MG-132 化学構造
分子量: 475.62

品質と確認

製品表彰状(40)

カスタマーレビュー(6)

Quality Control & MSDS

製品情報

  • Compare Proteasome Inhibitors
    Proteasome阻害剤を比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

情報 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。
目標

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 M3v4N2Z2dmO2aX;uJGF{e2G7 MVyyOUDPxE1? NVHFXHV1TE2VTx?= Ml3pTY5pcWKrdIOgcol1emmlIH;4bYRmKHC{b3T1Z5Rqd25id3n0bEBKSzVyIH;mJFAvOSEQvF2=
HL-60 NVTiRlV7S3m2b4TvfIlkKEG|c3H5 MVW0NEDPxE1? NWjzOYJzPDhiaB?= MkPXSG1UVw>? M1TIT2lEPTB:MUCg{txO
SMMC-7721 NFjrNpVEgXSxdH;4bYMhSXO|YYm= NEjVVmQ1OCEQvF2= NYrKd5l7PDhiaB?= MkTQSG1UVw>? MV7JR|UxRTdwMTFOwG0>
A-549 M1Xt[2N6fG:2b4jpZ{BCe3OjeR?= NFHFSIk1OCEQvF2= NV7FVJkyPDhiaB?= NULIRnppTE2VTx?= MkTsTWM2ODxzMDFOwG0>
MCF-7 MmDTR5l1d3SxeHnjJGF{e2G7 NFPRUpM1OCEQvF2= NHfx[|U1QCCq MYDEUXNQ M4fX[WlEPTB;Nz6zJO69VQ>?
SW-480 M1PjV2N6fG:2b4jpZ{BCe3OjeR?= NWTlSGdvPDBizszN M33GNVQ5KGh? MXrEUXNQ M1vVVmlEPTB;NDFOwG0>
NCI-H929 MXXDfZRwfG:6aXOgRZN{[Xl? MV6xJO69VQ>? MVi3NkBp MYLEUXNQ M3rLXmlEPTB;MD6xO{DPxE1?
293T M3q3dWN6fG:2b4jpZ{BCe3OjeR?= NXnRVJdFOTBizszN M1XmSFczKGh? NHjSfYlFVVOR MkHtTWM2ODx{IN88US=>
293T MmS1SpVv[3Srb36gRZN{[Xl? M3PkeFExKM7:TR?= M4\rTlI1KGh? M{Xzb2ROW09? MmnHUY9l\XKjdHXsfUBqdmS3Y3XzJIhm[XRvc3jvZ4shKA>?
HeLa M4D5OGtqdmG|ZTDBd5NigQ>? MVWxNEDPxE1? MkjKNUBp NHj6OWdFVVOR M3TF[mlv\HWlZYOgVGFTWCClbHXheoFo\SCkeTDpcohq[mm2aX7nJJBzd3OnYYPvcYUh[WO2aY\peJk>
MDA-MB-231 NF;HZ4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX:xJO69VQ>? NH;oWGY4OiCq NHrWOWhFVVOR MW\JR|UxRTBwMUig{txO
MCF-7 NXL2NVI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvldWdUOSEQvF2= NFTKUGM4OiCq MX;EUXNQ NEDacmZKSzVyPUCuNVMh|ryP
MCF10A NGHiRoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV[xJO69VQ>? NWW1bWN1PzJiaB?= NIWzO3hFVVOR NYrOW5lYUUN3ME2wMlI6KM7:TR?=
HEK-293 NWixNFFvU2mwYYPlJGF{e2G7 M1zs[FIh[W6mIEKwJO69VQ>? M4nBdVIhcA>? NGjuZXBFVVOR NHvncJJKdmirYnn0d{BEcFRvTDDhZ5Rqfmm2eTD3bZRpKEmFNUCgc4YhQSCwTTC=
Calu6 NH;BV4lHfW6ldHnvckBCe3OjeR?= MVmxNEDPxE1? M1nqSlE5KGh? MV;EUXNQ MnvpV4lodmmoaXPhcpRtgSCjY3P1cZVt[XSnczDmdoF1[XirbjDwdoVkfXK|b4K=
IFN-gamma-induced RAW264.7 NXe5NFNMTnWwY4Tpc44hSXO|YYm= NHXt[WxFVVOR NGHQR|JKdmirYnn0d{BvcXS{aXOgc5hq\GVicILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhOC5yN{eg{txO
IPC227F Mn;IR5l1d3SxeHnjJGF{e2G7 NGfCVZgyKM7:TR?= MofmOFghcA>? NGjFbXZFVVOR M1L2Z2lEPTB;MD6wO|ch|ryP
Hepa-1c1c7 MY\GeY5kfGmxbjDBd5NigQ>? NFrEWYwzPSEQvF2= NFPjbpA3KGh? MoK0SG1UVw>? MmPXTY5kemWjc3XzJG5z\jJicILveIVqdiCuZY\lcC=>
COS-7 NXT3bpNCS3m2b4TvfIlkKEG|c3H5 MX2xNEDPxE1? NYfPNmVmTE2VTx?= MWPJR|UxRDFyIN88US=>
HuH-7 NFHiN4lEgXSxdH;4bYMhSXO|YYm= NH\HUocyOCEQvF2= MoXwSG1UVw>? MkHZTWM2ODxzMDFOwG0>
OCI-Ly3 Mm\kSpVv[3Srb36gRZN{[Xl? NIrvVJgyOCEQvF5CpC=> NG\KbGM1KGh? MkTnSG1UVw>? MWjJcoR2[2W|IHj1cYFvKEmtYYDwZWJidHCqYTDzeIFjcWyrenH0bY9vKHerdHigSWM2OCCxZjCxJO69VQ>?
A2780 cDDP M3\wbGFxd3C2b4Ppd{BCe3OjeR?= MYCyOEBp MljhSG1UVw>? M3\Bd2lv\HWlZYOgZZBweHSxc3nzJIJ6KGmwaHnibZRqdmdiUGTFUkBl\We{YXTheIlwdg>?
LPS-stimulated RAW264.7 cells MmLYSpVv[3Srb36gRZN{[Xl? M3fv[GROW09? NYnVdWREUW6qaXLpeJMhVkZva3HwdIFDKESQQTDibY5lcW6p
PC12 MV3GeY5kfGmxbjDBd5NigQ>? Ml:1NVAxKM7:TdMg MmjtNlQhcA>? M{\SWmROW09? MknaTY5pcWKrdIOgOk1QUESDLTDhcoQhUDKRMj3pcoR2[2WmIHP5eI91d3irY3n0fS=>
PC3 NETsNWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fZPVIxKM7:TR?= M3PGe|Q5KGh? MoHkSG1UVw>? NEPndFBKSzVyPUCuOkDPxE1?
LP-1 Mn7zRZBweHSxc3nzJGF{e2G7 M2HhR|MxOCCwTR?= MWOyOEBp NF;0eotFVVOR MnnGTY5lfWOnczDhdI9xfG:|aYOgZpkhcW6lcnXhd4lv\yClbHXheoVlKFCDUmCgcIV3\WxiYX7kJJJm\HWlaX7nJG1kdC1zIIDyc5RmcW5ibHX2[Yw>
ES6 M1jXT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwMEGzNFYh|ryP
A101D NXHIO|B6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7HN5l6UUN3ME2wMlA{Ojd7IN88US=>
OCUB-M M3nCWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTBwMEO3N|ch|ryP
