MG-132 化学構造
分子量: 475.62

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Quality Control & MSDS

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 M2\LUmZ2dmO2aX;uJGF{e2G7 NUjDVnBQOjVizszN NUDrWGJOTE2VTx?= MlHZTY5pcWKrdIOgcol1emmlIH;4bYRmKHC{b3T1Z5Rqd25id3n0bEBKSzVyIH;mJFAvOSEQvF2= MkPUNlQ3QTd2OU[=
HL-60 M3LyXWN6fG:2b4jpZ{BCe3OjeR?= NG\uWG81OCEQvF2= M1:3cFQ5KGh? NHfzPWpFVVOR NX\RT3VsUUN3MEyxNEDPxE1? NEPPOo8zPDZ7N{S5Oi=>
SMMC-7721 M3;BXGN6fG:2b4jpZ{BCe3OjeR?= Ml76OFAh|ryP MWm0PEBp MWTEUXNQ NITQd|JKSzVyPUeuNUDPxE1? MVuyOFY6PzR7Nh?=
A-549 NWny[|VVS3m2b4TvfIlkKEG|c3H5 NUDJZY5VPDBizszN M{D6cVQ5KGh? NYPQN3lWTE2VTx?= NEf4RVFKSzVyPEGwJO69VQ>? MWeyOFY6PzR7Nh?=
MCF-7 MkLxR5l1d3SxeHnjJGF{e2G7 MkTsOFAh|ryP NELmeGk1QCCq Mk[5SG1UVw>? MX\JR|UxRTdwMzFOwG0> NX:zS|VtOjR4OUe0PVY>
SW-480 NXj5TYdiS3m2b4TvfIlkKEG|c3H5 Ml6zOFAh|ryP NYXDVod6PDhiaB?= NWjlRo9xTE2VTx?= M2LyXWlEPTB;NDFOwG0> M4[0NVI1Pjl5NEm2
NCI-H929 NGDCWpdEgXSxdH;4bYMhSXO|YYm= M123XFEh|ryP M4D5T|czKGh? M1PkbmROW09? NUfkSnhXUUN3ME2wMlE4KM7:TR?= NEL1e3YzPDZ{NUC4PC=>
293T NIDzTZREgXSxdH;4bYMhSXO|YYm= NX3aR3N3OTBizszN NHTzU3Y4OiCq NHLh[FZFVVOR NUS1eG9bUUN3MEyyJO69VQ>? M37VcVI1PjJ3MEi4
293T MoDESpVv[3Srb36gRZN{[Xl? MnjXNVAh|ryP NGXIOoUzPCCq MYfEUXNQ NIW0TmJOd2SncnH0[Yx6KGmwZIXj[ZMhcGWjdD3zbI9kcyBi M3H6XlI1PjJ3MEi4
HeLa MnzFT4lv[XOnIFHzd4F6 MWSxNEDPxE1? NYLPXlBxOSCq MUjEUXNQ MX;JcoR2[2W|IGDBVnAh[2ynYY\h[4Uh[nliaX7obYJqfGmwZzDwdo9{\WG|b33lJIFkfGm4aYT5 MYOyOFMzOTh|Mx?=
MDA-MB-231 NE\EVJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnv4NUDPxE1? M1TsSFczKGh? MoXGSG1UVw>? Moj3TWM2OD1yLkG4JO69VQ>? M374bFI1OTV|MkC2
MCF-7 NFPQVGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzFNUDPxE1? NGrrcHk4OiCq MlHtSG1UVw>? NILSOZdKSzVyPUCuNVMh|ryP NXmxNnZOOjRzNUOyNFY>
MCF10A Mn\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXGxJO69VQ>? M3vYPVczKGh? Ml32SG1UVw>? NH3QenBKSzVyPUCuNlkh|ryP NYXSfWFKOjRzNUOyNFY>
HEK-293 Mn:wT4lv[XOnIFHzd4F6 NFPUUowzKGGwZDCyNEDPxE1? MVyyJIg> NEO0XplFVVOR NYHyfHAyUW6qaXLpeJMhS2iWLVygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDlibl2g MlfVNlM2PDB5OUC=
Calu6 NGPjXWNHfW6ldHnvckBCe3OjeR?= NH7vT3MyOCEQvF2= MWixPEBp MkOySG1UVw>? M4HreXNq\26rZnnjZY51dHliYXPjeY12dGG2ZYOg[pJifGG6aX6gdJJm[3W{c3;y MXWyN|UxPjR6Nh?=
