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 DescriptionPMID
LPS-stimulated RAW264.7 cells MVTGeY5kfGmxbjDBd5NigQ>? NGPSOYwzPSEQvF2= M1XJbWROW09? MX7Jcohq[mm2czDubZRzcWNib4jp[IUheHKxZIXjeIlwdiC5aYToJGlEPTBib3[gNE4yKM7:TR?= MYSyOFY6PzR7Nh?=
HL-60 MUHDfZRwfG:6aXOgRZN{[Xl? MX20NEDPxE1? MVi0PEBp M3fFWGROW09? MYDJR|UxRDFyIN88US=> MmjkNlQ3QTd2OU[=
SMMC-7721 NXfic5hIS3m2b4TvfIlkKEG|c3H5 MnTLOFAh|ryP MVq0PEBp M2GySGROW09? NGK5cGhKSzVyPUeuNUDPxE1? NX7Qe2VjOjR4OUe0PVY>
A-549 NETxN3pEgXSxdH;4bYMhSXO|YYm= NGTUeYg1OCEQvF2= M{j0SlQ5KGh? MXvEUXNQ MULJR|UxRDFyIN88US=> NVzubFZKOjR4OUe0PVY>
MCF-7 NEi1Rm5EgXSxdH;4bYMhSXO|YYm= NWjHZ3hvPDBizszN M1PVR|Q5KGh? M{faeGROW09? NUXPNZhIUUN3ME23MlMh|ryP NFzmVI0zPDZ7N{S5Oi=>
SW-480 MV3DfZRwfG:6aXOgRZN{[Xl? MUS0NEDPxE1? NXK1Z3lVPDhiaB?= NFPNcW1FVVOR MUjJR|UxRTRizszN MX2yOFY6PzR7Nh?=
NCI-H929 NVrKU3pJS3m2b4TvfIlkKEG|c3H5 MoW1NUDPxE1? MVG3NkBp NWSwcVFRTE2VTx?= M1vpVGlEPTB;MD6xO{DPxE1? NYr5WI9YOjR4MkWwPFg>
293T M{e0TmN6fG:2b4jpZ{BCe3OjeR?= NHP2NFAyOCEQvF2= NHO4TFc4OiCq NYW1ZotCTE2VTx?= NXfJfZVXUUN3MEyyJO69VQ>? NGrJdlkzPDZ{NUC4PC=>
293T MmD2SpVv[3Srb36gRZN{[Xl? NUfmbZRKOTBizszN M2q1OVI1KGh? MXnEUXNQ MX;Nc4RmemG2ZXz5JIlv\HWlZYOgbIVifC2|aH;jb{Ah MYWyOFYzPTB6OB?=
HeLa NHrv[GlMcW6jc3WgRZN{[Xl? MYSxNEDPxE1? MlPPNUBp MXnEUXNQ M2\5OWlv\HWlZYOgVGFTWCClbHXheoFo\SCkeTDpcohq[mm2aX7nJJBzd3OnYYPvcYUh[WO2aY\peJk> NHziRoUzPDN{MUizNy=>
MDA-MB-231 NXvuN291T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HDPVEh|ryP NID6SWc4OiCq NULPT|k6TE2VTx?= MWrJR|UxRTBwMUig{txO M2XiS|I1OTV|MkC2
MCF-7 M1zYcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\tSVEh|ryP NF[0dIQ4OiCq NHnVNpRFVVOR M3PEVmlEPTB;MD6xN{DPxE1? NGnLfXczPDF3M{KwOi=>
MCF10A M{XaPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrZNUDPxE1? NFK0cI84OiCq MlLLSG1UVw>? M1jBVWlEPTB;MD6yPUDPxE1? M3T4b|I1OTV|MkC2
HEK-293 M{PBNWtqdmG|ZTDBd5NigQ>? MXyyJIFv\CB{MDFOwG0> NWCybZV{OiCq MYfEUXNQ MnfsTY5pcWKrdIOgR4hVNUxiYXP0bZZqfHlid3n0bEBKSzVyIH;mJFkhdk1i NWXPV29tOjN3NEC3PVA>
Calu6 MljpSpVv[3Srb36gRZN{[Xl? NH\NfFQyOCEQvF2= NXjFToNVOThiaB?= MUTEUXNQ MnrCV4lodmmoaXPhcpRtgSCjY3P1cZVt[XSnczDmdoF1[XirbjDwdoVkfXK|b4K= NGL3VoMzOzVyNkS4Oi=>