LB2518-MEL NUXKUYduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUe4fZFoUUN3ME2wMlA{PzZizszN
SH-4 M4DXdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\McmlEPTB;MD6wOFMyKM7:TR?=
KNS-42 NVHkXWlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHETWM2OD1yLkC0OFQyKM7:TR?=
DSH1 M4HEUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTBwMEWyPFkh|ryP
NTERA-S-cl-D1 NX3VZ4NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmKwTWM2OD1yLkC1O|czKM7:TR?=
D-542MG NIfSZZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1i2VGlEPTB;MD6wOVk2PyEQvF2=
KS-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfwTmY2UUN3ME2wMlA3PDV6IN88US=>
BL-41 MkDYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;oVWtKSzVyPUCuNFY6PDdizszN
LXF-289 MmjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3q1UWlEPTB;MD6wO|A3PiEQvF2=
D-247MG NWTvRXpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXBOWpKSzVyPUCuNFczODlizszN
MMAC-SF MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDLOGhKSzVyPUCuNFczPjhizszN
CP66-MEL NYrGZpE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGK3fW1KSzVyPUCuNFc2KM7:TR?=
LB771-HNC MnLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwMEiwN|Yh|ryP
no-10 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDucJVKSzVyPUCuNFg6ODlizszN
A388 NFnR[IVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUHrOHp7UUN3ME2wMlA6ODZ3IN88US=>
OPM-2 M3zUdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDqbpZKSzVyPUCuNVA1PzRizszN
OVCAR-4 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33ZbWlEPTB;MD6xNFk{QCEQvF2=
HOP-62 M13PN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmizTWM2OD1yLkGwPVQ6KM7:TR?=
ML-2 NIn0WI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK2cYZzUUN3ME2wMlEyQDB4IN88US=>
UACC-257 NUX3PZdwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTyTWM2OD1yLkGxPVI4KM7:TR?=
NEC8 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP2TWM2OD1yLkGxPVk2KM7:TR?=
ONS-76 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\lTWM2OD1yLkGyPVM2KM7:TR?=
KE-37 NW\0d2J{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTBwMUOyO|gh|ryP
HT-144 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELieI5KSzVyPUCuNVM5QTVizszN
LB2241-RCC MlrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLsfmVOUUN3ME2wMlE1OjR5IN88US=>
TE-5 M3LO[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUWwUo03UUN3ME2wMlE1Ojd6IN88US=>
KINGS-1 M4L5bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPQcVl5UUN3ME2wMlE1PzlizszN
NCI-H69 M4D4PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTBwMUWxOFEh|ryP
CAS-1 MkXrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorvTWM2OD1yLkG1OFgzKM7:TR?=
D-263MG NHvBfG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHZ[llGUUN3ME2wMlE3ODB4IN88US=>
A253 NYHHeJZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7wWlk{UUN3ME2wMlE3OTJ6IN88US=>
PF-382 M1\ufmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;ERXJKSzVyPUCuNVY4ODZizszN
CESS M4nsfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzxUmdSUUN3ME2wMlE4ODZizszN
MZ2-MEL NHnOVopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTBwMUe1OVkh|ryP
HEL MmnuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwMUi1NVch|ryP
D-392MG MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LpemlEPTB;MD6xPVEyPSEQvF2=
SK-LMS-1 MlfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;xSYFDUUN3ME2wMlE6OzB|IN88US=>
GI-ME-N MoKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTBwMUmzNFYh|ryP
LB831-BLC NHnTZXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTBwMUmzOEDPxE1?
DU-4475 M3TES2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7OTFJKSzVyPUCuNVk3PThizszN
IST-SL1 MnnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTBwMkCwPVQh|ryP
GAK NYPV[I1wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4qzVGlEPTB;MD6yNFU{PCEQvF2=
EW-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXuTWM2OD1yLkKxNFQ4KM7:TR?=