IFN-gamma-induced RAW264.7 M3LBN2Z2dmO2aX;uJGF{e2G7 NUnvd4FvTE2VTx?= NXzMWWtEUW6qaXLpeJMhdmm2cnnjJI95cWSnIIDyc4R2[3Srb36ge4l1cCCLQ{WwJI9nKDBwMEe3JO69VQ>? MWWyNlI4PzJ5Nx?=
IPC227F MnzXR5l1d3SxeHnjJGF{e2G7 Mk\nNUDPxE1? NHPWOI81QCCq M1f4RmROW09? MXrJR|UxRTBwMEe3JO69VQ>? NIHYNJIzOTl{NEWyPC=>
Hepa-1c1c7 MVTGeY5kfGmxbjDBd5NigQ>? Mn36NlUh|ryP NUHkTYNmPiCq MXLEUXNQ M1Wxdmlv[3KnYYPld{BPemZ{IIDyc5RmcW5ibHX2[Yw> MVKyNFM6OjV2NB?=
COS-7 NEjsZ2lEgXSxdH;4bYMhSXO|YYm= M{HQbFExKM7:TR?= NYX1NoI6TE2VTx?= NGfKc2pKSzVyPEGwJO69VQ>? MV:xPFA5QDB7Nx?=
HuH-7 NX\IRm1LS3m2b4TvfIlkKEG|c3H5 NIPBNlEyOCEQvF2= MX\EUXNQ M3nTbmlEPTB:MUCg{txO Ml64NVgxQDhyOUe=
OCI-Ly3 NGPJUmxHfW6ldHnvckBCe3OjeR?= MUmxNEDPxE4EoB?= M1fhXlQhcA>? MVjEUXNQ NWXzdXNnUW6mdXPld{BpfW2jbjDJb4FxeGGEYXzwbIEhe3SjYnnsbZpifGmxbjD3bZRpKEWFNUCgc4YhOSEQvF2= M3LkPFE5ODJ2MUGz
A2780 cDDP M3f4b2Fxd3C2b4Ppd{BCe3OjeR?= NHr4bIUzPCCq Mnr5SG1UVw>? MXvJcoR2[2W|IHHwc5B1d3OrczDifUBqdmirYnn0bY5oKFCWRV6g[IVoemGmYYTpc44> MYqxO|Y5PDBzOB?=
LPS-stimulated RAW264.7 cells MX7GeY5kfGmxbjDBd5NigQ>? NUjxV3IxTE2VTx?= MoPMTY5pcWKrdIOgUmYuc2GycHHCJGRPSSCkaX7kbY5o M4frVlE4PDB5Mke3
PC12 Mn73SpVv[3Srb36gRZN{[Xl? MU[xNFAh|ryPwrC= NUfTVGkzOjRiaB?= MojvSG1UVw>? NHrweIZKdmirYnn0d{A3NU:KRFGtJIFv\CCKMl:yMYlv\HWlZXSgZ5l1d3SxeHnjbZR6 MYqxO|E2QDR3NB?=
PC3 Mn2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqyNEDPxE1? NVyzVnFJPDhiaB?= MneySG1UVw>? NXnmfnVUUUN3ME2wMlYh|ryP NWe1e4t4OTZ4OE[1N|c>
LP-1 NYPSO41pSXCxcITvd4l{KEG|c3H5 MUGzNFAhdk1? NFzwW2wzPCCq NEfTfHVFVVOR NEXab3RKdmS3Y3XzJIFxd3C2b4Ppd{BjgSCrbnPy[YF{cW6pIHPs[YF3\WRiUFHSVEBt\X[nbDDhcoQhemWmdXPpcochVWOuLUGgdJJwfGWrbjDs[ZZmdA>? NYC3PZpGOTV7NUi1PFk>
ES6 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTBwMEGzNFYh|ryP M{fzcHNCVkeHUh?=
A101D NILqXHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXiTWM2OD1yLkCzNlc6KM7:TR?= M33Gc3NCVkeHUh?=
OCUB-M MknTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTBwMEO3N|ch|ryP NGXTfXNUSU6JRWK=
LB2518-MEL MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwMEO3OkDPxE1? NGX4bm1USU6JRWK=
SH-4 NIfGToVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzOTWM2OD1yLkC0N|Eh|ryP MnrGV2FPT0WU
KNS-42 MoW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfKTWM2OD1yLkC0OFQyKM7:TR?= MXrTRW5ITVJ?
