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 17 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 NHu1U3NHfW6ldHnvckBie3OjeR?= M2\DOGlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IIDyc4xq\mW{YYTpc44hd2ZiTVPGMVchMEWUIGDvd4l1cX[nKTDidoVie3RiY3HuZ4VzKGOnbHzzMEBKSzVyPUCuNFXPxE1? NI\FUGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNUO2PVM6Pid-MUWzOlk{QTZ:L3G+
BMDM NIP6cmFEgXSxdH;4bYNqfHliYYPzZZk> NWjIXZd7OjRiaILz M1\4WGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KEN3N1LMM|YhdW:3c3WgRm1FVSClZXzsd{Bie3Onc4Pl[EBieyCORFigdoVt\WG|ZTDh[pRmeiB{NDDodpMtKE2QVFS9NE42|ryP MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjV|M{e5NEc,OjJ3M{O3PVA9N2F-
BMDM Ml7RRY51cWmwZnzhcY1ifG:{eTDhd5NigQ>? M{fsVFAvPSC3TR?= NFPkVosyKGi{ MXzBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHnuJGM2P0KOL{[gcY92e2ViQl3EUUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFzQV{1{fGmvdXzheIVlKFSQRnHsdIhiKHC{b3T1Z5Rqd25iYYSgNE42KHWPIIDy[ZRz\WG2ZXSg[o9zKDFiaIKgZoVnd3KnIFzQV{BkcGGubHXu[4Uh[W[2ZYKgPEB1dyB{NDDodpMh[nliaX3teY5w[XO|YYm= NUjve|E1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1N|M4QTBpPkKyOVM{PzlyPD;hQi=>
PANC1343 MUjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NVj5UI95OzByIITvJFExODBibl2= NUW5fJVMPzJiaILz MoTQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCSQV7DNVM1OyClZXzsd{BifCB|MECgeI8hOTByMDDuUUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 MmnuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|OEi4NFYoRjJ2M{i4PFA3RC:jPh?=
RAW264.7 NH;sTJhCdnSrb4jp[IFvfCCjc4PhfS=> MUexNFAhdk1? NXzGc3lMOThiaILz NGnQRo9CdnSrb4jp[IFvfCCjY4Tpeol1gSCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJJRDUFBvaX7keYNm\CCUT2OgdJJw\HWldHnvckBifCBzMECgcm0heHKndILlZZRm\CCob4KgNVghcHK|IHLl[o9z\SClaHHscIVv\2VibXXhd5Vz\WRiYX\0[ZIhOTVibXnud{BjgSCKMlTDSmEu[mG|ZXSg[oxwfyCleYTvcYV1enl? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN6OEiwOkc,OjR|OEi4NFY9N2F-
HepG2 NHrnXVFEgXSxdH;4bYNqfHliYYPzZZk> MX20PEBpenN? MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUSuPVnPxE1? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ6NUW0OUc,OjR4OEW1OFU9N2F-
B16F10 NEjOXVZEgXSxdH;4bYNqfHliYYPzZZk> MkXkOFghcHK| NH7n[3pEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBDOT[IMUCgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF02Njh3zszN MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ6NUW0OUc,OjR4OEW1OFU9N2F-
CCD-841-CoN M3OwPWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NXTMdZRzPzJiaILz MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOFRD24OFEuS2:QIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4{OTcQvF2= NH;SbFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[3OVE1PCd-MkW2O|UyPDR:L3G+
HCT8 NHnX[WVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M1y4dFczKGi{cx?= NUPEdmpZSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEA2NU[XIILld4l{fGGwdDDoeY1idiCKQ2S4JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC5|NkROwG0> MkjiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4N{WxOFQoRjJ3Nke1NVQ1RC:jPh?=
HCT8 M2LyV2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MnjtO|IhcHK| MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEigZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjN7Od88US=> MnTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4N{WxOFQoRjJ3Nke1NVQ1RC:jPh?=
HCT8 MYfGeY5kfGmxbjDhd5NigQ>? Mo\lNUB2VQ>? NID2bnczPCCqcoO= NY\yfG9HUW6qaXLpeIlwdiCxZjDITWYuOWGucHjhJJBzd3SnaX6g[ZhxemW|c3nvckBqdiCqdX3hckBJS1R6IHPlcIx{KGG2IEGgeW0hcW6ldXLheIVlKG[xcjCyOEBpenNiYomgW4V{fGW{bjDicI91fGmwZzDt[ZRpd2R? NYjvNpdzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2O|UyPDRpPkK1Olc2OTR2PD;hQi=>
HCT8 MXrGeY5kfGmxbjDhd5NigQ>? NIniSosyKHWP MlTnNlQhcHK| MX7Jcohq[mm2aX;uJI9nKEiLRj2xZYxxcGFicILveIVqdiCneIDy[ZN{cW:wIHnuJGZWNXKnc3nzeIFvfCCqdX3hckBJS1R6IHPlcIx{KGG2IEGgeW0hcW6ldXLheIVlKG[xcjCyOEBpenNiYomgW4V{fGW{bjDicI91fGmwZzDt[ZRpd2R? MnrKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4N{WxOFQoRjJ3Nke1NVQ1RC:jPh?=
