I-BET151 (GSK1210151A)

For research use only.

Catalog No.S2780

29 publications

I-BET151 (GSK1210151A) Chemical Structure

CAS No. 1300031-49-5

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 29 publications

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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 NYG2NZJH[3m2b4TvfIlkcXS7IHHzd4F6 MofHglExOCEQvF2= M3vhVmROW09? M4PvdmlEPTB;Mk[gcm0> NXPlbY9pOjF7NkSzOFA>
RS4;11 M1TPc4N6fG:2b4jpZ4l1gSCjc4PhfS=> MWP+NVAxKM7:TR?= NVHLcoY2TE2VTx?= MX7JR|UxRTF7MjDuUS=> NF[weHMzOTl4NEO0NC=>
MOLM13 NYrORYJr[3m2b4TvfIlkcXS7IHHzd4F6 NGLHS2R,OTByIN88US=> MmfSSG1UVw>? MV7JR|UxRTF{MDDuUS=> M2jrUlIyQTZ2M{Sw
NOMO1 M3nyOYN6fG:2b4jpZ4l1gSCjc4PhfS=> NHuwXJN,OTByIN88US=> NV;1[YlVTE2VTx?= M4jVfmlEPTB;MUWgcm0> NY[z[5hQOjF7NkSzOFA>
HEL MV7jfZRwfG:6aXPpeJkh[XO|YYm= NGTGSml,OTByIN88US=> MYXEUXNQ M4j0RmlEPTB;MTFOwG0> NGXB[YEzOTl4NEO0NC=>
K562 MlLwZ5l1d3SxeHnjbZR6KGG|c3H5 MWD+NVAxKM7:TR?= NEH2WmdFVVOR M3q1WWlEPTB-MUCwJO69VQ>? NYnXR5Q{OjF7NkSzOFA>
MEG01 NGDSUphkgXSxdH;4bYNqfHliYYPzZZk> NVvxeoNuhjFyMDFOwG0> NIrQZXVFVVOR MljKTWM2OD1{NTFOwG0> MUWyNVk3PDN2MB?=
HL60 MojyZ5l1d3SxeHnjbZR6KGG|c3H5 NFnuU4h,OTByIN88US=> M{XIT2ROW09? NXfYfG1LUUN3ME24PVAhdk1? NInYRYgzOTl4NEO0NC=>
MV4;11 MVfBdI9xfG:|aYOgZZN{[Xl? NU\pOFFHhjFyMDFOwG0> M{HnZWROW09? M3nke4lv\HWlZYOgZZBweHSxc3nz MXyyNVk3PDN2MB?=
MOLM13 M1u0[2Fxd3C2b4Ppd{Bie3OjeR?= M{jNRp4yODBizszN M3;xWGROW09? Mlm3bY5lfWOnczDhdI9xfG:|aYO= NWDtUHFiOjF7NkSzOFA>
MV4;11 NGjvZphHfW6ldHnvckBie3OjeR?= M4DiNmROW09? MWXk[YNz\WG|ZYOgeIhmKHKnY4L1bZRu\W62IH;mJGJTTDNxNDDhcoQhcW2yYXny[YQhemWlcoXpeI1mdnRib3[gR2RMQSCjbnSgVGFHOSC2bzD0bIUhfHKjboPjdolxfGmxbnHsJJN1[XK2IIPpeIU> MVWyNVk3PDN2MB?=
PBMC NHK0b|BHfW6ldHnvckBie3OjeR?= NX;kcoJjTE2VTx?= NFPKPZdqdmirYnn0d{BKVC14IIfpeIgheEmFNUCgc4YhPi55 M3nYXFIzPDN5MUG1
A2 MWTGeY5kfGmxbjDhd5NigQ>? M4DtWp4yOCEQvF2= MmLMSG1UVw>? M2jZfpJm[WO2aY\heIV{KGyjdHXueEBJUVZvMR?= NHm5ZlkzOzJ3NUKxPC=>
A72 NWrOWWttTnWwY4Tpc44h[XO|YYm= NXq3O3l6hjFyIN88US=> M4D1TWROW09? MlHhdoVi[3SrdnH0[ZMhdGG2ZX70JGhKXi1z Ml;PNlMzPTV{MUi=
BC1 NXPjb2dPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NIHFWZJ,OSEQvF2= MlLPSG1UVw>? MUPJR|UxRTJ{MDDuUS=> MW[yN|c6OjR2OB?=
BC3 NULxWlVDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWX+NUDPxE1? NXjjcYpXTE2VTx?= NWP5XIxrUUN3ME20OlAhdk1? M1fV[|I{Pzl{NES4
BCBL1 MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M1rZWZ4yKM7:TR?= M1fldmROW09? NXfS[4R4UUN3ME2zN|Ahdk1? MkLmNlM4QTJ2NEi=