DSH1 Mn:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\lcXVFUUN3ME2wMlA2Ojh7IN88US=> NEjHRoNUSU6JRWK=
NTERA-S-cl-D1 NV3j[JV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDoTWM2OD1yLkC1O|czKM7:TR?= MkjGV2FPT0WU
D-542MG MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPme5NKSzVyPUCuNFU6PTdizszN MkP6V2FPT0WU
KS-1 NFrK[FlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTBwME[0OVgh|ryP M{joNnNCVkeHUh?=
BL-41 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\NcWs{UUN3ME2wMlA3QTR5IN88US=> NUXX[2V2W0GQR1XS
LXF-289 M3TGTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rpdWlEPTB;MD6wO|A3PiEQvF2= M1PIdnNCVkeHUh?=
D-247MG MmjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MorKTWM2OD1yLkC3NlA6KM7:TR?= MUTTRW5ITVJ?
MMAC-SF Mmj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nUb2lEPTB;MD6wO|I3QCEQvF2= Mn;WV2FPT0WU
CP66-MEL MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTBwMEe1JO69VQ>? MV7TRW5ITVJ?
LB771-HNC MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofMTWM2OD1yLkC4NFM3KM7:TR?= M1TjOXNCVkeHUh?=
no-10 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv1TWM2OD1yLkC4PVA6KM7:TR?= NFTDSnBUSU6JRWK=
A388 MkDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTBwMEmwOlUh|ryP MmrNV2FPT0WU
OPM-2 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fNZmlEPTB;MD6xNFQ4PCEQvF2= NX3GdZBxW0GQR1XS
OVCAR-4 NV[1SY1GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;URWlEPTB;MD6xNFk{QCEQvF2= MmiyV2FPT0WU
HOP-62 M4S1SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUThV4EyUUN3ME2wMlExQTR7IN88US=> NEDQcmtUSU6JRWK=
ML-2 NIK2NFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3FTWM2OD1yLkGxPFA3KM7:TR?= MVrTRW5ITVJ?
UACC-257 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1G1NWlEPTB;MD6xNVkzPyEQvF2= NWPBb4E5W0GQR1XS
NEC8 Mlm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTBwMUG5PVUh|ryP MVfTRW5ITVJ?
ONS-76 NEfwflVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3y2NGlEPTB;MD6xNlk{PSEQvF2= NEPhSFVUSU6JRWK=
KE-37 M4ruNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTLPZBKSzVyPUCuNVMzPzhizszN NF\uT5VUSU6JRWK=
HT-144 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTBwMUO4PVUh|ryP MWLTRW5ITVJ?
LB2241-RCC NFy2NI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\GR3NWUUN3ME2wMlE1OjR5IN88US=> MoXJV2FPT0WU
TE-5 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTpOY5DUUN3ME2wMlE1Ojd6IN88US=> NV;kTFZ2W0GQR1XS
KINGS-1 M{nIRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFqyW3lKSzVyPUCuNVQ4QSEQvF2= M2Hj[nNCVkeHUh?=
NCI-H69 M{\rcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXpTWM2OD1yLkG1NVQyKM7:TR?= MV;TRW5ITVJ?
CAS-1 M{mwN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLudFhKSzVyPUCuNVU1QDJizszN M{nx[nNCVkeHUh?=
D-263MG MmrsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwMU[wNFYh|ryP NGjtUGVUSU6JRWK=
A253 NFzCbGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PVXmlEPTB;MD6xOlEzQCEQvF2= NUPB[mFWW0GQR1XS
PF-382 NHvKd49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUDJR|UxRTBwMU[3NFYh|ryP MVHTRW5ITVJ?
