BM MWPBdI9xfG:|aYOgZZN{[Xl? NGjoco1,OSEQvF2= NF65PGRFVVOR NV25VWtkcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= M2fkfVI1OzN3NEm5
KMS18 M33iZWFxd3C2b4Ppd{Bie3OjeR?= NXP5enNphjFizszN NFOzWpdFVVOR MmixbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NXPCd2toOjR|M{W0PVk>
KMS11 MmLaRZBweHSxc3nzJIF{e2G7 NF7qNlN,OSEQvF2= M3uzcGROW09? MXzpcoR2[2W|IHPlcIwh[XCxcITvd4l{ M4LIdVI1OzN3NEm5
RPMI8226 NGL3cWhCeG:ydH;zbZMh[XO|YYm= MmO4glEh|ryP M3W1WmROW09? MnnlbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MUCyOFM{PTR7OR?=
U87MG NHzBdm9HfW6ldHnvckBie3OjeR?= Mnn2glExKM7:TR?= MXLEUXNQ MYfy[YR2[2W|IGW4O21IKGOnbHz1cIFzKEGWUDD3bZRpKEmFNUCgc4YhOS5yNTFOwG0> NV:2OGhJOjR2OU[zPFE>
A172 NWraZ21tTnWwY4Tpc44h[XO|YYm= MV7+NVAh|ryP NXvtUpB2TE2VTx?= NVXLcmNEemWmdXPld{Bk\WyudXzhdkBCXFBid3n0bEBKSzVyIH;mJFEvOjhizszN Ml7oNlQ1QTZ|OEG=
SW1783 NHnYdGxHfW6ldHnvckBie3OjeR?= MXj+NVAh|ryP MXnEUXNQ NEXqOJJz\WS3Y3XzJINmdGy3bHHyJGFVWCC5aYToJGlEPTBib3[gNk43QCEQvF2= NGP0WVczPDR7NkO4NS=>
U87MG MWjGeY5kfGmxbjDhd5NigQ>? Mni3glExKM7:TR?= NIjIVoVFVVOR MYHpcoNz\WG|ZYOgdJJweG:{dHnvckBw\iClZXzsd{BqdiC2aHWgS|EwWyC2cnHud4l1cW:w M{\3OlI1PDl4M{ix
RAW267.4 MnHuSpVv[3Srb36gZZN{[Xl? MXmxJO69VQ>? MlLXSG1UVw>? M3L1UJJm\HWlZYOgTWwuPiCycn;keYN1cW:wIHnu[JVk\WRiYomgUHBU NUXOVIVvOjR6NUmwNFg>
RAW267.4 MnjtSpVv[3Srb36gZZN{[Xl? NWfwOXNbOSEQvF2= NVnqS4NiTE2VTx?= MlXIdoVlfWOnczD0bIUh[XO|b3PpZZRqd25iYnX0e4VmdiCEUlS0JIFv\CCjY3X0fYxifGWmIIC2OS=> NGDEXnczPDh3OUCwPC=>
Me007 MnXJS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXLZ[YtMhjFyMDFOwG0> M{DhTGROW09? MX;pcohq[mm2czD0bIUh\3Kxd4To M{XONFI1QTB4MUO3
SK-Mel-28 NYDMXVhpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NYj6VVIzhjFyMDFOwG0> M1PrV2ROW09? MmLVbY5pcWKrdIOgeIhmKGe{b4f0bC=> MonaNlQ6ODZzM{e=
Mel-RMU M4j5XGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUPIOXl3hjFyMDFOwG0> NHTxTolFVVOR NYrjXY5jcW6qaXLpeJMhfGinIHfyc5d1cA>? M1;XO|I1QTB4MUO3
Mel-JD M4i3W2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NFXGfZN,OTByIN88US=> Mn7MSG1UVw>? M3:yPYlvcGmkaYTzJJRp\SCpcn;3eIg> MnfRNlQ6ODZzM{e=
Mel-RM M3m0UGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWj+NVAxKM7:TR?= M4\C[GROW09? NGr4XI5qdmirYnn0d{B1cGViZ4Lve5Rp NXzlXZR7OjR7ME[xN|c>
Me007 M1ewWGFxd3C2b4Ppd{Bie3OjeR?= MnnOglExOCEQvF2= NGSxRohFVVOR MkXMbY5lfWOnczDhdI9xfG:|aYO= MnTyNlQ6ODZzM{e=
