MG-132

Catalog No.S2619 Synonyms: Z-Leu-Leu-Leu-al

For research use only.

MG132 (Z-Leu-Leu-Leu-al) 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.

MG-132 Chemical Structure

CAS No. 1211877-36-9

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 1625 publications

Purity & Quality Control

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Biological Activity

Description MG132 (Z-Leu-Leu-Leu-al) 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{P5VGFxd3C2b4Ppd{BCe3OjeR?= Mn3NN|AxKG6P NHvXNpczPCCq NX3zNHl2TE2VTx?= NX;MbHFkUW6mdXPld{BieG:ydH;zbZMh[nliaX7jdoVie2mwZzDjcIVifmWmIGDBVnAhdGW4ZXygZY5lKHKnZIXjbY5oKE2lbD2xJJBzd3SnaX6gcIV3\Wx? M3\nVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3OUW4OVg6Lz5zNUm1PFU5QTxxYU6=
PC3 NFjpRZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVmyNEDPxE1? NXPaPW1GPDhiaB?= NIHDbmRFVVOR NILt[WxKSzVyPUCuOkDPxE1? MkfBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ4OE[1N|coRjF4Nki2OVM4RC:jPh?=
PC12 Mly2SpVv[3Srb36gRZN{[Xl? NUT4VpJvOTByIN88UeKh MnKxNlQhcA>? M3X1cmROW09? Mlz3TY5pcWKrdIOgOk1QUESDLTDhcoQhUDKRMj3pcoR2[2WmIHP5eI91d3irY3n0fS=> NYHjRnF2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUexOVg1PTRpPkG3NVU5PDV2PD;hQi=>
LPS-stimulated RAW264.7 cells NXT3RnhwTnWwY4Tpc44hSXO|YYm= M3jNT2ROW09? MmLETY5pcWKrdIOgUmYuc2GycHHCJGRPSSCkaX7kbY5o NXT2[ZpnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe0NFczPzdpPkG3OFA4Ojd5PD;hQi=>
OCI-Ly3 MYHGeY5kfGmxbjDBd5NigQ>? NEDETlIyOCEQvF5CpC=> MnexOEBp MkfQSG1UVw>? NYfkdodyUW6mdXPld{BpfW2jbjDJb4FxeGGEYXzwbIEhe3SjYnnsbZpifGmxbjD3bZRpKEWFNUCgc4YhOSEQvF2= M3LxOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEK0NVE{Lz5zOECyOFEyOzxxYU6=
A2780 cDDP MU\BdI9xfG:|aYOgRZN{[Xl? NFrPcnMzPCCq M{i4dWROW09? M1rBbGlv\HWlZYOgZZBweHSxc3nzJIJ6KGmwaHnibZRqdmdiUGTFUkBl\We{YXTheIlwdg>? M4rNc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5Nki0NFE5Lz5zN{[4OFAyQDxxYU6=
COS-7 NW\4TYdtS3m2b4TvfIlkKEG|c3H5 NHfvUW8yOCEQvF2= NWfkWFJ[TE2VTx?= MkXuTWM2ODxzMDFOwG0> M1vzZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEi4NFk4Lz5zOEC4PFA6PzxxYU6=
HuH-7 Mor1R5l1d3SxeHnjJGF{e2G7 M{XCe|ExKM7:TR?= MmD5SG1UVw>? M3PFTmlEPTB:MUCg{txO MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDB6OEC5O{c,OThyOEiwPVc9N2F-
Hepa-1c1c7 NXnVZXN7TnWwY4Tpc44hSXO|YYm= MXeyOUDPxE1? NFzucno3KGh? NVfWfoVxTE2VTx?= NGfkNZZKdmO{ZXHz[ZMhVnKoMjDwdo91\WmwIHzleoVt MkftQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|OUK1OFQoRjJyM{myOVQ1RC:jPh?=
IPC227F NXHQUFlRS3m2b4TvfIlkKEG|c3H5 NGPLTmkyKM7:TR?= NY\wPGNMPDhiaB?= NI\NcmpFVVOR NUXDWHp4UUN3ME2wMlA4PyEQvF2= NG\uWlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUmyOFUzQCd-MkG5NlQ2Ojh:L3G+
Calu6 MmTvSpVv[3Srb36gRZN{[Xl? M4rQO|ExKM7:TR?= MYmxPEBp NUnLWpo{TE2VTx?= MV;TbYdvcW[rY3HueIx6KGGlY4XteYxifGW|IH\yZZRigGmwIIDy[YN2enOxch?= M1TwbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NUC2OFg3Lz5{M{WwOlQ5PjxxYU6=