IFN-gamma-induced RAW264.7 Mkf5SpVv[3Srb36gRZN{[Xl? MXnEUXNQ NY\SWItNUW6qaXLpeJMhdmm2cnnjJI95cWSnIIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDBwMEe3JO69VQ>? NYDuemk5OjJ{N{eyO|c>
IPC227F NEjLWJREgXSxdH;4bYMhSXO|YYm= M{O3SFEh|ryP NGTyOYc1QCCq M32wPWROW09? MmnXTWM2OD1yLkC3O{DPxE1? M2DS[|IyQTJ2NUK4
Hepa-1c1c7 M{\OO2Z2dmO2aX;uJGF{e2G7 NIHHVWMzPSEQvF2= NV;kNoNKPiCq NIHmdpVFVVOR MUjJcoNz\WG|ZYOgUpJnOiCycn;0[YlvKGyndnXs M17EUFIxOzl{NUS0
COS-7 NWi5OZJXS3m2b4TvfIlkKEG|c3H5 MkG0NVAh|ryP MY\EUXNQ MWLJR|UxRDFyIN88US=> M4XER|E5ODh6MEm3
HuH-7 M4T1PGN6fG:2b4jpZ{BCe3OjeR?= NEX5UlQyOCEQvF2= NXXpU5RMTE2VTx?= NWrGO5BVUUN3MEyxNEDPxE1? MVuxPFA5QDB7Nx?=
OCI-Ly3 NXnFOFhNTnWwY4Tpc44hSXO|YYm= NWTTTHg{OTBizszNxsA> NWP2[WxEPCCq NXvhUYY3TE2VTx?= NETqTHlKdmS3Y3XzJIh2dWGwIFnrZZBx[UKjbIDoZUB{fGGkaXzpfoF1cW:wIIfpeIghTUN3MDDv[kAyKM7:TR?= MnfTNVgxOjRzMUO=
A2780 cDDP NUTOfFVmSXCxcITvd4l{KEG|c3H5 NYXoTZZxOjRiaB?= NVHwRopyTE2VTx?= M3nUcWlv\HWlZYOgZZBweHSxc3nzJIJ6KGmwaHnibZRqdmdiUGTFUkBl\We{YXTheIlwdg>? M3j6SlE4Pjh2MEG4
LPS-stimulated RAW264.7 cells NV;RUVF3TnWwY4Tpc44hSXO|YYm= MlTESG1UVw>? NWLrU21kUW6qaXLpeJMhVkZva3HwdIFDKESQQTDibY5lcW6p Ml3SNVc1ODd{N{e=
PC12 M4\RbWZ2dmO2aX;uJGF{e2G7 M{LNPVExOCEQvF5CpC=> MlXmNlQhcA>? MlzUSG1UVw>? MWPJcohq[mm2czC2MW9JTEFvIHHu[EBJOk9{LXnu[JVk\WRiY4n0c5RwgGmlaYT5 MUmxO|E2QDR3NB?=
PC3 M134VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3IbVkyOjBizszN MX20PEBp M{TvOGROW09? NXvzPWZYUUN3ME2wMlYh|ryP MlP1NVY3QDZ3M{e=
LP-1 MXLBdI9xfG:|aYOgRZN{[Xl? M{TXTFMxOCCwTR?= NWPvR3hjOjRiaB?= NH\DT4dFVVOR MVzJcoR2[2W|IHHwc5B1d3OrczDifUBqdmO{ZXHzbY5oKGOuZXH2[YQhWEGUUDDs[ZZmdCCjbnSgdoVlfWOrbnegUYNtNTFicILveIVqdiCuZY\lcC=> NXPic2pGOTV7NUi1PFk>
ES6 Ml7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDkVG1KSzVyPUCuNFE{ODZizszN Ml3GV2FPT0WU
A101D M1PCR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXYUVJKSzVyPUCuNFMzPzlizszN M1H0dnNCVkeHUh?=
OCUB-M MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\XTWM2OD1yLkCzO|M4KM7:TR?= MVLTRW5ITVJ?
