MG-132

For research use only.

Catalog No.S2619

1265 publications

MG-132 Chemical Structure

CAS No. 1211877-36-9

MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells.

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Selleck's MG-132 had a noticeably greater effect when compared with similar products from Sigma: This is directly due to using the (S, R, S) - (-) - 2 configuration.

P21 protein can be degraded through ubiquitylation pathway. Inhibition of proteasome activities results in the accumulation of P21 protein, therefore, the more powerful the inhibiting effect, the more P21 protein is accumulated. (testing protein: P21; Cell line: Hela; treatment condition: final concentration of MG-132 is 5μM, with a 6 hour treatment time)

Selleck's MG-132 has been cited by 1265 publications

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Choose Selective Proteasome Inhibitors

Biological Activity

Description MG132 is a potent cell-permeable proteasome and calpain inhibitor with IC50s of 0.1 μM and 1.2 μM for the inhibition of proteasome and calpain, respectively. MG132 activates autophagy and induces apoptosis in tumor cells.
Targets
Proteasome [9]
(Cell-free assay)
100 nM
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LP-1 M{\GR2Fxd3C2b4Ppd{BCe3OjeR?= NUSwZVZPOzByIH7N M4D5U|I1KGh? NWKwSWtWTE2VTx?= M3fsfGlv\HWlZYOgZZBweHSxc3nzJIJ6KGmwY4LlZZNqdmdiY3zlZZZm\CCSQWLQJIxmfmWuIHHu[EBz\WS3Y3nu[{BO[2xvMTDwdo91\WmwIHzleoVt M3TEdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OUW4OVg6Lz5zNUm1PFU5QTxxYU6=
PC3 MljWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUWyNEDPxE1? M4[3NVQ5KGh? MlWzSG1UVw>? NYC1b3dqUUN3ME2wMlYh|ryP NHrN[lM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNk[4OlU{Pyd-MU[2PFY2Ozd:L3G+
PC12 NV\MbmlzTnWwY4Tpc44hSXO|YYm= MlXZNVAxKM7:TdMg NFHW[oQzPCCq M4PEdmROW09? M1Hye2lvcGmkaYTzJFYuV0iGQT2gZY5lKEh{T{KtbY5lfWOnZDDjfZRwfG:6aXPpeJk> MofwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTdzNUi0OVQoRjF5MUW4OFU1RC:jPh?=
LPS-stimulated RAW264.7 cells M4jEUWZ2dmO2aX;uJGF{e2G7 M33Re2ROW09? Mkn5TY5pcWKrdIOgUmYuc2GycHHCJGRPSSCkaX7kbY5o NWruUY5rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe0NFczPzdpPkG3OFA4Ojd5PD;hQi=>
OCI-Ly3 NHe4RYFHfW6ldHnvckBCe3OjeR?= MnWxNVAh|ryPwrC= M1y2W|QhcA>? M1X3e2ROW09? MmTHTY5lfWOnczDoeY1idiCLa3HwdIFD[WyyaHGgd5Ri[mmuaYrheIlwdiC5aYToJGVEPTBib3[gNUDPxE1? MnTrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyMkSxNVMoRjF6MEK0NVE{RC:jPh?=
