Rel/NF-κB proteins are dimeric, DNA sequence-specific transcription factors that coordinate inflammatory responses; innate and adaptive immunity; and cellular differentiation, proliferation, and survival in almost all multicellular organisms. In most cells NF-κB exists in the cytoplasm in an inactive complex bound to IkappaB. The NF-κB network consists of five family member protein monomers (p65/RelA, RelB, cRel, p50, and p52) that form homodimers or heterodimers that bind DNA differentially and are regulated by two pathways: the canonical, NF-κB essential modulator (NEMO)-dependent pathway and the noncanonical, NEMO-independent pathway.

The I Bs bind to NF-κB dimers and sterically block the function of their NLSs, thereby causing their cytoplasmic retention. Potent NF-κB activators, such as TNFα and IL-1, cause almost complete degradation of IκBs (especially I B ) by the 26S proteasome, and NF-κB is activated and enters the nucleus. Nfkb2/p100 is the primary signaling node at which canonical and noncanonical signals interact. NIK/IKK1 processes p100 into p52, enabling the activity of RelB, NIK degrades IκBδ, allowing for sustained RelA activity, and canonical pathway activity may boost noncanonical pathway activation of RelB:p52.

Activation of the NF-κB pathway is involved in the pathogenesis of chronic inflammatory diseases, such as asthma, rheumatoid arthritis, and inflammatory bowel disease. In addition, altered NF-κB regulation may be involved in other diseases such as atherosclerosis and Alzheimer’s disease and a variety of human cancers. Therefore, numerous drugs, natural products, and normal or recombinant proteins that inhibits NF-κB activation can used in the treatment of NF-κB-related diseases.

References:
[1] Karin M. Oncogene. 1999 Nov 22;18(49):6867-74.
[2] Yamamoto Y, et al. J Clin Invest. 2001 Jan;107(2):135-42.
[3] Mitchell S, et al. Wiley Interdiscip Rev Syst Biol Med. 2016 May;8(3):227-41.


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Nrf2 activator-5

Nrf2 activator-5 (compound 1) is a potent Nrf2 activator that can attenuate H2O2-induced oxidative stress and LPS-stimulated inflammation in BV-2 microglial cells. Nrf2 activator-5 exhibits antioxidant and anti-inflammatory activities[1].

  • CAS Number: 1012860-13-7
  • MF: C25H30Cl2O6
  • MW: 497.41
  • Catalog: Keap1-Nrf2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydrangenol

Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level[1].

  • CAS Number: 480-47-7
  • MF: C15H12O4
  • MW: 256.253
  • Catalog: COX
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 528.3±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 206.4±23.6 °C

Keap1-Nrf2-IN-14

Keap1-Nrf2-IN-14 (compound 20c) is a KEAP1-NRF2 inhibitor that effectively disrupts the KEAP1-NRF2 interaction (IC50=75 nM) with a Kd value of 24 nM for KEAP1. Keap1-Nrf2-IN-14 induces the expression of NRF2 target genes and enhances the downstream antioxidant and anti-inflammatory activities. Keap1-Nrf2-IN-14 can be used in the study of oxidative stress-related inflammation[1].

  • CAS Number: 1928782-31-3
  • MF: C30H29NO8S
  • MW: 563.62
  • Catalog: Keap1-Nrf2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mangiferin

Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50.

  • CAS Number: 4773-96-0
  • MF: C19H18O11
  • MW: 422.340
  • Catalog: Keap1-Nrf2
  • Density: 1.8±0.1 g/cm3
  • Boiling Point: 842.7±65.0 °C at 760 mmHg
  • Melting Point: 269-270ºC
  • Flash Point: 303.6±27.8 °C

TPNA10168

TPNA10168 is an Nrf-2 activator that activates the Keap1-Nrf2-ARE pathway. TPNA10168 is neuroprotective against oxidative stress-induced damage. TPNA10168 significantly reduces the transcription of inflammatory genes, including TNF-α, IL-1β, IL-6, and iNOS. TPNA10168 can be used in research on anti-inflammatory and neurological diseases[1].

  • CAS Number: 957942-34-6
  • MF: C9H9ClO2S2
  • MW: 248.75
  • Catalog: Keap1-Nrf2
  • Density: 1.54±0.1 g/cm3 (20 °C, 760 mmHg)
  • Boiling Point: 490.3±45.0 °C (760 mmHg)
  • Melting Point: N/A
  • Flash Point: N/A

SC-514

SC-514 is a selective IKK-2 inhibitor (IC50=11.2±4.7 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.