LAMA-84 MnTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1nBSGlEPTB;MD6yNVg2OSEQvF2=
SK-UT-1 MlfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDRTWM2OD1yLkKyNFQ6KM7:TR?=
VA-ES-BJ M2DtWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHkTWM2OD1yLkKyNlU4KM7:TR?=
ACN Mm\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLQfm5vUUN3ME2wMlIzPjN6IN88US=>
SK-PN-DW M3vZWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\udpJvUUN3ME2wMlI{OTlizszN
HD-MY-Z M2faXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTSTWM2OD1yLkKzN|A{KM7:TR?=
LB373-MEL-D NH3wN4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljKTWM2OD1yLkK0NVk5KM7:TR?=
COLO-829 NUfKVYtjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXHSpJKSzVyPUCuNlQzPTdizszN
ES8 MlroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwMkS3OlMh|ryP
RXF393 M1zqb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mor0TWM2OD1yLkK1NFE2KM7:TR?=
TK10 NHHaXXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHvSWFSUUN3ME2wMlI2PDN3IN88US=>
LOUCY NWn0N4g6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTBwMkW0OVYh|ryP
MZ7-mel MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjQNHdQUUN3ME2wMlI3Ozd2IN88US=>
CP67-MEL M33Tb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTBwMk[3N{DPxE1?
C2BBe1 MofoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH0TWM2OD1yLkK3PVA4KM7:TR?=
K052 NGX0Z|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwMki5PUDPxE1?
MOLT-16 MoDnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDLR41VUUN3ME2wMlI6PTJ2IN88US=>
KNS-81-FD NUTCUFhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\Nb2dKSzVyPUCuN|A{OjNizszN
CMK NFH6W4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXYTWM2OD1yLkOxNVIh|ryP
LAN-6 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nU[mlEPTB;MD6zNVMh|ryP
KLE NVv4dpBWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml[xTWM2OD1yLkOxN|A3KM7:TR?=
NCCIT NGK4NFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknzTWM2OD1yLkOxO|g{KM7:TR?=
HH M1\3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjOb2Z1UUN3ME2wMlMzQDl5IN88US=>
TE-8 MnTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrzfG9pUUN3ME2wMlM1Ojd7IN88US=>
GDM-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnQZ|FPUUN3ME2wMlM2OTB2IN88US=>
NCI-H747 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4X3dmlEPTB;MD6zO|ExOyEQvF2=
NCI-H1092 M2\ndmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\wRW5KSzVyPUCuN|g5PDRizszN
8-MG-BA NHPoSmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTBwM{m4N|ch|ryP
NB17 Mo\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHu5V2xKSzVyPUCuOFI6PyEQvF2=
LC4-1 NGPYTlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHDN4FKSzVyPUCuOFM3ODdizszN
TE-1 NVfQW5RnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;mTWM2OD1yLkS1NVE6KM7:TR?=
KALS-1 MoP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\4TmpKSzVyPUCuOFY2QDRizszN
CCRF-CEM M3vwOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\qTWM2OD1yLkS3Olc1KM7:TR?=
OS-RC-2 M{jLdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTLe4dKSzVyPUCuOFc6PzJizszN
A704 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vxcmlEPTB;MD60PFY6OiEQvF2=
BB49-HNC MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nOOWlEPTB;MD60PVA6PiEQvF2=
EVSA-T MlrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C5d2lEPTB;MD60PVkyOSEQvF2=
Mo-T NIHvTmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nnbmlEPTB;MD61NVc3OiEQvF2=
MONO-MAC-6 NVXRVGN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1fWPWlEPTB;MD61N|YyOSEQvF2=
BB65-RCC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDNeZBKSzVyPUCuOVY5OTFizszN
NCI-H1882 NVv0TFV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTBwNUmwN|Yh|ryP
TE-9 NV:5dHE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\KZ5M5UUN3ME2wMlYyODN|IN88US=>
