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 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 NIrtdmhkgXSxdH;4bYNqfHliYYPzZZk> Ml;OglExOCEQvF2= Ml;GSG1UVw>? MoDWTWM2OD1{NjDuUS=> MYeyNVk3PDN2MB?=
RS4;11 NVrsfnRr[3m2b4TvfIlkcXS7IHHzd4F6 Ml;vglExOCEQvF2= MmrISG1UVw>? NYDGPGl3UUN3ME2xPVIhdk1? MkLQNlE6PjR|NEC=
MOLM13 MWPjfZRwfG:6aXPpeJkh[XO|YYm= M{D6Wp4yODBizszN MkDPSG1UVw>? MWLJR|UxRTF{MDDuUS=> MUmyNVk3PDN2MB?=
NOMO1 NFLMVJBkgXSxdH;4bYNqfHliYYPzZZk> MmTmglExOCEQvF2= M{W0c2ROW09? NV;CRoo2UUN3ME2xOUBvVQ>? NVzlXol3OjF7NkSzOFA>
HEL MkfKZ5l1d3SxeHnjbZR6KGG|c3H5 M1jX[J4yODBizszN NF:3cZNFVVOR MmW3TWM2OD1zIN88US=> M2Dse|IyQTZ2M{Sw
K562 NYDiTG4x[3m2b4TvfIlkcXS7IHHzd4F6 Ml;WglExOCEQvF2= NHOzR4hFVVOR M4XxRmlEPTB-MUCwJO69VQ>? MmLSNlE6PjR|NEC=
MEG01 M4\ibYN6fG:2b4jpZ4l1gSCjc4PhfS=> MoHiglExOCEQvF2= M4npfmROW09? NI\ITWJKSzVyPUK1JO69VQ>? NYm4U4p3OjF7NkSzOFA>
HL60 M4\KSoN6fG:2b4jpZ4l1gSCjc4PhfS=> M{TyWZ4yODBizszN MV\EUXNQ MlvlTWM2OD16OUCgcm0> NXXzUYJ4OjF7NkSzOFA>
MV4;11 MVjBdI9xfG:|aYOgZZN{[Xl? MmPXglExOCEQvF2= NXzvTJpnTE2VTx?= NVPGOm1UcW6mdXPld{BieG:ydH;zbZM> NUfodpg5OjF7NkSzOFA>
MOLM13 M{LL[WFxd3C2b4Ppd{Bie3OjeR?= M{i4Up4yODBizszN MmSwSG1UVw>? NFPnfZZqdmS3Y3XzJIFxd3C2b4Ppdy=> MXKyNVk3PDN2MB?=
MV4;11 MoLMSpVv[3Srb36gZZN{[Xl? NXTOTXlYTE2VTx?= NXTaO2h2\GWlcnXhd4V{KHSqZTDy[YNzfWm2bXXueEBw\iCEUlSzM|Qh[W6mIHntdIFqemWmIILlZ5J2cXSvZX70JI9nKEOGS{mgZY5lKFCDRkGgeI8hfGinIITyZY5{[3KrcITpc45idCC|dHHyeEB{cXSn M4jTc|IyQTZ2M{Sw
PBMC M37aOmZ2dmO2aX;uJIF{e2G7 M{nHUWROW09? NWjmdGt6cW6qaXLpeJMhUUxvNjD3bZRpKHCLQ{WwJI9nKDZwNx?= NX3jVY9QOjJ2M{exNVU>
A2 NVfUZ3dvTnWwY4Tpc44h[XO|YYm= M3z4Tp4yOCEQvF2= MVPEUXNQ M1fORZJm[WO2aY\heIV{KGyjdHXueEBJUVZvMR?= MYKyN|I2PTJzOB?=
A72 NXHEUHJ4TnWwY4Tpc44h[XO|YYm= MmrWglExKM7:TR?= NYTUcJpXTE2VTx?= MVXy[YFkfGm4YYTld{Bt[XSnboSgTGlXNTF? NV6xPGlLOjN{NUWyNVg>
BC1 MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkjBglEh|ryP Mn7WSG1UVw>? MoT5TWM2OD1{MkCgcm0> NXLKfpl{OjN5OUK0OFg>
BC3 NYm5NJNGT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYH+NUDPxE1? MUXEUXNQ NF\wUZBKSzVyPUS2NEBvVQ>? NGO4cHozOzd7MkS0PC=>
BCBL1 NEG3TpJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWPWcJlohjFizszN NGPLdJNFVVOR MX7JR|UxRTN|MDDuUS=> NWLHe2g{OjN5OUK0OFg>
BJAB M1rkfmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEL1doR,OSEQvF2= M2f3XWROW09? MnfDTWM2OD17N{Cgcm0> NXjMbFJxOjN5OUK0OFg>