A2780 cDDP MknpRZBweHSxc3nzJGF{e2G7 Mnz6NlQhcA>? M1mye2ROW09? NH;jTmlKdmS3Y3XzJIFxd3C2b4Ppd{BjgSCrbnjpZol1cW6pIGDUSW4h\GWpcnHkZZRqd25? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZ6NECxPEc,OTd4OESwNVg9N2F-
COS-7 NITqd4ZEgXSxdH;4bYMhSXO|YYm= NIDLcI8yOCEQvF2= M3\VcGROW09? NFrvO3VKSzVyPEGwJO69VQ>? NETaTo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEC4PFA6Pyd-MUiwPFgxQTd:L3G+
HuH-7 NYC3fnY4S3m2b4TvfIlkKEG|c3H5 M1HPZ|ExKM7:TR?= M2D6e2ROW09? NGHrV5RKSzVyPEGwJO69VQ>? Mn63QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyOEiwPVcoRjF6MEi4NFk4RC:jPh?=
Hepa-1c1c7 NVPNfmpRTnWwY4Tpc44hSXO|YYm= NX;jXlNYOjVizszN NWHxPYJEPiCq NFzHTJhFVVOR Ml7MTY5kemWjc3XzJG5z\jJicILveIVqdiCuZY\lcC=> M17uXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{myOVQ1Lz5{MEO5NlU1PDxxYU6=
IPC227F NUP2XVk3S3m2b4TvfIlkKEG|c3H5 MWWxJO69VQ>? MmHpOFghcA>? M1;5T2ROW09? NEC5WItKSzVyPUCuNFc4KM7:TR?= M{jQT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOUK0OVI5Lz5{MUmyOFUzQDxxYU6=
Calu6 M2Hlb2Z2dmO2aX;uJGF{e2G7 NVrLZ2FJOTBizszN M17ZVVE5KGh? MkLUSG1UVw>? MVLTbYdvcW[rY3HueIx6KGGlY4XteYxifGW|IH\yZZRigGmwIIDy[YN2enOxch?= NVmwZ4xWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1NFY1QDZpPkKzOVA3PDh4PD;hQi=>
IFN-gamma-induced RAW264.7 NGiwTIFHfW6ldHnvckBCe3OjeR?= M3;meGROW09? MorUTY5pcWKrdIOgcol1emmlIH;4bYRmKHC{b3T1Z5Rqd25id3n0bEBKSzVyIH;mJFAvODd5IN88US=> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjJ5N{K3O{c,OjJ{N{eyO|c9N2F-
HEK-293 M4PwNmtqdmG|ZTDBd5NigQ>? NWHUeYFFOiCjbnSgNlAh|ryP MYiyJIg> M1r6V2ROW09? NWLtd5dKUW6qaXLpeJMhS2iWLVygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDlibl2= NVH5V4JwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA4QTBpPkKzOVQxPzlyPD;hQi=>
MCF10A NVm2cFRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17rW|Eh|ryP M1OwblczKGh? MXzEUXNQ M1nLT2lEPTB;MD6yPUDPxE1? NW\OPW5HRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOVMzODZpPkK0NVU{OjB4PD;hQi=>
MCF-7 NEftboNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmxJO69VQ>? M1TTOVczKGh? M3POcmROW09? MoOwTWM2OD1yLkGzJO69VQ>? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF3M{KwOkc,OjRzNUOyNFY9N2F-
HeLa NHT3U2hMcW6jc3WgRZN{[Xl? NUfY[5pnOTBizszN NXzPUHcxOSCq MXfEUXNQ MWnJcoR2[2W|IGDBVnAh[2ynYY\h[4Uh[nliaX7obYJqfGmwZzDwdo9{\WG|b33lJIFkfGm4aYT5 MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN{MUizN{c,OjR|MkG4N|M9N2F-
MDA-MB-231 M3PJfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVOxJO69VQ>? MUC3NkBp M4W1[2ROW09? M1K1bmlEPTB;MD6xPEDPxE1? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF3M{KwOkc,OjRzNUOyNFY9N2F-
