Bardoxolone Methyl

Catalog No.S8078 Synonyms: RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me

For research use only.

Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.

Bardoxolone Methyl Chemical Structure

CAS No. 218600-53-4

Selleck's Bardoxolone Methyl has been cited by 19 publications

Purity & Quality Control

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Biological Activity

Description Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.
Features The only IKKβ inhibitor in clinical use for solid tumors, type 2 diabetes, and chronic kidney disease. An orally-available antioxidant inflammation modulator.
Targets
IKK [3]
(Cell-free assay)
Ferroptosis [7] Nrf2 [6] NF-κB [6]
In vitro

Bardoxolone Methyl exhibits potent inhibitory activities against production of nitric oxide induced by interferon-Ƴ in mouse macrophages with IC50 of 0.1 nM. [1] Bardoxolone Methyl decreases the viability of leukemic HL-60, KG-1, and NB4 cells with IC50 of 0.4, 0.4, and 0.27 μM, respectively. CDDO-Me induces pro-apoptotic Bax protein, inhibits the activation of ERK1/2, and it blocks Bcl-2 phosphorylation, which contributes to the induction of apoptosis. [2] Bardoxolone Methyl potently inhibits both constitutive and inducible NF-kappaB activated by TNF, interleukin (IL)-1beta, phorbol ester, okadaic acid, hydrogen peroxide, lipopolysaccharide, and cigarette smoke. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 MnWxSpVv[3Srb36gZZN{[Xl? MXvJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCycn;sbYZmemG2aX;uJI9nKE2FRj23JEhGWiCSb4PpeIl3\SliYoLlZZN1KGOjbnPldkBk\WyuczygTWM2OD1yLkC1{txO MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPTN4OUO5Okc,OTV|NkmzPVY9N2F-
BMDM Mn;yR5l1d3SxeHnjbZR6KGG|c3H5 M3XqNFI1KGi{cx?= MoXwR5l1d3SxeHnjbZR6KGGpYXnud5QhSzV5QlyvOkBud3W|ZTDCUWROKGOnbHzzJIF{e2W|c3XkJIF{KEyGSDDy[Yxm[XOnIHHmeIVzKDJ2IHjyd{whVU6WRE2wMlXPxE1? NXzsRW4xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1N|M4QTBpPkKyOVM{PzlyPD;hQi=>
BMDM M4Tme2FvfGmrbn\sZY1u[XSxcomgZZN{[Xl? MmDGNE42KHWP NHPYVWUyKGi{ M{nBfGFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgbY4hSzV5QlyvOkBud3W|ZTDCUWROKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gUHBUNXO2aX31cIF1\WRiVF7GZYxxcGFicILv[JVkfGmxbjDheEAxNjVidV2gdJJmfHKnYYTl[EBnd3JiMTDodkBj\W[xcnWgUHBUKGOqYXzs[Y5o\SCjZoTldkA5KHSxIEK0JIhzeyCkeTDpcY12dm:jc4PhfS=> M333S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUOzO|kxLz5{MkWzN|c6ODxxYU6=
PANC1343 NYD3PY1lSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M4TzflMxOCC2bzCxNFAxKG6P MYC3NkBpenN? MlvXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCSQV7DNVM1OyClZXzsd{BifCB|MECgeI8hOTByMDDuUUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN6OEiwOkc,OjR|OEi4NFY9N2F-
RAW264.7 MWPBcpRqd3irZHHueEBie3OjeR?= NYLu[2d1OTByIH7N MnPhNVghcHK| M4[3OmFvfGmxeHnkZY51KGGldHn2bZR6KGmwIH3veZNmKFKDV{K2OE44KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geGJJWC2rbnT1Z4VlKFKRUzDwdo9lfWO2aX;uJIF1KDFyMDDuUUBxemW2cnXheIVlKG[xcjCxPEBpenNiYnXmc5JmKGOqYXzs[Y5o\SCvZXHzeZJm\CCjZoTldkAyPSCvaX7zJIJ6KEh{RFPGRU1j[XOnZDDmcI94KGO7dH;t[ZRzgQ>? M4LCblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{i4PFA3Lz5{NEO4PFgxPjxxYU6=
HepG2 M3\UZmN6fG:2b4jpZ4l1gSCjc4PhfS=> MVq0PEBpenN? MY\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSuPVnPxE1? M3PLVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nki1OVQ2Lz5{NE[4OVU1PTxxYU6=
B16F10 MVjDfZRwfG:6aXPpeJkh[XO|YYm= MXO0PEBpenN? NFvxbFFEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDOT[IMUCgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF02Njh3zszN Mn;XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4OEW1OFUoRjJ2Nki1OVQ2RC:jPh?=
