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 MULGeY5kfGmxbjDBd5NigQ>? MYqyOUDPxE1? M2jiRWROW09? M3HXW2lvcGmkaYTzJI5qfHKrYzDvfIll\SCycn;keYN1cW:wIIfpeIghUUN3MDDv[kAxNjFizszN
HL-60 NGTJbFZEgXSxdH;4bYMhSXO|YYm= MoTjOFAh|ryP NIPXPFg1QCCq NYDOWJY1TE2VTx?= NVP4cGw2UUN3MEyxNEDPxE1?
SMMC-7721 NXfZeo52S3m2b4TvfIlkKEG|c3H5 MVq0NEDPxE1? Ml7GOFghcA>? NH7KbI5FVVOR M{TnTmlEPTB;Nz6xJO69VQ>?
A-549 NYXhd|FkS3m2b4TvfIlkKEG|c3H5 NITve5U1OCEQvF2= NX\ZSnAxPDhiaB?= MXzEUXNQ NU\xZ5k3UUN3MEyxNEDPxE1?
MCF-7 NVG0Wm5JS3m2b4TvfIlkKEG|c3H5 M1;EU|QxKM7:TR?= NVy0e|d1PDhiaB?= NXHxPGVTTE2VTx?= MmPOTWM2OD15LkOg{txO
SW-480 MYXDfZRwfG:6aXOgRZN{[Xl? MoPoOFAh|ryP M1[2OlQ5KGh? NWDMRWZrTE2VTx?= NXnLN5JiUUN3ME20JO69VQ>?
NCI-H929 NGHOfphEgXSxdH;4bYMhSXO|YYm= NEnlV3UyKM7:TR?= M3HENlczKGh? NG\S[XFFVVOR NVTCXJhUUUN3ME2wMlE4KM7:TR?=
293T M4DremN6fG:2b4jpZ{BCe3OjeR?= MknpNVAh|ryP MoPRO|IhcA>? MkPySG1UVw>? NUPUcGYzUUN3MEyyJO69VQ>?
293T NWXOb3dLTnWwY4Tpc44hSXO|YYm= MlfDNVAh|ryP NILmeWczPCCq NHvSd2RFVVOR MXLNc4RmemG2ZXz5JIlv\HWlZYOgbIVifC2|aH;jb{Ah
HeLa MYHLbY5ie2ViQYPzZZk> NYrO[YR6OTBizszN MYOxJIg> NVHzPYVITE2VTx?= M2PubWlv\HWlZYOgVGFTWCClbHXheoFo\SCkeTDpcohq[mm2aX7nJJBzd3OnYYPvcYUh[WO2aY\peJk>
MDA-MB-231 M4m1cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVixJO69VQ>? MVO3NkBp MmXFSG1UVw>? M2PIfGlEPTB;MD6xPEDPxE1?
MCF-7 Mm\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4KxWFEh|ryP MlLwO|IhcA>? NWP0TVVVTE2VTx?= MWHJR|UxRTBwMUOg{txO
MCF10A MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\FNUDPxE1? NIDzb2U4OiCq NYXDSpQ{TE2VTx?= M3PDPGlEPTB;MD6yPUDPxE1?
HEK-293 MnjZT4lv[XOnIFHzd4F6 M1rLPFIh[W6mIEKwJO69VQ>? MX[yJIg> MnXzSG1UVw>? NV\BUHh2UW6qaXLpeJMhS2iWLVygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDlibl2g
Calu6 MkHwSpVv[3Srb36gRZN{[Xl? MUexNEDPxE1? MXWxPEBp MWfEUXNQ MWfTbYdvcW[rY3HueIx6KGGlY4XteYxifGW|IH\yZZRigGmwIIDy[YN2enOxch?=
IFN-gamma-induced RAW264.7 NWPpW4k3TnWwY4Tpc44hSXO|YYm= M3OzOGROW09? MWnJcohq[mm2czDubZRzcWNib4jp[IUheHKxZIXjeIlwdiC5aYToJGlEPTBib3[gNE4xPzdizszN
IPC227F NEXFS4xEgXSxdH;4bYMhSXO|YYm= MVKxJO69VQ>? NVPZVVJSPDhiaB?= Ml7lSG1UVw>? NYjNc3ZoUUN3ME2wMlA4PyEQvF2=
Hepa-1c1c7 M4j1bGZ2dmO2aX;uJGF{e2G7 MoXUNlUh|ryP MoW3OkBp MWXEUXNQ NEfjVnZKdmO{ZXHz[ZMhVnKoMjDwdo91\WmwIHzleoVt
COS-7 M4fHO2N6fG:2b4jpZ{BCe3OjeR?= NEWyOJAyOCEQvF2= MmC3SG1UVw>? MnLsTWM2ODxzMDFOwG0>
HuH-7 NEnweG1EgXSxdH;4bYMhSXO|YYm= NHq0NYMyOCEQvF2= M3zFRmROW09? M3X5SGlEPTB:MUCg{txO
OCI-Ly3 MWnGeY5kfGmxbjDBd5NigQ>? M{TWXFExKM7:TdMg NGG2cnA1KGh? MljESG1UVw>? M4\0XWlv\HWlZYOgbJVu[W5iSXvhdJBiSmGucHjhJJN1[WKrbHn6ZZRqd25id3n0bEBGSzVyIH;mJFEh|ryP
A2780 cDDP NXfG[GVMSXCxcITvd4l{KEG|c3H5 M4WwSlI1KGh? M2mwVGROW09? M1;OSWlv\HWlZYOgZZBweHSxc3nzJIJ6KGmwaHnibZRqdmdiUGTFUkBl\We{YXTheIlwdg>?