293T NUW3U5liS3m2b4TvfIlkKEG|c3H5 NE\UOGYyOCEQvF2= MkTEO|IhcA>? MXvEUXNQ MWTJR|UxRDJizszN M{O4e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkK1NFg5Lz5{NE[yOVA5QDxxYU6=
293T NF2wR|RHfW6ldHnvckBCe3OjeR?= Mkn6NVAh|ryP M17tZ|I1KGh? NHfibmxFVVOR NUnvb3p7VW:mZYLheIVtgSCrbnT1Z4V{KGinYYStd4hw[2t? M2XWfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkK1NFg5Lz5{NE[yOVA5QDxxYU6=
NCI-H929 MWLDfZRwfG:6aXOgRZN{[Xl? MlzLNUDPxE1? M{foXVczKGh? M{TZSmROW09? MYLJR|UxRTBwMUeg{txO MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ{NUC4PEc,OjR4MkWwPFg9N2F-
A-549 MWfDfZRwfG:6aXOgRZN{[Xl? MXO0NEDPxE1? NGTxc4U1QCCq M3j2[2ROW09? NGr4TXBKSzVyPEGwJO69VQ>? M4HvOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nkm3OFk3Lz5{NE[5O|Q6PjxxYU6=
MCF-7 NXHJTZAzS3m2b4TvfIlkKEG|c3H5 MoLqOFAh|ryP NIS0dZA1QCCq MWTEUXNQ Mn\yTWM2OD15LkOg{txO MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ7N{S5Okc,OjR4OUe0PVY9N2F-
SW-480 MWrDfZRwfG:6aXOgRZN{[Xl? M4[4OFQxKM7:TR?= M1\2XVQ5KGh? NWDtTml6TE2VTx?= MYPJR|UxRTRizszN NYj2SXZwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2PVc1QTZpPkK0Olk4PDl4PD;hQi=>
HL-60 M{\lWmN6fG:2b4jpZ{BCe3OjeR?= M3LQcVQxKM7:TR?= NYq5TYZUPDhiaB?= MYXEUXNQ MXrJR|UxRDFyIN88US=> NETyTW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[5O|Q6Pid-MkS2PVc1QTZ:L3G+
SMMC-7721 NVPYR2Y4S3m2b4TvfIlkKEG|c3H5 NWLOWmd{PDBizszN NXLveZZ4PDhiaB?= M3HDOWROW09? M2TjUmlEPTB;Nz6xJO69VQ>? MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ7N{S5Okc,OjR4OUe0PVY9N2F-
LPS-stimulated RAW264.7 cells M4C1bGZ2dmO2aX;uJGF{e2G7 MlrONlUh|ryP MlfHSG1UVw>? MV\Jcohq[mm2czDubZRzcWNib4jp[IUheHKxZIXjeIlwdiC5aYToJGlEPTBib3[gNE4yKM7:TR?= MkHlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4OUe0PVYoRjJ2Nkm3OFk3RC:jPh?=
lymphoblastoid M1;nfWZ2dmO2aX;uJIF{e2G7 MonvTWM2OCB;IECuNFAzKM7:TR?= Ml60QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd7OU[5PFcoRjF5OUm2PVg4RC:jPh?=
LCL M1jmOGZ2dmO2aX;uJIF{e2G7 NHjPenoyOiCq NX;LN2NwUUN3MDC9JFAvODB{IN88US=> NVTHNIVFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2PFc3ODlpPkKwOlg4PjB7PD;hQi=>
HL-60 NFHuXoZHfW6ldHnvckBie3OjeR?= NVzGXWI2UUN3MDC9JFAvODZ6IN88US=> NFnkVII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUe4NFYzOyd-MUW3PFA3OjN:L3G+
IPC227F NHu5bYpHfW6ldHnvckBie3OjeR?= NELOSXEyKGh? MW\JR|UxKD1iMD6wO|ch|ryP M{\QT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4MkKwPVg5Lz5zNkKyNFk5QDxxYU6=