IFN-gamma-induced RAW264.7 M2L4bmZ2dmO2aX;uJGF{e2G7 NHvZSllFVVOR MYHJcohq[mm2czDubZRzcWNib4jp[IUheHKxZIXjeIlwdiC5aYToJGlEPTBib3[gNE4xPzdizszN Mlf2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ{N{eyO|coRjJ{Mke3Nlc4RC:jPh?=
HEK-293 MWrLbY5ie2ViQYPzZZk> MnXzNkBidmRiMkCg{txO MVKyJIg> NEXwbo5FVVOR NXXuUGtNUW6qaXLpeJMhS2iWLVygZYN1cX[rdImge4l1cCCLQ{WwJI9nKDlibl2= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV2MEe5NEc,OjN3NEC3PVA9N2F-
MCF10A NXzUWmtXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[xJO69VQ>? MlS3O|IhcA>? NEfPPHBFVVOR MY\JR|UxRTBwMkmg{txO NUfuVYlORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOVMzODZpPkK0NVU{OjB4PD;hQi=>
MCF-7 NVzScmt2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPGNUDPxE1? MYS3NkBp M2rHfWROW09? M1TmbGlEPTB;MD6xN{DPxE1? NVrvOWZXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxOVMzODZpPkK0NVU{OjB4PD;hQi=>
HeLa MoSxT4lv[XOnIFHzd4F6 MVyxNEDPxE1? NETzUnYyKGh? MYTEUXNQ MXTJcoR2[2W|IGDBVnAh[2ynYY\h[4Uh[nliaX7obYJqfGmwZzDwdo9{\WG|b33lJIFkfGm4aYT5 MnLhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|MkG4N|MoRjJ2M{KxPFM{RC:jPh?=
MDA-MB-231 NFv4elVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjqUWcyKM7:TR?= MU[3NkBp NHuxfFVFVVOR MkjGTWM2OD1yLkG4JO69VQ>? MkTGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzNUOyNFYoRjJ2MUWzNlA3RC:jPh?=
293T NFX2RmhEgXSxdH;4bYMhSXO|YYm= MX:xNEDPxE1? M3fYRVczKGh? M{PzRWROW09? MofVTWM2ODx{IN88US=> NHTyNXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[yOVA5QCd-MkS2NlUxQDh:L3G+
293T MYTGeY5kfGmxbjDBd5NigQ>? MVOxNEDPxE1? MXOyOEBp NH;ub5VFVVOR MYTNc4RmemG2ZXz5JIlv\HWlZYOgbIVifC2|aH;jby=> NGiwXW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[yOVA5QCd-MkS2NlUxQDh:L3G+
NCI-H929 NViycod3S3m2b4TvfIlkKEG|c3H5 M1\5dVEh|ryP M4TNR|czKGh? NEDGbFdFVVOR NFrRO5RKSzVyPUCuNVch|ryP M2fBeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkK1NFg5Lz5{NE[yOVA5QDxxYU6=
A-549 NEXWV29EgXSxdH;4bYMhSXO|YYm= M{fuS|QxKM7:TR?= MWG0PEBp NEDjeZpFVVOR MYPJR|UxRDFyIN88US=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ7N{S5Okc,OjR4OUe0PVY9N2F-
MCF-7 NUXMXWdTS3m2b4TvfIlkKEG|c3H5 MnrlOFAh|ryP NXrzVXZqPDhiaB?= MYHEUXNQ M2jSUGlEPTB;Nz6zJO69VQ>? Mk\ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4OUe0PVYoRjJ2Nkm3OFk3RC:jPh?=
SW-480 M1;yNWN6fG:2b4jpZ{BCe3OjeR?= MXG0NEDPxE1? NILMR|Q1QCCq MUPEUXNQ NVPlVJc6UUN3ME20JO69VQ>? NITPPY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[5O|Q6Pid-MkS2PVc1QTZ:L3G+
HL-60 NVj4NIpxS3m2b4TvfIlkKEG|c3H5 MXO0NEDPxE1? MoLJOFghcA>? MWnEUXNQ M3zvc2lEPTB:MUCg{txO NIjkOFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[5O|Q6Pid-MkS2PVc1QTZ:L3G+
SMMC-7721 MljhR5l1d3SxeHnjJGF{e2G7 NH\yUpA1OCEQvF2= Mly4OFghcA>? MkXUSG1UVw>? NXmzUFRRUUN3ME23MlEh|ryP MoP3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4OUe0PVYoRjJ2Nkm3OFk3RC:jPh?=
LPS-stimulated RAW264.7 cells M4LuZmZ2dmO2aX;uJGF{e2G7 MnP5NlUh|ryP NXjwWGtOTE2VTx?= M37MfWlvcGmkaYTzJI5qfHKrYzDvfIll\SCycn;keYN1cW:wIIfpeIghUUN3MDDv[kAxNjFizszN NXO2[3pMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2PVc1QTZpPkK0Olk4PDl4PD;hQi=>