LB2518-MEL NH\Bd5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUX6bWhCUUN3ME2wMlA{PzZizszN NVGxOlVTW0GQR1XS
SH-4 Ml22S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwMESzNUDPxE1? MnTjV2FPT0WU
KNS-42 M4rLTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHG4V3dKSzVyPUCuNFQ1PDFizszN MYfTRW5ITVJ?
DSH1 MlriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXtNYxKSzVyPUCuNFUzQDlizszN NXLLUpNJW0GQR1XS
NTERA-S-cl-D1 MnqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTlO45KUUN3ME2wMlA2Pzd{IN88US=> M4[wcnNCVkeHUh?=
D-542MG Mn;RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHezZXdKSzVyPUCuNFU6PTdizszN MkTrV2FPT0WU
KS-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILtT45KSzVyPUCuNFY1PThizszN MWjTRW5ITVJ?
BL-41 NG[5TW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2P4[2lEPTB;MD6wOlk1PyEQvF2= NVXYToVIW0GQR1XS
LXF-289 NF;4eFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHTTWM2OD1yLkC3NFY3KM7:TR?= Ml33V2FPT0WU
D-247MG MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWO4UnMzUUN3ME2wMlA4OjB7IN88US=> MYjTRW5ITVJ?
MMAC-SF Mn;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfSTWM2OD1yLkC3NlY5KM7:TR?= NHjvOmNUSU6JRWK=
CP66-MEL NGDwV3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4f3d2lEPTB;MD6wO|Uh|ryP MYfTRW5ITVJ?
LB771-HNC NH3WW5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnT1TWM2OD1yLkC4NFM3KM7:TR?= MoPDV2FPT0WU
no-10 MlvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYW2e2FYUUN3ME2wMlA5QTB7IN88US=> NVixdpdFW0GQR1XS
A388 NGjwWJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3YTWM2OD1yLkC5NFY2KM7:TR?= M2jMZnNCVkeHUh?=
OPM-2 MnLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHf4cldKSzVyPUCuNVA1PzRizszN Mn3mV2FPT0WU
OVCAR-4 Mlm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTBwMUC5N|gh|ryP M4XO[XNCVkeHUh?=
HOP-62 MkfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTZWVdIUUN3ME2wMlExQTR7IN88US=> MkL3V2FPT0WU
ML-2 NI\xbVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjrTWM2OD1yLkGxPFA3KM7:TR?= M{\oNXNCVkeHUh?=
UACC-257 M1[5V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XmWGlEPTB;MD6xNVkzPyEQvF2= NWe4fm5VW0GQR1XS
NEC8 NFfEdIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUflbWRxUUN3ME2wMlEyQTl3IN88US=> M3jGVnNCVkeHUh?=
ONS-76 NUXyWGZHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXKTWM2OD1yLkGyPVM2KM7:TR?= M1L4WXNCVkeHUh?=
KE-37 MoniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnSVXVKSzVyPUCuNVMzPzhizszN NGPRTopUSU6JRWK=
HT-144 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrhSJMzUUN3ME2wMlE{QDl3IN88US=> NXnrRYliW0GQR1XS
LB2241-RCC M{\xUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjsPFJqUUN3ME2wMlE1OjR5IN88US=> M1ezRnNCVkeHUh?=
TE-5 MmHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXJXnNZUUN3ME2wMlE1Ojd6IN88US=> Mk\WV2FPT0WU
KINGS-1 MmDyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXSycIRZUUN3ME2wMlE1PzlizszN MkDXV2FPT0WU
NCI-H69 MkTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwMUWxOFEh|ryP NEHoOndUSU6JRWK=
CAS-1 MnPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHMR29KSzVyPUCuNVU1QDJizszN MoTSV2FPT0WU
D-263MG M1fEOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\pTWM2OD1yLkG2NFA3KM7:TR?= MWPTRW5ITVJ?
A253 NHLQPVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrvTWM2OD1yLkG2NVI5KM7:TR?= M2S2[nNCVkeHUh?=
PF-382 NFL3WWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTBwMU[3NFYh|ryP NHnaT|lUSU6JRWK=
CESS MlvzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DhN2lEPTB;MD6xO|A3KM7:TR?= NHLBS2RUSU6JRWK=
MZ2-MEL MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nrXWlEPTB;MD6xO|U2QSEQvF2= MYHTRW5ITVJ?
