| Cat. No. |
Product Name |
Information |
| PC-28167 |
NXPZ-2
Keap1-Nrf2 inhibitor
|
NXPZ-2 is a potent, direct, non-covalent inhibitor of Keap1-Nrf2 protein-protein interaction with Ki of 95 nM in FP assays and EC50 of 120 nM. |
| PC-28166 |
Keap1-Nrf2 inhibitor 6K
Keap1-Nrf2 inhibitor
|
Keap1-Nrf2 inhibitor 6K is a small molecule inhibitor of Keap1-Nrf2 interaction, exhibits high Keap1-binding affinity (KD2 values=210 nM). |
| PC-28128 |
CPUY192002
Keap1-Nrf2 inhibitor
|
CPUY192002 is a potent protein-protein interaction (PPI) inhibitor of Keap1-Nrf2 with KD of 3.59 nM, effectively disrupts the Nrf2-Keap1 interaction with an EC50 of 28.6 nM in FP assays, also activates the Nrf2 transcription activity in the cell-based ARE-luciferase reporter assay. |
| PC-28127 |
CPUY192018
Keap1-Nrf2 inhibitor
|
CPUY192018 is a potent small-molecule inhibitor of the Keap1-Nrf2 PPI, has binding affinity for Keap1 with IC50 of 14.4 nM in FP assays and ITC Kd of 39.8 nM. |
| PC-28126 |
GSK3227634
Keap1-Nrf2 inhibitor
|
GSK3227634 is a potent, ultrahigh-affinity, noncovalent, reversible inhibitor of KEAP1-NRF2 (SPR pKd=10.9, TR-FRET pIC50=9.0) and NRF2 activator. |
| PC-26889 |
SLOS-1811-06 tR1
Nrf2 activator
|
SLOS-1811-06 tR1 is a potent, small molecule activator of NRF2 with EC50 of 0.98 nM in ARE-luciferase reporter assays, shows inhibitory activity of NRF2-KEAP1 with IC50 of 0.17 nM in BRET assays, protects hiPSC-derived RGCs from hypoxia/reoxygenation injury. |
| PC-25722 |
Bardoxolone
Nrf2 agonist
|
Bardoxolone (RTA401, CDDO) is a covalent, orally active activator of NRF2, also inhibits SARS-CoV-2 3CL protease (EC50=0.43 uM), also inhibits necroptosis in HT-29 cells by blocking necrosome formation through inhibiting phosphorylation of RIPK1 and RIPK3. |
| PC-25721 |
CH7450924 hydrate
KEAP1-NRF2 inhibitor, NRF2 activator
|
CH7450924 hydrate is a highly potent and selective NRF2 activator, inhibits KEAP1-NRF2 interaction inhibitor, binds non-covalently to the NRF2 binding site of KEAP1. |
| PC-25720 |
CH7450924
KEAP1-NRF2 inhibitor, NRF2 activator
|
CH7450924 is a highly potent and selective NRF2 activator, inhibits KEAP1-NRF2 interaction inhibitor, binds non-covalently to the NRF2 binding site of KEAP1. |
| PC-25485 |
VVD-065
NRF2 inhibitor, KEAP1-CUL3 molecular glue
|
VVD-065 is a first-in-class, allosteric molecular glue of Keap1-Cul3 E3-ligase complex and NRF2 inhibitor, specifically and covalently engages C151 on KEAP1 with engagement potency (TE50) of 9 nM in KYSE70 cells, promotes KEAP1-CUL3 complex formation, leading to enhancement of NRF2 degradation. |
| PC-22348 |
4-octyl itaconate
NRF2 activator
|
4-Octyl Itaconate (4-OI) is a cell-permeable Itaconate derivative, activates Nrf2 via alkylation of KEAP1, is protective against lipopolysaccharide-induced lethality in vivo and decreases cytokine production. |
| PC-21180 |
NRF2 inhibitor R16
NRF2 inhibitor
|
NRF2 inhibitor R16 is a novel mutated KEAP1 (mKEAP1)-selective NRF2 inhibitor, binds KEAP1-mutated proteins (G333C mKEAP1, Kd=2.7 uM) and restores their interaction with NRF2, leading to proteasome-dependent NRF2 degradation. |
