I-BET151 (GSK1210151A)

Catalog No.S2780

For research use only.

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.

I-BET151 (GSK1210151A) Chemical Structure

CAS No. 1300031-49-5

Selleck's I-BET151 (GSK1210151A) has been cited by 39 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 Mo\LZ5l1d3SxeHnjbZR6KGG|c3H5 NWmyeGh3hjFyMDFOwG0> Mlv3SG1UVw>? NEXpZm1KSzVyPUK2JI5O MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTl4NEO0NEc,OjF7NkSzOFA9N2F-
RS4;11 M2\XZ4N6fG:2b4jpZ4l1gSCjc4PhfS=> Ml[5glExOCEQvF2= MmPUSG1UVw>? MVnJR|UxRTF7MjDuUS=> MnrXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
MOLM13 NXnaVm9H[3m2b4TvfIlkcXS7IHHzd4F6 NGHyZXh,OTByIN88US=> MWTEUXNQ NEPtWmRKSzVyPUGyNEBvVQ>? M1;3VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
NOMO1 NUfYO2lx[3m2b4TvfIlkcXS7IHHzd4F6 M1\JNp4yODBizszN M{TLZ2ROW09? MmDyTWM2OD1zNTDuUS=> NWLDfYltRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
HEL NFP6NJlkgXSxdH;4bYNqfHliYYPzZZk> MkTzglExOCEQvF2= NUXo[I1sTE2VTx?= NXPqVGM6UUN3ME2xJO69VQ>? M4TSb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[0N|QxLz5{MUm2OFM1ODxxYU6=
K562 M1m5V4N6fG:2b4jpZ4l1gSCjc4PhfS=> MWn+NVAxKM7:TR?= M{TrUWROW09? Mnj1TWM2OD5zMECg{txO NYDQfWt5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
MEG01 Mof2Z5l1d3SxeHnjbZR6KGG|c3H5 MVf+NVAxKM7:TR?= MnG1SG1UVw>? MYnJR|UxRTJ3IN88US=> Moq3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
HL60 MYfjfZRwfG:6aXPpeJkh[XO|YYm= MljFglExOCEQvF2= NUL1OHZqTE2VTx?= MlXwTWM2OD16OUCgcm0> NFfiOIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
MV4;11 MWDBdI9xfG:|aYOgZZN{[Xl? NHPGXph,OTByIN88US=> NH[2dZJFVVOR MXTpcoR2[2W|IHHwc5B1d3Orcx?= NHrLbo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUm2OFM1OCd-MkG5OlQ{PDB:L3G+
MOLM13 M{nBfGFxd3C2b4Ppd{Bie3OjeR?= MW\+NVAxKM7:TR?= MnL1SG1UVw>? MUjpcoR2[2W|IHHwc5B1d3Orcx?= Ml\yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF7NkSzOFAoRjJzOU[0N|QxRC:jPh?=
MV4;11 NF3uPZpHfW6ldHnvckBie3OjeR?= NFzPNpdFVVOR MlPn[IVkemWjc3XzJJRp\SC{ZXPyeYl1dWWwdDDv[kBDWkR|L{SgZY5lKGmvcHHpdoVlKHKnY4L1bZRu\W62IH;mJGNFUzliYX7kJHBCTjFidH:geIhmKHS{YX7zZ5JqeHSrb37hcEB{fGG{dDDzbZRm NUDLOWZbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlQ{PDBpPkKxPVY1OzRyPD;hQi=>
PBMC MlnuSpVv[3Srb36gZZN{[Xl? MnvNSG1UVw>? MlvybY5pcWKrdIOgTWwuPiC5aYToJJBKSzVyIH;mJFYvPw>? NHL5RWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkSzO|EyPSd-MkK0N|cyOTV:L3G+
A2 MXPGeY5kfGmxbjDhd5NigQ>? M2HaPZ4yOCEQvF2= NWL6T2piTE2VTx?= NHq4[5dz\WGldHn2ZZRmeyCuYYTlcpQhUEmYLUG= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ3NUKxPEc,OjN{NUWyNVg9N2F-
A72 MX3GeY5kfGmxbjDhd5NigQ>? M2\YRp4yOCEQvF2= M{TJfmROW09? NEnndHpz\WGldHn2ZZRmeyCuYYTlcpQhUEmYLUG= NUni[YZYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyOVUzOThpPkKzNlU2OjF6PD;hQi=>