lymphoblastoid NIfZbXBHfW6ldHnvckBie3OjeR?= NWnmZpZHUUN3MDC9JFAvODB{IN88US=> MnvyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd7OU[5PFcoRjF5OUm2PVg4RC:jPh?=
LCL M2DHbmZ2dmO2aX;uJIF{e2G7 NGrGXmwyOiCq NHjPVnBKSzVyIE2gNE4xODJizszN MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ6N{[wPUc,OjB4OEe2NFk9N2F-
HL-60 Mn3aSpVv[3Srb36gZZN{[Xl? MkHLTWM2OCB;IECuNFY5KM7:TR?= NWnpcWhzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUW3PFA3OjNpPkG1O|gxPjJ|PD;hQi=>
IPC227F NX\YO5Z7TnWwY4Tpc44h[XO|YYm= NF2x[GoyKGh? M2OyWWlEPTBiPTCwMlA4PyEQvF2= NYfFWJNkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[yNlA6QDhpPkG2NlIxQTh6PD;hQi=>
RAW264.7 Ml;FRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDhd5NigQ>? NITsUGgyQCCq NE\yXYFKSzVyIE2gNE4xQCEQvF2= MmW4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ4MkC2O|coRjJ{NkKwOlc4RC:jPh?=
RAW264.7 M33u[WFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZZN{[Xl? NVi0VXRSOThiaB?= MkT3TWM2OCB;IECuNUDPxE1? NV34TIdIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4NVk5PzFpPkKzPFE6QDdzPD;hQi=>
RAW264.7 MUXGeY5kfGmxbjDhd5NigQ>? M{\NUmlEPTBiPTCwMlEh|ryP M{HmfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NUm3PFk1Lz5{NEW5O|g6PDxxYU6=
RAW264.7 NYrKWVRqTnWwY4Tpc44h[XO|YYm= M{G1TFE5KGh? M36ySGlEPTBiPTCwMlEh|ryP M1W1VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkG5PFA6Lz5{NEKxPVgxQTxxYU6=
RAW264.7 Mn3pSpVv[3Srb36gZZN{[Xl? NIfHSowyQCCq NXfkfYdTUUN3MDC9JFAvOTVizszN NXPxfoFCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzNlc3PjhpPkKzN|I4PjZ6PD;hQi=>
RAW264.7 NYTaUFJETnWwY4Tpc44h[XO|YYm= NWHkW4FYOThiaB?= NHPWcIVKSzVyIE2gNE4yPSEQvF2= MlHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5NUewNVkoRjJ4N{W3NFE6RC:jPh?=
RAW264.7 MUXBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4F6 NGi2T4QyQCCq MWHJR|UxKD1iMD6xPEDPxE1? NXLzem9ORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkeyNFMzQTFpPkK3NlA{OjlzPD;hQi=>
RAW264.7 MlrFRY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDhd5NigQ>? NYTnZ2x1OSCq M{PPUmlEPTBiPTCwMlIh|ryP M1y2WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7M{O4NlYxLz5{OUOzPFI3ODxxYU6=
MDA-MB-231 NHHuRY5EgXSxdH;4bYNqfHliYYPzZZk> M2TnWWlEPTBiPTCwMlI2KM7:TR?= NYTyUlluRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi1PVgxOThpPkG4OVk5ODF6PD;hQi=>
MCF7 MlHwR5l1d3SxeHnjbZR6KGG|c3H5 NHnEelVKSzVyIE2gNE4{KM7:TR?= M3G4RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NUm4NFE5Lz5zOEW5PFAyQDxxYU6=
RAW264.7 MnrySpVv[3Srb36gZZN{[Xl? MXexPEBp NV;NUmY3UUN3MDC9JFAvOzVizszN NVr3blZoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGwOFQ5PDdpPkKxNFQ1QDR5PD;hQi=>
RAW264.7 MVHBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHHzd4F6 Mn[4TWM2OCB;IECuOFM6KM7:TR?= M3GyRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNU[xNFYxLz5{MUW2NVA3ODxxYU6=
