MG-132 化学構造
分子量: 475.62

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製品説明

  • Compare Proteasome Inhibitors
    Proteasome製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 MG-132は、100nMのIC50によるプロテアソームの強力な阻害剤です。
ターゲット

Proteasome

IC50

100 nM [1]

In vitro試験 MG-132 displays >1000 times more activity than ZLLal in inhibiting the ZLLL-MCA-degrading activity of 20S proteasome with IC50 of 100 nM versus 110 μM. MG-132 also inhibits calpain with IC50 of 1.2 μM. MG-132 induces neurite outgrowth in PC12 cells at an optimal concentration of 20 nM, displaying 500 times more potency than ZLLal. [1] MG-132 (10 μM) potently inhibits TNF-α-induced NF-κB activation, interleukin-8 (IL-8) gene transcription, and IL-8 protein release in A549 cells by inhibition of proteasome-mediated IκBα degradation. [2] MG-132 treatment potently induces p53-dependent apoptosis in KIM-2 cells by 26S proteasome inhibition. [3] Unlike BzLLLCOCHO or PS-341, MG-132 treatment results in weak inhibition of the chymotrypsinlike (CT-L) and peptidylglutamyl peptide hydrolysing (PGPH) activities of the 26S proteasome, whereas multiple myeloma cells (U266 and OPM-2) are more sensitive to induction of apoptosis by MG-132 than BzLLLCOCHO. [4] MG-132 (1 μM) sensitizes TRAIL-resistant prostate cancer cells by activating the AP-1 family members c-Fos and c-Jun, which, in turn, repress the antiapoptotic molecule c-FLIP(L). [5] MG-132 significantly enhances the ability of inositol hexakisphosphate (IP6) to reduce cellular metabolic activity in both PC3 and DU145 androgen-independent prostate cancer (AIPCa) cell lines. [6]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity Description
LPS-stimulated RAW264.7 cells MlHpSpVv[3Srb36gRZN{[Xl? NISxbHAzPSEQvF2= MY\EUXNQ NVPTcVdRUW6qaXLpeJMhdmm2cnnjJI95cWSnIIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDBwMTFOwG0>
HL-60 MWXDfZRwfG:6aXOgRZN{[Xl? Mlf1OFAh|ryP M4PlN|Q5KGh? MXTEUXNQ NVjINmtLUUN3MEyxNEDPxE1?
SMMC-7721 NVPGXmJTS3m2b4TvfIlkKEG|c3H5 NE\LS3Q1OCEQvF2= NUjEOFFDPDhiaB?= Mlj4SG1UVw>? M4\ES2lEPTB;Nz6xJO69VQ>?
A-549 MnXoR5l1d3SxeHnjJGF{e2G7 MYC0NEDPxE1? NYfjbZFKPDhiaB?= MliwSG1UVw>? MVjJR|UxRDFyIN88US=>
MCF-7 NH;mWpJEgXSxdH;4bYMhSXO|YYm= NX;QPVZqPDBizszN NX7aOpJCPDhiaB?= NFS2dYNFVVOR NYTCWHZsUUN3ME23MlMh|ryP
SW-480 NWiwOGpHS3m2b4TvfIlkKEG|c3H5 Mn\3OFAh|ryP NIX0d4c1QCCq NY\4[VBGTE2VTx?= MnPqTWM2OD12IN88US=>
NCI-H929 NVvrZmZmS3m2b4TvfIlkKEG|c3H5 NHPOU4kyKM7:TR?= Mnn5O|IhcA>? MXvEUXNQ NU\3fFZrUUN3ME2wMlE4KM7:TR?=
293T MYDDfZRwfG:6aXOgRZN{[Xl? NYnJS3A1OTBizszN MU[3NkBp NVvjWWxQTE2VTx?= NIDzToZKSzVyPEKg{txO
293T M1T4UWZ2dmO2aX;uJGF{e2G7 M1v2[|ExKM7:TR?= NVLIXJVkOjRiaB?= NUHu[IxnTE2VTx?= M4\YTW1w\GW{YYTlcJkhcW6mdXPld{Bp\WG2LYPoc4NsKCB?
HeLa MXLLbY5ie2ViQYPzZZk> MYqxNEDPxE1? M1fYPVEhcA>? NX;QcFhSTE2VTx?= NUX5NW5bUW6mdXPld{BRSVKSIHPs[YF3[WenIHL5JIlvcGmkaYTpcocheHKxc3Xhd49u\SCjY4Tpeol1gQ>?
MDA-MB-231 MojDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XQb|Eh|ryP MkHDO|IhcA>? MojVSG1UVw>? MXLJR|UxRTBwMUig{txO
MCF-7 M4rMeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK3NUDPxE1? M4H1fFczKGh? MnXsSG1UVw>? NF\3PWdKSzVyPUCuNVMh|ryP
MCF10A MkOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrrTo9iOSEQvF2= MYC3NkBp MWjEUXNQ NUDq[pRxUUN3ME2wMlI6KM7:TR?=
HEK-293 NYT2[poxU2mwYYPlJGF{e2G7 MXyyJIFv\CB{MDFOwG0> NE\xRmUzKGh? NETGNJFFVVOR M2L3U2lvcGmkaYTzJGNpXC2OIHHjeIl3cXS7IIfpeIghUUN3MDDv[kA6KG6PIB?=