SK-Mel-28 M2HuUWFxd3C2b4Ppd{Bie3OjeR?= NHK1UYx,OTByIN88US=> MmrQSG1UVw>? M33lU4lv\HWlZYOgZZBweHSxc3nz NHrPZYEzPDlyNkGzOy=>
Mel-RMU NWrke5hPSXCxcITvd4l{KGG|c3H5 NV;ocI1ihjFyMDFOwG0> MXLEUXNQ MnTLbY5lfWOnczDhdI9xfG:|aYO= NVm3cnZ3OjR7ME[xN|c>
Mel-JD MUjBdI9xfG:|aYOgZZN{[Xl? NWjtOoNrhjFyMDFOwG0> NVnVOYxjTE2VTx?= NHfEW5NqdmS3Y3XzJIFxd3C2b4Ppdy=> NIq4PWEzPDlyNkGzOy=>
Mel-RM M{DhSmFxd3C2b4Ppd{Bie3OjeR?= NV\z[2Z5hjFyMDFOwG0> MYXEUXNQ NEHiUVhqdmS3Y3XzJIFxd3C2b4Ppdy=> MnXiNlQ6ODZzM{e=
Me007 NIH2NlhHfW6ldHnvckBie3OjeR?= NIjRUm8yOCEQvF2= NWnHdVFUTE2VTx?= NYS2b|RDcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBjgSC3cILl[5Vt[XSrb36gc4YheDJz MWSyOFkxPjF|Nx?=
SK-Mel-28 NHXrdpZHfW6ldHnvckBie3OjeR?= MmrWNVAh|ryP NIX5UYdFVVOR NIPnNVFqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF? NXjORVNrOjR7ME[xN|c>
Mel-RMU NGTZRpJHfW6ldHnvckBie3OjeR?= MV2xNEDPxE1? M{HFfmROW09? NYLiXYF{cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBjgSC3cILl[5Vt[XSrb36gc4YheDJz NXXJUHRFOjR7ME[xN|c>
Mel-JD M4D6eWZ2dmO2aX;uJIF{e2G7 MmTGNVAh|ryP MWPEUXNQ M4TkcYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZpkhfXC{ZXf1cIF1cW:wIH;mJJAzOQ>? NX;reWR7OjR7ME[xN|c>
Mel-RM NWX2PYh7TnWwY4Tpc44h[XO|YYm= NXu4UJVDOTBizszN MlHsSG1UVw>? NXG4[pl[cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBjgSC3cILl[5Vt[XSrb36gc4YheDJz NFPOUIszPDlyNkGzOy=>
Me007 MnLGSpVv[3Srb36gZZN{[Xl? MUexNEDPxE1? NIqzXWdFVVOR MoDReZBz\We3bHH0[ZMheHKxYYDvdJRwfGmlIHHu[EBk\WyuIHP5Z4xmKGG{cnXzeEBo\W6ncx?= MYWyOFkxPjF|Nx?=
SK-Mel-28 M4fWRWZ2dmO2aX;uJIF{e2G7 MnntNVAh|ryP NVXtdXZoTE2VTx?= NX;tSpZPfXC{ZXf1cIF1\XNicILvZZBweHSxdHnjJIFv\CClZXzsJIN6[2ynIHHydoV{fCCpZX7ldy=> NX\wOmNOOjR7ME[xN|c>
Mel-RMU NF;Y[FZHfW6ldHnvckBie3OjeR?= MlnvNVAh|ryP NXS4dI5GTE2VTx?= MWH1dJJm\3WuYYTld{Bxem:jcH;weI91cWNiYX7kJINmdGxiY4njcIUh[XK{ZYP0JIdmdmW| NX3oXXJ1OjR7ME[xN|c>
Mel-JD MkHJSpVv[3Srb36gZZN{[Xl? NVWzOGZZOTBizszN M3vUZmROW09? MWX1dJJm\3WuYYTld{Bxem:jcH;weI91cWNiYX7kJINmdGxiY4njcIUh[XK{ZYP0JIdmdmW| NYC4VnRIOjR7ME[xN|c>
Mel-RM NYXUcVlOTnWwY4Tpc44h[XO|YYm= NVLzWplqOTBizszN NWi1NpZwTE2VTx?= NFL3SmF2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz NWDnTmZWOjR7ME[xN|c>

... 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

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 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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