  • CAS Number: 354812-17-2
  • MF: C9H8N2OS2
  • MW: 224.303
  • Catalog: IKK
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 399.2±42.0 °C at 760 mmHg
  • Melting Point: 209-211°C
  • Flash Point: 195.2±27.9 °C

MLT-747

MLT-748 is a allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 5 nM. MLT-748 also reversibly binds to human mutant MALT1(329-728)-W580S (Kd, 13 nM) with affinity similar to that of the wild type MALT1(329-728) (Kd, 42 nM)[1].

  • CAS Number: 2097853-86-4
  • MF: C20H21Cl2N7O3
  • MW: 478.33
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AChE/Nrf2 modulator 1

AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease[1].

  • CAS Number: 2417117-84-9
  • MF: C27H27FN4O2
  • MW: 458.53
  • Catalog: AChE
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Isophysalin A

Isophysalin A is a physalin with alpha and beta unsaturated ketone components. Isophysalin A binds to GSH and targets multiple cysteine residues on IKKβ. Isophysalin A also inhibits inducible NO synthase (iNOS) and nitric oxide (NO) production, showing anti-inflammatory activity[1].

  • CAS Number: 1363398-67-7
  • MF: C28H30O10
  • MW: 526.53
  • Catalog: NO Synthase
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 846.6±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 286.6±27.8 °C

(S)-Falcarinol

(S)-Falcarinol (Panaxynol), one of the major polyacetylenes isolated from Panax ginseng, has antitumor activity. (S)-Falcarinol (Panaxynol) is the most potent antiplatelet agent in ginseng and its mechanism of action is chiefly due to the inhibition of thromboxane formation. (S)-Falcarinol (Panaxynol) is a potent Nrf2 activator[1][2][3].

  • CAS Number: 81203-57-8
  • MF: C17H24O
  • MW: 244.37200
  • Catalog: Keap1-Nrf2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SN50

SN50 is a cell permeable inhibitor of NF-κB translocation. Sequence: Ala-Ala-Val-Ala-Leu-Leu-Pro-Ala-Val-Leu-Leu-Ala-Leu-Leu-Ala-Pro-Val-Gln-Arg-Lys-Arg-Gln-Lys-Leu-Met-Pro;AAVALLPAVLALLAPVQRKRQKLMP.

  • CAS Number: 213546-53-3
  • MF: C129H230N36O29S
  • MW: 2781.50000
  • Catalog: Peptides
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MALT1-IN-5

MALT1-IN-5 (compound 1) is a potent MALT1 protease inhibitor. MALT1-IN-5 can be used for cancer research[1].

  • CAS Number: 2434602-73-8
  • MF: C17H17ClF2N6O3
  • MW: 426.81
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(R)-MALT1-IN-3

(R)-MALT1-IN-3 (compound 121) is a potent MALT1 protease inhibitor with an IC50 of 20 nM. (R)-MALT1-IN-3 has IC50 of 60 nM, 40 nM for human IL6/IL10 in OCI-LY3 cells, respectively[1].

  • CAS Number: 2504229-61-0
  • MF: C21H19F3N8O2
  • MW: 472.42
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Trifluoromethyl-2'-methoxychalcone

2-Trifluoromethyl-2'-methoxychalcone is a chalcone derivative. 2-Trifluoromethyl-2'-methoxychalcone is a potent Nrf2 activator. 2-Trifluoromethyl-2'-methoxychalcone can be used for oxidative stress and inflammation related diseases research[1].

  • CAS Number: 1309371-03-6
  • MF: C17H13F3O2
  • MW: 306.28
  • Catalog: Keap1-Nrf2
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 395.6±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 186.4±22.8 °C

Oxaprozin, potassium salt

Oxaprozin potassium is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin potassium also inhibits the activation of NF-κB. Oxaprozin potassium induces cell apoptosis. Oxaprozin potassium shows anti-inflammatory activity. Oxaprozin potassium-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties[1][2].

  • CAS Number: 174064-08-5
  • MF: C18H14KNO3
  • MW: 331.40700
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: 467ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 236.2ºC

TAT 14TFA

TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1[1].

  • CAS Number: 1362661-34-4
  • MF: C137H230N48O39
  • MW: 3173.59
  • Catalog: Keap1-Nrf2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ginsenoside Rh3

Ginsenoside Rh3 is a bacterial metabolite of Ginsenoside Rg5. Ginsenoside Rh3 treatment in human retinal cells induces Nrf2 activation.