Namalwa NVnJNHduT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4DLd54yKM7:TR?= NFnRWXBFVVOR M3vMRWlEPTB;OUewJI5O M1zpPFI{Pzl{NES4
Jurkat NEH2cVFIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnvXglEh|ryP MXHEUXNQ M4LpfGlEPTB;MUKyNEBvVQ>? NU\OVIMyOjN5OUK0OFg>
MM1S MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUT+NUDPxE1? NYHqW49yTE2VTx?= MVLJR|UxRTd4MDDuUS=> NUDYNFlVOjN5OUK0OFg>
U266 NY\GOohkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M4\SbJ4yKM7:TR?= MXHEUXNQ NFXOUoVKSzVyPUm1NEBvVQ>? M3vFWVI{Pzl{NES4
UM-PEL-1 MWHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MWn+NUDPxE1? M2OwbWROW09? M2rPfGlEPTB;MkGwJI5O NVTC[|ZvOjN5OUK0OFg>
UM-PEL-3 NHvvT2dIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Ml\0glEh|ryP MojLSG1UVw>? NYrDeolXUUN3ME2xPFAhdk1? Mn\sNlM4QTJ2NEi=
BC1 MnjrSpVv[3Srb36gZZN{[Xl? Ml3POVAxKG6P MWPEUXNQ MUPpcoR2[2W|IHPlcIwu[3mlbHWgZZJz\XO2 M17QZVI{Pzl{NES4
BC3 NFXLfGdHfW6ldHnvckBie3OjeR?= Mo\1OVAxKG6P MmDOSG1UVw>? NGDwfIhqdmS3Y3XzJINmdGxvY4njcIUh[XK{ZYP0 MlziNlM4QTJ2NEi=
BC1 MVfGeY5kfGmxbjDhd5NigQ>? NEjlbIg5ODBibl2= NVyzWGdnTE2VTx?= Mn3GdoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> NXizNY9WOjN5OUK0OFg>
BC3 NIK5W3NHfW6ldHnvckBie3OjeR?= MVS4NFAhdk1? MlXaSG1UVw>? MnTRdoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> M1XxeFI{Pzl{NES4
H929 Mkn1SpVv[3Srb36gZZN{[Xl? NE\5cG9,OSEQvF2= MkfoSG1UVw>? NUS3c2ducW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NUnTSIg6OjR|M{W0PVk>
KMS12PE NWTZeWxyTnWwY4Tpc44h[XO|YYm= NIjpcHJ,OSEQvF2= NVftVmNTTE2VTx?= MnPNbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MkHjNlQ{OzV2OUm=
KMS12BM NFP1WFJHfW6ldHnvckBie3OjeR?= MlP4glEh|ryP M{jQTWROW09? NXy2WoZEcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MlvWNlQ{OzV2OUm=
KMS18 MV;GeY5kfGmxbjDhd5NigQ>? NVHSe48yhjFizszN MWLEUXNQ NHPHRYFqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M2TlcFI1OzN3NEm5
KMS11 NIP6dVFHfW6ldHnvckBie3OjeR?= M2HMVJ4yKM7:TR?= MYDEUXNQ MkfKbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M2H5dlI1OzN3NEm5
RPMI8226 MmrDSpVv[3Srb36gZZN{[Xl? MWn+NUDPxE1? MlLpSG1UVw>? M1O4folv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MXmyOFM{PTR7OR?=
H929 Mki0RZBweHSxc3nzJIF{e2G7 NYD3Z2p5hjFizszN M2T5SmROW09? NF;tU5RqdmS3Y3XzJINmdGxiYYDvdJRwe2m| M3;ZXFI1OzN3NEm5
KMS12PE MlvnRZBweHSxc3nzJIF{e2G7 MWL+NUDPxE1? NIrzPVRFVVOR M{[5WYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MXWyOFM{PTR7OR?=
