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Bardoxolone Methyl (RTA 402) NRF2 활성제

Name: Bardoxolone Methyl (RTA 402)
Brand: Selleck Chemicals
SKU: S8078
Rating: 5 (36 reviews)

제품 번호S8078

Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me)은 강력한 세포자멸사 촉진 및 항염증 활성을 나타내는 IKK 억제제이며, 강력한 Nrf2 활성제이자 핵인자-κB (NF-κB) 억제제입니다. Bardoxolone Methyl은 페로프토시스를 억제합니다. Bardoxolone Methyl은 암세포에서 세포자멸사 및 자가포식을 유도합니다.

Bardoxolone Methyl (RTA 402) Nrf2 활성제 Chemical Structure

화학 구조

분자량: 505.69

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품질 관리

배치: 순도: 99.86%

99.86

관련 타겟	NF-κB HDAC Antioxidant ROS IκB/IKK AP-1 MALT NOD
기타 Nrf2 억제제	ML385 Brusatol TBHQ Sulforaphane Oltipraz Bardoxolone (CDDO) 4-Octyl Itaconate (4-OI) KI696 CDDO-Im (RTA-403) Mangiferin

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
MCF-7	Function assay			Inhibitory concentration against proliferation of MCF-7 (ER Positive) breast cancer cells, IC50=0.05μM	15369396
BMDM	Cytotoxicity assay		24 hrs	Cytotoxicity against C57BL/6 mouse BMDM cells assessed as LDH release after 24 hrs, MNTD=0.5μM	22533790
BMDM	Antiinflammatory assay	0.5 uM	1 hr	Antiinflammatory activity in C57BL/6 mouse BMDM cells assessed as inhibition of LPS-stimulated TNFalpha production at 0.5 uM pretreated for 1 hr before LPS challenge after 8 to 24 hrs by immunoassay	22533790
PANC1343	Antiproliferative assay	300 to 1000 nM	72 hrs	Antiproliferative activity against mouse PANC1343 cells at 300 to 1000 nM after 72 hrs by MTT assay	24388806
RAW264.7	Antioxidant assay	100 nM	18 hrs	Antioxidant activity in mouse RAW264.7 cells assessed as inhibition of tBHP-induced ROS production at 100 nM pretreated for 18 hrs before challenge measured after 15 mins by H2DCFA-based flow cytometry	24388806
HepG2	Cytotoxicity assay		48 hrs	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50=4.99μM	24685545
B16F10	Cytotoxicity assay		48 hrs	Cytotoxicity against mouse B16F10 cells after 48 hrs by MTT assay, IC50=5.85μM	24685545
CCD-841-CoN	Antiproliferative assay		72 hrs	Antiproliferative activity against human CCD-841-CoN cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.316μM	25675144
HCT8	Antiproliferative assay		72 hrs	Antiproliferative activity against 5-FU resistant human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.363μM	25675144
HCT8	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT8 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.399μM	25675144
HCT8	Function assay	1 uM	24 hrs	Inhibition of HIF-1alpha protein expression in human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method	25675144
HCT8	Function assay	1 uM	24 hrs	Inhibition of HIF-1alpha protein expression in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method	25675144
HCT8	Function assay	1 uM	24 hrs	Inhibition of STAT3 protein phosphorylation in human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method	25675144
HCT8	Function assay	1 uM	24 hrs	Inhibition of STAT3 protein phosphorylation in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method	25675144
HCT8	Function assay	1 uM	24 hrs	Inhibition of AKT protein phosphorylation in human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method	25675144
HCT8	Function assay	1 uM	24 hrs	Inhibition of AKT protein phosphorylation in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method	25675144
HCT8	Function assay	1 uM	24 hrs	Inhibition of ERK protein phosphorylation in human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method	25675144
HCT8	Function assay	1 uM	24 hrs	Inhibition of ERK protein phosphorylation in FU-resistant human HCT8 cells at 1 uM incubated for 24 hrs by Western blotting method	25675144
HCT8	Antiproliferative assay	1 uM	72 hrs	Antiproliferative activity against human HCT8 cells assessed as inhibition of cell proliferation at 1 uM after 72 hrs by MTT assay	25675144
HCT8	Antiproliferative assay	1 uM	72 hrs	Antiproliferative activity against 5-FU resistant human HCT8 cells assessed as inhibition of cell proliferation at 1 uM after 72 hrs by MTT assay	25675144