  • CAS Number: 105558-26-7
  • MF: C36H60O7
  • MW: 604.857
  • Catalog: Keap1-Nrf2
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 695.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 374.1±31.5 °C

dehydrocurdione

Dehydrocurdione, a zedoary-derived sesquiterpene, induces heme oxygenase (HO)-1, an antioxidative enzyme, in RAW 264.7 macrophages. Dehydrocurdione interacts with Keap1, resulting in Nrf2 translocation followed by activation of the HO-1 E2 enhancer. Dehydrocurdione suppresses lipopolysaccharide-induced NO release, a marker of inflammation. Anti-inflammatory activity[1][2].

  • CAS Number: 38230-32-9
  • MF: C15H22O2
  • MW: 234.33400
  • Catalog: Keap1-Nrf2
  • Density: 0.962g/cm3
  • Boiling Point: 362.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 136.2ºC

8-Hydroxyquinoline-2-Carboxylic Acid

BAY32-5915 is a potent IKKα inhibitor with an IC50 value of 60 nM. BAY32-5915 has not affect Doxorubicin (HY-15142A)-induced NF-κB activation[1].

  • CAS Number: 1571-30-8
  • MF: C10H7NO3
  • MW: 189.167
  • Catalog: IKK
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 426.7±30.0 °C at 760 mmHg
  • Melting Point: 213-214 °C
  • Flash Point: 211.9±24.6 °C

IKK-IN-4

IKK-IN-4 is a potent and selective IkappaB kinase 2 (IKKβ orIKK2) inhibitor, with IC50s of 45 and 650 nM for IKKβ and IKKα, respectively[1].

  • CAS Number: 615529-94-7
  • MF: C18H19N5S
  • MW: 337.44
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Engeletin

Engeletin is a flavanonol glycoside isolated from hymenaea martiana, inhibits NF-κB signaling-pathway activation, and possesses anti-inflammatory, analgesic, diuresis, detumescence, and antibiosis effects.

  • CAS Number: 572-31-6
  • MF: C21H22O10
  • MW: 434.39
  • Catalog: NF-κB
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: 820.0±65.0 °C at 760 mmHg
  • Melting Point: 176-177ºC
  • Flash Point: 289.5±27.8 °C

Keap1-Nrf2 probe

Keap1-Nrf2 probe is a fluorescent Keap1-Nrf2 probe[1].

  • CAS Number: 2430031-36-8
  • MF: C48H72N10O19
  • MW: 1093.14
  • Catalog: Keap1-Nrf2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Desfluoro-ezetimibe

Desfluoro-ezetimibe is a desfluoro impurity of Ezetimibe. Ezetimibe is a potent, metabolically stable cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator[1][2].

  • CAS Number: 302781-98-2
  • MF: C24H22FNO3
  • MW: 391.435
  • Catalog: Autophagy
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 642.8±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 342.6±31.5 °C

SPC-180002

SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway[1].

  • CAS Number: 2170274-53-8
  • MF: C18H23NO4
  • MW: 317.38
  • Catalog: Sirtuin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Chicanine

Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity[1].

  • CAS Number: 78919-28-5
  • MF: C20H22O5
  • MW: 342.386
  • Catalog: ERK
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 483.8±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 246.4±28.7 °C

MALT1-IN-3

MALT1-IN-3 (compound 122) is a potent MALT1 protease inhibitor, with an IC50 of 0.06 μM. MALT1-IN-3 has IC50 of 0.14 and 0.13 μM for human IL6/IL10 in OCI-LY3 cells, respectively[1].

  • CAS Number: 2504229-63-2
  • MF: C21H19F3N8O2
  • MW: 472.42
  • Catalog: MALT1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

IKK-IN-1

IKK-IN-1 is an inhibitor of IKK extracted from patent WO2002024679A1, compound example 18-13.

  • CAS Number: 406211-06-1
  • MF: C22H26ClN3O4
  • MW: 431.913
  • Catalog: IKK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TML-6-d3

TML-6-d3 is the deuterium labeled TML-6. TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-

  • CAS Number: 2673270-28-3
  • MF: C30H34D3NO7
  • MW: 526.64
  • Catalog: Keap1-Nrf2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1,3-Diphenylpropane-1,3-dione

Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2[1].

  • CAS Number: 120-46-7
  • MF: C15H12O2
  • MW: 224.255
  • Catalog: Keap1-Nrf2
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 357.4±0.0 °C at 760 mmHg
  • Melting Point: 77-79 °C(lit.)
  • Flash Point: 146.9±20.2 °C

Keap1-Nrf2-IN-5

Keap1-Nrf2-IN-5 (compound 1) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 4.1 µM, Kd of 3.7 µM[1].

  • CAS Number: 2696272-70-3
  • MF: C23H30N4O6S
  • MW: 490.57
  • Catalog: Keap1-Nrf2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A