SH-4-54

Catalog No.S7337

For research use only.

SH-4-54 is a potent STAT inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively.

SH-4-54 Chemical Structure

CAS No. 1456632-40-8

Selleck's SH-4-54 has been cited by 42 publications

Purity & Quality Control

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Biological Activity

Description SH-4-54 is a potent STAT inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively.
Targets
STAT3 [1]
(Cell-free assay)
STAT5 [1]
(Cell-free assay)
300 nM(Kd) 464 nM(Kd)
In vitro

SH-4-54 shows unprecedented cytotoxicity in human glioblastoma brain cancer stem cells (BTSCs), while has no toxicity in human fetal astrocytes. In addition, SH-4-54 effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
127EF NFvzfXhEgXSxdH;4bYNqfHliYYPzZZk> MnXYN{Bl[Xm| NF\Cfo9EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckAyOjeHRjDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA{KGSjeYOgZpkhSWyjbXHyJGJtfWViYYPzZZktKEmFNUC9NE4xPjcQvF2u MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[xNkc,OjR7MEC2NVI9N2F-
30M MYjDfZRwfG:6aXPpeJkh[XO|YYm= NHnxR5M{KGSjeYO= MXPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjCzNG0h[2WubIOgZZN{\XO|ZXSgZZMh[2WubDD2bYFjcWyrdImgZYZ1\XJiMzDkZZl{KGK7IFHsZY1ieiCEbIXlJIF{e2G7LDDJR|UxRTBwMd88UU4> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[xNkc,OjR7MEC2NVI9N2F-
84EF M3rtTWN6fG:2b4jpZ4l1gSCjc4PhfS=> MYezJIRigXN? NHvmb2VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckA5PEWIIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFMh\GG7czDifUBCdGGvYYKgRox2\SCjc4PhfUwhUUN3ME2wMlExOs7:TT6= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[xNkc,OjR7MEC2NVI9N2F-
67EF M{S2NWN6fG:2b4jpZ4l1gSCjc4PhfS=> NInIbo8{KGSjeYO= MU\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjC2O2VHKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIFnfGW{IEOg[IF6eyCkeTDBcIFu[XJiQnz1[UBie3OjeTygTWM2OD1yLkGwOu69VS5? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[xNkc,OjR7MEC2NVI9N2F-
73EF NYT6WlJ6S3m2b4TvfIlkcXS7IHHzd4F6 NGfDR|I{KGSjeYO= MmfzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gO|NGTiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjCzJIRigXNiYomgRYxidWG{IFLseYUh[XO|YYmsJGlEPTB;MD6xOlLPxE1w M2fmOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlEzLz5{NEmwNFYyOjxxYU6=
25EF NEXHdIREgXSxdH;4bYNqfHliYYPzZZk> NHrvRpE{KGSjeYO= M2KyfmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJFI2TUZiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgN{Bl[Xm|IHL5JGFt[W2jcjDCcJVmKGG|c3H5MEBKSzVyPUCuNlM1|ryPLh?= NGHOWFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFYyOid-MkS5NFA3OTJ:L3G+
30M NW\aVFdrS3m2b4TvfIlkcXS7IHHzd4F6 MkDHPEBl[Xm| NV30TJMzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOzCPIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFgh\GG7czDifUBCdGGvYYKgRox2\SCjc4PhfUwhUUN3ME2wMlQ{|ryPLh?= Mn3lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2NVIoRjJ2OUCwOlEzRC:jPh?=
73M NGrNSIlEgXSxdH;4bYNqfHliYYPzZZk> NVrycVNxQCCmYYnz NXnEcIxvS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hPzOPIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFgh\GG7czDifUBCdGGvYYKgRox2\SCjc4PhfUwhUUN3ME2xMlA{|ryPLh?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[xNkc,OjR7MEC2NVI9N2F-
147EF M4XQSWFxd3C2b4Ppd{Bie3OjeR?= Mk\yNE4yKHSxIEGgeW0> NGf3bIg{KGi{cx?= M4PpRmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iMUS3SWYh[2WubIOgZZN{\XO|ZXSgZZMhWEGUUDDjcIVifmGpZTDheEAxNjFidH:gNUB2VSCjZoTldkA{KGi{czDifUBY\XO2ZYLuJIJtd3S2aX7nJIFv[Wy7c3nz NHH5TFg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFYyOid-MkS5NFA3OTJ:L3G+
147EF NGP0dIdHfW6ldHnvckBie3OjeR?= NEKwOJkxNjFidH:gNUB2VQ>? NUTBV5BqOyCqcoO= NVPweYFbUW6qaXLpeIlwdiCxZjDBT3QheGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJFE1P0WIIHPlcIx{KGG2IECuNUB1dyBzIIXNJIFnfGW{IEOgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdiYX7hcJl{cXN? NXn5NJpiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3OTJpPkK0PVAxPjF{PD;hQi=>