LPS-stimulated RAW264.7 cells MoC2SpVv[3Srb36gRZN{[Xl? NHfCTVJFVVOR NUi0dGRQUW6qaXLpeJMhVkZva3HwdIFDKESQQTDibY5lcW6p
PC12 MmTWSpVv[3Srb36gRZN{[Xl? MnW4NVAxKM7:TdMg MUSyOEBp MVTEUXNQ NWLnSIhoUW6qaXLpeJMhPi2RSFTBMUBidmRiSELPNk1qdmS3Y3XkJIN6fG:2b4jpZ4l1gQ>?
PC3 MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLEXoYzOCEQvF2= NFLOTmE1QCCq NYrpeZhpTE2VTx?= NVPPS28zUUN3ME2wMlYh|ryP
LP-1 MWTBdI9xfG:|aYOgRZN{[Xl? MVuzNFAhdk1? MkHWNlQhcA>? MWfEUXNQ Mn\uTY5lfWOnczDhdI9xfG:|aYOgZpkhcW6lcnXhd4lv\yClbHXheoVlKFCDUmCgcIV3\WxiYX7kJJJm\HWlaX7nJG1kdC1zIIDyc5RmcW5ibHX2[Yw>
ES6 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHnH[5VKSzVyPUCuNFE{ODZizszN
A101D MonGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDzWYxyUUN3ME2wMlA{Ojd7IN88US=>
OCUB-M MmmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrMTWM2OD1yLkCzO|M4KM7:TR?=
LB2518-MEL MmjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmG1TWM2OD1yLkCzO|Yh|ryP
SH-4 MnzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwMESzNUDPxE1?
KNS-42 Mn3aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPZTWM2OD1yLkC0OFQyKM7:TR?=
DSH1 M4TEOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTBwMEWyPFkh|ryP
NTERA-S-cl-D1 MmHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3zb|FKSzVyPUCuNFU4PzJizszN
D-542MG M17qNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;vTXNKSzVyPUCuNFU6PTdizszN
KS-1 NEH0N2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTBwME[0OVgh|ryP
BL-41 M1HHNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjaTWM2OD1yLkC2PVQ4KM7:TR?=
LXF-289 NFXvRXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDBTWM2OD1yLkC3NFY3KM7:TR?=
D-247MG MkjzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4H5eGlEPTB;MD6wO|IxQSEQvF2=
MMAC-SF NWToUmNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfYNYd[UUN3ME2wMlA4OjZ6IN88US=>
CP66-MEL MkXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLKTWM2OD1yLkC3OUDPxE1?
