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 19 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 M{TLPIN6fG:2b4jpZ4l1gSCjc4PhfS=> NF3LNo9,OTByIN88US=> M{fUTmROW09? NWfhVJFnUUN3ME2yOkBvVQ>? NHGwWJozOTl4NEO0NC=>
RS4;11 NWn4bGdE[3m2b4TvfIlkcXS7IHHzd4F6 NFPGSY1,OTByIN88US=> NXzFe2x3TE2VTx?= NV3uWnhCUUN3ME2xPVIhdk1? MofXNlE6PjR|NEC=
MOLM13 M{DFRoN6fG:2b4jpZ4l1gSCjc4PhfS=> M2i2Tp4yODBizszN MmfoSG1UVw>? NYPlNJU3UUN3ME2xNlAhdk1? M3XETFIyQTZ2M{Sw
NOMO1 MYXjfZRwfG:6aXPpeJkh[XO|YYm= NEnnXWl,OTByIN88US=> MWLEUXNQ MXjJR|UxRTF3IH7N MomyNlE6PjR|NEC=
HEL MWnjfZRwfG:6aXPpeJkh[XO|YYm= NF24RZh,OTByIN88US=> MmHjSG1UVw>? NUfiT3Y4UUN3ME2xJO69VQ>? M1rzd|IyQTZ2M{Sw
K562 MkK2Z5l1d3SxeHnjbZR6KGG|c3H5 M176SZ4yODBizszN MW\EUXNQ M{Dod2lEPTB-MUCwJO69VQ>? MlftNlE6PjR|NEC=
MEG01 NWrrPIJt[3m2b4TvfIlkcXS7IHHzd4F6 NGeyVVR,OTByIN88US=> MWnEUXNQ MkHwTWM2OD1{NTFOwG0> NEXIPFIzOTl4NEO0NC=>
HL60 M3TROIN6fG:2b4jpZ4l1gSCjc4PhfS=> NYPJNJd[hjFyMDFOwG0> MnHvSG1UVw>? M1HnOGlEPTB;OEmwJI5O NFXOdXczOTl4NEO0NC=>
MV4;11 MmrNRZBweHSxc3nzJIF{e2G7 MmLZglExOCEQvF2= Mn;2SG1UVw>? M2Lab4lv\HWlZYOgZZBweHSxc3nz M1\NPVIyQTZ2M{Sw
MOLM13 MUHBdI9xfG:|aYOgZZN{[Xl? NEPEVWt,OTByIN88US=> M2X1WGROW09? NHW4NG1qdmS3Y3XzJIFxd3C2b4Ppdy=> NVrqSHN7OjF7NkSzOFA>
MV4;11 NIThW4NHfW6ldHnvckBie3OjeR?= NUnsc5A5TE2VTx?= Mn3I[IVkemWjc3XzJJRp\SC{ZXPyeYl1dWWwdDDv[kBDWkR|L{SgZY5lKGmvcHHpdoVlKHKnY4L1bZRu\W62IH;mJGNFUzliYX7kJHBCTjFidH:geIhmKHS{YX7zZ5JqeHSrb37hcEB{fGG{dDDzbZRm NUWxe3Y{OjF7NkSzOFA>
PBMC M33rbWZ2dmO2aX;uJIF{e2G7 MVTEUXNQ Mn3zbY5pcWKrdIOgTWwuPiC5aYToJJBKSzVyIH;mJFYvPw>? M3fKRVIzPDN5MUG1
A2 NGC2WY5HfW6ldHnvckBie3OjeR?= M1;H[p4yOCEQvF2= MmHOSG1UVw>? MkezdoVi[3SrdnH0[ZMhdGG2ZX70JGhKXi1z M2DUblI{OjV3MkG4
A72 MmLESpVv[3Srb36gZZN{[Xl? M{LBdJ4yOCEQvF2= M{[0VmROW09? MWPy[YFkfGm4YYTld{Bt[XSnboSgTGlXNTF? M1vad|I{OjV3MkG4
BC1 MUHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MVH+NUDPxE1? MWHEUXNQ NVXsSlFYUUN3ME2yNlAhdk1? NUKxR5N{OjN5OUK0OFg>
BC3 Mli0S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkH5glEh|ryP Ml34SG1UVw>? NWPvOnl3UUN3ME20OlAhdk1? NIKyXlYzOzd7MkS0PC=>
BCBL1 MYPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NEnNWJR,OSEQvF2= Mo\qSG1UVw>? MnzmTWM2OD1|M{Cgcm0> MYmyN|c6OjR2OB?=
BJAB M1j2dmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MWP+NUDPxE1? M37RfGROW09? MXjJR|UxRTl5MDDuUS=> NV7neGhlOjN5OUK0OFg>