147EF M4K0SWZ2dmO2aX;uJIF{e2G7 NX7KPVhkOC5zIITvJFEhfU1? NUXpOWd5OyCqcoO= MXPJcohq[mm2aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEB[PzB3IHnuJIh2dWGwIEG0O2VHKGOnbHzzJIF1KDBwMTD0c{AyKHWPIHHmeIVzKDNiaILzJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZM> NVqzb|hYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3OTJpPkK0PVAxPjF{PD;hQi=>
73M MmH3SpVv[3Srb36gZZN{[Xl? MUGxJJVO NFK5NYZKdmirYnn0bY9vKG:oIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBifCC\N{C1JIlvKGi3bXHuJFc{VSClZXzsd{BifCBzIIXN MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[xNkc,OjR7MEC2NVI9N2F-
147EF M17jbmZ2dmO2aX;uJIF{e2G7 M1Wx[VIhfG9iN{KgbJJ{ NEHxRlZKdmirYnn0bY9vKG:oIGPURXQ{KGmwIHj1cYFvKDF2N1XGJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iCyaH;zdIhwenmuYYTl[EBD[2xveFygcIV3\WxiYX\0[ZIhOiC2bzC3NkBpenNiYomgW4V{fGW{bjDicI91fGmwZzDhcoFtgXOrcx?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[xNkc,OjR7MEC2NVI9N2F-
147EF MknNSpVv[3Srb36gZZN{[Xl? MlzWNkB1dyB5MjDodpM> MWXJcohq[mm2aX;uJI9nKFOWQWSzJIlvKGi3bXHuJFE1P0WIIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBxcG:|cHjvdplt[XSnZDDjfYNtcW5iREGgcIV3\WxiYX\0[ZIhOiC2bzC3NkBpenNiYomgW4V{fGW{bjDicI91fGmwZzDhcoFtgXOrcx?= NXL3VVNHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3OTJpPkK0PVAxPjF{PD;hQi=>
BT73 MlHSSpVv[3Srb36gZZN{[Xl? NUnxeFJ{OTBibXevb4c> NGXlVlY{KGSjeYO= NYDIW2xVUW5idnn2c{BqdmirYnn0bY9vKG:oIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBqdiC2dX3vdkBw\iCQT1StV2NKTCCvb4Xz[UB5\W6xZ4Lh[pRm\CC5aYToJIh2dWGwIFLUO|Mh[2WubIOgZZQhOTBibXevb4ctKGmyIHHkcYlvcXO2ZYLl[EBieyB2IHThfZMhd25xMzDkZZl{KG:oZjDzZ4hm\HWuZTDt[YF{fXKnZDCyJIhzeyCyb4P0JIxie3RiZH;z[S=> NFG0[oU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFYyOid-MkS5NFA3OTJ:L3G+
BT73 M{DVUWFvfGm2dX3vdkBie3OjeR?= NYHGR2FNOTBibXevb4c> MnfBN{Bl[Xm| M1\0RWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUO|Mh[2WubIOgfIVvd2e{YX\0[YQhcW5iTl;EMXNEUURibX;1d4Uh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6geJVud3Jic3n6[UBifCBzMDDt[{9s\yxiaYCgZYRucW6rc4TldoVlKGG|IESg[IF6eyCxbj:zJIRigXNib3\mJJNkcGWmdXzlJI1m[XO3cnXkJFIhcHK|IIDvd5QhdGG|dDDkc5NmKGK7IHjlcYF1d3i7bHnuM4Vwe2mwIIP0ZYlvcW6p Mkm3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MEC2NVIoRjJ2OUCwOlEzRC:jPh?=
BT73 NEe1PZBCdnSrdIXtc5Ih[XO|YYm= NUPKU3ZEOTBibXevb4c> NILHUHg{KGSjeYO= M1KxWWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUO|Mh[2WubIOgfIVvd2e{YX\0[YQhcW5iTl;EMXNEUURibX;1d4Uh[XO|ZYPz[YQh[XNiaX7keYN1cW:wIH;mJIFxd3C2b4Ppd{BqdiC2dX3vdkBifCBzMDDt[{9s\yxiaYCgZYRucW6rc4TldoVlKGG|IESg[IF6eyCxbj:zJIRigXNib3\mJJNkcGWmdXzlJI1m[XO3cnXkJFIhcHK|IIDvd5QhdGG|dDDkc5NmKGK7IGTVUmVNKGG|c3H5 M4f5R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlEzLz5{NEmwNFYyOjxxYU6=
BT73 NEfyXG5CdnSrdIXtc5Ih[XO|YYm= MYKxNEBu\y:tZx?= NXj3[nhpOyCmYYnz M1GwNGFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUO|Mh[2WubIOgfIVvd2e{YX\0[YQhcW5iTl;EMXNEUURibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[nlibXXhd5VzcW6pIHTve45z\We3bHH0bY9vKG:oIFvpOlcheHKxdHXpckBmgHC{ZYPzbY9vKGG2IEGwJI1oN2upLDDpdEBi\G2rbnnzeIVz\WRiYYOgOEBl[Xm|IH;uM|Mh\GG7czDv[oYhe2OqZXT1cIUhdWWjc4Xy[YQhOiCqcoOgdI9{fCCuYYP0JIRwew>? NEHYPYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFYyOid-MkS5NFA3OTJ:L3G+
Vero NYnMRVBETnWwY4Tpc44h[XO|YYm= MWTW[ZJwKGOnbHzzJJZq[WKrbHn0fUBkd3WwdHXyd4Nz\WWwIH\vdkByWlRvUFPSJJFJXFNiYYPzZZkhd2Zic3Xs[YN1\WRiWnnrZUB3cXK3czDpcohq[mm2b4Lz MmfGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzN{Mkm1OFUoRjN|MkK5OVQ2RC:jPh?=
Assay
Methods Test Index PMID
Western blot LMP1 / p-STAT3 / STAT3 28445949
In vivo In mice orthotopically xenografted with BT73, SH-4-54 (10 mg/kg i.p.) exhibits BBB permeability, potently suppresses glioma tumor growth, and inhibits pSTAT3. [1]