CESS NVrM[oc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TqbWlEPTB;MD6xO|A3KM7:TR?= M1XiO3NCVkeHUh?=
MZ2-MEL MlfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTYN5ZlUUN3ME2wMlE4PTV7IN88US=> NH\iXpJUSU6JRWK=
HEL NGrBOm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTBwMUi1NVch|ryP Mo\QV2FPT0WU
D-392MG NWnqU2h[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTBwMUmxNVUh|ryP M4XTWnNCVkeHUh?=
SK-LMS-1 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWSyOYxHUUN3ME2wMlE6OzB|IN88US=> MkTxV2FPT0WU
GI-ME-N NGryRmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mor3TWM2OD1yLkG5N|A3KM7:TR?= MVfTRW5ITVJ?
LB831-BLC Mm\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3v0T2lEPTB;MD6xPVM1KM7:TR?= MUHTRW5ITVJ?
DU-4475 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVr1XItOUUN3ME2wMlE6PjV6IN88US=> MlHsV2FPT0WU
IST-SL1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTBwMkCwPVQh|ryP MVfTRW5ITVJ?
GAK MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHT2TXFKSzVyPUCuNlA2OzRizszN NWD3b|FzW0GQR1XS
EW-1 NIC1ZYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYroSG1oUUN3ME2wMlIyODR5IN88US=> M3m5NHNCVkeHUh?=
LAMA-84 M3fNfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTBwMkG4OVEh|ryP M3rZcXNCVkeHUh?=
SK-UT-1 MkPTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTBwMkKwOFkh|ryP Mli1V2FPT0WU
VA-ES-BJ MmXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTBwMkKyOVch|ryP M4PyNnNCVkeHUh?=
ACN MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfBfYJKSzVyPUCuNlI3OzhizszN M{\3eXNCVkeHUh?=
SK-PN-DW MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1WxTWlEPTB;MD6yN|E6KM7:TR?= MlLlV2FPT0WU
HD-MY-Z Mn\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwMkOzNFMh|ryP NFvVSmVUSU6JRWK=
LB373-MEL-D NYTZTI41T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2H2SGlEPTB;MD6yOFE6QCEQvF2= NXyye2ppW0GQR1XS
COLO-829 NWPEOJFrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTBwMkSyOVch|ryP NYPUeXFJW0GQR1XS
ES8 MnXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTBwMkS3OlMh|ryP MorMV2FPT0WU
RXF393 NIfR[GtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXiTWM2OD1yLkK1NFE2KM7:TR?= NGHvUXRUSU6JRWK=
TK10 MkC1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHKwUZJKSzVyPUCuNlU1OzVizszN NF;te5hUSU6JRWK=
LOUCY MlnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rnXWlEPTB;MD6yOVQ2PiEQvF2= M2HFUHNCVkeHUh?=
MZ7-mel M4nn[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\vcGlEPTB;MD6yOlM4PCEQvF2= M{fNcHNCVkeHUh?=
CP67-MEL M{LOSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1f1eWlEPTB;MD6yOlc{KM7:TR?= NUPmNYNwW0GQR1XS
C2BBe1 MnzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF75XWJKSzVyPUCuNlc6ODdizszN MYDTRW5ITVJ?
K052 NUHRZWRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPQTWM2OD1yLkK4PVkh|ryP NWfFZ|RYW0GQR1XS
MOLT-16 M4HVdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DBemlEPTB;MD6yPVUzPCEQvF2= MYTTRW5ITVJ?
KNS-81-FD MkDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTBwM{CzNlMh|ryP MXHTRW5ITVJ?
CMK MnPOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfJTWM2OD1yLkOxNVIh|ryP M3f2SXNCVkeHUh?=
LAN-6 MoTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTBwM{GzJO69VQ>? MWrTRW5ITVJ?
KLE M2rpUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzHfJFKSzVyPUCuN|E{ODZizszN M1jp[XNCVkeHUh?=
NCCIT Moq1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3D[Ih{UUN3ME2wMlMyPzh|IN88US=> NInkXYRUSU6JRWK=
HH M1W3XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn34TWM2OD1yLkOyPFk4KM7:TR?= NVTFfnA5W0GQR1XS
TE-8 NWTFdFduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlK2TWM2OD1yLkO0Nlc6KM7:TR?= M4C4cnNCVkeHUh?=
GDM-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjkTWM2OD1yLkO1NVA1KM7:TR?= MU\TRW5ITVJ?