KMS12BM NGj3UmlCeG:ydH;zbZMh[XO|YYm= M{TmTZ4yKM7:TR?= MkK4SG1UVw>? M4PhZolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NFHaTYszPDN|NUS5PS=>
KMS18 NX[xSYQ5SXCxcITvd4l{KGG|c3H5 NYXpTZl[hjFizszN MVfEUXNQ M2HEeIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NETYVGozPDN|NUS5PS=>
KMS11 NInUW5ZCeG:ydH;zbZMh[XO|YYm= NIO5V4d,OSEQvF2= MoHMSG1UVw>? M{nURYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MVSyOFM{PTR7OR?=
RPMI8226 MVfBdI9xfG:|aYOgZZN{[Xl? M4DjT54yKM7:TR?= M3TiVmROW09? MlK1bY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MmrXNlQ{OzV2OUm=
U87MG NF[zS|NHfW6ldHnvckBie3OjeR?= MUD+NVAh|ryP MlvDSG1UVw>? NE[wc|Fz\WS3Y3XzJHU5P02JIHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMT6wOUDPxE1? MYSyOFQ6PjN6MR?=
A172 MoXCSpVv[3Srb36gZZN{[Xl? NVuzd4d[hjFyIN88US=> MXvEUXNQ MYny[YR2[2W|IHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMT6yPEDPxE1? MVSyOFQ6PjN6MR?=
SW1783 MlPVSpVv[3Srb36gZZN{[Xl? MX7+NVAh|ryP NXzWZnF1TE2VTx?= NIPuWXRz\WS3Y3XzJINmdGy3bHHyJGFVWCC5aYToJGlEPTBib3[gNk43QCEQvF2= MX2yOFQ6PjN6MR?=
U87MG MmPwSpVv[3Srb36gZZN{[Xl? M2PNR54yOCEQvF2= NIfi[YFFVVOR MoD4bY5kemWjc3XzJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5idHjlJGcyN1NidILhcpNqfGmxbh?= NUnJSYc{OjR2OU[zPFE>
RAW267.4 MlP1SpVv[3Srb36gZZN{[Xl? NHTsdVUyKM7:TR?= MmjGSG1UVw>? MVHy[YR2[2W|IFnMMVYheHKxZIXjeIlwdiCrbnT1Z4VlKGK7IFzQVy=> MVuyOFg2QTByOB?=
RAW267.4 NGPDVI1HfW6ldHnvckBie3OjeR?= NV\LVIV6OSEQvF2= NYjFVIR4TE2VTx?= NFXG[YZz\WS3Y3XzJJRp\SCjc4PvZ4lifGmxbjDi[ZR4\WWwIFLSSFQh[W6mIHHj[ZR6dGG2ZXSgdFY2 MVyyOFg2QTByOB?=
Me007 MmrFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1va[Z4yODBizszN MWnEUXNQ MWfpcohq[mm2czD0bIUh\3Kxd4To NH7pXIIzPDlyNkGzOy=>
SK-Mel-28 NXvNR3E5T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MofHglExOCEQvF2= M1TOcGROW09? NUf0e4hJcW6qaXLpeJMhfGinIHfyc5d1cA>? NGrGN4QzPDlyNkGzOy=>
Mel-RMU M{ntfWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 M4PDSp4yODBizszN NVf1Tog5TE2VTx?= Ml7LbY5pcWKrdIOgeIhmKGe{b4f0bC=> NIXTUlQzPDlyNkGzOy=>
Mel-JD MXrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXLvenJUhjFyMDFOwG0> MnrDSG1UVw>? NXTKNo1WcW6qaXLpeJMhfGinIHfyc5d1cA>? NXu1cpFpOjR7ME[xN|c>
Mel-RM NHLuNW5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NGHiVlZ,OTByIN88US=> NHXnS49FVVOR MnvQbY5pcWKrdIOgeIhmKGe{b4f0bC=> M{HYUFI1QTB4MUO3
