2. NF-κB Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. Keap1-Nrf2 NO Synthase ROS Kinase
  4. Keap1-Nrf2-IN-11

Keap1-Nrf2-IN-11 是一种 Keap1-Nrf2 抑制剂，其 KD2 值为 0.21 nM。Keap1-Nrf2-IN-11 抑制 ROS 和 NO 的产生以及 TNF-α 的表达。Keap1-Nrf2-IN-11 通过增加 Nrf2 核易位来缓解炎症。Keap1-Nrf2-IN-11 可用于抗炎研究。

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Keap1-Nrf2-IN-11 Chemical Structure

Keap1-Nrf2-IN-11 Chemical Structure

CAS No. : 2796292-75-4

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Keap1-Nrf2-IN-11 相关抗体

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nNOS iNOS eNOS

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Keap1-Nrf2-IN-11 (compound 6k) is a Keap1-Nrf2 inhibitor with KD2 value of 0.21 nM. Keap1-Nrf2-IN-11 inhibits the productions of ROS and NO and the expression of TNF-α. Keap1-Nrf2-IN-11 relieves inflammations by increasing the Nrf2 nuclear translocation. Keap1-Nrf2-IN-11 can be used for anti-inflammatory research[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Peritoneal macrophage CC50
> 100 μM
Compound: 6k
Cytotoxicity against mouse peritoneal macrophages assessed as reduction in cell viability measured after 24 hrs by Cell Titer-Blue assay
Cytotoxicity against mouse peritoneal macrophages assessed as reduction in cell viability measured after 24 hrs by Cell Titer-Blue assay
[PMID: 35687391]
Peritoneal macrophage EC50
0.97 μM
Compound: 6k
Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as suppression of NO level pretreated with LPS followed by compound addition and measured after 24 hrs by Griess reagent based assay
Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as suppression of NO level pretreated with LPS followed by compound addition and measured after 24 hrs by Griess reagent based assay
[PMID: 35687391]
Peritoneal macrophage EC50
1.14 μM
Compound: 6k
Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as inhibition of TNF alpha level after 4 hrs by ELISA method
Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as inhibition of TNF alpha level after 4 hrs by ELISA method
[PMID: 35687391]
体外研究
(In Vitro)

Keap1-Nrf2-IN-11 (compound 6k) (10 μΜ) suppresses the production of ROS and NO and inhibits the concentration of proinflammatory cytokine TNF-α in LPS-induced murine peritoneal macrophage model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Keap1-Nrf2-IN-11 相关抗体:
体内研究
(In Vivo)

Keap1-Nrf2-IN-11 (compound 6k) (5-10 mg/kg; i.p.; ALI mouse model) has anti-inflammatory activity in vivo[1].
Keap1-Nrf2-IN-11 (compound 6k) (5 mg/kg; i.v.; SD rats) has the half time (T1/2), the clearance rate (CL) and apparent distribution volume (V) were 4.31 h, 5.57 mL/min/kg and 959 L/kg, respectively[1].
Keap1-Nrf2-IN-11 (compound 6k) (5 mg/kg; i.p.; ALI mouse model) has the half time (T1/2), maximum plasma concentration (Cmax), area under curve (AUC) and oral bioavailability (F) were 10.92 h, 707 ng/mL, 3702 ng•h/mL and 19.86%, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ALI mouse model[1]
Dosage: 5, 10 and 20 mg/kg
Administration: Intraperitoneal injection; 30 mins.
Result: Had lower TNF-α, IL-1β and IL-6 levels in BALF in a dose-dependent manner.
Animal Model: ALI mouse model[1]
Dosage: 5, 10 and 20 mg/kg
Administration: Intraperitoneal injection; 30 mins.
Result: Induced the Nrf2 nuclear accumulation in lung tissue cells by decreasing the cytosolic Nrf2 and increasing the nuclear Nrf2 in a dose−response manner.
Animal Model: SD rats[1]
Dosage: 5 and 20 mg/kg
Administration: Intraperitoneal injection and oral gavage
Result: 1.19
Administration i.g. (20 mg/kg) i.v. (5 mg/kg)
Tmax (h) 1.38 0.72
Tmax (h) 10.92 4.31
Cmax (ng/mL) 707.62 2631.69
AUC0-24 (ng·h/mL) 3061.55 4561.21
AUC0-∞ (ng·h/mL)CL (mL/min/kg) 3702.22 4799.24
CL (L/h/kg) 6503.05 5.57
V (L/kg) 114127.5 959.54
MRT0-24 (h) 6.71 4.64
MRT0-∞ (h) 13.97 5.94
F % 19.86
分子量

765.90

Formula

C36H43N7O8S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Keap1-Nrf2-IN-11 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Keap1-Nrf2-IN-112796292-75-4Keap1-Nrf2NO SynthaseROS KinaseNitric oxide synthasesNOSanti-inflammatoryNrf2 nuclear translocationROSNOInhibitorinhibitorinhibit

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