NCI-H747 Mn7QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTBwM{exNFMh|ryP NVHoVnR[W0GQR1XS
NCI-H1092 NY\nRlhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml60TWM2OD1yLkO4PFQ1KM7:TR?= MXzTRW5ITVJ?
8-MG-BA NYHGc5ZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnmdJZKSzVyPUCuN|k5OzdizszN MknkV2FPT0WU
NB17 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjIeXhKSzVyPUCuOFI6PyEQvF2= MYjTRW5ITVJ?
LC4-1 NWLJOld6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTBwNEO2NFch|ryP M1rDVXNCVkeHUh?=
TE-1 NEK2R2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vRU2lEPTB;MD60OVEyQSEQvF2= MWfTRW5ITVJ?
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TE-9 M{P2PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1OySmlEPTB;MD62NVA{OyEQvF2= MniwV2FPT0WU
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GB-1 NGX3fpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHtbnR2UUN3ME2wMlczOTJ2IN88US=> M3e2TnNCVkeHUh?=
CTB-1 MmXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWCzd|FlUUN3ME2wMlc4QTV3IN88US=> MlHxV2FPT0WU
Becker NF7YPIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\vXlNKSzVyPUCuO|k3OjFizszN MmnIV2FPT0WU
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NCI-H23 MnPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4T3eGlEPTB;MT6yNFQyKM7:TR?= NYDQNVdkW0GQR1XS
IA-LM NVvmZ|h6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nNdmlEPTB;MT6yOFEyPiEQvF2= M4jGRXNCVkeHUh?=
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NCI-H719 NH7DdZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3z0fmlEPTB;MT6yO|QyOSEQvF2= MW\TRW5ITVJ?
SW684 MmjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXjPR2FMUUN3ME2xMlI5PjV7IN88US=> NXOzPXoxW0GQR1XS
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EW-16 M4TLS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvmRnRPUUN3ME2xMlMyOzR5IN88US=> M{e3UnNCVkeHUh?=
NCI-H128 NWDWO3FJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPNOnpiUUN3ME2xMlM2QDF2IN88US=> M3rUN3NCVkeHUh?=
HC-1 MnnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGH2OZVKSzVyPUGuN|gyPyEQvF2= MUTTRW5ITVJ?
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Raji MlLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XvbmlEPTB;MT60NVg2KM7:TR?= NE\wc5dUSU6JRWK=
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NCI-H2081 MoHsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDHdIRpUUN3ME2xMlU2OTl4IN88US=> MnW0V2FPT0WU
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NCI-H2227 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTFwNkG1OlEh|ryP NX;MOG11W0GQR1XS
D-502MG M13zTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\uVGlEPTB;MT62O|IyOSEQvF2= M{HreXNCVkeHUh?=
NCI-H2141 NXXMW2pGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTFwNkezNVch|ryP NV:1VIZUW0GQR1XS
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SU-DHL-1 Mo\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[2dY9jUUN3ME2xMlcyOjhzIN88US=> MmrvV2FPT0WU
BB30-HNC NEDKWZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTFwN{K2PFUh|ryP MkWxV2FPT0WU
TE-15 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[5O4YxUUN3ME2xMlkzOzd|IN88US=> NIfXfFZUSU6JRWK=
JVM-3 NFPoToxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrOTWM2OD1zLkmzPVA1KM7:TR?= NU\Yb2M6W0GQR1XS
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no-11 MkmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHQRo9ZUUN3ME2yMlA{OTB2IN88US=> MXTTRW5ITVJ?