RAW264.7 M3fBdmFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZZN{[Xl? Mlr6NVghcA>? NEXoW2lKSzVyIE2gNE4xQCEQvF2= NXXuZnlnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK2NlA3PzdpPkKyOlIxPjd5PD;hQi=>
RAW264.7 NED5OnpCdnSraX7mcIFudWG2b4L5JIFkfGm4aYT5JIF{e2G7 NHvn[GkyQCCq NFvqWGpKSzVyIE2gNE4yKM7:TR?= MmDLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MUm4O|EoRjJ|OEG5PFcyRC:jPh?=
RAW264.7 NUDFV5BYTnWwY4Tpc44h[XO|YYm= M4XhV2lEPTBiPTCwMlEh|ryP MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDV7N{i5OEc,OjR3OUe4PVQ9N2F-
RAW264.7 MnL4SpVv[3Srb36gZZN{[Xl? Ml24NVghcA>? NHGyUIRKSzVyIE2gNE4yKM7:TR?= MnfwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{MUm4NFkoRjJ2MkG5PFA6RC:jPh?=
RAW264.7 MWTGeY5kfGmxbjDhd5NigQ>? MXixPEBp M{XnfGlEPTBiPTCwMlE2KM7:TR?= NGPIV4c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OyO|Y3QCd-MkOzNlc3Pjh:L3G+
RAW264.7 NFH6Z2xHfW6ldHnvckBie3OjeR?= MVexPEBp M4HROWlEPTBiPTCwMlE2KM7:TR?= M3f6O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{W3NFE6Lz5{Nke1O|AyQTxxYU6=
RAW264.7 MmL2RY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDhd5NigQ>? NHzPeI4yQCCq M2TZbmlEPTBiPTCwMlE5KM7:TR?= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzJyM{K5NUc,Ojd{MEOyPVE9N2F-
RAW264.7 NYrsSYpwSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBie3OjeR?= NIi5ZXgyKGh? NEjzcpVKSzVyIE2gNE4zKM7:TR?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTN|OEK2NEc,Ojl|M{iyOlA9N2F-
MDA-MB-231 Mmn0R5l1d3SxeHnjbZR6KGG|c3H5 Mn7zTWM2OCB;IECuNlUh|ryP Ml61QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh3OUiwNVgoRjF6NUm4NFE5RC:jPh?=
MCF7 NHXUU|VEgXSxdH;4bYNqfHliYYPzZZk> M1XZVGlEPTBiPTCwMlMh|ryP NYLwN2V2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi1PVgxOThpPkG4OVk5ODF6PD;hQi=>
RAW264.7 M3KwNWZ2dmO2aX;uJIF{e2G7 M3HZT|E5KGh? MlzCTWM2OCB;IECuN|Uh|ryP M3vXU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMES0PFQ4Lz5{MUC0OFg1PzxxYU6=
RAW264.7 MofoRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDhd5NigQ>? NIPPR3VKSzVyIE2gNE41OzlizszN NEXqS5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW2NVA3OCd-MkG1OlExPjB:L3G+
HEK293 M{P5cWZ2dmO2aX;uJIF{e2G7 NIjJUG4zKGh? MVvJR|UxKD1iMD62JO69VQ>? MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2MEe5NEc,OjN3NEC3PVA9N2F-
RAW264.7 NGnOb3hVd3irY3n0fUBie3OjeR?= NGe5bHlKSzVyIE2gNE43OyEQvF2= MmHTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ6NUiyPVcoRjJ{OEW4Nlk4RC:jPh?=
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western Blot
Bcr-Abl; 