BEAS2B	Function assay	10 uM	6 hrs	Activation of Nrf2 in human BEAS2B cells assessed as increase in HO1 gene expression at 10 uM incubated for 6 hrs by qPCR method	26278028
H42E	Function assay		24 hrs	Induction of NRF2 activation in rat H42E cells expressing ARE8L assessed as reporter transgene activity after 24 hrs by luminescence assay, CD=0.0005μM	26908173
H42E	Cytotoxicity assay		24 hrs	Cytotoxicity against rat H42E cells expressing ARE8L assessed as cellular ATP level after 24 hrs by Celltiter-Glo luminescent cell viability assay, IC50=1.4μM	26908173
H42E	Function assay	0.01 to 30 nM	1 hr	Stabilization of NRF2 in rat H42E cells expressing ARE8L at 0.01 to 30 nM after 1 hr by Western blot analysis	26908173
NHBE	Cytoprotective assay	0.001 to 0.1 uM	18 hrs	Cytoprotective activity in NHBE cells assessed as inhibition of tBHP-induced GSH depletion at 0.001 to 0.1 uM preincubated for 18 hrs followed by tBHP addition for 4 hrs by thiostar dye based fluorescence assay	27031670
NHBE	Function assay	100 nM	24 hrs	Inhibition of KEAP1/NRF2 interaction in NHBE cells assessed as increase in GCLM mRNA expression at 100 nM incubated for 24 hrs in presence of non targeting siRNA by qRT-PCR method	27031670
NHBE	Function assay	100 nM	24 hrs	Inhibition of KEAP1/NRF2 interaction in NHBE cells assessed as increase in NQO1 mRNA expression at 100 nM incubated for 24 hrs in presence of non targeting siRNA by qRT-PCR method	27031670
NHBE	Function assay	100 nM	48 hrs	Inhibition of KEAP1/NRF2 interaction in NHBE cells assessed as induction of NQO1 specific activity at 100 nM incubated for 48 hrs in presence of non targeting siRNA by MTT reduction assay	27031670
HaCaT-ARE-luc	Function assay		6 hrs	Activation of Nrf2 (unknown origin) expressed in human HaCaT-ARE-luc cells after 6 hrs by luciferase reporter gene assay, EC50=0.06μM	28753294
NIH/3T3	Function assay		6 hrs	Inhibition of TNF-alpha stimulated NF-kappaB (unknown origin) expressed in mouse NIH/3T3 cells after 6 hrs by luciferase reporter gene assay, IC50=1.2μM	28753294
HeLa	Function assay		6 hrs	Inhibition of IFN-gamma stimulated STAT3 (unknown origin) expressed in human HeLa cells after 6 hrs by luciferase reporter gene assay, IC50=2.38μM	28753294
RAW264.7	Anti-inflammatory assay			Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of nitric oxide production, IC50=4μM	28754470
HEK293	Cytotoxicity assay		24 hrs	Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50=2.2μM	28994286
H9c2	Cytotoxicity assay		24 hrs	Cytotoxicity against rat H9c2 cells assessed as reduction in cell viability after 24 hrs by MTT assay, IC50=5.2μM	28994286
HEK293	Function assay	200 to 1000 nM	24 hrs	Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as TNFalpha-induced NFkappaB activation at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by NFkappaB-driven luciferase reporter gene assay	28994286
HEK293	Function assay	200 to 1000 nM	24 hrs	Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of iNOS mRNA expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by quantitative RT-PCR an	28994286
HEK293	Function assay	200 to 1000 nM	24 hrs	Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of COX2 mRNA expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by quantitative RT-PCR an	28994286
HEK293	Function assay	200 to 1000 nM	24 hrs	Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of MCP1 mRNA expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by quantitative RT-PCR an	28994286
intraglomerular mesangial cells	Function assay	0.65 mg/kg	12 weeks	Renoprotective activity in db/db mouse assessed as increase in number of intraglomerular mesangial cells at 0.65 mg/kg, ip administered trice per week for 12 consecutive weeks measured at 11 weeks post dose by H/E-staining based microscopic analysis	28994286
HEK293	Function assay	200 to 1000 nM	24 hrs	Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of COX2 protein expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by Western blot method	28994286
HEK293	Function assay	200 to 1000 nM	24 hrs	Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of iNOS protein expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by Western blot method	28994286