Calu6 NVK0eHhpTnWwY4Tpc44hSXO|YYm= NInoUmQyOCEQvF2= NVO5cXF2OThiaB?= M3faXWROW09? NYrVbGZrW2mpbnnmbYNidnSueTDhZ4N2dXWuYYTld{BnemG2YYjpckBxemWldYLzc5I>
IFN-gamma-induced RAW264.7 NGr2XIxHfW6ldHnvckBCe3OjeR?= MWfEUXNQ Mm\aTY5pcWKrdIOgcol1emmlIH;4bYRmKHC{b3T1Z5Rqd25id3n0bEBKSzVyIH;mJFAvODd5IN88US=>
IPC227F MmW3R5l1d3SxeHnjJGF{e2G7 MXyxJO69VQ>? MkX0OFghcA>? M2rPW2ROW09? NIj2[4JKSzVyPUCuNFc4KM7:TR?=
Hepa-1c1c7 MUDGeY5kfGmxbjDBd5NigQ>? M1zBZlI2KM7:TR?= Mnz6OkBp NYKwT2pkTE2VTx?= MlzkTY5kemWjc3XzJG5z\jJicILveIVqdiCuZY\lcC=>
COS-7 MV\DfZRwfG:6aXOgRZN{[Xl? MoX5NVAh|ryP M{jxfGROW09? MoXSTWM2ODxzMDFOwG0>
HuH-7 M4j4[2N6fG:2b4jpZ{BCe3OjeR?= MW[xNEDPxE1? M{\SfmROW09? M17HW2lEPTB:MUCg{txO
OCI-Ly3 MWLGeY5kfGmxbjDBd5NigQ>? MVixNEDPxE4EoB?= MVu0JIg> M{jSNWROW09? NEDN[FNKdmS3Y3XzJIh2dWGwIFnrZZBx[UKjbIDoZUB{fGGkaXzpfoF1cW:wIIfpeIghTUN3MDDv[kAyKM7:TR?=
A2780 cDDP NYD1[otmSXCxcITvd4l{KEG|c3H5 NIHUUpgzPCCq NVHjNmpyTE2VTx?= NY\GbFdmUW6mdXPld{BieG:ydH;zbZMh[nliaX7obYJqfGmwZzDQWGVPKGSnZ4Lh[IF1cW:w
LPS-stimulated RAW264.7 cells M{fhWGZ2dmO2aX;uJGF{e2G7 M2\jeWROW09? MnH2TY5pcWKrdIOgUmYuc2GycHHCJGRPSSCkaX7kbY5o
PC12 NF\6W3pHfW6ldHnvckBCe3OjeR?= MWKxNFAh|ryPwrC= MkLONlQhcA>? M4rLeWROW09? M2i4N2lvcGmkaYTzJFYuV0iGQT2gZY5lKEh{T{KtbY5lfWOnZDDjfZRwfG:6aXPpeJk>
PC3 M4r5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWP4VHhnOjBizszN NIPyTYc1QCCq NUTMZlNXTE2VTx?= NYWy[VNVUUN3ME2wMlYh|ryP
LP-1 Mni4RZBweHSxc3nzJGF{e2G7 MleyN|AxKG6P NHHSUVEzPCCq M3vrOmROW09? NWrLXYhTUW6mdXPld{BieG:ydH;zbZMh[nliaX7jdoVie2mwZzDjcIVifmWmIGDBVnAhdGW4ZXygZY5lKHKnZIXjbY5oKE2lbD2xJJBzd3SnaX6gcIV3\Wx?
ES6 NYjVcFlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrTTWM2OD1yLkCxN|A3KM7:TR?=
A101D NUT1OFRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvSdoNKSzVyPUCuNFMzPzlizszN
OCUB-M NEDBbo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml[zTWM2OD1yLkCzO|M4KM7:TR?=
LB2518-MEL NFXrSJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LE[2lEPTB;MD6wN|c3KM7:TR?=
SH-4 NHrPcYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnv1TWM2OD1yLkC0N|Eh|ryP
KNS-42 Mn;NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LaSWlEPTB;MD6wOFQ1OSEQvF2=
DSH1 Mm[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYGy[lNsUUN3ME2wMlA2Ojh7IN88US=>
NTERA-S-cl-D1 MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLaTWM2OD1yLkC1O|czKM7:TR?=
D-542MG M1LHcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwMEW5OVch|ryP
KS-1 M2rFd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mny2TWM2OD1yLkC2OFU5KM7:TR?=
BL-41 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\4TWM2OD1yLkC2PVQ4KM7:TR?=
LXF-289 Mn:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;SSZBKSzVyPUCuNFcxPjZizszN
D-247MG NYfyOWhOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTBwMEeyNFkh|ryP
MMAC-SF MljGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfMTWM2OD1yLkC3NlY5KM7:TR?=
CP66-MEL M1m0dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTBwMEe1JO69VQ>?
LB771-HNC NHOzSFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHFTWM2OD1yLkC4NFM3KM7:TR?=
no-10 NHLj[oRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjxdmJYUUN3ME2wMlA5QTB7IN88US=>
A388 MnHlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTBwMEmwOlUh|ryP
OPM-2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrnO3hmUUN3ME2wMlExPDd2IN88US=>
OVCAR-4 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3IdHJYUUN3ME2wMlExQTN6IN88US=>
HOP-62 M4P2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTBwMUC5OFkh|ryP
