I-BET151 (GSK1210151A)

For research use only.

Catalog No.S2780

26 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 26 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 MnjFZ5l1d3SxeHnjbZR6KGG|c3H5 M2W4cZ4yODBizszN NHzHc4FFVVOR Mk[1TWM2OD1{NjDuUS=> NU\GOGhtOjF7NkSzOFA>
RS4;11 MkLDZ5l1d3SxeHnjbZR6KGG|c3H5 MlTBglExOCEQvF2= M4HaNGROW09? MYHJR|UxRTF7MjDuUS=> MV2yNVk3PDN2MB?=
MOLM13 MXvjfZRwfG:6aXPpeJkh[XO|YYm= MonuglExOCEQvF2= MVHEUXNQ MV;JR|UxRTF{MDDuUS=> MnvnNlE6PjR|NEC=
NOMO1 Mny0Z5l1d3SxeHnjbZR6KGG|c3H5 MYL+NVAxKM7:TR?= NEHWdohFVVOR Mlr2TWM2OD1zNTDuUS=> MnW3NlE6PjR|NEC=
HEL NVvDPVZl[3m2b4TvfIlkcXS7IHHzd4F6 MUf+NVAxKM7:TR?= NHPPbJpFVVOR NGDMNnRKSzVyPUGg{txO NIXUZnQzOTl4NEO0NC=>
K562 MXHjfZRwfG:6aXPpeJkh[XO|YYm= M2DuRZ4yODBizszN MX\EUXNQ NWnySG92UUN3ME6xNFAh|ryP M3PNXlIyQTZ2M{Sw
MEG01 NWrmVXFD[3m2b4TvfIlkcXS7IHHzd4F6 MV;+NVAxKM7:TR?= MV7EUXNQ Mk\oTWM2OD1{NTFOwG0> MXeyNVk3PDN2MB?=
HL60 MmTkZ5l1d3SxeHnjbZR6KGG|c3H5 MVj+NVAxKM7:TR?= MVvEUXNQ NXvIOWIyUUN3ME24PVAhdk1? NFXjRpUzOTl4NEO0NC=>
MV4;11 NUHkSHBISXCxcITvd4l{KGG|c3H5 MUn+NVAxKM7:TR?= NHq0NHpFVVOR MUXpcoR2[2W|IHHwc5B1d3Orcx?= NHi2R|UzOTl4NEO0NC=>
MOLM13 M{C2XmFxd3C2b4Ppd{Bie3OjeR?= NFGyb5F,OTByIN88US=> NGrK[IFFVVOR NHmyV|FqdmS3Y3XzJIFxd3C2b4Ppdy=> M1KxPFIyQTZ2M{Sw
MV4;11 Ml;jSpVv[3Srb36gZZN{[Xl? MmrCSG1UVw>? NUHDNYVs\GWlcnXhd4V{KHSqZTDy[YNzfWm2bXXueEBw\iCEUlSzM|Qh[W6mIHntdIFqemWmIILlZ5J2cXSvZX70JI9nKEOGS{mgZY5lKFCDRkGgeI8hfGinIITyZY5{[3KrcITpc45idCC|dHHyeEB{cXSn NYmxXoppOjF7NkSzOFA>
PBMC NV3hUnd4TnWwY4Tpc44h[XO|YYm= MkX4SG1UVw>? MljmbY5pcWKrdIOgTWwuPiC5aYToJJBKSzVyIH;mJFYvPw>? MUmyNlQ{PzFzNR?=
A2 MoDrSpVv[3Srb36gZZN{[Xl? M1O1cp4yOCEQvF2= MlP4SG1UVw>? MXTy[YFkfGm4YYTld{Bt[XSnboSgTGlXNTF? MnPxNlMzPTV{MUi=
A72 Mlu5SpVv[3Srb36gZZN{[Xl? MVf+NVAh|ryP MkTlSG1UVw>? NI\NNIZz\WGldHn2ZZRmeyCuYYTlcpQhUEmYLUG= MnXZNlMzPTV{MUi=
BC1 NWm1XpdqT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFPSR2x,OSEQvF2= MnzaSG1UVw>? NULZS4g{UUN3ME2yNlAhdk1? M{nlcFI{Pzl{NES4
BC3 M1jINGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnrVglEh|ryP NHPF[3NFVVOR NYHvWYtIUUN3ME20OlAhdk1? NYWybGVIOjN5OUK0OFg>
BCBL1 NUHOOZZTT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MlzyglEh|ryP NW[zdW5tTE2VTx?= MmfpTWM2OD1|M{Cgcm0> MUCyN|c6OjR2OB?=
BJAB M1u4ZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUPDeWhDhjFizszN MUXEUXNQ MXLJR|UxRTl5MDDuUS=> MWeyN|c6OjR2OB?=