QIMR-WIL M17YTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILVfVRKSzVyPUKuNVY4PjJizszN M1\q[nNCVkeHUh?=
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MFM-223 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUHMbHN3UUN3ME2yMlUxQDdzIN88US=> NIHxZoRUSU6JRWK=
SW982 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTJwNUG0PEDPxE1? NWfYTVFXW0GQR1XS
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SCC-3 Ml;ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnKWW1KSzVyPUOuNVA5PDhizszN MnvZV2FPT0WU
RH-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjHdJNHUUN3ME2zMlM5PzR6IN88US=> NEKySWpUSU6JRWK=
NCI-H748 NIjMOJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTNwNESyOlYh|ryP MlrTV2FPT0WU
HCC2218 MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2GzNGlEPTB;Mz60Olk{PyEQvF2= M2L2PHNCVkeHUh?=
MEG-01 NYnhfZB3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MojTTWM2OD1|LkW5Olgh|ryP NH7nNnZUSU6JRWK=
NB12 M4HVVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PwNWlEPTB;Mz61PVg5QCEQvF2= M3frcHNCVkeHUh?=
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KMS-12-PE MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYr4dYh6UUN3ME2zMlY4PzJ|IN88US=> MnPPV2FPT0WU
SKM-1 MlfuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITIWFJKSzVyPUOuO|E{PzZizszN M1:5cXNCVkeHUh?=
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D-336MG MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTRwMEGxOlYh|ryP M2DkWnNCVkeHUh?=
NCI-H1650 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEOxXppKSzVyPUSuNVU4QTdizszN NFLhXWdUSU6JRWK=
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LB647-SCLC NFjOTWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPJTWM2OD12LkW2N|A5KM7:TR?= NXzHSXl7W0GQR1XS
HAL-01 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjWXFlJUUN3ME20MlU4ODN2IN88US=> NITI[ZdUSU6JRWK=
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BC-1 MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULEWnVbUUN3ME21MlAxPDR5IN88US=> NYjVT2NPW0GQR1XS
EB-3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LnRWlEPTB;NT6wN|A1OSEQvF2= M{PISnNCVkeHUh?=
GT3TKB MlPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXmNVFZUUN3ME21MlE4PjZ{IN88US=> NXjYe4lMW0GQR1XS
NCI-H209 NF;1TYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXCcoZKSzVyPUWuNVk{PTJizszN M1ywenNCVkeHUh?=
BT-474 NX\YO49lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nVTGlEPTB;NT6yN|ExOiEQvF2= NF7RS5hUSU6JRWK=
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SIMA M4n3V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXJTWM2OD13LkOwO|Y2KM7:TR?= MV;TRW5ITVJ?
RL NVXQdmtnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLufol2UUN3ME21MlM4PTRzIN88US=> M1vSW3NCVkeHUh?=
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NCI-H1581 NYn5c4x2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{P1UmlEPTB;Nj6yN|g1QSEQvF2= NVzV[lV2W0GQR1XS
HUTU-80 NHzXdmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTZwM{[4PVch|ryP MkXRV2FPT0WU
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SK-N-FI NFW5UJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3OXFZoUUN3ME22MlQ2QDV2IN88US=> MoDPV2FPT0WU
U-266 M4TuR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzKTWM2OD14LkWxPVI3KM7:TR?= NVmzW3FGW0GQR1XS
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NALM-6 MkjyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzOcIZKSzVyPU[uPFY4PTRizszN NXP4TGtpW0GQR1XS
OCI-AML2 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnzTYlFUUN3ME23MlAxOzJ4IN88US=> NW\VN2JuW0GQR1XS
SHP-77 NEnTZ2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEL1RXpKSzVyPUeuNlI1OyEQvF2= MmTrV2FPT0WU
NOMO-1 NXzEN241T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlOzTWM2OD15LkK0NlU1KM7:TR?= MUPTRW5ITVJ?
SK-N-DZ MlfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFe3WGZKSzVyPUeuO|ExQDlizszN NX3xOmpuW0GQR1XS
LB1047-RCC Mm\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTdwN{KyN|Eh|ryP MnjPV2FPT0WU
MZ1-PC MmXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4H5SWlEPTB;Nz64OlU2QCEQvF2= NF3WeYVUSU6JRWK=
NB10 MkPiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3oVVVyUUN3ME23Mlk6PTV4IN88US=> Moq0V2FPT0WU
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RPMI-8866 Mmi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjE[YdKSzVyPUe0Mlc2ODlizszN NHXpOYpUSU6JRWK=
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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 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 95 mg/mL (199.73 mM)
Ethanol 95 mg/mL (199.73 mM)
Water <1 mg/mL
In vivo 4% DMSO+30% PEG 300+20% propylene glycol+ddH2O 2mg/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

文献中の引用 (47)

Frequently Asked Questions

  • Question 1
    I want to know whether it contains EDTA or other chelating agent in this product(S2619)?

    Answer: Our S2619 MG-132 doesn't contain EDTA or other chelating agent.

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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