LB771-HNC NHruR4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Kzd2lEPTB;MD6wPFA{PiEQvF2=
no-10 MkDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjHSohkUUN3ME2wMlA5QTB7IN88US=>
A388 MmnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTBwMEmwOlUh|ryP
OPM-2 NF\SW4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXiTWM2OD1yLkGwOFc1KM7:TR?=
OVCAR-4 M2i0[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHe3UmVKSzVyPUCuNVA6OzhizszN
HOP-62 M3;TXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoT1TWM2OD1yLkGwPVQ6KM7:TR?=
ML-2 M4fQWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfOXVBKSzVyPUCuNVE5ODZizszN
UACC-257 MoK5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwMUG5Nlch|ryP
NEC8 M4XLSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrsSo1KSzVyPUCuNVE6QTVizszN
ONS-76 NXj4[IhNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTBwMUK5N|Uh|ryP
KE-37 M333V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHYdJp4UUN3ME2wMlE{Ojd6IN88US=>
HT-144 NHLqb2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LPfWlEPTB;MD6xN|g6PSEQvF2=
LB2241-RCC MnTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTBwMUSyOFch|ryP
TE-5 M4fJSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLQTodIUUN3ME2wMlE1Ojd6IN88US=>
KINGS-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjZcWFTUUN3ME2wMlE1PzlizszN
NCI-H69 M4m5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn5NnVEUUN3ME2wMlE2OTRzIN88US=>
CAS-1 M2Hr[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nCeGlEPTB;MD6xOVQ5OiEQvF2=
D-263MG NEHHN2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33EU2lEPTB;MD6xOlAxPiEQvF2=
A253 NYXmOpk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITjUINKSzVyPUCuNVYyOjhizszN
PF-382 M4j4XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;CTWM2OD1yLkG2O|A3KM7:TR?=
CESS Mn;wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHhXpBQUUN3ME2wMlE4ODZizszN
MZ2-MEL NVfGWoNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[yV2lEPTB;MD6xO|U2QSEQvF2=
HEL NIDSR|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFmzSWJKSzVyPUCuNVg2OTdizszN
D-392MG NGPhTGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGC5fldKSzVyPUCuNVkyOTVizszN
SK-LMS-1 M13pe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\adIloUUN3ME2wMlE6OzB|IN88US=>
GI-ME-N MlXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\TTlRKSzVyPUCuNVk{ODZizszN
LB831-BLC M{Ladmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLEfmp1UUN3ME2wMlE6OzRizszN
DU-4475 MlfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTBwMUm2OVgh|ryP
IST-SL1 NGH6bZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\lS2lEPTB;MD6yNFA6PCEQvF2=
GAK NWXxNHF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1f1[WlEPTB;MD6yNFU{PCEQvF2=
EW-1 M1Hhfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3raUGlEPTB;MD6yNVA1PyEQvF2=
LAMA-84 MnjVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPqTWM2OD1yLkKxPFUyKM7:TR?=
SK-UT-1 MnuxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwMkKwOFkh|ryP
VA-ES-BJ MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUjJR|UxRTBwMkKyOVch|ryP
ACN NWLENo95T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPnd5h2UUN3ME2wMlIzPjN6IN88US=>
SK-PN-DW M4rqTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknkTWM2OD1yLkKzNVkh|ryP
HD-MY-Z MojuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nD[mlEPTB;MD6yN|MxOyEQvF2=
LB373-MEL-D M2DUdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwMkSxPVgh|ryP
COLO-829 MlLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\mTWM2OD1yLkK0NlU4KM7:TR?=
ES8 MlW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjpbJVjUUN3ME2wMlI1PzZ|IN88US=>
RXF393 M4\UR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTBwMkWwNVUh|ryP
TK10 NUfaeGd6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTBwMkW0N|Uh|ryP
LOUCY MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LURWlEPTB;MD6yOVQ2PiEQvF2=
MZ7-mel NUnEd|dtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\EZWlEPTB;MD6yOlM4PCEQvF2=
CP67-MEL MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3P3XGlEPTB;MD6yOlc{KM7:TR?=
C2BBe1 M4HESWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTBwMke5NFch|ryP
K052 NFHkUItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjwR|FKSzVyPUCuNlg6QSEQvF2=
MOLT-16 NVO2VmRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXwZ|hKSzVyPUCuNlk2OjRizszN
KNS-81-FD NEWwUZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTBwM{CzNlMh|ryP
CMK Mn7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;vc2lEPTB;MD6zNVEzKM7:TR?=
LAN-6 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\G[2RKSzVyPUCuN|E{KM7:TR?=