Namalwa NEXKPFlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mn3YglEh|ryP NWj2eYNKTE2VTx?= MWjJR|UxRTl5MDDuUS=> NYO2dGR6OjN5OUK0OFg>
Jurkat MoKxS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWf+NUDPxE1? NF;wPWlFVVOR M162NGlEPTB;MUKyNEBvVQ>? M33nRVI{Pzl{NES4
MM1S Mlv0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MmfzglEh|ryP NH;DZ3hFVVOR NHKyZZpKSzVyPUe2NEBvVQ>? NFvTeXEzOzd7MkS0PC=>
U266 MonXS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MWX+NUDPxE1? NWjZeplLTE2VTx?= M4P6dmlEPTB;OUWwJI5O NIn3eFMzOzd7MkS0PC=>
UM-PEL-1 NHLhfWJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1rOO54yKM7:TR?= M2DnSGROW09? NEnUOVBKSzVyPUKxNEBvVQ>? NXL2cZB7OjN5OUK0OFg>
UM-PEL-3 MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? Mnm4glEh|ryP M1H6PGROW09? MVLJR|UxRTF6MDDuUS=> M2m4N|I{Pzl{NES4
BC1 M4DDfWZ2dmO2aX;uJIF{e2G7 NXfsToJ[PTByIH7N M2fRbGROW09? MmezbY5lfWOnczDj[YxtNWO7Y3zlJIFzemW|dB?= NGTzeJczOzd7MkS0PC=>
BC3 M1:3WmZ2dmO2aX;uJIF{e2G7 Mn\hOVAxKG6P NYfiO|ZiTE2VTx?= NXLBbmxLcW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> M2X3OFI{Pzl{NES4
BC1 M2fKfWZ2dmO2aX;uJIF{e2G7 MoX2PFAxKG6P NGTNUmJFVVOR M3q1O5Jm\HWlZYOgZ{1OgWNicILveIVqdiCuZY\lcJM> NYjP[4k2OjN5OUK0OFg>
BC3 MmTRSpVv[3Srb36gZZN{[Xl? M{XZTlgxOCCwTR?= M3:0RmROW09? Ml30doVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> Mn;UNlM4QTJ2NEi=
H929 M3ztVGZ2dmO2aX;uJIF{e2G7 NXvmWJMyhjFizszN MlPqSG1UVw>? M3W2colv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MXSyOFM{PTR7OR?=
KMS12PE MYnGeY5kfGmxbjDhd5NigQ>? M3;BTp4yKM7:TR?= Mn[4SG1UVw>? M2LPRolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= NGW3T4EzPDN|NUS5PS=>
KMS12BM MW\GeY5kfGmxbjDhd5NigQ>? M3;zTp4yKM7:TR?= M1LGd2ROW09? NYT5XIhXcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MoS4NlQ{OzV2OUm=
KMS18 MYXGeY5kfGmxbjDhd5NigQ>? NU\LUJE2hjFizszN MkW2SG1UVw>? M1LsUIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MUiyOFM{PTR7OR?=
KMS11 MXnGeY5kfGmxbjDhd5NigQ>? NHvPeWZ,OSEQvF2= M17Fc2ROW09? M4nFNolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MYmyOFM{PTR7OR?=
RPMI8226 MnjySpVv[3Srb36gZZN{[Xl? M3nyR54yKM7:TR?= NIewVIdFVVOR NYToe|RbcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> M2mwcFI1OzN3NEm5
H929 NYPYToNpSXCxcITvd4l{KGG|c3H5 M33ESZ4yKM7:TR?= M3\XTWROW09? MnXybY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NFz4eZAzPDN|NUS5PS=>
KMS12PE NFrnbnFCeG:ydH;zbZMh[XO|YYm= MVr+NUDPxE1? MlPvSG1UVw>? NEXvTopqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NYPHcXFjOjR|M{W0PVk>