CCD-841-CoN M17CWWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NVHN[pVlPzJiaILz M3zIe2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1PEMVg1OS2Fb16gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjNzNt88US=> MkKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4N{WxOFQoRjJ3Nke1NVQ1RC:jPh?=
HCT8 NEjxZpFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NEjuVFQ4OiCqcoO= NFfZNnBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JFUuTlVicnXzbZN1[W62IHj1cYFvKEiFVEigZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjN4M988US=> M4fZTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Nke1NVQ1Lz5{NU[3OVE1PDxxYU6=
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HCT8 M2O4emZ2dmO2aX;uJIF{e2G7 MnzvNUB2VQ>? Mn\FNlQhcHK| M17ZV2lvcGmkaYTpc44hd2ZiSFnGMVFidHCqYTDwdo91\WmwIHX4dJJme3Orb36gbY4hcHWvYX6gTGNVQCClZXzsd{BifCBzIIXNJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdibXX0bI9l NFPHZWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[3OVE1PCd-MkW2O|UyPDR:L3G+
HCT8 M2DTWGZ2dmO2aX;uJIF{e2G7 M4jse|EhfU1? M4jjSlI1KGi{cx?= NWK4cFJ2UW6qaXLpeIlwdiCxZjDITWYuOWGucHjhJJBzd3SnaX6g[ZhxemW|c3nvckBqdiCIVT3y[ZNqe3SjboSgbJVu[W5iSFPUPEBk\WyuczDheEAyKHWPIHnuZ5Vj[XSnZDDmc5IhOjRiaILzJIJ6KFenc4Tldo4h[myxdITpcochdWW2aH;k MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ5NUG0OEc,OjV4N{WxOFQ9N2F-
HCT8 NUTXfXpoTnWwY4Tpc44h[XO|YYm= Mk[2NUB2VQ>? MXSyOEBpenN? NIrtOmpKdmirYnn0bY9vKG:oIGPURXQ{KHC{b4TlbY4heGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJGhEXDhiY3XscJMh[XRiMTD1UUBqdmO3YnH0[YQh\m:{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6pIH3leIhw\A>? Mmi3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4N{WxOFQoRjJ3Nke1NVQ1RC:jPh?=
HCT8 NXnnNINwTnWwY4Tpc44h[XO|YYm= M3[z[VEhfU1? NUTTdpJmOjRiaILz M2rITmlvcGmkaYTpc44hd2ZiU2TBWFMheHKxdHXpckBxcG:|cHjvdplt[XSrb36gbY4hTlVvcnXzbZN1[W62IHj1cYFvKEiFVEigZ4VtdHNiYYSgNUB2VSCrbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBY\XO2ZYLuJIJtd3S2aX7nJI1mfGixZB?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ5NUG0OEc,OjV4N{WxOFQ9N2F-
HCT8 NVHLO|JSTnWwY4Tpc44h[XO|YYm= Ml;oNUB2VQ>? MX:yOEBpenN? NF24XWFKdmirYnn0bY9vKG:oIFHLWEBxem:2ZXnuJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDIR3Q5KGOnbHzzJIF1KDFidV2gbY5kfWKjdHXkJIZweiB{NDDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> M2PhOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Nke1NVQ1Lz5{NU[3OVE1PDxxYU6=
HCT8 MVvGeY5kfGmxbjDhd5NigQ>? NVW2fmM6OSC3TR?= MkfFNlQhcHK| NYP6NYFjUW6qaXLpeIlwdiCxZjDBT3QheHKxdHXpckBxcG:|cHjvdplt[XSrb36gbY4hTlVvcnXzbZN1[W62IHj1cYFvKEiFVEigZ4VtdHNiYYSgNUB2VSCrbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBY\XO2ZYLuJIJtd3S2aX7nJI1mfGixZB?= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ5NUG0OEc,OjV4N{WxOFQ9N2F-
HCT8 M1nIcmZ2dmO2aX;uJIF{e2G7 NHrxT40yKHWP M4P5[VI1KGi{cx?= MVTJcohq[mm2aX;uJI9nKEWUSzDwdo91\WmwIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCKQ2S4JINmdGy|IHH0JFEhfU1iaX7jeYJifGWmIH\vdkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2dHnu[{Bu\XSqb3S= NUXMTGJ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2O|UyPDRpPkK1Olc2OTR2PD;hQi=>
HCT8 MVfGeY5kfGmxbjDhd5NigQ>? NILFZ4wyKHWP M4HHdFI1KGi{cx?= MXXJcohq[mm2aX;uJI9nKEWUSzDwdo91\WmwIIDoc5NxcG:{eXzheIlwdiCrbjDGWU1z\XOrc4ThcpQhcHWvYX6gTGNVQCClZXzsd{BifCBzIIXNJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdibXX0bI9l M1rFXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Nke1NVQ1Lz5{NU[3OVE1PDxxYU6=