ML-2 M2P4[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWK5cnV{UUN3ME2wMlEyQDB4IN88US=>
UACC-257 NYHqXVRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjiRWg6UUN3ME2wMlEyQTJ5IN88US=>
NEC8 NXn3bYF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEP5PWVKSzVyPUCuNVE6QTVizszN
ONS-76 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjvdnVKSzVyPUCuNVI6OzVizszN
KE-37 M3voRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn75TWM2OD1yLkGzNlc5KM7:TR?=
HT-144 Ml\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfWTWM2OD1yLkGzPFk2KM7:TR?=
LB2241-RCC NYCwZ4FFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTBwMUSyOFch|ryP
TE-5 MonhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwMUSyO|gh|ryP
KINGS-1 MmXLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfmTWM2OD1yLkG0O|kh|ryP
NCI-H69 MoSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGO3emJKSzVyPUCuNVUyPDFizszN
CAS-1 M4[wfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\oTWM2OD1yLkG1OFgzKM7:TR?=
D-263MG MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPxb29KSzVyPUCuNVYxODZizszN
A253 NIr3T4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPiTWM2OD1yLkG2NVI5KM7:TR?=
PF-382 NU\LVoh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTBwMU[3NFYh|ryP
CESS NWnCUIMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\jb5lmUUN3ME2wMlE4ODZizszN
MZ2-MEL NHv2fIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mki3TWM2OD1yLkG3OVU6KM7:TR?=
HEL NWW4d4dFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rkZWlEPTB;MD6xPFUyPyEQvF2=
D-392MG MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTBwMUmxNVUh|ryP
SK-LMS-1 M4rieWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{OzOGlEPTB;MD6xPVMxOyEQvF2=
GI-ME-N Mmq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwMUmzNFYh|ryP
LB831-BLC MkLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEC3[FlKSzVyPUCuNVk{PCEQvF2=
DU-4475 MlvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;ieHVKSzVyPUCuNVk3PThizszN
IST-SL1 NELUOIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\CV5pVUUN3ME2wMlIxODl2IN88US=>
GAK MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHn5clZKSzVyPUCuNlA2OzRizszN
EW-1 NH3WcYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfLNm5RUUN3ME2wMlIyODR5IN88US=>
LAMA-84 NWnr[JlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmixTWM2OD1yLkKxPFUyKM7:TR?=
SK-UT-1 NHfWc5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M12wTmlEPTB;MD6yNlA1QSEQvF2=
VA-ES-BJ MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojoTWM2OD1yLkKyNlU4KM7:TR?=
ACN NEHxUIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4q4TmlEPTB;MD6yNlY{QCEQvF2=
SK-PN-DW MoHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnDTWM2OD1yLkKzNVkh|ryP
HD-MY-Z NYLnRZNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTBwMkOzNFMh|ryP
LB373-MEL-D M{TmNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\1emlEPTB;MD6yOFE6QCEQvF2=
COLO-829 NHOyWJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHzpXIlKSzVyPUCuNlQzPTdizszN
ES8 M4XJN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfHT|FlUUN3ME2wMlI1PzZ|IN88US=>
RXF393 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;kRWlEPTB;MD6yOVAyPSEQvF2=
TK10 NF[x[3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jiOmlEPTB;MD6yOVQ{PSEQvF2=
LOUCY M2fTVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHn3dGVKSzVyPUCuNlU1PTZizszN
MZ7-mel NHL2ZmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTBwMk[zO|Qh|ryP