Namalwa M3TyNGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NYr1SYtjhjFizszN M{D5WWROW09? NHLhRWdKSzVyPUm3NEBvVQ>? MkHoNlM4QTJ2NEi=
Jurkat NVjLd29ZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MV\+NUDPxE1? MYjEUXNQ M4HQbGlEPTB;MUKyNEBvVQ>? NX:zOIpGOjN5OUK0OFg>
MM1S MnTkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUX+NUDPxE1? M3fYO2ROW09? MkHjTWM2OD15NkCgcm0> M3T2TVI{Pzl{NES4
U266 M3j2UGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MXP+NUDPxE1? Mnf0SG1UVw>? M2TXOWlEPTB;OUWwJI5O NXPaZY9vOjN5OUK0OFg>
UM-PEL-1 MXLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MlPaglEh|ryP M1HmTWROW09? MXPJR|UxRTJzMDDuUS=> MkCwNlM4QTJ2NEi=
UM-PEL-3 MWrHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NXztblFPhjFizszN Ml64SG1UVw>? M{jBdWlEPTB;MUiwJI5O NFqwTlYzOzd7MkS0PC=>
BC1 NEfPbXNHfW6ldHnvckBie3OjeR?= MmnuOVAxKG6P MnfySG1UVw>? NELHVIxqdmS3Y3XzJINmdGxvY4njcIUh[XK{ZYP0 MUGyN|c6OjR2OB?=
BC3 MnTYSpVv[3Srb36gZZN{[Xl? M1P5ZVUxOCCwTR?= MUfEUXNQ NWDZTWV2cW6mdXPld{Bk\WyuLXP5Z4xmKGG{cnXzeC=> MnfpNlM4QTJ2NEi=
BC1 NWHYfGR6TnWwY4Tpc44h[XO|YYm= M3rnO|gxOCCwTR?= NFvLRYFFVVOR NEfYT45z\WS3Y3XzJIMuVXmlIIDyc5RmcW5ibHX2[Yx{ NULDVlJ6OjN5OUK0OFg>
BC3 NYG5dmRLTnWwY4Tpc44h[XO|YYm= MXG4NFAhdk1? MV7EUXNQ M2PBdZJm\HWlZYOgZ{1OgWNicILveIVqdiCuZY\lcJM> MoLVNlM4QTJ2NEi=
H929 NIfreHhHfW6ldHnvckBie3OjeR?= M2i4Tp4yKM7:TR?= MnXwSG1UVw>? M4jl[olv\HWlZYOgZ4VtdCCleXPs[UBienKnc4S= Mlf6NlQ{OzV2OUm=
KMS12PE MVLGeY5kfGmxbjDhd5NigQ>? MVX+NUDPxE1? Mn6zSG1UVw>? MoDpbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= MmixNlQ{OzV2OUm=
KMS12BM M1fiO2Z2dmO2aX;uJIF{e2G7 NX\CcZF6hjFizszN M3HuNmROW09? NIPxOZpqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0 NF[0OGkzPDN|NUS5PS=>
KMS18 NWO0S4hWTnWwY4Tpc44h[XO|YYm= MXj+NUDPxE1? NGDZfVBFVVOR NU\wVnB7cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeC=> NX6yNVZDOjR|M{W0PVk>
KMS11 NVq1WYdYTnWwY4Tpc44h[XO|YYm= Mof6glEh|ryP M2rjUGROW09? Mn7hbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= M3jZUVI1OzN3NEm5
RPMI8226 NH\4UFdHfW6ldHnvckBie3OjeR?= NXL5WYRnhjFizszN MWXEUXNQ MYDpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MYOyOFM{PTR7OR?=
H929 Mlu4RZBweHSxc3nzJIF{e2G7 NGHp[49,OSEQvF2= MmX6SG1UVw>? MVjpcoR2[2W|IHPlcIwh[XCxcITvd4l{ M1z4TVI1OzN3NEm5
KMS12PE NWXaZpZMSXCxcITvd4l{KGG|c3H5 NUPUOGJUhjFizszN MUDEUXNQ M1HDXYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MoPFNlQ{OzV2OUm=