BC1 MXTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVLUOIhEhjFizszN NXLuUJZyTE2VTx?= MYXJR|UxRTJ{MDDuUS=> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BC3 NYf3dG9xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVX+NUDPxE1? NXjvO3BKTE2VTx?= NHjkOVJKSzVyPUS2NEBvVQ>? M{[zbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BCBL1 MmXpS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MXj+NUDPxE1? NXr4dIxLTE2VTx?= NXPrT|RJUUN3ME2zN|Ahdk1? M3\3R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BJAB NVnDXnU3T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MYH+NUDPxE1? MoHYSG1UVw>? MVLJR|UxRTl5MDDuUS=> NIO5Xnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
Namalwa NGr3O|ZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NESzN4h,OSEQvF2= NEH3THBFVVOR Ml;yTWM2OD17N{Cgcm0> M1PlOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
Jurkat M3HQZmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXv+NUDPxE1? M{PtU2ROW09? NF:5[Y5KSzVyPUGyNlAhdk1? NXPCcJRlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVI1PDhpPkKzO|kzPDR6PD;hQi=>
MM1S M1rjWWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MoDnglEh|ryP M4rTS2ROW09? MlvGTWM2OD15NkCgcm0> NEjBeHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
U266 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NX3YZoh5hjFizszN M4\hW2ROW09? NWD3Z4xDUUN3ME25OVAhdk1? Mm\IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
UM-PEL-1 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NYn4TI5ohjFizszN Ml25SG1UVw>? MoW5TWM2OD1{MUCgcm0> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
UM-PEL-3 MnTFS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MVP+NUDPxE1? M{fLcmROW09? M{PUNmlEPTB;MUiwJI5O NEi0[YY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlQ1QCd-MkO3PVI1PDh:L3G+
BC1 MmjJSpVv[3Srb36gZZN{[Xl? Mo\kOVAxKG6P M2q4ZmROW09? Mk\FbY5lfWOnczDj[YxtNWO7Y3zlJIFzemW|dB?= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkS0PEc,OjN5OUK0OFg9N2F-
BC3 Ml2xSpVv[3Srb36gZZN{[Xl? MUW1NFAhdk1? MkTrSG1UVw>? NGCyZ5NqdmS3Y3XzJINmdGxvY4njcIUh[XK{ZYP0 MoThQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
BC1 M2jibmZ2dmO2aX;uJIF{e2G7 NFmzWJU5ODBibl2= M3H0XWROW09? NXf5TnFPemWmdXPld{BkNU27YzDwdo91\WmwIHzleoVtew>? M13sVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{myOFQ5Lz5{M{e5NlQ1QDxxYU6=
BC3 MYnGeY5kfGmxbjDhd5NigQ>? MkiwPFAxKG6P MXrEUXNQ M3K1OpJm\HWlZYOgZ{1OgWNicILveIVqdiCuZY\lcJM> MkDsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK0OFgoRjJ|N{myOFQ5RC:jPh?=
H929 M{mzTmZ2dmO2aX;uJIF{e2G7 NVPiZoRYhjFizszN MUHEUXNQ M3frVolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
KMS12PE M1zlO2Z2dmO2aX;uJIF{e2G7 NWfxboMyhjFizszN M1rHOmROW09? NYH4VIVncW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN|NUS5PUc,OjR|M{W0PVk9N2F-
KMS12BM Mn2xSpVv[3Srb36gZZN{[Xl? M1LBSJ4yKM7:TR?= MX\EUXNQ MYjpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 NUTvRZdKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
KMS18 M3zCVWZ2dmO2aX;uJIF{e2G7 NFjibFF,OSEQvF2= MmLySG1UVw>? MnjFbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= Mmq2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
KMS11 MlnvSpVv[3Srb36gZZN{[Xl? NXThN5R5hjFizszN M4qyOWROW09? NIPDXYRqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 M4TtbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
