Keap1-Nrf2-IN-11

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Keap1-Nrf2-IN-11 (compound 6k) is a Keap1-Nrf2 inhibitor with K_D2 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

CAS No. : 2796292-75-4

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nNOS iNOS eNOS

Biological Activity
Purity & Documentation
References
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Description

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]

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 (T_1/2), 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 (T_1/2), maximum plasma concentration (C_max), 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)
T_max (h)	1.38	0.72
T_max (h)	10.92	4.31
C_max (ng/mL)	707.62	2631.69
AUC_0-24 (ng·h/mL)	3061.55	4561.21
AUC_0-∞ (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
MRT_0-24 (h)	6.71	4.64
MRT_0-∞ (h)	13.97	5.94
F %	19.86

Molecular Weight

765.90

Formula

C₃₆H₄₃N₇O₈S₂

CAS No.

2796292-75-4

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Liu G, et al. Crystallography-Guided Optimizations of the Keap1-Nrf2 Inhibitors on the Solvent Exposed Region: From Symmetric to Asymmetric Naphthalenesulfonamides. J Med Chem. 2022 Jun 23;65(12):8289-8302. [Content Brief]

Keap1-Nrf2-IN-11 Related Classifications

Inflammation/Immunology

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Help & FAQs

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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