Keap1-Nrf2-IN-14_product_DataBase

Bioactivity	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].
Invitro	Keap1-Nrf2-IN-14 effectively activated NRF2-ARE regulated cytoprotective defense system in both concentration- and time- dependent manner in RAW264.7 cells[1].Keap1-Nrf2-IN-14 (1, 10 µM; 12 h) enhanced the antioxidant capacity in macrophage RAW 264.7 cells[1].Keap1-Nrf2-IN-14 (1, 10 µM; 12 h) attenuates LPS-induced production of inflammation factors in RAW 264.7 cells[1].Keap1-Nrf2-IN-14 shows high metabolic stability (in co-incubation with rat liver microsomes with half-life of 10.5 h), and have no CYP inhibition on 1A2, 2C9, 2C19, 2D6 and 3A4 when at 10 µM. Cell Viability Assay[1] Cell Line:
In Vivo	Keap1-Nrf2-IN-14 (10 mg/kg; i.p.; single daily for 3 days) reduces the LPS-induced production of the proinflammatory factors in vivo[1].Keap1-Nrf2-IN-14 (1 mg/kg; i.v.; single) shows half-life of 1.72 h in vivo[1]. Animal Model:
Name	Keap1-Nrf2-IN-14
CAS	1928782-31-3
Formula	C30H29NO8S
Molar Mass	563.62
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Lu M C, et al. Discovery of 2-oxy-2-phenylacetic acid substituted naphthalene sulfonamide derivatives as potent KEAP1-NRF2 protein-protein interaction inhibitors for inflammatory conditions. European Journal of Medicinal Chemistry, 2020, 207: 112734.

PeptideDB

Keap1-Nrf2-IN-14

CAS: 1928782-31-3 F: C30H29NO8S W: 563.62