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 6 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 NWXWW|dQ[3m2b4TvfIlkcXS7IHHzd4F6 M4Tt[p4yODBizszN MV\EUXNQ NF3hfXdKSzVyPUK2JI5O NWmzVm1oOjF7NkSzOFA>
RS4;11 NGjDUZRkgXSxdH;4bYNqfHliYYPzZZk> NIjDfFN,OTByIN88US=> NYjqXIFjTE2VTx?= NUHDNml4UUN3ME2xPVIhdk1? MnqzNlE6PjR|NEC=
MOLM13 M2ft[4N6fG:2b4jpZ4l1gSCjc4PhfS=> M1PYR54yODBizszN NU\tZWo6TE2VTx?= NGDPe21KSzVyPUGyNEBvVQ>? NUXQbWNsOjF7NkSzOFA>
NOMO1 M36w[IN6fG:2b4jpZ4l1gSCjc4PhfS=> NHzUd4d,OTByIN88US=> M3m1ZWROW09? NV[5OVdPUUN3ME2xOUBvVQ>? MVeyNVk3PDN2MB?=
HEL MmPnZ5l1d3SxeHnjbZR6KGG|c3H5 MmT5glExOCEQvF2= MoeySG1UVw>? MlizTWM2OD1zIN88US=> NUnZUpQ1OjF7NkSzOFA>
K562 MXnjfZRwfG:6aXPpeJkh[XO|YYm= MWD+NVAxKM7:TR?= Mn;FSG1UVw>? MoTDTWM2OD5zMECg{txO NHnTe4EzOTl4NEO0NC=>
MEG01 NH34e|hkgXSxdH;4bYNqfHliYYPzZZk> MkLwglExOCEQvF2= MXrEUXNQ M324ZmlEPTB;MkWg{txO M4rBV|IyQTZ2M{Sw
HL60 NHvNVVNkgXSxdH;4bYNqfHliYYPzZZk> NEPPPJV,OTByIN88US=> NVjYemN1TE2VTx?= MoezTWM2OD16OUCgcm0> Mmm3NlE6PjR|NEC=
MV4;11 MXHBdI9xfG:|aYOgZZN{[Xl? NGfZfWR,OTByIN88US=> MkfOSG1UVw>? M2XoZ4lv\HWlZYOgZZBweHSxc3nz M3PUWVIyQTZ2M{Sw
MOLM13 NX\hclRISXCxcITvd4l{KGG|c3H5 M4GwRp4yODBizszN MlHKSG1UVw>? NF7WeY1qdmS3Y3XzJIFxd3C2b4Ppdy=> M1v1TFIyQTZ2M{Sw
MV4;11 M1uzOGZ2dmO2aX;uJIF{e2G7 MUHEUXNQ MXPk[YNz\WG|ZYOgeIhmKHKnY4L1bZRu\W62IH;mJGJTTDNxNDDhcoQhcW2yYXny[YQhemWlcoXpeI1mdnRib3[gR2RMQSCjbnSgVGFHOSC2bzD0bIUhfHKjboPjdolxfGmxbnHsJJN1[XK2IIPpeIU> MXqyNVk3PDN2MB?=
PBMC M1\MTmZ2dmO2aX;uJIF{e2G7 MVHEUXNQ NYnjc3pDcW6qaXLpeJMhUUxvNjD3bZRpKHCLQ{WwJI9nKDZwNx?= MnTCNlI1OzdzMUW=
A2 MoXhSpVv[3Srb36gZZN{[Xl? NVvuS3QzhjFyIN88US=> MUnEUXNQ NHTQVoNz\WGldHn2ZZRmeyCuYYTlcpQhUEmYLUG= MUOyN|I2PTJzOB?=
A72 MonTSpVv[3Srb36gZZN{[Xl? NH\P[Jh,OTBizszN MnrwSG1UVw>? Mk[xdoVi[3SrdnH0[ZMhdGG2ZX70JGhKXi1z MoC5NlMzPTV{MUi=
BC1 MkDlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4eyep4yKM7:TR?= M2jobmROW09? NEHuOFJKSzVyPUKyNEBvVQ>? M12yXFI{Pzl{NES4
BC3 NYXYbXNzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NEfi[Gp,OSEQvF2= MY\EUXNQ NFrOWYNKSzVyPUS2NEBvVQ>? MX6yN|c6OjR2OB?=
BCBL1 MVLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M{Thcp4yKM7:TR?= M3PqfWROW09? NU\TepE3UUN3ME2zN|Ahdk1? MUSyN|c6OjR2OB?=
BJAB MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYW3U4R7hjFizszN MkPYSG1UVw>? MmP0TWM2OD17N{Cgcm0> M1PwSVI{Pzl{NES4
Namalwa NEXXVHBIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUD+NUDPxE1? M4K3WmROW09? NFHxS5NKSzVyPUm3NEBvVQ>? M2r1S|I{Pzl{NES4
