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KI696

Catalog No. T11758L CAS 1799974-70-1

KI696 is a high-affinity probe that potently inhibits the interaction of Keap1 and Nrf2.

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KI696, CAS 1799974-70-1

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	KI696 is a high-affinity probe that potently inhibits the interaction of Keap1 and NRF2.
In vitro	KI696 displays high affinity for the KEAP1 Kelch domain with ITC Kd of 1.3 nM with the exception of the organic anion transporting polypeptide 1B1, the bile salt export pump BSEP and the phosphodiesterase PDE3A with an IC50 of 2.5 µM, 4.0 µM and 10 µM). KI696 causes an increase of NRF2 Nuclear Translocation in Normal Human Bronchial Epithelial cells and mRNA expression of the NRF2-dependent genes NQO1 and GCLM in NHBE cells transfected with the non-targeting siRNA in an NRF2-dependent manner[1].
In vivo	KI696 induces the expression of the Nqo1, Ho-1, Txnrd1, Srxn1, Gsta3, and Gclc genes in a dose-dependent manner with EC50s of 44.0, 25.7, 42.6, 33.8, 28.4, and 44.1 µmol/kg, respectively. KI696 attenuates ozone-Induced pulmonary inflammation and restores depletion of lung GSH levels. In rats, intravenous administration of KI696(10-50 µmol/kg) results in steady state compound concentrations in the blood of 407-1437 nM[1].

Molecular Weight	550.63
Formula	C28H30N4O6S
CAS No.	1799974-70-1

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 45.0 mg/mL (81.7 mMc), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Davies TG, et al. Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery. J Med Chem. 2016 Apr 28;59(8):3991-4006.

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

KI696 1799974-70-1 Immunology/Inflammation Nrf2 KI-696 Inhibitor inhibitor inhibit

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