HEL M4rI[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3ywPGlEPTB;MD6xPFUyPyEQvF2= MkXnV2FPT0WU
D-392MG M3yxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfsTWM2OD1yLkG5NVE2KM7:TR?= MlnzV2FPT0WU
SK-LMS-1 NVTaZmR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1KyOWlEPTB;MD6xPVMxOyEQvF2= M1\TV3NCVkeHUh?=
GI-ME-N MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4KyZmlEPTB;MD6xPVMxPiEQvF2= M1\0NXNCVkeHUh?=
LB831-BLC MoTPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mmn3TWM2OD1yLkG5N|Qh|ryP NWT4c2dHW0GQR1XS
DU-4475 M4C3PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3u4[WlEPTB;MD6xPVY2QCEQvF2= NF20PGlUSU6JRWK=
IST-SL1 NUXwPI97T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTBwMkCwPVQh|ryP MXLTRW5ITVJ?
GAK MkLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnm1TWM2OD1yLkKwOVM1KM7:TR?= MVvTRW5ITVJ?
EW-1 NVvwW5BST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTBwMkGwOFch|ryP NIjUVo9USU6JRWK=
LAMA-84 M1O1T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHETWZMUUN3ME2wMlIyQDVzIN88US=> NXTET|FXW0GQR1XS
SK-UT-1 MkHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnraTWM2OD1yLkKyNFQ6KM7:TR?= MkfyV2FPT0WU
VA-ES-BJ MlvyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTBwMkKyOVch|ryP MnrrV2FPT0WU
ACN M1To[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1y0W2lEPTB;MD6yNlY{QCEQvF2= MWHTRW5ITVJ?
SK-PN-DW MoDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TJPWlEPTB;MD6yN|E6KM7:TR?= NFfjZW9USU6JRWK=
HD-MY-Z NFm4UHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofsTWM2OD1yLkKzN|A{KM7:TR?= MV3TRW5ITVJ?
LB373-MEL-D MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XUO2lEPTB;MD6yOFE6QCEQvF2= NGW0cJlUSU6JRWK=
COLO-829 M1rZRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHmyW2FKSzVyPUCuNlQzPTdizszN NV7sdlZ[W0GQR1XS
ES8 M4H0PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TH[GlEPTB;MD6yOFc3OyEQvF2= NYnucndqW0GQR1XS
RXF393 M4C4Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLiRYtOUUN3ME2wMlI2ODF3IN88US=> MmrQV2FPT0WU
TK10 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;2Zm1NUUN3ME2wMlI2PDN3IN88US=> NF;HXolUSU6JRWK=
LOUCY NULRTHlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTBwMkW0OVYh|ryP M2HkSHNCVkeHUh?=
MZ7-mel M2PHSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofyTWM2OD1yLkK2N|c1KM7:TR?= NFjTNYdUSU6JRWK=
CP67-MEL NVfaVnBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTBwMk[3N{DPxE1? MkHpV2FPT0WU
C2BBe1 M4jNfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwMke5NFch|ryP Mlr1V2FPT0WU
K052 Moe5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTBwMki5PUDPxE1? MYfTRW5ITVJ?
MOLT-16 M1zqdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXPTWM2OD1yLkK5OVI1KM7:TR?= MXLTRW5ITVJ?
KNS-81-FD NELRflFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLLe3BKSzVyPUCuN|A{OjNizszN NF\lV3hUSU6JRWK=
CMK NGjIXHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXQTWM2OD1yLkOxNVIh|ryP MX7TRW5ITVJ?
LAN-6 NInOO4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDzXHJ6UUN3ME2wMlMyOyEQvF2= NFzjTpdUSU6JRWK=
KLE Ml3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwM{GzNFYh|ryP MoLJV2FPT0WU
NCCIT NGTnVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTBwM{G3PFMh|ryP MV\TRW5ITVJ?