PubMed: 26722260     


(C) K562 cells were treated with SAHA (1 µM or 2 µM), MG-132 (400 nM) or SAHA plus MG-132 (400 nM) for 24 h. Western blot analysis was performed, using antibodies against Bcr-Abl, Ac-histone H3, caspase-3 and PARP. β-actin was used as a loading control. (D) K562G cells were treated with SAHA (1 µM or 2 µM), MG-132 (200 nM) or SAHA plus MG-132 (200 nM) for 24 h. Western blot analysis was performed, using antibodies against Bcr-Abl, Ac-histone H3, caspase-3 and PARP. β-actin was used as a loading control. Representative blots from three independent experiments are shown.

Ac-histone H3; 

PubMed: 26722260     


(C) K562 cells were treated with SAHA (1 µM or 2 µM), MG-132 (400 nM) or SAHA plus MG-132 (400 nM) for 24 h. Western blot analysis was performed, using antibodies against Bcr-Abl, Ac-histone H3, caspase-3 and PARP. β-actin was used as a loading control. (D) K562G cells were treated with SAHA (1 µM or 2 µM), MG-132 (200 nM) or SAHA plus MG-132 (200 nM) for 24 h. Western blot analysis was performed, using antibodies against Bcr-Abl, Ac-histone H3, caspase-3 and PARP. β-actin was used as a loading control. Representative blots from three independent experiments are shown.

Cleaved-caspase3; 

PubMed: 26722260     


(C) K562 cells were treated with SAHA (1 µM or 2 µM), MG-132 (400 nM) or SAHA plus MG-132 (400 nM) for 24 h. Western blot analysis was performed, using antibodies against Bcr-Abl, Ac-histone H3, caspase-3 and PARP. β-actin was used as a loading control. (D) K562G cells were treated with SAHA (1 µM or 2 µM), MG-132 (200 nM) or SAHA plus MG-132 (200 nM) for 24 h. Western blot analysis was performed, using antibodies against Bcr-Abl, Ac-histone H3, caspase-3 and PARP. β-actin was used as a loading control. Representative blots from three independent experiments are shown.

Cleaved-PARP; 

PubMed: 26722260     


(C) K562 cells were treated with SAHA (1 µM or 2 µM), MG-132 (400 nM) or SAHA plus MG-132 (400 nM) for 24 h. Western blot analysis was performed, using antibodies against Bcr-Abl, Ac-histone H3, caspase-3 and PARP. β-actin was used as a loading control. (D) K562G cells were treated with SAHA (1 µM or 2 µM), MG-132 (200 nM) or SAHA plus MG-132 (200 nM) for 24 h. Western blot analysis was performed, using antibodies against Bcr-Abl, Ac-histone H3, caspase-3 and PARP. β-actin was used as a loading control. Representative blots from three independent experiments are shown.

ASCL1; 

PubMed: 19765735     


MG-132 decreases the levels of ASCL1 and CgA in carcinoid cancer cells. Pulmonary (NCI-H727) (A) carcinoid cancer cells were treated with MG-132 (0 to 4µM) for 48 hours and cell lysates were analyzed by Western blotting for the expression of ASCL1 and CgA. Treatment with MG-132 results in a dose dependent inhibition of the two neuroendocrine tumor markers. Analysis for GAPDH confirmed equal loading.

CgA; 

PubMed: 19765735     


MG-132 decreases the levels of ASCL1 and CgA in carcinoid cancer cells. Pulmonary (NCI-H727) (A) carcinoid cancer cells were treated with MG-132 (0 to 4µM) for 48 hours and cell lysates were analyzed by Western blotting for the expression of ASCL1 and CgA. Treatment with MG-132 results in a dose dependent inhibition of the two neuroendocrine tumor markers. Analysis for GAPDH confirmed equal loading.

Nrf2; 

PubMed: 23604711     


MG-132 stimulates Nrf2 and HO-1 protein expression in HAECs in a time-dependent fashion. Cells were treated with MG-132 (2 μM) for various times (0–24 h), and Nrf2 and HO-1 protein were quantified by scanning densitometry, normalized with respect to β-actin, and expressed relative to those of control cells.

HO-1; 

PubMed: 23604711     


MG-132 stimulates Nrf2 and HO-1 protein expression in HAECs in a time-dependent fashion. Cells were treated with MG-132 (2 μM) for various times (0–24 h), and Nrf2 and HO-1 protein were quantified by scanning densitometry, normalized with respect to β-actin, and expressed relative to those of control cells.

26722260 19765735 23604711
Immunofluorescence
C2GnT-M / NMIIA; 

PubMed: 22525330     


Confocal images of bC2GnT-M and NMIIA in cells treated with DMSO (D) or MG-132 (E).