RPMI8226 M3HDV2Z2dmO2aX;uJIF{e2G7 MUn+NUDPxE1? NYrveG5vTE2VTx?= MlfTbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M17kclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
H929 MlfqRZBweHSxc3nzJIF{e2G7 MkDzglEh|ryP M3PtXWROW09? NF7GZ5BqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NVnidZpORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzN|U1QTlpPkK0N|M2PDl7PD;hQi=>
KMS12PE M3L4S2Fxd3C2b4Ppd{Bie3OjeR?= NIrsXVJ,OSEQvF2= NX\5dZlJTE2VTx?= NHjlPJJqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MojWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
KMS12BM M3;KbWFxd3C2b4Ppd{Bie3OjeR?= MUn+NUDPxE1? M2DicWROW09? M2nzeIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M2TmUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
KMS18 MYfBdI9xfG:|aYOgZZN{[Xl? MWr+NUDPxE1? NFXBc4JFVVOR MkS2bY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MkfrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|M{W0PVkoRjJ2M{O1OFk6RC:jPh?=
KMS11 NEfxWmZCeG:ydH;zbZMh[XO|YYm= MWT+NUDPxE1? M2PlfGROW09? NWj4[4Q1cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= M37GWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{O1OFk6Lz5{NEOzOVQ6QTxxYU6=
RPMI8226 MkC5RZBweHSxc3nzJIF{e2G7 NH\ZV2x,OSEQvF2= MX;EUXNQ NUfCNIREcW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NIfQS2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOzOVQ6QSd-MkSzN|U1QTl:L3G+
U87MG M4q0XWZ2dmO2aX;uJIF{e2G7 NXPMO4JThjFyIN88US=> MUjEUXNQ MV3y[YR2[2W|IGW4O21IKGOnbHz1cIFzKEGWUDD3bZRpKEmFNUCgc4YhOS5yNTFOwG0> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR7NkO4NUc,OjR2OU[zPFE9N2F-
A172 MXrGeY5kfGmxbjDhd5NigQ>? NY\iPGxKhjFyIN88US=> MoG3SG1UVw>? NWXGWphNemWmdXPld{Bk\WyudXzhdkBCXFBid3n0bEBKSzVyIH;mJFEvOjhizszN NF3rWIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES5OlM5OSd-MkS0PVY{QDF:L3G+
SW1783 M1;a[GZ2dmO2aX;uJIF{e2G7 MWf+NVAh|ryP NXHuO3BnTE2VTx?= MX;y[YR2[2W|IHPlcIx2dGG{IFHUVEB4cXSqIFnDOVAhd2ZiMj62PEDPxE1? MnfjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2OU[zPFEoRjJ2NEm2N|gyRC:jPh?=
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RAW267.4 NUXtTYhUTnWwY4Tpc44h[XO|YYm= NGXSXpgyKM7:TR?= MlWzSG1UVw>? MYTy[YR2[2W|IFnMMVYheHKxZIXjeIlwdiCrbnT1Z4VlKGK7IFzQVy=> NHzVOHg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi1PVAxQCd-MkS4OVkxODh:L3G+
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SK-Mel-28 NF;B[WtCeG:ydH;zbZMh[XO|YYm= NUHMZo11hjFyMDFOwG0> M{HWOWROW09? MnTKbY5lfWOnczDhdI9xfG:|aYO= NFy1[3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwOlE{Pyd-MkS5NFYyOzd:L3G+
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Me007 NHjDSIdHfW6ldHnvckBie3OjeR?= MWSxNEDPxE1? NYn2fXJWTE2VTx?= NFLuO4RqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0JIJ6KHWycnXneYxifGmxbjDv[kBxOjF? NYXZfXdWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFYyOzdpPkK0PVA3OTN5PD;hQi=>
SK-Mel-28 MnG3SpVv[3Srb36gZZN{[Xl? NFqyXXUyOCEQvF2= MXnEUXNQ M2fNNolv\HWlZYOgZ4VtdCCleXPs[UBienKnc4SgZpkhfXC{ZXf1cIF1cW:wIH;mJJAzOQ>? M1zHeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC2NVM4Lz5{NEmwOlE{PzxxYU6=
