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

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.

For research use only. We do not sell to patients.

Keap1-Nrf2-IN-11 Chemical Structure

Keap1-Nrf2-IN-11 Chemical Structure

CAS No. : 2796292-75-4

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Description

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].

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].

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

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].

MedChemExpress (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
Molecular Weight

765.90

Formula

C36H43N7O8S2

CAS No.
SMILES

O=S(N(C1=C2C(C=CC=C2)=C(C=C1)N(S(=O)(C3=CC=C(C=C3)NC(CCN4CCN(CC4)CC)=O)=O)CC(N)=O)CC(N)=O)(C5=CC=C(C=C5)OC)=O

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    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.

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Keap1-Nrf2-IN-11
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