Jurkat M{jEcGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M3HFcJ4yKM7:TR?= MlTWSG1UVw>? M4PIVGlEPTB;MUKyNEBvVQ>? NYnlcWR{OjN5OUK0OFg>
MM1S M3zmUmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIfQfFV,OSEQvF2= MXrEUXNQ NUXFNYpnUUN3ME23OlAhdk1? M{f2[lI{Pzl{NES4
U266 NWrSO5Z5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGTyNI9,OSEQvF2= MUXEUXNQ MVTJR|UxRTl3MDDuUS=> NWPTZ|lmOjN5OUK0OFg>
UM-PEL-1 MnzxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1PsN54yKM7:TR?= M3jMeGROW09? NYG1ZVdWUUN3ME2yNVAhdk1? NF30c48zOzd7MkS0PC=>
UM-PEL-3 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYfjdZlPhjFizszN Mnn3SG1UVw>? NVKydJV{UUN3ME2xPFAhdk1? NXjaXHluOjN5OUK0OFg>
BC1 NUG3bXdoTnWwY4Tpc44h[XO|YYm= MnnBOVAxKG6P NHLZS4NFVVOR MoHBbY5lfWOnczDj[YxtNWO7Y3zlJIFzemW|dB?= NEjaS3ozOzd7MkS0PC=>
BC3 NVXISIxTTnWwY4Tpc44h[XO|YYm= MXe1NFAhdk1? MV\EUXNQ NXPlemhQcW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> MWiyN|c6OjR2OB?=
BC1 MU\GeY5kfGmxbjDhd5NigQ>? NUPkTnlnQDByIH7N M1;JTGROW09? MmHhdoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> MmP0NlM4QTJ2NEi=
BC3 MUfGeY5kfGmxbjDhd5NigQ>? NVfld3I1QDByIH7N M1fYV2ROW09? NGLsNY1z\WS3Y3XzJIMuVXmlIIDyc5RmcW5ibHX2[Yx{ MlvJNlM4QTJ2NEi=
H929 NVPWcIY2TnWwY4Tpc44h[XO|YYm= M1TNd54yKM7:TR?= MX\EUXNQ NHj4Z|ZqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 MnfoNlQ{OzV2OUm=
KMS12PE MXTGeY5kfGmxbjDhd5NigQ>? MYT+NUDPxE1? MYXEUXNQ NXvKZ3N4cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MkjmNlQ{OzV2OUm=
KMS12BM NWTYRmpLTnWwY4Tpc44h[XO|YYm= MVH+NUDPxE1? NVPlWm1ETE2VTx?= MoTqbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MVSyOFM{PTR7OR?=
KMS18 MX7GeY5kfGmxbjDhd5NigQ>? NEnMbmh,OSEQvF2= M2D5R2ROW09? NYGzT|lMcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M3i5elI1OzN3NEm5
KMS11 NYfHb5ZLTnWwY4Tpc44h[XO|YYm= MoXBglEh|ryP NYXvd3RtTE2VTx?= NHnETIxqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M1zjd|I1OzN3NEm5
RPMI8226 MkX5SpVv[3Srb36gZZN{[Xl? NG\BR49,OSEQvF2= M3\6PGROW09? MUDpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NF7yTXEzPDN|NUS5PS=>
H929 M2m3VWFxd3C2b4Ppd{Bie3OjeR?= Mlz0glEh|ryP NV3WUmo{TE2VTx?= M2fscIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MnjDNlQ{OzV2OUm=
KMS12PE MYDBdI9xfG:|aYOgZZN{[Xl? M{HpZZ4yKM7:TR?= NUXs[ZQ2TE2VTx?= NXHsSFZMcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MX:yOFM{PTR7OR?=