HEK293	Function assay	200 to 1000 nM	24 hrs	Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as mitigation of TNFalpha-induced increase in ratio of nuclear to cytosolic p65 at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by Western blot	28994286
HEK293	Function assay	200 to 1000 nM	24 hrs	Inhibition of IKKbeta (unknown origin) transfected in HEK293 cells assessed as reduction in TNFalpha-induced upregulation of MCP1 protein expression at 200 to 1000 nM administered 6 hrs after TNFalpha stimulation measured for 24 hrs by Western blot method	28994286
HEK293	Function assay	200 to 1000 nM	48 hrs	Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as upregulation of HO-1 mRNA expression at 200 to 1000 nM after 48 hrs by quantitative RT-PCR analysis	28994286
HEK293	Function assay	200 to 1000 nM	48 hrs	Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as upregulation of NQO1 mRNA expression at 200 to 1000 nM after 48 hrs by quantitative RT-PCR analysis	28994286
HEK293	Function assay	200 to 1000 nM	48 hrs	Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as activation of Nrf2 at 200 to 1000 nM after 48 hrs by ARE-driven luciferase reporter gene assay	28994286
HEK293	Function assay	200 to 1000 nM	48 hrs	Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as increase in nuclear to cytosolic Nfr2 ratio at 200 to 1000 nM after 48 hrs by Western blot analysis	28994286
HEK293	Function assay	200 to 1000 nM	48 hrs	Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as increase in cytosolic HO-1 levels at 200 to 1000 nM after 48 hrs by Western blot analysis	28994286
HEK293	Function assay	200 to 1000 nM	48 hrs	Inhibition of Keap1/Nrf2 (unknown origin) interaction transfected in HEK293 cells assessed as increase in cytosolic NQO1 levels at 200 to 1000 nM after 48 hrs by Western blot analysis	28994286
A549/TR	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549/TR cells after 72 hrs by MTT assay, IC50=1.703μM	29501947
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=2.074μM	29501947
A549/TR	Function assay	2.4 to 9.6 uM	24 hrs	Induction of ROS generation in human A549/TR cells at 2.4 to 9.6 uM after 24 hrs by DCFH-DA dye-based flow cytometric analysis	29501947
A549/TR	Function assay	4.8 uM	24 hrs	Downregulation of Lon expression in human A549/TR cells at 4.8 uM after 24 hrs by Western blot analysis	29501947
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.00025μM	30429953
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay, IC50=0.28μM	30429953
HCT8	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT8 cells after 72 hrs by SRB assay, IC50=0.29μM	30429953
HCT116	Function assay		8 hrs	Inhibition of Bmi1 protein expression in human HCT116 cells after 8 hrs by Western blot analysis	30429953
BEAS2B	Function assay		48 hrs	Activation of Keap1/Cul3/Nrf2 in human BEAS2B cells assessed as increase in NQO1 levels measured after 48 hrs, EC50=0.00871μM	30626555
HepG2	Cytotoxicity assay		48 hrs	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=0.26μM	31051401
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=0.35μM	31051401
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay, IC50=0.36μM	31051401
A549	Antiproliferative assay		48 hrs	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay, IC50=0.52μM	31725288
HepG2	Antiproliferative assay		48 hrs	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay, IC50=0.52μM	31725288
HOS	Antiproliferative assay		48 hrs	Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay, IC50=0.66μM	31725288
MCF7	Antiproliferative assay		48 hrs	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay, IC50=0.85μM	31725288
HEK293FT	Function assay		24 hrs	Inhibition of mouse GOAT expressed in HEK293FT cells co-expressing pre-proghrelin assessed as reduction in ghrelin octanoylation incubated for 24 hrs by ELISA, IC50=0.035μM	ChEMBL
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	505.69	화학식	C₃₂H₄₃NO₄	보관 (수령일로부터)	3년-20°C분말
CAS 번호	218600-53-4	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me			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