HCT8 MmjsRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NX\uNm5yOSC3TR?= NFPOdoc4OiCqcoO= M2XjUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUPEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwheHKxbHnm[ZJifGmxbjDheEAyKHWPIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[Xl? NHTDOXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[3OVE1PCd-MkW2O|UyPDR:L3G+
HCT8 M4LqOWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MkjCNUB2VQ>? MmHrO|IhcHK| NW\4Zpg3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEA2NU[XIILld4l{fGGwdDDoeY1idiCKQ2S4JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHH0JFEhfU1iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigQ>? NYG2dVllRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2O|UyPDRpPkK1Olc2OTR2PD;hQi=>
BEAS2B NV7l[GFMTnWwY4Tpc44h[XO|YYm= M3jVOlExKHWP MYq2JIhzew>? MoXXRYN1cX[jdHnvckBw\iCQcn[yJIlvKGi3bXHuJGJGSVN{QjDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBJVzFiZ3Xu[UBmgHC{ZYPzbY9vKGG2IEGwJJVOKGmwY4XiZZRm\CCob4KgOkBpenNiYomgdXBEWiCvZYToc4Q> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ5OECyPEc,OjZ{N{iwNlg9N2F-
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H42E NUnvSIVCTnWwY4Tpc44h[XO|YYm= NF:zdmoxNjBzIITvJFMxKG6P NVHzW3RmOSCqch?= NXfmZnEzW3SjYnnsbZpifGmxbjDv[kBPWkZ{IHnuJJJifCCKNELFJINmdGy|IHX4dJJme3OrbnegRXJGQExiYYSgNE4xOSC2bzCzNEBvVSCjZoTldkAyKGi{IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? M13CZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4OUC4NVc{Lz5{NkmwPFE4OzxxYU6=
NHBE M2PoVWN6fG:ycn;0[YN1cX[nIHHzd4F6 NI\ublIxNjByMTD0c{AxNjFidV2= NVuxZoJtOThiaILz MXTDfZRweHKxdHXjeIl3\SCjY4Tpeol1gSCrbjDOTGJGKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[geGJJWC2rbnT1Z4VlKEeVSDDk[ZBt\XSrb36gZZQhOC5yMEGgeI8hOC5zIIXNJJBz\WmwY4XiZZRm\CCob4KgNVghcHK|IH\vcIxwf2WmIHL5JJRDUFBiYXTkbZRqd25iZn;yJFQhcHK|IHL5JJRpcW:|dHHyJIR6\SCkYYPl[EBndHWxcnXzZ4Vv[2ViYYPzZZk> NVz4V|lnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewN|E3PzBpPkK3NFMyPjdyPD;hQi=>
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A549/TR NEHKSoJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Ml7NO|IhcHK| M3G4U2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PU9VWiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuO|A{|ryP Mm\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MEG5OFcoRjJ7NUCxPVQ4RC:jPh?=
A549 MXfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M2[5N|czKGi{cx?= MmD3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:Oi5yN{VOwG0> M4LjcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUCxPVQ4Lz5{OUWwNVk1PzxxYU6=
A549/TR MnuxSpVv[3Srb36gZZN{[Xl? MnTvNk41KHSxIEmuOkB2VQ>? NGXjVHEzPCCqcoO= NWCwNnJ3UW6mdXP0bY9vKG:oIGLPV{Bo\W6ncnH0bY9vKGmwIHj1cYFvKEF3NEmvWHIh[2WubIOgZZQhOi52IITvJFkvPiC3TTDh[pRmeiB{NDDodpMh[nliRFPGTE1FSSCmeXWtZoF{\WRiZnzve{BkgXSxbXX0dolkKGGwYXz5d4l{ M{\5cFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUCxPVQ4Lz5{OUWwNVk1PzxxYU6=
A549/TR NWr0OZhvTnWwY4Tpc44h[XO|YYm= NILwOJc1NjhidV2= M4\NTlI1KGi{cx?= MU\Ec5dvemWpdXzheIlwdiCxZjDMc44h\XiycnXzd4lwdiCrbjDoeY1idiCDNUS5M3RTKGOnbHzzJIF1KDRwODD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NUe4c5NoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NFE6PDdpPkK5OVAyQTR5PD;hQi=>
HCT116 NHe2TnhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NE\3bGY4OiCqcoO= MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxRTBwMECwNlXPxE1? MoDmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB2Mkm5OVMoRjNyNEK5PVU{RC:jPh?=
HT-29 NIixNodCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Mn[wO|IhcHK| NXjSOYZDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNljPxE1? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODR{OUm1N{c,OzB2Mkm5OVM9N2F-