HH NIS4NGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrIO|lKSzVyPUCuN|I5QTdizszN NH7Ze3hUSU6JRWK=
TE-8 NVzOd5dnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXuxWWVoUUN3ME2wMlM1Ojd7IN88US=> NFKzPW1USU6JRWK=
GDM-1 MmDpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvFTWM2OD1yLkO1NVA1KM7:TR?= MkDMV2FPT0WU
NCI-H747 NETNZZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTBwM{exNFMh|ryP NF\NSXFUSU6JRWK=
NCI-H1092 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFqy[JJKSzVyPUCuN|g5PDRizszN NEfGTpNUSU6JRWK=
8-MG-BA NXLJWFhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXP0VGdRUUN3ME2wMlM6QDN5IN88US=> NWjZTWRlW0GQR1XS
NB17 NVzpb4VzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXDTId6UUN3ME2wMlQzQTdizszN NGfhN4pUSU6JRWK=
LC4-1 NXP0OmhMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTCXll[UUN3ME2wMlQ{PjB5IN88US=> NI\wdodUSU6JRWK=
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NCI-H2227 NVrEXZE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfJZpp7UUN3ME2xMlYyPTZzIN88US=> M3:x[nNCVkeHUh?=
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HAL-01 NFjMem5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTRwNUewN|Qh|ryP NYryUVlJW0GQR1XS
LP-1 MkfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HoSmlEPTB;ND63NlM4OSEQvF2= MX\TRW5ITVJ?
BC-1 NVjrO|lLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzHOWg5UUN3ME21MlAxPDR5IN88US=> NHjXco9USU6JRWK=
EB-3 Mo[xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlS5TWM2OD13LkCzNFQyKM7:TR?= Ml\qV2FPT0WU
GT3TKB MnrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnGOpRuUUN3ME21MlE4PjZ{IN88US=> M3rqUnNCVkeHUh?=
NCI-H209 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\PcGlEPTB;NT6xPVM2OiEQvF2= MXrTRW5ITVJ?
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SIMA NIDpUo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3TZm1bUUN3ME21MlMxPzZ3IN88US=> Ml7WV2FPT0WU
RL NFq4OoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H4emlEPTB;NT6zO|U1OSEQvF2= MnPRV2FPT0WU
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NCI-H1581 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPWe3NKSzVyPU[uNlM5PDlizszN Mnv6V2FPT0WU
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LB1047-RCC MkPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fmOmlEPTB;Nz63NlI{OSEQvF2= NFz5[odUSU6JRWK=
MZ1-PC MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3zTWM2OD15Lki2OVU5KM7:TR?= NYXpNppGW0GQR1XS
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HCC1599 MkXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\HXGlEPTB;N{SuPFc{OiEQvF2= MXrTRW5ITVJ?
NCI-H1155 NGnudphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofMTWM2OD15ND65N|Y4KM7:TR?= M1zLWnNCVkeHUh?=
DOHH-2 NIfLPZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\zb4VmUUN3ME23OE46PTF2IN88US=> NV\r[5NrW0GQR1XS
SK-NEP-1 NELaRmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3IT|NKSzVyPUe1MlA4PTRizszN MX3TRW5ITVJ?
HCC1187 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTd5Lk[xNlIh|ryP M{nuWXNCVkeHUh?=
NCI-H322M MoTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYH2V29rUUN3ME23PE4{PzB7IN88US=> MmTZV2FPT0WU
NCI-H526 NXnjUIJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTd6LkW4O|ch|ryP NWfZUnB[W0GQR1XS
NCI-H2171 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\qTWM2OD15OT60NVM3KM7:TR?= Mmm0V2FPT0WU
COLO-668 NULiSGpkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRThzLkW4PFQh|ryP NVG2R2Y3W0GQR1XS
RS4-11 NUjtPZJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\T[phUUUN3ME24Nk4zPTB3IN88US=> NW[yUYlIW0GQR1XS
NCI-H716 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPlTWM2OD16Mj65NFc2KM7:TR?= M17mfHNCVkeHUh?=
LU-134-A NYLjU4x2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XGXWlEPTB;OEOuNVM2OSEQvF2= NX7KVmxGW0GQR1XS
RPMI-8226 NX3WSpN{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2roVWlEPTB;OESuNlExPyEQvF2= M3PFbHNCVkeHUh?=
KY821 NYXt[mozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3j6UGlEPTB;OUGuOlU2OSEQvF2= MnrLV2FPT0WU
ECC4 NVWyXZRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTl|LkiyOlkh|ryP NVfJV5JIW0GQR1XS
EW-3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTl2LkmwPFEh|ryP MoPJV2FPT0WU
NB7 M1XoVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTlbGxKSzVyPUm1Mlc4QDZizszN M3O5N3NCVkeHUh?=
NCI-H720 MmTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIr0fm1KSzVyPUm4MlQxPjFizszN Mn\QV2FPT0WU