용해도

In vitro
배치:

DMSO : 26 mg/mL (51.41 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 13 mg/mL (25.7 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 50 mg/mL (98.87 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (197.74 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 20 mg/mL (39.54 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	4%DMSO 1 30%PEG300 2 5%Tween80 3 61%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.500mg/ml (4.94mM)	Taking the 1 mL working solution as an example, add 40 μL of clarified DMSO stock solution of 62.5 mg/ml to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 610 μL of ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

특징	The only IKKβ inhibitor in clinical use for solid tumors, type 2 diabetes, and chronic kidney disease. An orally-available antioxidant inflammation modulator.
Targets/IC₅₀/Ki	IKK (Cell-free assay) Ferroptosis Nrf2 NF-κB
시험관 내(In vitro)	Bardoxolone Methyl은 마우스 대식세포에서 인터페론-Ƴ에 의해 유도된 산화질소 생성에 대해 0.1 nM의 IC50을 갖는 강력한 억제 활성을 나타냅니다. 이 화합물은 백혈병 HL-60, KG-1 및 NB4 세포의 생존력을 각각 0.4, 0.4 및 0.27 μM의 IC50으로 감소시킵니다. 이는 세포자멸사 촉진 Bax 단백질을 유도하고, ERK1/2 활성화를 억제하며, Bcl-2 인산화를 차단하여 세포자멸사 유도에 기여합니다. 이 화학 물질은 TNF, 인터루킨(IL)-1beta, 포르볼 에스터, 오카다산, 과산화수소, 리포폴리사카라이드 및 담배 연기에 의해 활성화되는 구성적 및 유도성 NF-kappaB를 강력하게 억제합니다.
키나아제 분석	IKK 분석
키나아제 분석	CDDO-Me가 TNF 유도 IKK 활성화에 미치는 영향을 확인하기 위해 IKK를 분석합니다. 간략하게, 전체 세포 추출물로부터 IKK 복합체를 IKKα 및 IKKβ에 대한 항체로 침전시킨 다음 Protein A/G-Sepharose 비드로 처리했습니다. 2시간 후, 비드를 용해 완충액으로 세척한 다음 50 mmol/L HEPES (pH 7.4), 20 mmol/L MgCl₂, 2 mmol/L DTT, 20 μCi [γ-³²P]ATP, 10 μmol/L 비표지 ATP, 2 μg의 기질 글루타티온 S-트랜스퍼라제-IκBα (아미노산 1-54)를 포함하는 키나제 분석 혼합물에 재현탁했습니다. 30°C에서 30분 동안 배양한 후, SDS 시료 완충액으로 5분 동안 끓여 반응을 종료했습니다. 마지막으로, 단백질을 10% SDS-PAGE에서 분리하고, 겔을 건조한 다음, Storm820으로 방사능 밴드를 시각화했습니다. 각 시료에서 IKK-α 및 IKK-β의 총량을 결정하기 위해 50 μg의 전체 세포 단백질을 7.5% SDS-PAGE에서 분리하고, 니트로셀룰로스 막으로 전기 전이한 다음, 항-IKK-α 또는 항-IKK-β 항체로 블로팅했습니다.
생체 내(In vivo)	Bardoxolone Methyl (60 mg/kg)은 생체 내 폐 종양의 수, 크기 및 심각도를 감소시킵니다. 이 화합물은 LPS 공격 후 생체 내 염증성 사이토카인 반응을 유의하게 감소시키고, 비장에서 HO-1 단백질 발현을 유도하며, 치사량의 LPS로부터 마우스를 보호합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/11063620/ [2] https://pubmed.ncbi.nlm.nih.gov/11756188/ [3] https://pubmed.ncbi.nlm.nih.gov/16551868/ [4] https://pubmed.ncbi.nlm.nih.gov/17363558/ [5] https://pubmed.ncbi.nlm.nih.gov/20626291/ [6] https://pubmed.ncbi.nlm.nih.gov/20234191/ [7] https://pubmed.ncbi.nlm.nih.gov/31541463/

적용 분야

방법	바이오마커	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
Immunofluorescence	PDI / SDHA c-PARP / Cytochrome C / COX IV	26053096
Growth inhibition assay	Cell viability	25733817

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT02316821	Completed	Chronic Kidney Disease\|Type 2 Diabetes	Kyowa Kirin Co. Ltd.	December 2014	Phase 2
NCT02036970	Completed	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 a wholly owned subsidiary of Biogen\|Biogen	May 31 2014	Phase 2
NCT01598363	Completed	Healthy Volunteers	Reata a wholly owned subsidiary of Biogen\|Biogen	June 30 2012	Phase 1
NCT01551446	Withdrawn	Renal Insufficiency Chronic\|Diabetes Mellitus Type 2	Reata a wholly owned subsidiary of Biogen\|Biogen	April 30 2012	Phase 1
NCT01503866	Completed	Healthy	Reata a wholly owned subsidiary of Biogen\|Biogen	December 1 2011	Phase 1

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