CP67-MEL MoTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnzTWM2OD1yLkK2O|Mh|ryP
C2BBe1 M32xRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXOXWQ3UUN3ME2wMlI4QTB5IN88US=>
K052 NH7tN|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHGfYl1UUN3ME2wMlI5QTlizszN
MOLT-16 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjVfpVTUUN3ME2wMlI6PTJ2IN88US=>
KNS-81-FD NWrHNYdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\kTWM2OD1yLkOwN|I{KM7:TR?=
CMK M3XRXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwM{GxNkDPxE1?
LAN-6 Mk\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTt[m9KSzVyPUCuN|E{KM7:TR?=
KLE MkGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwM{GzNFYh|ryP
NCCIT NWHqfVNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTBwM{G3PFMh|ryP
HH NHr6OotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnNTWM2OD1yLkOyPFk4KM7:TR?=
TE-8 MnXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwM{SyO|kh|ryP
GDM-1 NGLiNI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XnbmlEPTB;MD6zOVExPCEQvF2=
NCI-H747 NFq0[o1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTBwM{exNFMh|ryP
NCI-H1092 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwM{i4OFQh|ryP
8-MG-BA NFrre49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTMTWM2OD1yLkO5PFM4KM7:TR?=
NB17 NETMcXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVruWmVnUUN3ME2wMlQzQTdizszN
LC4-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTXNnN6UUN3ME2wMlQ{PjB5IN88US=>
TE-1 NXXzdnI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fBNmlEPTB;MD60OVEyQSEQvF2=
KALS-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3JTWM2OD1yLkS2OVg1KM7:TR?=
CCRF-CEM NXfrd3R2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPJTWM2OD1yLkS3Olc1KM7:TR?=
OS-RC-2 NITpdXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTBwNEe5O|Ih|ryP
A704 NUP3UYJYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjKNWZKSzVyPUCuOFg3QTJizszN
BB49-HNC M13hTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\GTWM2OD1yLkS5NFk3KM7:TR?=
EVSA-T NVS4R21VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTBwNEm5NVEh|ryP
Mo-T M1W1R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETMdpJKSzVyPUCuOVE4PjJizszN
MONO-MAC-6 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLrboZKSzVyPUCuOVM3OTFizszN
BB65-RCC NVzUV2JDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULlPG5sUUN3ME2wMlU3QDFzIN88US=>
NCI-H1882 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mke2TWM2OD1yLkW5NFM3KM7:TR?=
TE-9 NVyzdJdUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkS5TWM2OD1yLk[xNFM{KM7:TR?=
NCI-H2126 NXXhd29VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTBwNkK2Olkh|ryP
SF268 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfmUlV2UUN3ME2wMlY2PjRzIN88US=>
SW872 NGXkcIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvIbYVKSzVyPUCuOlU4OjlizszN
LS-513 NGCz[oVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4r0cGlEPTB;MD62Olc2OSEQvF2=
NCI-H1355 MlnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoexTWM2OD1yLk[4OlE6KM7:TR?=
BL-70 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIricG1KSzVyPUCuOlk{QDhizszN
NCI-SNU-5 MmPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDKcJhWUUN3ME2wMlY6PTR3IN88US=>
SNU-C2B NGX0Z3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTr[ZBKSzVyPUCuO|A4OzlizszN
GB-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTBwN{KxNlQh|ryP
CTB-1 NXLVTlU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LtT2lEPTB;MD63O|k2PSEQvF2=