HCT8 MWrGeY5kfGmxbjDhd5NigQ>? MUKxJJVO MYSyOEBpenN? MnXHTY5pcWKrdHnvckBw\iCVVFHUN{Bxem:2ZXnuJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDIR3Q5KGOnbHzzJIF1KDFidV2gbY5kfWKjdHXkJIZweiB{NDDodpMh[nliV3XzeIVzdiCkbH;0eIlv\yCvZYToc4Q> MknVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4N{WxOFQoRjJ3Nke1NVQ1RC:jPh?=
HCT8 MU\GeY5kfGmxbjDhd5NigQ>? MnzDNUB2VQ>? NHHueGMzPCCqcoO= NWL2bnFkUW6qaXLpeIlwdiCxZjDTWGFVOyCycn;0[YlvKHCqb4PwbI9zgWyjdHnvckBqdiCIVT3y[ZNqe3SjboSgbJVu[W5iSFPUPEBk\WyuczDheEAyKHWPIHnuZ5Vj[XSnZDDmc5IhOjRiaILzJIJ6KFenc4Tldo4h[myxdITpcochdWW2aH;k NUPPVYg5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2O|UyPDRpPkK1Olc2OTR2PD;hQi=>
HCT8 MYfGeY5kfGmxbjDhd5NigQ>? MVyxJJVO MkPHNlQhcHK| NWL1W4R5UW6qaXLpeIlwdiCxZjDBT3QheHKxdHXpckBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gTGNVQCClZXzsd{BifCBzIIXNJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdibXX0bI9l MknaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4N{WxOFQoRjJ3Nke1NVQ1RC:jPh?=
HCT8 NYrneHZmTnWwY4Tpc44h[XO|YYm= NH21T5kyKHWP NGPPS3gzPCCqcoO= M{Cw[2lvcGmkaYTpc44hd2ZiQVvUJJBzd3SnaX6gdIhwe3Cqb4L5cIF1cW:wIHnuJGZWNXKnc3nzeIFvfCCqdX3hckBJS1R6IHPlcIx{KGG2IEGgeW0hcW6ldXLheIVlKG[xcjCyOEBpenNiYomgW4V{fGW{bjDicI91fGmwZzDt[ZRpd2R? NGL5VVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[3OVE1PCd-MkW2O|UyPDR:L3G+
HCT8 MnSySpVv[3Srb36gZZN{[Xl? MXuxJJVO NXTmS5NkOjRiaILz NXfDeYpHUW6qaXLpeIlwdiCxZjDFVmsheHKxdHXpckBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gTGNVQCClZXzsd{BifCBzIIXNJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdibXX0bI9l MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ5NUG0OEc,OjV4N{WxOFQ9N2F-
HCT8 NFHWSIxHfW6ldHnvckBie3OjeR?= NXzFb4VMOSC3TR?= MnfxNlQhcHK| MYXJcohq[mm2aX;uJI9nKEWUSzDwdo91\WmwIIDoc5NxcG:{eXzheIlwdiCrbjDGWU1z\XOrc4ThcpQhcHWvYX6gTGNVQCClZXzsd{BifCBzIIXNJIlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdibXX0bI9l NV\6c5l{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW2O|UyPDRpPkK1Olc2OTR2PD;hQi=>
HCT8 MkfiRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NU\1W|VOOSC3TR?= MWe3NkBpenN? NIWwOnVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFgh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKHC{b3zp[oVz[XSrb36gZZQhOSC3TTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7 M1m2UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Nke1NVQ1Lz5{NU[3OVE1PDxxYU6=
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BEAS2B MYTGeY5kfGmxbjDhd5NigQ>? NEPYRYwyOCC3TR?= MVK2JIhzew>? NXz1cIpDSWO2aY\heIlwdiCxZjDOdoYzKGmwIHj1cYFvKEKHQWOyRkBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCKT{Gg[4Vv\SCneIDy[ZN{cW:wIHH0JFExKHWPIHnuZ5Vj[XSnZDDmc5IhPiCqcoOgZpkheVCFUjDt[ZRpd2R? M2HQTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mke4NFI5Lz5{NkK3PFAzQDxxYU6=
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H42E NUXOZXlkTnWwY4Tpc44h[XO|YYm= NX6xZplEOC5yMTD0c{A{OCCwTR?= MWexJIhz NEm0dWJUfGGkaXzpfoF1cW:wIH;mJG5TTjJiaX6gdoF1KEh2MlWgZ4VtdHNiZYjwdoV{e2mwZzDBVmU5VCCjdDCwMlAyKHSxIEOwJI5OKGGodHXyJFEhcHJiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NGj2W3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkmwPFE4Oyd-Mk[5NFgyPzN:L3G+
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A549/TR MXrGeY5kfGmxbjDhd5NigQ>? MnW0Nk41KHSxIEmuOkB2VQ>? M2nwRlI1KGi{cx?= NF[3XY1KdmS3Y4Tpc44hd2ZiUl;TJIdmdmW{YYTpc44hcW5iaIXtZY4hSTV2OT;UVkBk\WyuczDheEAzNjRidH:gPU43KHWPIHHmeIVzKDJ2IHjyd{BjgSCGQ1\IMWRCKGS7ZT3iZZNm\CCobH;3JIN6fG:vZYTybYMh[W6jbInzbZM> Mo\MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3MEG5OFcoRjJ7NUCxPVQ4RC:jPh?=
A549/TR MnfaSpVv[3Srb36gZZN{[Xl? NX;CZ|JVPC56IIXN NE[3foQzPCCqcoO= MUjEc5dvemWpdXzheIlwdiCxZjDMc44h\XiycnXzd4lwdiCrbjDoeY1idiCDNUS5M3RTKGOnbHzzJIF1KDRwODD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M3G4ZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUCxPVQ4Lz5{OUWwNVk1PzxxYU6=