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SK-Mel-28 M37XdmZ2dmO2aX;uJIF{e2G7 NFvFNpUyOCEQvF2= MXPEUXNQ NHrXWmd2eHKnZ4XsZZRmeyCycn;hdI9xfG:2aXOgZY5lKGOnbHygZ5lkdGViYYLy[ZN1KGenbnXz NWS0[HRWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFYyOzdpPkK0PVA3OTN5PD;hQi=>
Mel-RMU Mm\RSpVv[3Srb36gZZN{[Xl? MoTCNVAh|ryP NFHVfJVFVVOR M3PYZZVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= M{fndlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUC2NVM4Lz5{NEmwOlE{PzxxYU6=
Mel-JD MkDRSpVv[3Srb36gZZN{[Xl? MlrmNVAh|ryP NIiydVJFVVOR M1vCbpVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= NE\ySIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwOlE{Pyd-MkS5NFYyOzd:L3G+
Mel-RM NEfWTnlHfW6ldHnvckBie3OjeR?= MkfXNVAh|ryP M{\aO2ROW09? NU\5ZnFOfXC{ZXf1cIF1\XNicILvZZBweHSxdHnjJIFv\CClZXzsJIN6[2ynIHHydoV{fCCpZX7ldy=> NYDOT3R5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFYyOzdpPkK0PVA3OTN5PD;hQi=>
HepG2 NXrzbpFxTnWwY4Tpc44h[XO|YYm= MUSxPEBpenN? NELsZ3NWeHKnZ4XsZZRqd25ib3[gRZBwSTFiZYjwdoV{e2mxbjDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyClb37j[Y51emG2aX;uJJJmeXWrcnXkJJRwKGmwY4LlZZNmKDdyJTDv[kBtfWOrZnXyZZNmKGGldHn2bZR6KGGodHXyJFE5KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDNVcxKD1iMD6wPUDPxE1w NXHtR5Y{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzPFY2OjlpPkKyN|g3PTJ7PD;hQi=>
Raji MV7GeY5kfGmxbjDhd5NigQ>? MX20JIhzew>? Mn\WTY5pcWKrdHnvckBw\iCEUlS0JIlvKGi3bXHuJHJicmliY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJG1[SyCneIDy[ZN{cW:wIHHmeIVzKDRiaILzMEBKSzVyIE2gNE4yOyEQvF2u NFvQN|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFc2QCd-MkS5NFA4PTh:L3G+
MV4-11 M2jucmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUW3NkBpenN? NEXpW4JIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOXjRvMUGgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDBwMUG5JO69VS5? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV3OUSyPEc,OjV3NUm0Nlg9N2F-
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MV4-11 MYXDfZRwfG:6aXPpeJkh[XO|YYm= Mln4OEBl[Xm| MXPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMhcGG{Yn;ybY5oKE2OTEGg[pV{cW:wIHflcoUh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPCCmYYnzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[XO|YYmsJGlEPTBiPTCwMlE3OiEQvF2u NIS2PIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3 Mnj1SpVv[3Srb36gZZN{[Xl? MV6zNEBucW6| MW\EbZNxdGGlZX3lcpQhd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IH\yc40hSlKGNDDCSFIhMDN|MzD0c{A1PjBiYX3pco8h[WOrZDDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hWm:|ZYT0ZVIhTEV|IHPlcIx{KGGodHXyJFMxKG2rboOgZpkh\my3b4Lld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeTygTWM2OCB;IECuNlI3KM7:TT6= Mk[3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