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HCC1599 NULMdIZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4T6V2lEPTB;N{SuPFc{OiEQvF2=
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DOHH-2 NFrI[IZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTd2Lkm1NVQh|ryP
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LU-134-A NGTPXZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPHU5NQUUN3ME24N{4yOzVzIN88US=>
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NCI-H720 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXs[XhKSzVyPUm4MlQxPjFizszN
NCI-H446 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTl7Lke1PFgh|ryP
NCI-H889 MkmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkK0TWM2OD1zMESuNlQzKM7:TR?=
EW-22 M2PMd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX24RnJEUUN3ME2xNFYvOTlizszN
BV-173 M4Wwc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTOWpZKSzVyPUGwPE44OjhizszN
WSU-NHL NXvxT3ZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLDTWM2OD1zMEmuOlcyKM7:TR?=
MN-60 Ml62S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3G1dGlEPTB;MUC5MlY6KM7:TR?=
DG-75 NGflVndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYKwfI53UUN3ME2xNVMvOzV{IN88US=>
DMS-79 M3vHXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13TNWlEPTB;MUG3MlM5OiEQvF2=
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DMS-153 M4rhU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXLPGRKSzVyPUGyNU44PDVizszN
NCI-H510A NYX3SFRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTF{Nz6zNkDPxE1?
BE-13 NV30Tnp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTF|ND6wOFQh|ryP
KP-N-YS NGrDfHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfjSZBKSzVyPUGzPU44OzZizszN
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EW-12 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHZUY1IUUN3ME2xOFQvPjl7IN88US=>
NB14 NGT1UJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4D0ZmlEPTB;MUS3MlA5OiEQvF2=
MDA-MB-134-VI M{Ltd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTF2OD6yOlgh|ryP
NCI-H1770 MnPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknNTWM2OD1zNU[uNlc6KM7:TR?=
TUR MmnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nSZmlEPTB;MU[3Mlg4KM7:TR?=
NCI-H1417 NEfF[pRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H5SWlEPTB;MUiwMlM{OSEQvF2=
IMR-5 M3\hNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe2W|VKSzVyPUG4NU42PzFizszN
NCI-H226 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVewSlVoUUN3ME2xPFgvQDZ4IN88US=>
NCI-H187 MonYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTF7MD6wOlQh|ryP
SF539 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M131VWlEPTB;MUmyMlczQCEQvF2=
TALL-1 NITUXlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfVUnRKSzVyPUG5PE4{ODRizszN
TE-441-T NEDueWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2jOWGlEPTB;MUm5Mlc{QSEQvF2=
REH MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;6TWM2OD1{M{[uOlI3KM7:TR?=
MS-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFO1Wm5KSzVyPUKzPU4yOjFizszN
THP-1 MkLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEi0cFhKSzVyPUK2OE44OzhizszN
NCI-H1838 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XYS2lEPTB;MkexMlQ2PiEQvF2=
P30-OHK M4DnbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PabGlEPTB;MkizMlg1PyEQvF2=
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... Click to View More Cell Line Experimental Data