KLE NFrObI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{DIRWlEPTB;MD6zNVMxPiEQvF2=
NCCIT MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlntTWM2OD1yLkOxO|g{KM7:TR?=
HH M4izZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1f4N2lEPTB;MD6zNlg6PyEQvF2=
TE-8 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;VTWM2OD1yLkO0Nlc6KM7:TR?=
GDM-1 NEXFV2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTBwM{WxNFQh|ryP
NCI-H747 M{XETWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\temlEPTB;MD6zO|ExOyEQvF2=
NCI-H1092 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGL1WnFKSzVyPUCuN|g5PDRizszN
8-MG-BA NUXiZldCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jrOmlEPTB;MD6zPVg{PyEQvF2=
NB17 NX3zS4c{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2j2R2lEPTB;MD60Nlk4KM7:TR?=
LC4-1 M{P5S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfBTWM2OD1yLkSzOlA4KM7:TR?=
TE-1 MlLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGe1Xo5KSzVyPUCuOFUyOTlizszN
KALS-1 NXG1NW57T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ixemlEPTB;MD60OlU5PCEQvF2=
CCRF-CEM NYXPNJo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37n[2lEPTB;MD60O|Y4PCEQvF2=
OS-RC-2 NGPFeFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3WwUWlEPTB;MD60O|k4OiEQvF2=
A704 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTBwNEi2PVIh|ryP
BB49-HNC NGnPd4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPqO|FTUUN3ME2wMlQ6ODl4IN88US=>
EVSA-T NH\5XFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTBwNEm5NVEh|ryP
Mo-T MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LoR2lEPTB;MD61NVc3OiEQvF2=
MONO-MAC-6 MoW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnZTWM2OD1yLkWzOlEyKM7:TR?=
BB65-RCC M1Xs[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rsNmlEPTB;MD61OlgyOSEQvF2=
NCI-H1882 NHzJUpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrlW2xnUUN3ME2wMlU6ODN4IN88US=>
TE-9 NVj0d|RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTBwNkGwN|Mh|ryP
NCI-H2126 NVTFenRwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHZOWZKSzVyPUCuOlI3PjlizszN
SF268 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXrTWM2OD1yLk[1OlQyKM7:TR?=
SW872 Ml7zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTBwNkW3Nlkh|ryP
LS-513 NInEVJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XReWlEPTB;MD62Olc2OSEQvF2=
NCI-H1355 NH3KXVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:wTWM2OD1yLk[4OlE6KM7:TR?=
BL-70 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoK0TWM2OD1yLk[5N|g5KM7:TR?=
NCI-SNU-5 MkPyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;ZVWlEPTB;MD62PVU1PSEQvF2=
SNU-C2B MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rvdGlEPTB;MD63NFc{QSEQvF2=
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P31-FUJ MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTJyLkS3OVMh|ryP
IM-9 M4OyTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWi5OZdVUUN3ME2yNE43OjJ2IN88US=>
HDLM-2 M1WwZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LZSWlEPTB;MkCuPFgzOSEQvF2=
NCI-H1304 NG\XWGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{W3TGlEPTB;MkGuNFMyOSEQvF2=
NCI-H345 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DHNGlEPTB;MkGuNFY1OyEQvF2=
RPMI-6666 M4mzNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2faWGlEPTB;MkGuN|YxOiEQvF2=
GR-ST NFvFdYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTJzLkSxO{DPxE1?
CHP-126 NUXP[YQ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPrWGJKSzVyPUKxMlYyQDFizszN
EHEB NVvXXWpbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3jmNGlEPTB;MkGuOlc{OSEQvF2=
CPC-N MmTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3T6UGlEPTB;MkSuNFIxOSEQvF2=
NB1 M3\Vdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3X3VWlEPTB;MkSuOlk{QSEQvF2=
LS-123 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTJ2LkmwNVIh|ryP
ST486 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnqzTWM2OD1{NT6xNVE{KM7:TR?=
NCI-H1963 NXjlelN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWWyPGpzUUN3ME2yOk4xPjJ|IN88US=>
U-87-MG Mn;LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfRZ3VCUUN3ME2yOk44PjR2IN88US=>
COR-L279 M1jNUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPvRXNQUUN3ME2yOk44QTJ{IN88US=>
LU-165 NIXLOm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Sx[GlEPTB;MkiuNFg3OSEQvF2=
COLO-800 NV\FdHRXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHhTWM2OD1{OD6yPVU3KM7:TR?=
ETK-1 NFLROJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnLUTWM2OD1{OD6zOFQ3KM7:TR?=
LNCaP-Clone-FGC MlvJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTJ7LkmyPFEh|ryP