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Rosetta2 DE3 MkXhSpVv[3Srb36gZZN{[Xl? MYWzNEBucW6| MoruTY5pcWKrdHnvckBw\iCIQV2tcIFj\WynZDDaRmEzPDhiYnnu[Ilv\yC2bzDy[YNwdWKrbnHueEBpfW2jbjDOMZRmem2rbnHsJGhqezZvdHHn[4VlKEKURESgZpJwdW:mb33hbY4hOSBqNESgeI8hOTZ6IILld4llfWW|KTDlfJBz\XO|ZXSgbY4hWm:|ZYT0ZVIhTEV|IHPlcIx{KGGodHXyJFMxKG2rboOgZpkhTmyxdYLld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeTygTWM2OCB;IECuNFMyPyEQvF2u NWXaWJA1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki0OlM1QDdpPkK4OFY{PDh5PD;hQi=>
MV4-11 M3TNRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH;Kd|E1KGSjeYO= MWrHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNWlQuOTFiY3XscJMh[W[2ZYKgOEBl[Xm|IHL5JHdUXC16IHHzd4F6NCCLQ{WwJF0hOC5zNkKg{txONg>? M{LyVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NE[zOFg4Lz5{OES2N|Q5PzxxYU6=
Rosetta2 DE3 NFT0UWVHfW6ldHnvckBie3OjeR?= MX:zNEBucW6| NFnsO5lKdmirYnn0bY9vKG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDibY5lcW6pIITvJJJm[2:vYnnuZY51KGi3bXHuJG4ufGW{bXnuZYwhUGm|Nj30ZYdo\WRiQmLEOEBjem:vb3TvcYFqdiB{IDizN|MhfG9iNE[wJJJme2mmdXXzLUBmgHC{ZYPz[YQhcW5iUn;z[ZR1[TJiRFWzJINmdGy|IHHmeIVzKDNyIH3pcpMh[nliRnzveZJme2OnbnPlJJBwdGG{aYrheIlwdiCjc4PhfUwhUUN3MDC9JFAvOjJ4IN88UU4> M{fNZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NE[zOFg4Lz5{OES2N|Q5PzxxYU6=
MOLM13 MnPzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2HSNlQh\GG7cx?= NVjXZY9bT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OTUGzJINmdGy|IHHmeIVzKDRiZHH5d{BjgSCZU2StPEBie3OjeTygTWM2OCB;IECuNlI5KM7:TT6= MmLKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2NkO0PFcoRjJ6NE[zOFg4RC:jPh?=
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Rosetta2 DE3 M4nSNGZ2dmO2aX;uJIF{e2G7 NHO0UphDcW6maX7nJIFn\mmwaYT5JJRwKGKrb4Tpcplt[XSnZDDCVmQ{KEKGMjCoN|A3KHSxIESxO{BidWmwbzDhZ4llKHKnc3nkeYV{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDSc5NmfHSjMjDESVMh[2WubIOgZpkh[mmxLXzhfYVzKGmwdHXy[oVzd22ndIL5JI1mfGixZDygT4QhRSByLkC0NFUh|ryPLh?= Ml\KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
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Rosetta2 DE3 MVHGeY5kfGmxbjDhd5NigQ>? NWf1UmhpOzBibXnudy=> MnjpSIl{eGyjY3Xt[Y51KG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDmdo9uKEKURESgRmQyKCh2NDD0c{AyPjhiYX3pco8h[WOrZDDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hWm:|ZYT0ZVIhTEV|IHPlcIx{KGGodHXyJFMxKG2rboOgZpkh\my3b4Lld4NmdmOnIIDvcIFzcXqjdHnvckBie3OjeTygT4khRSByLkCwPUDPxE1w NID6RWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
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Rosetta2 DE3 NGi2U3hHfW6ldHnvckBie3OjeR?= Mn;yN|AhdWmwcx?= Mn71SIl{eGyjY3Xt[Y51KG:oIF\BUU1t[WKnbHXkJHpDSTJ2ODDmdo9uKEKUREOgRmQzKCh|ME[geI8hPDF5IHHtbY5wKGGlaXSgdoV{cWS3ZYOpJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO|YYmsJGtqKD1iMD6wNlI{KM7:TT6= M{e4bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
Rosetta2 DE3 NXrRZXp[TnWwY4Tpc44h[XO|YYm= MoLXN|AhdWmwcx?= NVz0eGpETGm|cHzhZ4Vu\W62IH;mJGZCVS2uYXLlcIVlKFqEQUK0PEBnem:vIFLSSFIhSkR{IDizOFkhfG9iNE[wJIFucW6xIHHjbYQhemW|aXT1[ZMqKCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIGLvd4V1fGF{IFTFN{Bk\WyuczDh[pRmeiB|MDDtbY5{KGK7IH\seY9z\XOlZX7j[UBxd2yjcnn6ZZRqd25iYYPzZZktKEurIE2gNE4xPDl4IN88UU4> NWfvco17RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