NCI-H2126 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLvTWM2OD1yLk[yOlY6KM7:TR?=
SF268 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTBwNkW2OFEh|ryP
SW872 NFfzemtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwNkW3Nlkh|ryP
LS-513 NGPWdJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHTTW9bUUN3ME2wMlY3PzVzIN88US=>
NCI-H1355 NVnpfWluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3i4S2lEPTB;MD62PFYyQSEQvF2=
BL-70 MniyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTBwNkmzPFgh|ryP
NCI-SNU-5 MonkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEG0SFBKSzVyPUCuOlk2PDVizszN
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HL-60 M{L5VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJyLkG5OlUh|ryP
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NCI-H1304 NIG5TlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnkTWM2OD1{MT6wN|EyKM7:TR?=
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NCI-H1963 NGntXVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfEOJdKSzVyPUK2MlA3OjNizszN
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SNU-C1 NILKZZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnnd3FKSzVyPUOxMlMyOjZizszN
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Ramos-2G6-4C10 NV;6XXhuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTN2LkK5PVMh|ryP
TE-11 NUTBbXl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTN2LkS4NlIh|ryP
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RCC10RGB NIXCR4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTN6LkKwPFMh|ryP
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NCI-H64 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfVUlZKSzVyPUSwMlA6PDhizszN
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U-698-M NXPTZmNiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTZ6LkW2PFch|ryP
NCI-H1522 NFLJU3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTZ7LkCwOFch|ryP
UACC-812 MmPxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTZ7LkWyNFkh|ryP
MHH-CALL-2 M17MeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDCTWM2OD15MD6wOkDPxE1?
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NCI-H1436 M1znSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWWxelJNUUN3ME23Nk44PDV4IN88US=>
ATN-1 MnHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTd2LkWwOUDPxE1?
RPMI-8866 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTd2Lke1NFkh|ryP
HCC1599 NFO3dIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3Hqd2lEPTB;N{SuPFc{OiEQvF2=
NCI-H1155 NHvGS3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnlTWM2OD15ND65N|Y4KM7:TR?=
DOHH-2 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\4bmlEPTB;N{SuPVUyPCEQvF2=
SK-NEP-1 NGLU[IRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4m1cGlEPTB;N{WuNFc2PCEQvF2=
HCC1187 NF34UFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\WTWM2OD15Nz62NVIzKM7:TR?=
NCI-H322M NYjhZ3VYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\uO2w3UUN3ME23PE4{PzB7IN88US=>
NCI-H526 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HJOWlEPTB;N{iuOVg4PyEQvF2=
NCI-H2171 M2nlUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTd7LkSxN|Yh|ryP
COLO-668 MnX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTmTWM2OD16MT61PFg1KM7:TR?=
RS4-11 MnW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHn6O4FKSzVyPUiyMlI2ODVizszN
NCI-H716 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLr[GFnUUN3ME24Nk46ODd3IN88US=>
LU-134-A NWLSSIoyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTh|LkGzOVEh|ryP
RPMI-8226 NXjJb45{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVm1Z2JtUUN3ME24OE4zOTB5IN88US=>
KY821 MmP0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmW0TWM2OD17MT62OVUyKM7:TR?=
ECC4 NEDGcJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4CzdmlEPTB;OUOuPFI3QSEQvF2=