SIG-M5 MmHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoniTWM2OD1|MD63PVUzKM7:TR?=
NB6 NHG4T2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTNyLkm1NFMh|ryP
NCI-H2107 NHvB[mlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\rU2lEPTB;M{GuNlM{QCEQvF2=
SNU-C1 NInDOoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFqyS3JKSzVyPUOxMlMyOjZizszN
JAR MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTNzLkO3PVkh|ryP
L-363 NIT1TWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTN{LkKxOFQh|ryP
EW-24 NEPvfHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDLOJNNUUN3ME2zNk4{PDd2IN88US=>
NB69 M1H3UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTN|Lk[0OVQh|ryP
EW-13 NWO0VY5{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjWTWM2OD1|Mz64PVY6KM7:TR?=
Ramos-2G6-4C10 M1XQemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrCZWl5UUN3ME2zOE4zQTl|IN88US=>
TE-11 NV;1dG1UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLZepVKSzVyPUO0MlQ5OjJizszN
L-428 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXTTWM2OD1|ND63OVM3KM7:TR?=
KP-N-YN NXLKWotuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33XcmlEPTB;M{SuPVA2PyEQvF2=
CGTH-W-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofWTWM2OD1|Nj65NFQ5KM7:TR?=
K-562 NEnpS4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfXdVBKSzVyPUO3MlA5PjRizszN
NCI-H1299 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[0TWM2OD1|OD6xOlA{KM7:TR?=
RCC10RGB MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LVXmlEPTB;M{iuNlA5OyEQvF2=
NCI-SNU-16 NVywbXFGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDUTWM2OD1|OD61OlU{KM7:TR?=
LC-2-ad MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnG4TWM2OD1|OT60N|M4KM7:TR?=
MHH-PREB-1 NYTSUmc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHP5WI9KSzVyPUO5Mlc{QDhizszN
NCI-H64 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILoZVNKSzVyPUSwMlA6PDhizszN
LB996-RCC MnrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUj3bXhCUUN3ME20NE45PzF4IN88US=>
DEL NGPWdItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTRzLkS0NFUh|ryP
MLMA NF\0b|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fnO2lEPTB;NEGuO|U6PSEQvF2=
SBC-1 NVfsPXVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTW[lVKSzVyPUSyMlE5ODZizszN
MPP-89 NGPkS5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTR{LkW4O|Uh|ryP
MV-4-11 NGjqPG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjLTHhlUUN3ME20Nk46ODZ5IN88US=>
EoL-1- NWDh[XFWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTR2LkG1Olgh|ryP
CW-2 NUW3TYhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTR2LkizOFIh|ryP
HT M1Lq[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTR3LkewNFch|ryP
SW954 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXvTWM2OD12Nz60NVI5KM7:TR?=
A3-KAW M3zJWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDsTWM2OD12OT64NFYyKM7:TR?=
TC-YIK NWLQWHVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4S0UWlEPTB;NUCuNFM3OyEQvF2=
SW962 NXjHWXB3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHiTmlKSzVyPUW0Mlg{PTdizszN
KP-N-RT-BM-1 NG\FNVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEn6XoZKSzVyPUW2MlY3OzhizszN
NCI-H1395 NIfRO25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTV6LkixO|Ih|ryP
RPMI-8402 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLrXpdqUUN3ME21PE46PTJ4IN88US=>
SCH MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrmZpZKSzVyPU[wMlk3OzhizszN
NCI-H2196 NXSyRnltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHHU|lNUUN3ME22NU4zOzFizszN
LOXIMVI NXWwWG5qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2i2dGlEPTB;NkGuPFI3PiEQvF2=
TGBC24TKB Ml74S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rNUmlEPTB;NkKuNVQ6OSEQvF2=
SK-MEL-2 MlTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTZ|Lkm4PVIh|ryP
U-698-M M{PRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPsWoVLUUN3ME22PE42Pjh5IN88US=>
NCI-H1522 NGTnOHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rBfmlEPTB;NkmuNFA1PyEQvF2=
UACC-812 NFznbmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTZ7LkWyNFkh|ryP
MHH-CALL-2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEftVIZKSzVyPUewMlA3KM7:TR?=
NB5 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWHCRYtKUUN3ME23NE4{PDZ6IN88US=>
KARPAS-299 NX7YcnR5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTdyLkS0OFch|ryP
NCI-H1694 M4j2dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\DfItKSzVyPUexMlA{OiEQvF2=
NCI-H82 Ml;4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;mTWM2OD15MT65OVA4KM7:TR?=
SCC-15 M2jMT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTd{LkO0JO69VQ>?
