MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

KI696

CAS No. : 1799974⁻⁷0-1

MCE 国际站：KI696

产品活性：KI696 是一种干扰 Keap1/NRF2 相互作用的高亲和力探针。KI696 是有效、选择性的 KEAP1/NRF2 相互作用抑制剂。

研究领域：NF-κB

作用靶点：Keap1-Nrf2

In Vitro: KI696 (compound 7) exhibits very high affinity for the KEAP1 Kelch domain (ITC K_d=1.3 nM with the exception of the organic anion transporting polypeptide 1B1 (OATP1B1) (IC₅₀=2.5 µM), the bile salt export pump BSEP (IC₅₀=4.0 µM), ａnd the phosphodiesterase PDE3A (IC₅₀=10 µM), no significant cross-reactivity is observed. No cytotoxicity is observed towards BEAS-2B cells with KI696 at concentrations up to 10 µM. KI696 increases NRF2 Nuclear Translocation in Normal Human Bronchial Epithelial cells. KI696 increases mRNA expression of the NRF2-dependent genes NQO1 ａnd GCLM in NHBE cells transfected with the non-targeting siRNA, while NRF2 gene silencing significantly decreases compound activity. KI696 increases NQO1 Activity in an NRF2-Dependent Manner. Treatment with tBHP clearly has a detrimental effect on cell health ａnd appearance while pre-treatment of cells with 1 µM KI696 before the exposure to tBHP maintained cell morphology consistent with the DMSO control. KI696 Induces the Expression of NRF2-Regulated Genes in COPD patient-derived bronchial epithelial cells.

In Vivo: KI696 induces the expression of each of the Nqo1, Ho-1, Txnrd1, Srxn1, Gsta3, Gclc genes in a dose-dependent manner, with maximum increases over vehicle controls of 37-(Nqo1), 17-(Ho-1), 9-(Txnrd1), 28-(Srxn1), 15-(Gsta3) ａnd 13-fold (Gclc) occurring at the 50 µmol/kg dose. EC₅₀ values are 44.0, 25.7, 42.6, 33.8, 28.4, ａnd 44.1 µmol/kg, respectively, giving an average EC₅₀ value of 36.4±3.4 µmol/kg. KI696 attenuates ozone-Induced pulmonary inflammation. KI696 restores ozone-induced depletion of lung GSH levels. KI696 is administered to rats at 10, 35 ａnd 50 µmol/kg by IV infusion, resulting in steady state compound concentrations in the blood of 407±44 nM, 946±50 nM ａnd 1437±186 nM, respectively, over the 6 hour infusion period. Exposure to ozone 24 hours post-dose produces a significant depletion in lung levels of the anti-oxidant molecule, GSH, which is restored by KI696 in a dose-dependent manner.

相关产品：Bioactive Compound Library Plus | Resveratrol | 4-Octyl Itaconate | Curcumin | TBHQ | Sulforaphane | Bardoxolone methyl | Luteolin | Dimethyl fumarate | Oltipraz | Ezetimibe | Brusatol | Mangiferin | NK-252 | Carnosol | Hinokitiol | Danshensu | ML334 | Nrf2-IN-1 | CDDO-EA | Pyridoxine hydrochloride | Garci D | Methyl 3,4-dihydroxybenzoate | Eriodictyol | Astilbin | Hesperin | 4-Hydroxyphenylacetic acid | Corynoline | (+)-DHMEQ | CBR-470-2

品牌介绍:
• MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；
• 10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
• 设有专业的实验中心和严格的质控、验证体系；
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
• 产品的生物活性多经各国客户实验验证；
• Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
• 专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
• 与世界各大制药公司及知名科研机构建立了长期的合作。