NCI-H446 NGjkUZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fzc2lEPTB;OUmuO|U5QCEQvF2= MljZV2FPT0WU
NCI-H889 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknRTWM2OD1zMESuNlQzKM7:TR?= NFfUfHdUSU6JRWK=
EW-22 MkjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjkUGpGUUN3ME2xNFYvOTlizszN M4\rb3NCVkeHUh?=
BV-173 MlvpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TFUmlEPTB;MUC4MlczQCEQvF2= NIjsbXVUSU6JRWK=
WSU-NHL MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIr2N|NKSzVyPUGwPU43PzFizszN MkXXV2FPT0WU
MN-60 M{[4N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfHTWM2OD1zMEmuOlkh|ryP MnTnV2FPT0WU
DG-75 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFzMz6zOVIh|ryP M{e0THNCVkeHUh?=
DMS-79 NEXDOW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17qNGlEPTB;MUG3MlM5OiEQvF2= M4DhdHNCVkeHUh?=
SK-MEL-1 NULRZ5FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfScXhUUUN3ME2xNVgvODB7IN88US=> M1nBc3NCVkeHUh?=
DMS-153 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHIXnJFUUN3ME2xNlEvPzR3IN88US=> MmHGV2FPT0WU
NCI-H510A NWLpUWNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIf3SHhKSzVyPUGyO{4{OiEQvF2= M1vTTHNCVkeHUh?=
BE-13 NX\Gd5lET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlyyTWM2OD1zM{SuNFQ1KM7:TR?= M{X1[HNCVkeHUh?=
KP-N-YS NVqwT5hJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\HNHhKSzVyPUGzPU44OzZizszN NF7afG1USU6JRWK=
SUP-T1 M3\KfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH[yXFlKSzVyPUG0N{44ODhizszN NUTiR5FxW0GQR1XS
EW-12 NITvb3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPqTWM2OD1zNESuOlk6KM7:TR?= MV\TRW5ITVJ?
NB14 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYjWb|FUUUN3ME2xOFcvODh{IN88US=> MYjTRW5ITVJ?
MDA-MB-134-VI MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTF2OD6yOlgh|ryP MUnTRW5ITVJ?
NCI-H1770 NULGcoQzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorzTWM2OD1zNU[uNlc6KM7:TR?= MX;TRW5ITVJ?
TUR NV32NllxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTF4Nz64O{DPxE1? MlXyV2FPT0WU
NCI-H1417 NXvuZ3ZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\WPJJKSzVyPUG4NE4{OzFizszN MVvTRW5ITVJ?
IMR-5 Ml\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknrTWM2OD1zOEGuOVcyKM7:TR?= Mn7BV2FPT0WU
NCI-H226 NXK3eWlrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTF6OD64OlYh|ryP M1rn[nNCVkeHUh?=
NCI-H187 Mm\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TTcmlEPTB;MUmwMlA3PCEQvF2= MYDTRW5ITVJ?
SF539 NEfTTZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT6W2hrUUN3ME2xPVIvPzJ6IN88US=> M3;BXHNCVkeHUh?=
TALL-1 NIPSbpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTF7OD6zNFQh|ryP NU\INnhmW0GQR1XS
TE-441-T Mn;RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYPMbWZYUUN3ME2xPVkvPzN7IN88US=> MYnTRW5ITVJ?
REH MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DRO2lEPTB;MkO2MlYzPiEQvF2= NYXB[XRyW0GQR1XS
MS-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPY[mlKSzVyPUKzPU4yOjFizszN NVrsbY9bW0GQR1XS
THP-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULmT4p{UUN3ME2yOlQvPzN6IN88US=> M1LHXnNCVkeHUh?=
NCI-H1838 NGL2fWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHQdo9KSzVyPUK3NU41PTZizszN NEO0[4NUSU6JRWK=
P30-OHK MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTJ6Mz64OFch|ryP MlrvV2FPT0WU
C8166 M3eydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTN2NT6zN|gh|ryP NHL2dlFUSU6JRWK=

... 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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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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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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Rating
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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Rating
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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Rating
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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Rating
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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Rating
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 .

Click to enlarge
Rating
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).

Click to enlarge
Rating
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.

文献中の引用 (42)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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