KMS12BM NGm2V2hCeG:ydH;zbZMh[XO|YYm= NHvVPYd,OSEQvF2= M3TUO2ROW09? NXzzNFlLcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= MUCyOFM{PTR7OR?=
KMS18 MXTBdI9xfG:|aYOgZZN{[Xl? NWe2V3FthjFizszN NU\yT4VGTE2VTx?= MWPpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NX\lVJBNOjR|M{W0PVk>
KMS11 NWPWNm9XSXCxcITvd4l{KGG|c3H5 NXXiNoJ6hjFizszN MkP0SG1UVw>? NVe4eXZScW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NYG5PFBGOjR|M{W0PVk>
RPMI8226 MnfrRZBweHSxc3nzJIF{e2G7 M{Trdp4yKM7:TR?= NITFNmdFVVOR NF7qPYlqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NXnGPFFnOjR|M{W0PVk>
U87MG NIPuTnJHfW6ldHnvckBie3OjeR?= Mni1glExKM7:TR?= Mlf2SG1UVw>? MlH1doVlfWOnczDVPFdOTyClZXzseYxieiCDVGCge4l1cCCLQ{WwJI9nKDFwMEWg{txO M4H6blI1PDl4M{ix
A172 MWHGeY5kfGmxbjDhd5NigQ>? NVT2b|l[hjFyIN88US=> NEHHZZBFVVOR MmXFdoVlfWOnczDj[YxtfWyjcjDBWHAhf2m2aDDJR|UxKG:oIEGuNlgh|ryP M2TkeVI1PDl4M{ix
SW1783 NF7Te3VHfW6ldHnvckBie3OjeR?= NYXF[2RHhjFyIN88US=> MUTEUXNQ MmnQdoVlfWOnczDj[YxtfWyjcjDBWHAhf2m2aDDJR|UxKG:oIEKuOlgh|ryP MlrvNlQ1QTZ|OEG=
U87MG MXjGeY5kfGmxbjDhd5NigQ>? MUX+NVAh|ryP MULEUXNQ M{PJfolv[3KnYYPld{Bxem:yb4L0bY9vKG:oIHPlcIx{KGmwIITo[UBIOS:VIITyZY5{cXSrb36= NH;uNXEzPDR7NkO4NS=>
RAW267.4 Mo[xSpVv[3Srb36gZZN{[Xl? MkjhNUDPxE1? M172T2ROW09? NVz1N|lbemWmdXPld{BKVC14IIDyc4R2[3Srb36gbY5lfWOnZDDifUBNWFN? NVLj[W92OjR6NUmwNFg>
RAW267.4 NVnMNXpGTnWwY4Tpc44h[XO|YYm= MoHWNUDPxE1? NGeyS2ZFVVOR NXrmOYtDemWmdXPld{B1cGViYYPzc4Nq[XSrb36gZoV1f2WnbjDCVmQ1KGGwZDDhZ4V1gWyjdHXkJJA3PQ>? MXWyOFg2QTByOB?=
Me007 M3nrN2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M1nPcJ4yODBizszN MV7EUXNQ NF7MPZFqdmirYnn0d{B1cGViZ4Lve5Rp MoXzNlQ6ODZzM{e=
SK-Mel-28 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MoPXglExOCEQvF2= NFi4dpRFVVOR M3;mcIlvcGmkaYTzJJRp\SCpcn;3eIg> MXyyOFkxPjF|Nx?=
Mel-RMU NHPNOGpIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXLSZZF6hjFyMDFOwG0> NUHMT3M{TE2VTx?= NGHoUplqdmirYnn0d{B1cGViZ4Lve5Rp NXHKXYtPOjR7ME[xN|c>
Mel-JD M3[5c2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MUj+NVAxKM7:TR?= NGDLfpNFVVOR NUfCW4RPcW6qaXLpeJMhfGinIHfyc5d1cA>? NFS2VZgzPDlyNkGzOy=>
Mel-RM MVTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXjhW3ZJhjFyMDFOwG0> M{Dje2ROW09? M{Xn[4lvcGmkaYTzJJRp\SCpcn;3eIg> Mn\SNlQ6ODZzM{e=
Me007 NVT5WXZsSXCxcITvd4l{KGG|c3H5 MWL+NVAxKM7:TR?= NVHwWHNLTE2VTx?= NYK0bHBqcW6mdXPld{BieG:ydH;zbZM> NEe2U4szPDlyNkGzOy=>