In vivo試験 Administration of MG-132 effectively rescues the expression levels and plasma membrane localization of dystrophin, β-dystroglycan, α-bdystroglycan, and α-sarcoglycan in skeletal muscle fibers from mdx mice, reduces muscle membrane damage, and ameliorates the histopathological signs of muscular dystrophy. [7] MG-132 treatment significantly reduces immobilization-induced skeletal muscle atrophy in mice, by downregulating the muscle-specific ubiquitin ligases atrogin-1/MAFbx and MuRF-1 mRNA. [8]
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

Measurement of inhibitory activities of MG-132 against 20S proteasome The reaction mixture for the 20S proteasome inhibitory assay contains 0.1 M Tris-acetate, pH 7.0, 20S proteasome, MG-132, and 25 μM substrate dissolved in dimethyl sulfoxide in a final volume of 1 mL. After incuba tion at 37 °C for 15 minutes, the reaction is stopped by the addition of 0.1 mL of 10% SDS and 0.9 mL of 0.1M Tris acetate, pH 9.0. The fluorescence of the reaction products is measured. To determine the IC50 against 20S proteasome, various concentrations of MG-132 are included in the assay mixture.

細胞アッセイ:

[3]

細胞株 KIM-2, HC11, and ES
濃度 Dissolved in DMSO, final concentrations ~25 μM
反応時間 24, and 48 hours
実験の流れ

Cells are exposed to various concentrations of MG-132 for 24, and 48 hours. Supernatant and monolayer cells are harvested by centrifugation and fixed in 70% ethanol in PBS for staining with acridine orange. Equal volumes of cells and acridine orange (5 mg/mL in PBS) are mixed on a microscope slide and examined by fluorescence microscopy. For annexin V analysis, cells are harvested by centrifugation and stained with annexin V and propidium iodide. For cell cycle analysis, cells are rehydrated in PBS at room temperature for 10 minutes, followed by staining with propidium iodide (5 mg/mL). All samples are analyzed using a Coulter Epics XL flow cytometer.

動物実験:

[7]

動物モデル Male mdx (C57BL/10ScSn DMD mdx) mice
製剤 Dissolved in DMSO, and diluted in PBS
投薬量 ~10 μg/kg/day
投与方法 Injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download MG-132 SDF
分子量 475.62
化学式

C26H41N3O5

CAS No. 133407-82-6
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 95 mg/mL (199.73 mM)
エタノール 95 mg/mL (199.73 mM)
<1 mg/mL (<1 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80, pH 4 6 mg/mL
* <1 mg/ml means slightly soluble or 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.
化学名 benzyl (S)-4-methyl-1-((S)-4-methyl-1-((S)-4-methyl-1-oxopentan-2-ylamino)-1-oxopentan-2-ylamino)-1-oxopentan-2-ylcarbamate

カスタマーフィードバック (9)


Click to enlarge
Rating
Source Nat Cell Biol, 2015, 17(1), 95-103. MG-132 purchased from Selleck
Method Immunoprecipitation
Cell Lines MDA-MB-231 cells
Concentrations 10 uM
Incubation Time 6 h
Results SIAH2 destabilizes LATS2 through proteasome. SIAH2-mediated LATS2 degradation was inhibited by proteasomal inhibitor MG132, but not by lysosomal inhibitor BA-1. The half-life of LATS2 was shortened by SIAH2.