Protocol (from reference)

Kinase Assay:

[1]

  • Surface Plasmon Resonance (SPR) studies:

    The binding experiments are carried out on a ProteOn XPR36 biosensor at 25°C using the HTE sensor chip. The flow cells of the sensor chip are loaded with a nickel solution at 30 μL/min for 120 s to saturate the Tris–NTA surface with Ni(II) ions. Purified His-tagged STAT3 and STAT5 in PBST buffer (PBS with 0.005% (v/v) Tween-20 and 0.001% DMSO pH 7.4) is injected in the first and second channels of the chip respectively in the vertical direction at a flow rate of 25 μg/μL for 300 s, which attained, on average, ~8000 resonance unit (RU). After a wash with PBST buffer, inhibitors binding to the immobilized proteins is monitored by injecting a range of concentrations along with a blank at a flow rate of 100 μL/min for 200 s for each of these small molecules. When the injection of the small molecule inhibitor is completed, running buffer is allowed to flow over the immobilized substrates for the non-specifically bound inhibitors to dissociate for 600 s. Following dissociation of the inhibitors, the chip surface is regenerated with an injection of 1 M NaCl at a flow rate of 100 μL/ml for 18 s. Interspot channel reference is used for non-specific binding corrections and the blank channel used with each analyte injection served as a double reference to correct for possible baseline drift. Data are analyzed using ProteOn Manager Software version 3.1. The Langmuir 1:1 binding model was used to determine the KD values.

Cell Research:

[1]

  • Cell lines: BTSC lines 25M, 67EF, 73EF, 84EF and 127EF
  • Concentrations: ~25 μM
  • Incubation Time: 72 hours
  • Method:

    BTSC spheres are dissociated to single cells with the enzyme Accumax, seeded at 1500 cells/ 96-well and treated with drug or vehicle (DMSO) one day after plating. Cytotoxicity studies are repeated independently using BTSC lines 25M, 67EF, 73EF, 84EF and 127EF. BTSC spheres are dissociated to single cells as above and plated in 96 well plates in triplicate at 3000 cells/ 96-well. In both sets of experiments drugs are used as serial dilutions within the range of 5 μM to 100 nM in the first set and 25 μM to 10 nM. Cell viability following drug treatment is assessed three days later using the alamarBlue assay according to the manufacturer’s instructions. All culture experiments are performed in triplicate with a minimum of three wells per condition.

Animal Research:

[1]

  • Animal Models: NOD-SCID bearing ed with BT73 glioma xenografts
  • Dosages: Suspended in 50% polyethylene glycol 300 in water
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(163.77 mM)
Ethanol 50 mg/mL warmed
(81.88 mM)
Water Insoluble

Chemical Information

Molecular Weight 610.59
Formula

C29H27F5N2O5

CAS No. 1456632-40-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(CC(=O)N(CC1=CC=C(C=C1)C2CCCCC2)C3=CC=C(C=C3)C(=O)O)S(=O)(=O)C4=C(C(=C(C(=C4F)F)F)F)F

In vivo Formulation Calculator (Clear solution)

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

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% 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

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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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