Me007 M3fIfWFxd3C2b4Ppd{Bie3OjeR?= MkPoglExOCEQvF2= Ml6zSG1UVw>? NX;kOoVScW6mdXPld{BieG:ydH;zbZM> MYGyOFkxPjF|Nx?=
SK-Mel-28 NFuwdXBCeG:ydH;zbZMh[XO|YYm= MmTsglExOCEQvF2= NIm3UJlFVVOR MnPBbY5lfWOnczDhdI9xfG:|aYO= NWr2R4hLOjR7ME[xN|c>
Mel-RMU M{LYVWFxd3C2b4Ppd{Bie3OjeR?= NGnWcVV,OTByIN88US=> MYHEUXNQ MYPpcoR2[2W|IHHwc5B1d3Orcx?= NWW2WYxbOjR7ME[xN|c>
Mel-JD M1rEWGFxd3C2b4Ppd{Bie3OjeR?= NY\UfIR5hjFyMDFOwG0> MlyzSG1UVw>? NIT2cFVqdmS3Y3XzJIFxd3C2b4Ppdy=> M1vjVlI1QTB4MUO3
Mel-RM NGfSOmRCeG:ydH;zbZMh[XO|YYm= Mn7sglExOCEQvF2= M1vVXGROW09? M1PKVYlv\HWlZYOgZZBweHSxc3nz NHfmd3IzPDlyNkGzOy=>
Me007 NFzoOYdHfW6ldHnvckBie3OjeR?= MnXNNVAh|ryP NXjKUIdmTE2VTx?= M1[1cYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZpkhfXC{ZXf1cIF1cW:wIH;mJJAzOQ>? MVWyOFkxPjF|Nx?=
SK-Mel-28 MlroSpVv[3Srb36gZZN{[Xl? NWXySGZXOTBizszN MVrEUXNQ NV3ONW9ncW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBjgSC3cILl[5Vt[XSrb36gc4YheDJz MkXUNlQ6ODZzM{e=
Mel-RMU MUfGeY5kfGmxbjDhd5NigQ>? MXOxNEDPxE1? M4rE[WROW09? NI\MNYRqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF? NXTXd|JGOjR7ME[xN|c>
Mel-JD M3LHU2Z2dmO2aX;uJIF{e2G7 MVGxNEDPxE1? NFHwc4lFVVOR M2TTO4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZpkhfXC{ZXf1cIF1cW:wIH;mJJAzOQ>? M{\vc|I1QTB4MUO3
Mel-RM M3\RbGZ2dmO2aX;uJIF{e2G7 M3nJNFExKM7:TR?= NHH0[WFFVVOR MkDYbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDifUB2eHKnZ4XsZZRqd25ib3[gdFIy MWCyOFkxPjF|Nx?=
Me007 NXn2WW5oTnWwY4Tpc44h[XO|YYm= MnfLNVAh|ryP Mki0SG1UVw>? NGroclh2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz M{LYUVI1QTB4MUO3
SK-Mel-28 M{fjUGZ2dmO2aX;uJIF{e2G7 MV2xNEDPxE1? M3fCXmROW09? M{C0SZVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= NHLJcmEzPDlyNkGzOy=>
Mel-RMU NGThPZRHfW6ldHnvckBie3OjeR?= MWmxNEDPxE1? M3H0W2ROW09? MonLeZBz\We3bHH0[ZMheHKxYYDvdJRwfGmlIHHu[EBk\WyuIHP5Z4xmKGG{cnXzeEBo\W6ncx?= M3O5RlI1QTB4MUO3
Mel-JD NYXLdGxpTnWwY4Tpc44h[XO|YYm= NILpflYyOCEQvF2= M1G1O2ROW09? NIKxNIZ2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz NIHlcHozPDlyNkGzOy=>
Mel-RM NED2WIdHfW6ldHnvckBie3OjeR?= MWKxNEDPxE1? NXjPRXVFTE2VTx?= MV71dJJm\3WuYYTld{Bxem:jcH;weI91cWNiYX7kJINmdGxiY4njcIUh[XK{ZYP0JIdmdmW| NV;NRpVYOjR7ME[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

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    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