HEK293 NVzKflNOTnWwY4Tpc44h[XO|YYm= M3vUSFIhcA>? MkX0TWM2OCB;IECuOkDPxE1? NVPCUWlTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO1OFA4QTBpPkKzOVQxPzlyPD;hQi=>
RAW264.7 MVnUc5hq[2m2eTDhd5NigQ>? NV7melRFUUN3MDC9JFAvPjNizszN NUTYRo9IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK4OVgzQTdpPkKyPFU5Ojl5PD;hQi=>
lymphoblastoid MUDGeY5kfGmxbjDhd5NigQ>? NULDVnI4UUN3MDC9JFEvODd5IN88US=> NHP3[Is9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{m5Olk5Pyd-MUe5PVY6QDd:L3G+
LCL M3jUSWZ2dmO2aX;uJIF{e2G7 MWSxNkBp M2fG[GlEPTBiPTCxMlA4PyEQvF2= NYrYfVYzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2PFc3ODlpPkKwOlg4PjB7PD;hQi=>
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NCI-H226 NEDXOZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fHfGlEPTB;MUG0MlM4PiEQvF2= NFP5[Gs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw3PDl{NT:nQnNCVkeHUkyvZV4>
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MFM-223 M{LtTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vMb2lEPTB;M{SwMlQ5PiEQvF2= NFjuVVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw3PDl{NT:nQnNCVkeHUkyvZV4>
EW-11 NGC3Z2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH:wU2ZKSzVyPUO0PE4yOjNizszN Mmf0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOlQ6OjVxJ{7TRW5ITVJ:L3G+
KG-1 NH3KU5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTwTWM2OD1|OEeuO|c5KM7:TR?= MoHSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOlQ6OjVxJ{7TRW5ITVJ:L3G+
NCI-H1155 NEW2RopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PjcmlEPTB;NEG0MlYzPiEQvF2= NHPvUY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw3PDl{NT:nQnNCVkeHUkyvZV4>
NCI-H187 MofsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGW1em5KSzVyPUSyPE42PDFizszN NEnXXlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw3PDl{NT:nQnNCVkeHUkyvZV4>
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EW-18 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzPToNWUUN3ME22O|IvPjZ3IN88US=> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQly2OFkzPS9pPmPBUmdGWjxxYU6=
Assay
Methods Test Index PMID
Western Blot Bcr-Abl ; Ac-histone H3 ; Cleaved-caspase3 ; Cleaved-PARP ; ASCL1 ; CgA ; Nrf2 ; HO-1 26722260 19765735 23604711
Immunofluorescence C2GnT-M / NMIIA ; AGS3 / Vimentin ; Bak 22525330 20065032 20557369
Growth inhibition assay Apoptosis assay ; Cell viability ; cell proliferation 20557369 26137056 19765735
ELISA IL-8 ; IL-1beta 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 (from reference)

Kinase Assay:

[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.

Cell Research:

[3]

  • 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.

Animal Research:

[7]

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

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 475.62
Formula

C26H41N3O5

CAS No. 1211877-36-9
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

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