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Rosetta2 DE3 M3;tO2Z2dmO2aX;uJIF{e2G7 M1zzVFMxKG2rboO= M3O4[WlvcGmkaYTpc44hd2ZiRlHNMYxi[mWuZXSgXmJCOjR6IHLpcoRqdmdidH:gdoVkd22kaX7hcpQhcHWvYX6gUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCEUlS0JIJzd22xZH;tZYlvKDFiKES0JJRwKDF4ODDy[ZNq\HWnczmg[ZhxemW|c3XkJIlvKFKxc3X0eIEzKESHMzDj[YxteyCjZoTldkA{OCCvaX7zJIJ6KE[ub4Xy[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO|YYmsJGtqKD1iMD6wNFkh|ryPLh?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
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HT-29 M3LKb2Z2dmO2aX;uJIF{e2G7 MkLlNE4{OTJ3IIXNJJRwKDVidV2= MlHSNlQhcHK| M{LFS2lvcGmkaYTpc44hd2ZiQmLEOEBqdiCqdX3hckBJXC1{OTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[y2PeXOgdJJwfGWrbjDlfJBz\XO|aX;uJIF1KDBwM{GyOUB2VSC2bzC1JJVOKHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKG2ndHjv[C=> NUH2TIRpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW1OVk1OjhpPkK1OVU6PDJ6PD;hQi=>
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MV4-11 MnXxSpVv[3Srb36gZZN{[Xl? MlvWTY5pcWKrdHnvckBw\iCEUlS0JIlvKGi3bXHuJG1XPC1zMTDj[YxteyCjc4Pld5Nm\CCjczDkc5dvemWpdXzheIlwdiCxZjDjUXlEKFKQQTDlfJBz\XO|aX;uJIJ6KFKQQT3z[ZEh[W6jbInzbZM> NFfaVGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUK1PVc2OSd-MkmyOVk4PTF:L3G+
U-2 OS MoLydWhVWyCjc4PhfS=> NVXZWXlyeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGWtNkBQWyClZXzsdy=> M1:5VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 NYXzcZZmeUiWUzDhd5NigQ>? MmfqdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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MG 63 (6-TG R) MVvxTHRUKGG|c3H5 M3jRXZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= NFvZ[5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 Mk\CdWhVWyCjc4PhfS=> M3HvU5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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fibroblast cells M2mwT5FJXFNiYYPzZZk> M4H6OpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiClb370do9tKEiqIIfpcIQhfHmyZTDmbYJzd2KuYYP0JINmdGy| MlywQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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Rh30 M3j1UZFJXFNiYYPzZZk> NX\XSnl6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoN|Ah[2WubIO= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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Assay
Methods Test Index PMID
Western blot α-SMA / Fibronectin / Collagen-1 ; FoxM1 / AURKB / Survivin / cyclin B / PLK1 ; HP1α / HP1β / HP1γ 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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

Animal Research:

[1]

  • 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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 415.44
Formula

C23H21N5O3

CAS No. 1300031-49-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)C(C)C5=CC=CC=N5)OC

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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