KMS12BM NXv0[oJSSXCxcITvd4l{KGG|c3H5 NVLQbXJThjFizszN MWnEUXNQ MXPpcoR2[2W|IHPlcIwh[XCxcITvd4l{ M2jWXVI1OzN3NEm5
KMS18 MoHERZBweHSxc3nzJIF{e2G7 MmL3glEh|ryP NGHvOpFFVVOR MX\pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MVeyOFM{PTR7OR?=
KMS11 NWPOdINJSXCxcITvd4l{KGG|c3H5 M2ntVJ4yKM7:TR?= MYXEUXNQ MX;pcoR2[2W|IHPlcIwh[XCxcITvd4l{ MlX6NlQ{OzV2OUm=
RPMI8226 Ml\kRZBweHSxc3nzJIF{e2G7 M1exWp4yKM7:TR?= MoPSSG1UVw>? NHHuU2lqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MVWyOFM{PTR7OR?=
U87MG MW\GeY5kfGmxbjDhd5NigQ>? NX7yeVFphjFyIN88US=> NHnucHJFVVOR NYS2eFlyemWmdXPld{BWQDePRzDj[YxtfWyjcjDBWHAhf2m2aDDJR|UxKG:oIEGuNFUh|ryP NWXnUVdOOjR2OU[zPFE>
A172 M1TUcmZ2dmO2aX;uJIF{e2G7 M3flNZ4yOCEQvF2= MXLEUXNQ MYXy[YR2[2W|IHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMT6yPEDPxE1? M1XwUFI1PDl4M{ix
SW1783 NEn4TFBHfW6ldHnvckBie3OjeR?= M1vrdJ4yOCEQvF2= MoDYSG1UVw>? NWDjUZRNemWmdXPld{Bk\WyudXzhdkBCXFBid3n0bEBKSzVyIH;mJFIvPjhizszN NYrkS3h{OjR2OU[zPFE>
U87MG NYj2XoJDTnWwY4Tpc44h[XO|YYm= MluwglExKM7:TR?= MlLjSG1UVw>? MXnpcoNz\WG|ZYOgdJJweG:{dHnvckBw\iClZXzsd{BqdiC2aHWgS|EwWyC2cnHud4l1cW:w MVGyOFQ6PjN6MR?=
RAW267.4 NIj1dm5HfW6ldHnvckBie3OjeR?= MWexJO69VQ>? MmHESG1UVw>? M4m2dpJm\HWlZYOgTWwuPiCycn;keYN1cW:wIHnu[JVk\WRiYomgUHBU MXqyOFg2QTByOB?=
RAW267.4 MX3GeY5kfGmxbjDhd5NigQ>? NIj0SJQyKM7:TR?= NF;GRnJFVVOR Mnf4doVlfWOnczD0bIUh[XO|b3PpZZRqd25iYnX0e4VmdiCEUlS0JIFv\CCjY3X0fYxifGWmIIC2OS=> M13neFI1QDV7MEC4
Me007 M2HISGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NGTrNYd,OTByIN88US=> M2nrOWROW09? NY\G[|g{cW6qaXLpeJMhfGinIHfyc5d1cA>? MW[yOFkxPjF|Nx?=
SK-Mel-28 MnjvS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUP+NVAxKM7:TR?= MXHEUXNQ NV3X[3ZRcW6qaXLpeJMhfGinIHfyc5d1cA>? MViyOFkxPjF|Nx?=
Mel-RMU NYTOXYY{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWX+NVAxKM7:TR?= NGLmOZlFVVOR Ml;rbY5pcWKrdIOgeIhmKGe{b4f0bC=> M1fiblI1QTB4MUO3
Mel-JD NX;peHVpT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NG[5PHR,OTByIN88US=> Mon5SG1UVw>? MYDpcohq[mm2czD0bIUh\3Kxd4To MkW5NlQ6ODZzM{e=
Mel-RM MnXFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXf+NVAxKM7:TR?= MV7EUXNQ MlPJbY5pcWKrdIOgeIhmKGe{b4f0bC=> M4fh[FI1QTB4MUO3
Me007 MkDQRZBweHSxc3nzJIF{e2G7 MVv+NVAxKM7:TR?= M{TBVmROW09? NGHiW2pqdmS3Y3XzJIFxd3C2b4Ppdy=> M1jGXFI1QTB4MUO3