BJAB M1vPUGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHn6NJF,OSEQvF2= NGKxRYpFVVOR MlfFTWM2OD17N{Cgcm0> MlHlNlM4QTJ2NEi=
Namalwa NX7KeJRXT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MmLKglEh|ryP M2LtVmROW09? NGPBNnFKSzVyPUm3NEBvVQ>? NFzkTWEzOzd7MkS0PC=>
Jurkat MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2nPRp4yKM7:TR?= M3SzemROW09? MWnJR|UxRTF{MkCgcm0> NXjp[4hpOjN5OUK0OFg>
MM1S M4LV[Wdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MYf+NUDPxE1? M2nUTGROW09? NHO1OoxKSzVyPUe2NEBvVQ>? M1nzcFI{Pzl{NES4
U266 NUXwSlhFT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWD+NUDPxE1? MkHXSG1UVw>? MVvJR|UxRTl3MDDuUS=> MmCzNlM4QTJ2NEi=
UM-PEL-1 MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVzWSXlZhjFizszN M3u3N2ROW09? Ml7aTWM2OD1{MUCgcm0> NVXJ[IZJOjN5OUK0OFg>
UM-PEL-3 NIPmZ4RIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXTqWVhxhjFizszN NXHYOXdQTE2VTx?= NVjwNYhsUUN3ME2xPFAhdk1? Ml7rNlM4QTJ2NEi=
BC1 MoSwSpVv[3Srb36gZZN{[Xl? MXe1NFAhdk1? NH\HWIhFVVOR NYL5fpFucW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> M1Htd|I{Pzl{NES4
BC3 NIDXcHJHfW6ldHnvckBie3OjeR?= NW\LR4lMPTByIH7N NX3FcYU5TE2VTx?= NYjxVJpMcW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> M{\uOFI{Pzl{NES4
BC1 M1[zTGZ2dmO2aX;uJIF{e2G7 NEXxUWk5ODBibl2= MoDCSG1UVw>? MVvy[YR2[2W|IHOtUZlkKHC{b4TlbY4hdGW4ZXzz NUnvb4tROjN5OUK0OFg>
BC3 NWTKSGlYTnWwY4Tpc44h[XO|YYm= M4fIOFgxOCCwTR?= NV\SbYRQTE2VTx?= MkjjdoVlfWOnczDjMW16[yCycn;0[YlvKGyndnXsdy=> NHzzWnYzOzd7MkS0PC=>
H929 NV\oeYtXTnWwY4Tpc44h[XO|YYm= M1LFOp4yKM7:TR?= MVnEUXNQ NVPHTGV5cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NX7ZcG1ROjR|M{W0PVk>
KMS12PE M2DifmZ2dmO2aX;uJIF{e2G7 NFXpNW5,OSEQvF2= M{XuO2ROW09? MmrpbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MoX0NlQ{OzV2OUm=
KMS12BM NHPoZ29HfW6ldHnvckBie3OjeR?= M4H5eZ4yKM7:TR?= Ml7iSG1UVw>? MWDpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MYKyOFM{PTR7OR?=
KMS18 MVPGeY5kfGmxbjDhd5NigQ>? MYX+NUDPxE1? M2PjOGROW09? NWjKS2JwcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NX:4Tnd4OjR|M{W0PVk>
KMS11 NF;R[XdHfW6ldHnvckBie3OjeR?= NHn1b|l,OSEQvF2= MXTEUXNQ MlzZbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MX2yOFM{PTR7OR?=
RPMI8226 NYjRbplWTnWwY4Tpc44h[XO|YYm= NYCyV5VYhjFizszN NIjXN2VFVVOR MoXZbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MVeyOFM{PTR7OR?=
H929 MYTBdI9xfG:|aYOgZZN{[Xl? NEP1eHh,OSEQvF2= MV3EUXNQ NWTDTppxcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NV3kOYdoOjR|M{W0PVk>