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Source Nucleic Acids Res, 2014, 42(1), 458-74. MG-132 purchased from Selleck
Method Western blot
Cell Lines HeLa cells
Concentrations 20 uM
Incubation Time 8 h
Results As RMND5A downregulation resulted in a rapid decrease of protein Exportin-5, this effect was partially abolished by the proteasome inhibitor MG132, indicating that RMND5A protect Exportin-5 protein against proteasome degradation.

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Source Nucleic Acids Res, 2014, 42(1), 458-74. MG-132 purchased from Selleck
Method Immunocytochemistry
Cell Lines HeLa cells
Concentrations 20 uM
Incubation Time 8 h
Results It was surprised to observe that Exportin-5 retention in nucleus when its protein levels were downregulated by RMND5A siRNA or miR-138. The proteasome inhibitor MG132 could recover not only Exportin-5 protein levels but also its normal subcellular localization.

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Source EMBO Mol Med, 2013, 5, 397-412. MG-132 purchased from Selleck
Method Western Blot
Cell Lines MEF cells
Concentrations 30 uM
Incubation Time 6 h
Results Treatment of MEF with proteasome inhibitor MG132 resulted in similar increase of steady state levels of intracellular ATZ in both GFP- and TFEB- transfected Cells.

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Source Cell Rep, 2015, 11(9), 1458-73. MG-132 purchased from Selleck
Method Western Blot
Cell Lines A375, Lu1205 cells
Concentrations 5 uM
Incubation Time 10 h
Results MG132 treatment increased JAK1 steady-state levels, masking the effect of RNF125 depletion and partially blocking deregulated JAK1 expression by ectopically expressed RNF125.

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Source Plant Physiol, 2012, 60(1), 118-34. MG-132 purchased from Selleck
Method Immunoblot analysis
Cell Lines Arabidopsis thaliana
Concentrations 100 uM
Incubation Time 12 h
Results These rates of loss were markedly slower in the lrb1-1 lrb2-1 background. Importantly, phyB breakdown was also substantially attenuated upon exposing wild-type seedlings to the proteasome inhibitor MG132, thus implicating the 26S proteasome in particular. MG132 treatment also slightly stabilized phyB levels in lrb1-1 lrb2-1 seedlings, implying that other factors besides LRB1 and LRB2 might also direct phyB breakdown.

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Source Toxicol Appl Pharmacol, 2015, 286(2), 135-41. MG-132 purchased from Selleck
Method Immunofluorescence
Cell Lines γ-H2AX-stained cells
Concentrations 100 uM
Incubation Time 3 h
Results G2 cell cycle arrest usually reflects the formation of genomic damage in the preceding S-phase, which activates checkpoint response upon the entry of cells into G2 phase. Furthermore, MG132-treated cells also had larger amounts of γ-H2AX, as evidenced by the increased staining in individual nuclei .

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Source FEBS Lett, 2012, 586, 3787–3792. MG-132 purchased from Selleck
Method Western Blot
Cell Lines Hela cells
Concentrations
Incubation Time 12 h
Results When GSK-3 (Ser9) degradation was blocked by proteasome inhibitor (MG132), the increased amount of phosphorylated GSK-3 (Ser9) in responding to NOK was more clearly observed in the HeLa-NOK-HA cells (Fig. C).

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Source 2012, Dr. Edison DUKE-NUS Graduate Medical School Singapore.. MG-132 purchased from Selleck
Method Western blot
Cell Lines NIH3T3 cells
Concentrations 25 μM
Incubation Time 1-4 h
Results By adding MG132, a proteasome inhibitor, the degradation of Per2 was dramatically decreased within 4 hours treatment.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
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