HCT8 M17y[mFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NXezfZBOPzJiaILz MlexRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2S4JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5{Od88US=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODR{OUm1N{c,OzB2Mkm5OVM9N2F-
HCT116 MmThSpVv[3Srb36gZZN{[Xl? MUW4JIhzew>? NVvab2QxUW6qaXLpeIlwdiCxZjDCcYkyKHC{b4TlbY4h\XiycnXzd4lwdiCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZYZ1\XJiODDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NWP2eGdxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C0Nlk6PTNpPkOwOFI6QTV|PD;hQi=>
BEAS2B NX76eFNTTnWwY4Tpc44h[XO|YYm= NWX4b5E3PDhiaILz MULBZ5RqfmG2aX;uJI9nKEunYYCxM2N2dDNxToLmNkBqdiCqdX3hckBDTUGVMlKgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hVlGRMTDs[ZZmdHNibXXhd5Vz\WRiYX\0[ZIhPDhiaILzMEBGSzVyPUCuNFA5PzIQvF2= NFLwPIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|ME[yOlU2PSd-M{C2NlY2PTV:L3G+
HepG2 MX7DfZRwfG:6aXPpeJkh[XO|YYm= NUPtSIxRPDhiaILz NV\GXnpXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKGOnbHygeoli[mmuaYT5JIlv[3WkYYTl[EBnd3JiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkK2{txO NUHWSYZERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwOVE1ODFpPkOxNFUyPDBzPD;hQi=>
MCF7 M2HRR2N6fG:2b4jpZ4l1gSCjc4PhfS=> NHO3eXE1QCCqcoO= M3XQd2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHnuZ5Vj[XSnZDDmc5IhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjN3zszN NXnMcmZURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwOVE1ODFpPkOxNFUyPDBzPD;hQi=>
A549 MmLXR5l1d3SxeHnjbZR6KGG|c3H5 NH;OTpk1QCCqcoO= MljBR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliaX7jeYJifGWmIH\vdkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvOzcQvF2= MmXjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzFyNUG0NFEoRjNzMEWxOFAyRC:jPh?=
A549 MlnYRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NGHrZo01QCCqcoO= M1PsdGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkWy{txO M33FXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzN{K1Nlg5Lz5|MUeyOVI5QDxxYU6=
HepG2 NWTH[I5FSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MnXXOFghcHK| M4Ox[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD61Nu69VQ>? NYD0cYt5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G3NlUzQDhpPkOxO|I2Ojh6PD;hQi=>
HOS M4[4SmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NVfuS|FQPDhiaILz NV\Fe2NJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIU3Mh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD62Ou69VQ>? NV;jU5Q6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G3NlUzQDhpPkOxO|I2Ojh6PD;hQi=>
MCF7 NUj1dolDSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NGjoSII1QCCqcoO= M2fwPGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLki1{txO Mn[1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF5MkWyPFgoRjNzN{K1Nlg5RC:jPh?=
HEK293FT NXvqdms3TnWwY4Tpc44h[XO|YYm= MlyxNlQhcHK| MWTJcohq[mm2aX;uJI9nKG2xdYPlJGdQSVRiZYjwdoV{e2WmIHnuJGhGUzJ7M1\UJINmdGy|IHPvMYV5eHKnc4PpcocheHKnLYDyc4dpemWuaX6gZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIHfodoVtcW5ib3P0ZY5wgWyjdHnvckBqdmO3YnH0[YQh\m:{IEK0JIhzeyCkeTDFUGlUSSxiSVO1NF0xNjB|Nd88US=> M3P0elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE4PjJ4MkGvK|5EcEWPQly8M4E,
Assay
Methods Test Index PMID
Western blot p-IκBα / IκBα ; Bcl-xl / Bcl-2 / Bax / Cleaved caspase / Cytochrome C / PARP / Cleaved PARP ; p-PI3K / PI3K / p-AMPK / AMPK / p-p38 MAPK / p38 MAPK / p-AKT / AKT / p-mTOR / mTOR ; PTEN / PP2A / PHLPP1 25897966 25733817 22177954
Immunofluorescence PDI / SDHA ; c-PARP / Cytochrome C / COX IV 26053096
Growth inhibition assay Cell viability 25733817
In vivo