SK-Mel-28 NFnaenZCeG:ydH;zbZMh[XO|YYm= Mlj3glExOCEQvF2= NUfoSJRmTE2VTx?= MnfSbY5lfWOnczDhdI9xfG:|aYO= NFjq[lUzPDlyNkGzOy=>
Mel-RMU M4q1c2Fxd3C2b4Ppd{Bie3OjeR?= MXf+NVAxKM7:TR?= MnzGSG1UVw>? M4XDZ4lv\HWlZYOgZZBweHSxc3nz MlzMNlQ6ODZzM{e=
Mel-JD NY\yRZdKSXCxcITvd4l{KGG|c3H5 NVvoe4x3hjFyMDFOwG0> NV[2TmtHTE2VTx?= NVL5ZnNNcW6mdXPld{BieG:ydH;zbZM> NWLrR4RvOjR7ME[xN|c>
Mel-RM MmrhRZBweHSxc3nzJIF{e2G7 NFzjZot,OTByIN88US=> M3zQOmROW09? MoDPbY5lfWOnczDhdI9xfG:|aYO= MXuyOFkxPjF|Nx?=
Me007 MW\GeY5kfGmxbjDhd5NigQ>? M3:1V|ExKM7:TR?= MXrEUXNQ NELFc|FqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF? NInKR2YzPDlyNkGzOy=>
SK-Mel-28 MX7GeY5kfGmxbjDhd5NigQ>? M4TBUFExKM7:TR?= MlrBSG1UVw>? NYfs[GlWcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBjgSC3cILl[5Vt[XSrb36gc4YheDJz MXqyOFkxPjF|Nx?=
Mel-RMU MWfGeY5kfGmxbjDhd5NigQ>? NH\hUIsyOCEQvF2= M1rQSWROW09? NYHwcWZZcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBjgSC3cILl[5Vt[XSrb36gc4YheDJz MoL5NlQ6ODZzM{e=
Mel-JD NYC3OVhUTnWwY4Tpc44h[XO|YYm= NFrOSFgyOCEQvF2= M{DMNmROW09? NV;DN3I1cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeEBjgSC3cILl[5Vt[XSrb36gc4YheDJz NXqyRVFmOjR7ME[xN|c>
Mel-RM MWLGeY5kfGmxbjDhd5NigQ>? NEn3O4YyOCEQvF2= MYjEUXNQ M2X3O4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZpkhfXC{ZXf1cIF1cW:wIH;mJJAzOQ>? NFLDUnQzPDlyNkGzOy=>
Me007 NYnYUHZ6TnWwY4Tpc44h[XO|YYm= Mk[yNVAh|ryP M4PuVmROW09? NXy0bHNJfXC{ZXf1cIF1\XNicILvZZBweHSxdHnjJIFv\CClZXzsJIN6[2ynIHHydoV{fCCpZX7ldy=> NIDDfowzPDlyNkGzOy=>
SK-Mel-28 Mk[5SpVv[3Srb36gZZN{[Xl? MnXpNVAh|ryP MWPEUXNQ M3\PeZVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= MV2yOFkxPjF|Nx?=
Mel-RMU NXPRZnQ2TnWwY4Tpc44h[XO|YYm= M1j4PFExKM7:TR?= M1q4NGROW09? M1Xpc5VxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= NVfMXYZuOjR7ME[xN|c>
Mel-JD MnXxSpVv[3Srb36gZZN{[Xl? M3LxNVExKM7:TR?= NX6xem1KTE2VTx?= Mn\jeZBz\We3bHH0[ZMheHKxYYDvdJRwfGmlIHHu[EBk\WyuIHP5Z4xmKGG{cnXzeEBo\W6ncx?= M{ezR|I1QTB4MUO3
Mel-RM MVLGeY5kfGmxbjDhd5NigQ>? M{LHfFExKM7:TR?= MVTEUXNQ MkG4eZBz\We3bHH0[ZMheHKxYYDvdJRwfGmlIHHu[EBk\WyuIHP5Z4xmKGG{cnXzeEBo\W6ncx?= NH;YNYUzPDlyNkGzOy=>

... 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
  • 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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    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.

  • * Indicates a Required Field

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