SK-Mel-28 NGGyWJlCeG:ydH;zbZMh[XO|YYm= M37VNJ4yODBizszN MlXvSG1UVw>? Mn73bY5lfWOnczDhdI9xfG:|aYO= NVP1OINJOjR7ME[xN|c>
Mel-RMU MYrBdI9xfG:|aYOgZZN{[Xl? NHHZe2h,OTByIN88US=> Ml7SSG1UVw>? M4rF[4lv\HWlZYOgZZBweHSxc3nz NV3R[Iw6OjR7ME[xN|c>
Mel-JD MVjBdI9xfG:|aYOgZZN{[Xl? MVz+NVAxKM7:TR?= NFy4SVlFVVOR MoqybY5lfWOnczDhdI9xfG:|aYO= NVrRdXRnOjR7ME[xN|c>
Mel-RM MWPBdI9xfG:|aYOgZZN{[Xl? MWP+NVAxKM7:TR?= MWXEUXNQ MVvpcoR2[2W|IHHwc5B1d3Orcx?= NXvScndXOjR7ME[xN|c>
Me007 NXLLd5FUTnWwY4Tpc44h[XO|YYm= M4ThTFExKM7:TR?= M3vVPWROW09? M4LDUolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZpkhfXC{ZXf1cIF1cW:wIH;mJJAzOQ>? MWmyOFkxPjF|Nx?=
SK-Mel-28 NGTMbXNHfW6ldHnvckBie3OjeR?= NXy5b2dROTBizszN MX7EUXNQ NULEVlI1cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBjgSC3cILl[5Vt[XSrb36gc4YheDJz MWiyOFkxPjF|Nx?=
Mel-RMU MXXGeY5kfGmxbjDhd5NigQ>? NWWxblhNOTBizszN NHq3e|BFVVOR NE\vdXVqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF? Mm\ONlQ6ODZzM{e=
Mel-JD NY\sSIxOTnWwY4Tpc44h[XO|YYm= MYqxNEDPxE1? MVvEUXNQ M2XGTolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZpkhfXC{ZXf1cIF1cW:wIH;mJJAzOQ>? NWq2NW0yOjR7ME[xN|c>
Mel-RM MXPGeY5kfGmxbjDhd5NigQ>? NX\wUpJJOTBizszN Ml7hSG1UVw>? M1\4Uolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZpkhfXC{ZXf1cIF1cW:wIH;mJJAzOQ>? MWmyOFkxPjF|Nx?=
Me007 NULBNlYzTnWwY4Tpc44h[XO|YYm= M3nZOVExKM7:TR?= MmfUSG1UVw>? M2LRd5VxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= Mm\ENlQ6ODZzM{e=
SK-Mel-28 MknaSpVv[3Srb36gZZN{[Xl? MlG1NVAh|ryP M1;qOGROW09? MV\1dJJm\3WuYYTld{Bxem:jcH;weI91cWNiYX7kJINmdGxiY4njcIUh[XK{ZYP0JIdmdmW| M3vOSlI1QTB4MUO3
Mel-RMU NXjJUGJnTnWwY4Tpc44h[XO|YYm= MlnONVAh|ryP NGnrfHlFVVOR NUHqSlBEfXC{ZXf1cIF1\XNicILvZZBweHSxdHnjJIFv\CClZXzsJIN6[2ynIHHydoV{fCCpZX7ldy=> NXvlNnBJOjR7ME[xN|c>
Mel-JD NGH2U2hHfW6ldHnvckBie3OjeR?= NH:yNmcyOCEQvF2= NI\3UZRFVVOR NH\ZVpV2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz MVKyOFkxPjF|Nx?=
Mel-RM MnHmSpVv[3Srb36gZZN{[Xl? MonENVAh|ryP MVvEUXNQ NWCzd29TfXC{ZXf1cIF1\XNicILvZZBweHSxdHnjJIFv\CClZXzsJIN6[2ynIHHydoV{fCCpZX7ldy=> MoDvNlQ6ODZzM{e=

... 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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Molarity Calculator

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

Mass (g) = Concentration (mol/L) × Volume (L) × 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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