KMS12PE NFTv[3dCeG:ydH;zbZMh[XO|YYm= MVj+NUDPxE1? NV3B[XZpTE2VTx?= MVTpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NHXMdmUzPDN|NUS5PS=>
KMS12BM NILhRWRCeG:ydH;zbZMh[XO|YYm= MmThglEh|ryP NFG0Z25FVVOR MnzZbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? Mo\uNlQ{OzV2OUm=
KMS18 NH3lVlVCeG:ydH;zbZMh[XO|YYm= NXTYPVRWhjFizszN NGPZbnhFVVOR Mmm0bY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M{XuZ|I1OzN3NEm5
KMS11 NIrKXXFCeG:ydH;zbZMh[XO|YYm= NYnEWG15hjFizszN MXTEUXNQ MnTEbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? Ml:2NlQ{OzV2OUm=
RPMI8226 Ml\GRZBweHSxc3nzJIF{e2G7 NIH5UGN,OSEQvF2= MnTQSG1UVw>? NWjXcXpncW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= M{jocVI1OzN3NEm5
U87MG MmCxSpVv[3Srb36gZZN{[Xl? Mor2glExKM7:TR?= M{XK[WROW09? MXHy[YR2[2W|IGW4O21IKGOnbHz1cIFzKEGWUDD3bZRpKEmFNUCgc4YhOS5yNTFOwG0> M4jMR|I1PDl4M{ix
A172 NEnpemtHfW6ldHnvckBie3OjeR?= NHXJWlZ,OTBizszN NFLBe41FVVOR NHjkWlFz\WS3Y3XzJINmdGy3bHHyJGFVWCC5aYToJGlEPTBib3[gNU4zQCEQvF2= NHrXUYEzPDR7NkO4NS=>
SW1783 M17ifWZ2dmO2aX;uJIF{e2G7 M3vrRZ4yOCEQvF2= M2q1[WROW09? MXLy[YR2[2W|IHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMj62PEDPxE1? MUOyOFQ6PjN6MR?=
U87MG MmLKSpVv[3Srb36gZZN{[Xl? NVezTYF5hjFyIN88US=> MnnJSG1UVw>? NEPmbllqdmO{ZXHz[ZMheHKxcH;yeIlwdiCxZjDj[YxteyCrbjD0bIUhTzFxUzD0doFve2m2aX;u MXOyOFQ6PjN6MR?=
RAW267.4 Ml7iSpVv[3Srb36gZZN{[Xl? M1XST|Eh|ryP NFHONHdFVVOR M4L3c5Jm\HWlZYOgTWwuPiCycn;keYN1cW:wIHnu[JVk\WRiYomgUHBU NEjO[ZYzPDh3OUCwPC=>
RAW267.4 NHnmOopHfW6ldHnvckBie3OjeR?= MmPnNUDPxE1? NIfvO3FFVVOR Mn7odoVlfWOnczD0bIUh[XO|b3PpZZRqd25iYnX0e4VmdiCEUlS0JIFv\CCjY3X0fYxifGWmIIC2OS=> MnjONlQ5PTlyMEi=
Me007 NUTDeWNZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFjuO5R,OTByIN88US=> MXnEUXNQ MlrObY5pcWKrdIOgeIhmKGe{b4f0bC=> NH\tdXkzPDlyNkGzOy=>
SK-Mel-28 NFnFVmNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M{TWNJ4yODBizszN MVHEUXNQ NXK4ZZA4cW6qaXLpeJMhfGinIHfyc5d1cA>? MoXlNlQ6ODZzM{e=
Mel-RMU NWT4Zo1WT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MX3+NVAxKM7:TR?= MlnVSG1UVw>? M4npVIlvcGmkaYTzJJRp\SCpcn;3eIg> NHnQc4wzPDlyNkGzOy=>
Mel-JD NFfGfYVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NVS3UXRZhjFyMDFOwG0> NF;rWYtFVVOR MYrpcohq[mm2czD0bIUh\3Kxd4To M1fSSFI1QTB4MUO3
Mel-RM MmeyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXX+NVAxKM7:TR?= MXHEUXNQ NUjBZ4ozcW6qaXLpeJMhfGinIHfyc5d1cA>? MljLNlQ6ODZzM{e=