Bardoxolone Methyl (60 mg/kg) reduces the number, size, and severity of lung tumors in vivo. [4] Bardoxolone Methyl significantly reduces the in vivo inflammatory cytokine response following LPS challenge, induces HO-1 protein expression in the spleen, and protects mice against lethal-dose LPS. [5]

Protocol (from reference)

Kinase Assay:

[3]

  • IKK assay :

    To determine the effect of CDDO-Me on TNF-induced IKK activation, IKK is analyzed. Briefly, the IKK complex from whole-cell extracts was precipitated with antibody against IKKα and IKKβ and then treated with protein A/G-Sepharose beads. After 2 hours, the beads are washed with lysis buffer and then resuspended in a kinase assay mixture containing 50 mmol/L HEPES (pH 7.4), 20 mmol/L MgCl2, 2 mmol/L DTT, 20 μCi [γ-32P]ATP, 10 μmol/L unlabeled ATP, and 2 μg of substrate glutathione S-transferase-IκBα (amino acids 1-54). After incubation at 30°C for 30 minutes, the reaction is terminated by boiling with SDS sample buffer for 5 minutes. Finally, the protein is resolved on 10% SDS-PAGE, the gel is dried, and the radioactive bands are visualized with a Storm820. To determine the total amounts of IKK-α and IKK-β in each sample, 50 μg of whole-cell proteins are resolved on 7.5% SDS-PAGE, electrotransferred to a nitrocellulose membrane, and then blotted with either anti-IKK-α or anti-IKK-β antibody.

Cell Research:

[2]

  • Cell lines: HL-60, KG-1, and NB4 cells
  • Concentrations: ~5 μM
  • Incubation Time: 72 hours
  • Method:

    Leukemic cell lines are cultured at a density of 3.0 × 105 cells/mL, and AML mononuclear cells are cultured at 5 × 105 cells/mL in the presence or absence of indicated concentrations of CDDO-Me. Appropriate amounts of DMSO (final concentration less than 0.05%) are included as control. For cytotoxicity studies, 1 μM ara-C is added to the cultures. After 24 to 72 hours, viable cells are counted with the trypan blue dye exclusion method using a hematocytometer.

Animal Research:

[4]

  • Animal Models: Female A/J mice are injected i.p. with vinyl carbamate.
  • Dosages: ~60 mg/kg
  • Administration: Oral gavage

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% PEG300+5% Tween+61%ddH2O
For best results, use promptly after mixing.

2.5mg/mL

Chemical Information

Molecular Weight 505.69
Formula

C32H43NO4

CAS No. 218600-53-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1(CCC2(CCC3(C(C2C1)C(=O)C=C4C3(CCC5C4(C=C(C(=O)C5(C)C)C#N)C)C)C)C(=O)OC)C

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

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02316821 Completed Drug: RTA 402|Drug: Placebo Chronic Kidney Disease|Type 2 Diabetes Kyowa Kirin Co. Ltd. December 2014 Phase 2
NCT02036970 Completed Drug: Bardoxolone methyl|Drug: Placebo Pulmonary Arterial Hypertension|Pulmonary Hypertension|Interstitial Lung Disease|Idiopathic Interstitial Pneumonia|Idiopathic Pulmonary Fibrosis|Sarcoidosis|Respiratory Bronchiolitis Associated Interstitial Lung Disease|Desquamative Interstitial Pneumonia|Cryptogenic Organizing Pneumonia|Acute Interstitial Pneumonitis|Idiopathic Lymphoid Interstitial Pneumonia|Idiopathic Pleuroparenchymal Fibroelastosis Reata Pharmaceuticals Inc. May 2014 Phase 2
NCT01598363 Completed Drug: Digoxin|Drug: Rosuvastatin Healthy Volunteers Reata Pharmaceuticals Inc. June 2012 Phase 1
NCT01551446 Withdrawn Drug: Bardoxolone Methyl Renal Insufficiency Chronic|Diabetes Mellitus Type 2 Reata Pharmaceuticals Inc. April 2012 Phase 1
NCT01503866 Completed Drug: bardoxolone methyl Healthy Reata Pharmaceuticals Inc. December 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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