HCT116 M171VWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MWi3NkBpenN? NW\pcVJLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlAxODJ3zszN NUj0b3NuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C0Nlk6PTNpPkOwOFI6QTV|PD;hQi=>
HT-29 MWHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NYXPN|hnPzJiaILz NHWyTlRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6yPO69VQ>? M2nqVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNEK5PVU{Lz5|MESyPVk2OzxxYU6=
HCT8 Ml\4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NYDHToV2PzJiaILz M334[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUPEBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR|UxRTBwMkpOwG0> NW\vN5hLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C0Nlk6PTNpPkOwOFI6QTV|PD;hQi=>
HCT116 NXe1dmRHTnWwY4Tpc44h[XO|YYm= NFKyT4o5KGi{cx?= M2\ncWlvcGmkaYTpc44hd2ZiQn3pNUBxem:2ZXnuJIV5eHKnc4Ppc44hcW5iaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDhiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MmKwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB2Mkm5OVMoRjNyNEK5PVU{RC:jPh?=
BEAS2B NF\wepRHfW6ldHnvckBie3OjeR?= MnT2OFghcHK| MV;BZ5RqfmG2aX;uJI9nKEunYYCxM2N2dDNxToLmNkBqdiCqdX3hckBDTUGVMlKgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4hVlGRMTDs[ZZmdHNibXXhd5Vz\WRiYX\0[ZIhPDhiaILzMEBGSzVyPUCuNFA5PzIQvF2= NIm5TXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|ME[yOlU2PSd-M{C2NlY2PTV:L3G+
HepG2 MljyR5l1d3SxeHnjbZR6KGG|c3H5 M1nFVVQ5KGi{cx?= NGfDbGNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4h[2WubDD2bYFjcWyrdImgbY5kfWKjdHXkJIZweiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMkdOwG0> M1Xne|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMEWxOFAyLz5|MUC1NVQxOTxxYU6=
MCF7 NXXmVoxpS3m2b4TvfIlkcXS7IHHzd4F6 M3Psb|Q5KGi{cx?= M3jLVGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJINmdGxidnnhZoltcXS7IHnuZ5Vj[XSnZDDmc5IhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjN3zszN NE\MfoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUC1NVQxOSd-M{GwOVE1ODF:L3G+
A549 NFTiTW5EgXSxdH;4bYNqfHliYYPzZZk> MYq0PEBpenN? MYXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCrbnP1ZoF1\WRiZn;yJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4{Ps7:TR?= NVzYcnllRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwOVE1ODFpPkOxNFUyPDBzPD;hQi=>
A549 NF\RbJpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Mm\tOFghcHK| MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC53Mt88US=> M3H5WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzN{K1Nlg5Lz5|MUeyOVI5QDxxYU6=
HepG2 MUPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NYrOWVRqPDhiaILz NGHYU5dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCpcn;3eIghcW6ldXLheIVlKG[xcjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuOVLPxE1? M1jGbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzN{K1Nlg5Lz5|MUeyOVI5QDxxYU6=
HOS NHnBUllCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MU[0PEBpenN? M2XwcGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF;TJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwNkdOwG0> M3HUW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzN{K1Nlg5Lz5|MUeyOVI5QDxxYU6=
MCF7 NWDCOGpRSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MkDQOFghcHK| MmPURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwOEZOwG0> M2flfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzN{K1Nlg5Lz5|MUeyOVI5QDxxYU6=
HEK293FT NWDCT3QxTnWwY4Tpc44h[XO|YYm= M1fh[VI1KGi{cx?= MlrwTY5pcWKrdHnvckBw\iCvb4Xz[UBIV0GWIHX4dJJme3OnZDDpckBJTUt{OUPGWEBk\WyuczDjc{1mgHC{ZYPzbY5oKHC{ZT3wdo9ocHKnbHnuJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDnbJJmdGmwIH;jeIFvd3muYYTpc44hcW6ldXLheIVlKG[xcjCyOEBpenNiYomgSWxKW0FuIFnDOVA:OC5yM{ZOwG0> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxO|YzPjJzLze+R4hGVUKOPD;hQi=>
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

DMSO 21 mg/mL
(41.52 mM)
Water Insoluble
Ethanol Insoluble

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 2022-01-17)

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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