KMS12BM Mn\pRZBweHSxc3nzJIF{e2G7 NGK5Omx,OSEQvF2= MmTjSG1UVw>? M3yyeIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NXXtcJdsOjR|M{W0PVk>
KMS18 MXjBdI9xfG:|aYOgZZN{[Xl? MVv+NUDPxE1? M3zhcmROW09? M{exWYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? Mnj6NlQ{OzV2OUm=
KMS11 MYHBdI9xfG:|aYOgZZN{[Xl? NFvKNYt,OSEQvF2= M3ThRWROW09? M2\wfYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NGXmNowzPDN|NUS5PS=>
RPMI8226 Ml3URZBweHSxc3nzJIF{e2G7 MoH1glEh|ryP NXz5[3lITE2VTx?= M4j0dolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NVX3OllNOjR|M{W0PVk>
U87MG M{jEWGZ2dmO2aX;uJIF{e2G7 MkD4glExKM7:TR?= MUXEUXNQ NX3Re4RsemWmdXPld{BWQDePRzDj[YxtfWyjcjDBWHAhf2m2aDDJR|UxKG:oIEGuNFUh|ryP M3fsUlI1PDl4M{ix
A172 NE[4e5pHfW6ldHnvckBie3OjeR?= M{jjN54yOCEQvF2= MYXEUXNQ M3q2RZJm\HWlZYOgZ4VtdHWuYYKgRXRRKHerdHigTWM2OCCxZjCxMlI5KM7:TR?= NIi0TJQzPDR7NkO4NS=>
SW1783 NUHnNnhHTnWwY4Tpc44h[XO|YYm= NGfOR2N,OTBizszN M4n1bGROW09? M{\4eJJm\HWlZYOgZ4VtdHWuYYKgRXRRKHerdHigTWM2OCCxZjCyMlY5KM7:TR?= M3mxeVI1PDl4M{ix
U87MG MXXGeY5kfGmxbjDhd5NigQ>? M2\M[Z4yOCEQvF2= NITrcoVFVVOR MlzObY5kemWjc3XzJJBzd3CxcoTpc44hd2ZiY3XscJMhcW5idHjlJGcyN1NidILhcpNqfGmxbh?= Ml3ONlQ1QTZ|OEG=
RAW267.4 MXrGeY5kfGmxbjDhd5NigQ>? MV:xJO69VQ>? NWLCPY1bTE2VTx?= M17mcJJm\HWlZYOgTWwuPiCycn;keYN1cW:wIHnu[JVk\WRiYomgUHBU M3TNXlI1QDV7MEC4
RAW267.4 MV7GeY5kfGmxbjDhd5NigQ>? NWnSSnF5OSEQvF2= MYfEUXNQ NEHHb5Jz\WS3Y3XzJJRp\SCjc4PvZ4lifGmxbjDi[ZR4\WWwIFLSSFQh[W6mIHHj[ZR6dGG2ZXSgdFY2 NHr5cpQzPDh3OUCwPC=>
Me007 Mn;MS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NIDzU5h,OTByIN88US=> MkHNSG1UVw>? M4GybolvcGmkaYTzJJRp\SCpcn;3eIg> MViyOFkxPjF|Nx?=
SK-Mel-28 NIrLNFhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUniT5FVhjFyMDFOwG0> MoC0SG1UVw>? MU\pcohq[mm2czD0bIUh\3Kxd4To MWCyOFkxPjF|Nx?=
Mel-RMU MVPHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MmjkglExOCEQvF2= Mn3pSG1UVw>? NVPFd4NScW6qaXLpeJMhfGinIHfyc5d1cA>? MUKyOFkxPjF|Nx?=
Mel-JD NFfUWo5Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NYfiZY9MhjFyMDFOwG0> MkXHSG1UVw>? NYXz[3AzcW6qaXLpeJMhfGinIHfyc5d1cA>? MkPjNlQ6ODZzM{e=
Mel-RM NGDuZ4tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MoOyglExOCEQvF2= MoDjSG1UVw>? MoTJbY5pcWKrdIOgeIhmKGe{b4f0bC=> MXeyOFkxPjF|Nx?=
Me007 MojYRZBweHSxc3nzJIF{e2G7 M4\P[54yODBizszN Ml;BSG1UVw>? M4SxdIlv\HWlZYOgZZBweHSxc3nz Ml;yNlQ6ODZzM{e=