AGS3 / Vimentin; 

PubMed: 20065032     


COS-7 cells were transfected with wild-type or TPR-modified AGS3 (AGS3-TPR [M1 to E470] or AGS3-GPR [E470 to S650]) in pEGFP-N1. Thirty-six hours after transfection, cells were incubated with MG 132 (10 μM) for 12 h, and then the cells were processed for immunofluorescence microscopy. The images presented are representative of 2 to 10 separate transfections.

Bak; 

PubMed: 20557369     


Proteasome inhibitor induces Bak activation. Cells were treated with either vehicle or MG-132 at 10 µmol/L for 12 hours and were subjected to Bak immunofluorescence study using antiserum specific for the N terminus of Bak. Upon Bak activation, this epitope is no longer masked within the protein and becomes available for antibody binding upon Bak conformational change.

22525330 20065032 20557369
Growth inhibition assay
Apoptosis assay; 

PubMed: 20557369     


LX-2 cells were incubated for 24 hours in the presence of increasing concentrations of MG-132 (0, 2.5, 5, 10 µmol/L) and in the presence of the pan-caspase inhibitor QVD at 5 µmol/L for 24 hours. MG-132 and QVD were prepared in DMSO as a vehicle. All data were expressed as mean ± standard error from three individual experiments. * p < 0.01 (10 µmol/L MG-132 treated cells vs. 10 µmol/L MG-132 plus QVD treated cells)

Cell viability; 

PubMed: 26137056     


The proteasome inhibitor MG-132 significantly decreased the cell viability in EC9706 cells in a dose- and time-dependent manner.

cell proliferation ; 

PubMed: 19765735     


MG-132 significantly inhibits growth of carcinoid tumor cells in vitro. Pulmonary (NCI-H727) and GI (BON) carcinoid tumor cells were treated with MG-132 at the indicated concentrations (0 to 4µM) for up to 6 days and cell viability was measured every 2 days with the MTT assay (P<0.001). The results show that MG-132 leads to the suppression cellular proliferation in NCI-H727 (A) and BON (B) cells. (OD, optical density)

20557369 26137056 19765735
ELISA
IL-8; 

PubMed: 11160671     


ELISA of IL-8 from supernatant of eTat cells. eTat cells were blocked with Hu (2 mM) and released. MG-132 (50 μM) was added at the time of release. The supernatant was collected at 3 h postrelease and analyzed for IL-8 protein using ELISA. The result shown is representative of three independent experiments ± standard deviation. 

IL-1beta; 

PubMed: 22606244     


LPS-primed WT BMDM were incubated in control medium or medium containing 10 ng/ml ricin or 25 µg/ml cycloheximide for 4 h. MG-132 (30 µM) or Bortezimib (0.5 µM) was included as indicated. Secreted IL-1ß was measured by ELISA in triplicate wells.

11160671 22606244
In vivo

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]

Protocol

Kinase Assay:

[1]

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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.
Cell Research:

[3]

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  • Cell lines: KIM-2, HC11, and ES
  • Concentrations: Dissolved in DMSO, final concentrations ~25 μM
  • Incubation Time: 24 and 48 hours
  • Method:

    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.


    (Only for Reference)
Animal Research:

[7]

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  • Animal Models: Male mdx (C57BL/10ScSn DMD mdx) mice
  • Dosages: ~10 μg/kg/day
  • Administration: Injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (189.22 mM)
Ethanol 25 mg/mL (52.56 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+20% propylene glycol+ddH2O
For best results, use promptly after mixing.
2mg/mL

* 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.

Chemical Information

Molecular Weight 475.62
Formula

C26H41N3O5

CAS No. 1211877-36-9
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)CC(C=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)OCC1=CC=CC=C1

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
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    C4=C3/X C4: LOG(C4):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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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.

Proteasome Signaling Pathway Map