EW-3 NVL3WlI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTl2LkmwPFEh|ryP
NB7 NVjlRYZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NULCeoFrUUN3ME25OU44Pzh4IN88US=>
NCI-H720 NHXPcYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHJTWM2OD17OD60NFYyKM7:TR?=
NCI-H446 M{X0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPtU4dKSzVyPUm5Mlc2QDhizszN
NCI-H889 NW[4XYM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTFyND6yOFIh|ryP
EW-22 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vVSmlEPTB;MUC2MlE6KM7:TR?=
BV-173 NI\wV3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHhXJpKSzVyPUGwPE44OjhizszN
WSU-NHL NYPsWJBsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[2NJNwUUN3ME2xNFkvPjdzIN88US=>
MN-60 M1mySGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGr2TIFKSzVyPUGwPU43QSEQvF2=
DG-75 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYXXNplKUUN3ME2xNVMvOzV{IN88US=>
DMS-79 M3;Q[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTSS2IyUUN3ME2xNVcvOzh{IN88US=>
SK-MEL-1 M{O0eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mki0TWM2OD1zMUiuNFA6KM7:TR?=
DMS-153 M1jTeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmL3TWM2OD1zMkGuO|Q2KM7:TR?=
NCI-H510A NVK4TnBJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXCbVJKSzVyPUGyO{4{OiEQvF2=
BE-13 NIjvUpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmOwTWM2OD1zM{SuNFQ1KM7:TR?=
KP-N-YS NEL6e5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXLUGZKSzVyPUGzPU44OzZizszN
SUP-T1 M4nnV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDHfocxUUN3ME2xOFMvPzB6IN88US=>
EW-12 M1z1OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInsblFKSzVyPUG0OE43QTlizszN
NB14 Ml7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fI[2lEPTB;MUS3MlA5OiEQvF2=
MDA-MB-134-VI NUG1emp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV;5dIFrUUN3ME2xOFgvOjZ6IN88US=>
NCI-H1770 MlnkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjKblhFUUN3ME2xOVYvOjd7IN88US=>
TUR Ml7QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;6[mlEPTB;MU[3Mlg4KM7:TR?=
NCI-H1417 NVuwR4FQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DPdmlEPTB;MUiwMlM{OSEQvF2=
IMR-5 NU\TT|NLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\yTXpKSzVyPUG4NU42PzFizszN
NCI-H226 NFfEO5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPnXJJKSzVyPUG4PE45PjZizszN
NCI-H187 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\BPGlEPTB;MUmwMlA3PCEQvF2=
SF539 NYDwelBpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\le2lEPTB;MUmyMlczQCEQvF2=
TALL-1 M1[5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTF7OD6zNFQh|ryP
TE-441-T MlLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnoWJBKSzVyPUG5PU44OzlizszN
REH NWnFfVh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1juNWlEPTB;MkO2MlYzPiEQvF2=
MS-1 NGHuTFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTJ|OT6xNlEh|ryP
THP-1 M4T5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\ZXWlEPTB;Mk[0Mlc{QCEQvF2=
NCI-H1838 NHTERXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFraZWJKSzVyPUK3NU41PTZizszN
P30-OHK M3G1VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfITWM2OD1{OEOuPFQ4KM7:TR?=
C8166 NUi0Z2lTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37EbWlEPTB;M{S1MlM{QCEQvF2=

... 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

推薦された実験操作 (公開の文献だけ)

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]

細胞系 KIM-2, HC11, and ES
濃度 Dissolved in DMSO, final concentrations ~25 μM
処理時間 24, and 48 hours
方法

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
管理 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

カスタマーレビュー (6)


Click to enlarge
Rating
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 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 FEBS Letters, 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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