SK-Mel-28 NFHJNY1CeG:ydH;zbZMh[XO|YYm= M3TqTp4yODBizszN MYHEUXNQ M{T6[Ilv\HWlZYOgZZBweHSxc3nz MYOyOFkxPjF|Nx?=
Mel-RMU M37GSWFxd3C2b4Ppd{Bie3OjeR?= NUWx[lhYhjFyMDFOwG0> NILLZotFVVOR M1i0folv\HWlZYOgZZBweHSxc3nz MkfzNlQ6ODZzM{e=
Mel-JD NF;jT|FCeG:ydH;zbZMh[XO|YYm= MkHIglExOCEQvF2= NYfCdo55TE2VTx?= MlnFbY5lfWOnczDhdI9xfG:|aYO= M1X5eVI1QTB4MUO3
Mel-RM MVrBdI9xfG:|aYOgZZN{[Xl? NUPCcYZ3hjFyMDFOwG0> MWrEUXNQ MnLsbY5lfWOnczDhdI9xfG:|aYO= NICzeFQzPDlyNkGzOy=>
Me007 MnvQSpVv[3Srb36gZZN{[Xl? MWmxNEDPxE1? NX7td5BXTE2VTx?= MoXEbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDifUB2eHKnZ4XsZZRqd25ib3[gdFIy MUWyOFkxPjF|Nx?=
SK-Mel-28 M1LRZmZ2dmO2aX;uJIF{e2G7 M3uwNlExKM7:TR?= NFrubGhFVVOR MYLpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHL5JJVxemWpdXzheIlwdiCxZjDwNlE> MnvVNlQ6ODZzM{e=
Mel-RMU NXXZUIR5TnWwY4Tpc44h[XO|YYm= NHXueGMyOCEQvF2= M3HuNmROW09? MoXIbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dDDifUB2eHKnZ4XsZZRqd25ib3[gdFIy NEPCVm0zPDlyNkGzOy=>
Mel-JD NFWzXFJHfW6ldHnvckBie3OjeR?= NGqwZ3QyOCEQvF2= M4DrTmROW09? MVTpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHL5JJVxemWpdXzheIlwdiCxZjDwNlE> NWfXWZU5OjR7ME[xN|c>
Mel-RM MnHPSpVv[3Srb36gZZN{[Xl? MXyxNEDPxE1? NF3LZVlFVVOR MXLpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2IHL5JJVxemWpdXzheIlwdiCxZjDwNlE> MkW3NlQ6ODZzM{e=
Me007 NV3xV3RCTnWwY4Tpc44h[XO|YYm= NFK4V3AyOCEQvF2= MonhSG1UVw>? Ml3JeZBz\We3bHH0[ZMheHKxYYDvdJRwfGmlIHHu[EBk\WyuIHP5Z4xmKGG{cnXzeEBo\W6ncx?= MnrtNlQ6ODZzM{e=
SK-Mel-28 M13DfGZ2dmO2aX;uJIF{e2G7 NWPwXHU3OTBizszN MWTEUXNQ MoHJeZBz\We3bHH0[ZMheHKxYYDvdJRwfGmlIHHu[EBk\WyuIHP5Z4xmKGG{cnXzeEBo\W6ncx?= M3;yclI1QTB4MUO3
Mel-RMU MYTGeY5kfGmxbjDhd5NigQ>? NVHkTZVWOTBizszN M3XXeWROW09? M2HheZVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= M1\Q[lI1QTB4MUO3
Mel-JD MoK2SpVv[3Srb36gZZN{[Xl? M3;tPFExKM7:TR?= MkO2SG1UVw>? MmTEeZBz\We3bHH0[ZMheHKxYYDvdJRwfGmlIHHu[EBk\WyuIHP5Z4xmKGG{cnXzeEBo\W6ncx?= MlrWNlQ6ODZzM{e=
Mel-RM M2S5WmZ2dmO2aX;uJIF{e2G7 MmjKNVAh|ryP NYWxO4pyTE2VTx?= M2HvZpVxemWpdXzheIV{KHC{b3Hwc5B1d3SrYzDhcoQh[2WubDDjfYNt\SCjcoLld5Qh\2WwZYO= NFvnT5YzPDlyNkGzOy=>

... 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]

- Collapse

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]

- Collapse
  • 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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    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