Me007 NX\lTJNxSXCxcITvd4l{KGG|c3H5 NYXwcphthjFyMDFOwG0> NXv4PXF3TE2VTx?= MnrybY5lfWOnczDhdI9xfG:|aYO= NFLPd4szPDlyNkGzOy=>
SK-Mel-28 MofrRZBweHSxc3nzJIF{e2G7 NVnnSXV2hjFyMDFOwG0> MnjwSG1UVw>? MWPpcoR2[2W|IHHwc5B1d3Orcx?= MV:yOFkxPjF|Nx?=
Mel-RMU MVXBdI9xfG:|aYOgZZN{[Xl? Mnn4glExOCEQvF2= NYjpR3E3TE2VTx?= NYTjSYhUcW6mdXPld{BieG:ydH;zbZM> MoLYNlQ6ODZzM{e=
Mel-JD MlPlRZBweHSxc3nzJIF{e2G7 M1XnSp4yODBizszN MYfEUXNQ MVTpcoR2[2W|IHHwc5B1d3Orcx?= M{DMdVI1QTB4MUO3
Mel-RM MXPBdI9xfG:|aYOgZZN{[Xl? MmrsglExOCEQvF2= NYrUbJBuTE2VTx?= M3rweIlv\HWlZYOgZZBweHSxc3nz NF[wbpQzPDlyNkGzOy=>
Me007 NIXHVGVHfW6ldHnvckBie3OjeR?= M4G3V|ExKM7:TR?= NUPobolvTE2VTx?= MoHJbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDifUB2eHKnZ4XsZZRqd25ib3[gdFIy NEX6WVIzPDlyNkGzOy=>
SK-Mel-28 NH3STJdHfW6ldHnvckBie3OjeR?= M3rVbFExKM7:TR?= NEnKTHZFVVOR NHzU[W5qdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF? NYnZU29JOjR7ME[xN|c>
Mel-RMU Mn7VSpVv[3Srb36gZZN{[Xl? NVL6TVk3OTBizszN M4WySWROW09? M1\0OIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZpkhfXC{ZXf1cIF1cW:wIH;mJJAzOQ>? NILrR|QzPDlyNkGzOy=>
Mel-JD NF;j[WVHfW6ldHnvckBie3OjeR?= NEnaXYwyOCEQvF2= NHHYUlZFVVOR MVzpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHL5JJVxemWpdXzheIlwdiCxZjDwNlE> NYrL[JNwOjR7ME[xN|c>
Mel-RM M3mxTmZ2dmO2aX;uJIF{e2G7 NVPwUYVwOTBizszN Mo\NSG1UVw>? NFT1XZVqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF? MX6yOFkxPjF|Nx?=
Me007 MXHGeY5kfGmxbjDhd5NigQ>? M4Xr[VExKM7:TR?= MoXRSG1UVw>? M1;EPZVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= NGXRNIwzPDlyNkGzOy=>
SK-Mel-28 MkfCSpVv[3Srb36gZZN{[Xl? MWGxNEDPxE1? M3vhNGROW09? NFXNcWx2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz M136[VI1QTB4MUO3
Mel-RMU MV\GeY5kfGmxbjDhd5NigQ>? MWSxNEDPxE1? M2nUW2ROW09? NGW1eJd2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz Mke2NlQ6ODZzM{e=
Mel-JD M{TWWmZ2dmO2aX;uJIF{e2G7 MmnvNVAh|ryP MYHEUXNQ M{D0N5VxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= M2[5OVI1QTB4MUO3
Mel-RM M2LjSmZ2dmO2aX;uJIF{e2G7 M3i4elExKM7:TR?= NFnWb21FVVOR NUHDT3RNfXC{ZXf1cIF1\XNicILvZZBweHSxdHnjJIFv\CClZXzsJIN6[2ynIHHydoV{fCCpZX7ldy=> NYPI[FlXOjR7ME[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
  • 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 CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)C(C)C5=CC=CC=N5)OC

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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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