NCI-H1436 M2j2[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHiTWM2OD15Mj63OFU3KM7:TR?=
ATN-1 Ml\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nTXGlEPTB;N{SuOVA2KM7:TR?=
RPMI-8866 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTd2Lke1NFkh|ryP
HCC1599 Mnq2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDrV|RZUUN3ME23OE45PzN{IN88US=>
NCI-H1155 M3zqeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTd2LkmzOlch|ryP
DOHH-2 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmK1TWM2OD15ND65OVE1KM7:TR?=
SK-NEP-1 M{\hWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHxNWNKSzVyPUe1MlA4PTRizszN
HCC1187 MmTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTd5Lk[xNlIh|ryP
NCI-H322M M2T0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTd6LkO3NFkh|ryP
NCI-H526 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXW3WY1CUUN3ME23PE42QDd5IN88US=>
NCI-H2171 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvwVJhHUUN3ME23PU41OTN4IN88US=>
COLO-668 NWT1UHEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljNTWM2OD16MT61PFg1KM7:TR?=
RS4-11 NHX2ZoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVW5cVYzUUN3ME24Nk4zPTB3IN88US=>
NCI-H716 NIXqUnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTh{LkmwO|Uh|ryP
LU-134-A M1r3Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV\JR|UxRTh|LkGzOVEh|ryP
RPMI-8226 MnTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1eyfmlEPTB;OESuNlExPyEQvF2=
KY821 MlrvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTlzLk[1OVEh|ryP
ECC4 NUT1UnhzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYP6RY5IUUN3ME25N{45OjZ7IN88US=>
EW-3 NWLONoZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTl2LkmwPFEh|ryP
NB7 Mn\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUW0Tm1UUUN3ME25OU44Pzh4IN88US=>
NCI-H720 M3jDfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{f0bWlEPTB;OUiuOFA3OSEQvF2=
NCI-H446 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\BTWM2OD17OT63OVg5KM7:TR?=
NCI-H889 M1ixU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGS4T25KSzVyPUGwOE4zPDJizszN
EW-22 M17pdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HtXmlEPTB;MUC2MlE6KM7:TR?=
BV-173 NF7XfXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfMTWM2OD1zMEiuO|I5KM7:TR?=
WSU-NHL MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTNPG9KSzVyPUGwPU43PzFizszN
MN-60 NGfNVllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\rTWM2OD1zMEmuOlkh|ryP
DG-75 M33TWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13W[GlEPTB;MUGzMlM2OiEQvF2=
DMS-79 NEXyPWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\GSppKSzVyPUGxO{4{QDJizszN
SK-MEL-1 NFXt[VRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnj1TWM2OD1zMUiuNFA6KM7:TR?=
DMS-153 M4PDfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHuwcIdKSzVyPUGyNU44PDVizszN
NCI-H510A M2LScmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfBfpJoUUN3ME2xNlcvOzJizszN
BE-13 Mmf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3hXG02UUN3ME2xN|QvODR2IN88US=>
KP-N-YS M3qyR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DPe2lEPTB;MUO5Mlc{PiEQvF2=
SUP-T1 M2\nUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTF2Mz63NFgh|ryP
EW-12 NXjDXoRmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLhVoViUUN3ME2xOFQvPjl7IN88US=>
NB14 Mli2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7UOFdnUUN3ME2xOFcvODh{IN88US=>
MDA-MB-134-VI MnTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPTOZdXUUN3ME2xOFgvOjZ6IN88US=>
NCI-H1770 M1[4S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLpRpRiUUN3ME2xOVYvOjd7IN88US=>
TUR MoXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTF4Nz64O{DPxE1?
NCI-H1417 NX;sXo9VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVy0TGJ{UUN3ME2xPFAvOzNzIN88US=>
IMR-5 NU\4dYl6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTF6MT61O|Eh|ryP
NCI-H226 NG\VWJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTF6OD64OlYh|ryP
NCI-H187 NID6S2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWX5cXk2UUN3ME2xPVAvODZ2IN88US=>
SF539 NUPiUGpWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\kU4tKSzVyPUG5Nk44OjhizszN
TALL-1 MnXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;s[2lEPTB;MUm4MlMxPCEQvF2=
TE-441-T M3\vTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDYcoVoUUN3ME2xPVkvPzN7IN88US=>
REH NFPGTYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHxfoE4UUN3ME2yN|YvPjJ4IN88US=>
MS-1 NFTHb3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2[3RWlEPTB;MkO5MlEzOSEQvF2=
THP-1 Mn\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTiT3BKSzVyPUK2OE44OzhizszN
NCI-H1838 M4XQXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTJ5MT60OVYh|ryP
P30-OHK NH:0XlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK3TXVxUUN3ME2yPFMvQDR5IN88US=>
C8166 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;jS2FKSzVyPUO0OU4{OzhizszN

... 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)


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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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