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Cat. No.: HY-181907

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NBE5

NBE5 is an orally active hydrophobic tag-targeting (Hyt) degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C).
NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831).

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화학식: C₅₀H₇₃N₃O₄
분자량:780.13

보관:

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

NBE5 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

NBE5 is an orally active hydrophobic tag-targeting (Hyt) degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C)^[1].
NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831).

IC₅₀ & Target

HSP90

All HSP Isoforms :

In Vitro

NBE5 (1.0 μM; 12 h) induces potent Keap1 degradation in HCT116, RKO, and BEAS-2B cells, with the highest activity (92.5% degradation) observed in BEAS-2B cells^[1].
NBE5 (0.1-10.0 μM; 12 h) induces concentration-dependent Keap1 degradation in HCT116 and RKO cells over 12 h, with higher potency (lower DC₅₀, higher D_max) in HCT116 cells^[1].
NBE5 (1.0 μM; 1.5-24 h) induces time-dependent Keap1 degradation in HCT116 and RKO cells, with faster degradation kinetics (shorter DT₅₀) observed in HCT116 cells^[1].
NBE5 (2.0 μM; 6-18 h, plus washout culture) mediates Keap1 degradation in HCT116 and RKO cells that depends on both the ubiquitin-proteasome system and autophagy-lysosome system, involves enhanced Keap1-Hsp90 interaction, and produces sustained degradation after washout^[1].
NBE5 (0.5-2.5 μM; 12 h) activates the Nrf2 pathway in HCT116, RKO, and BEAS-2B cells via Keap1 degradation, leading to increased nuclear Nrf2, upregulated downstream antioxidant enzyme protein and mRNA levels, with no effect on Keap1 transcription^[1].
NBE5 (2.0 μM; 12 h) selectively induces Keap1 degradation in HCT116 cells, activates the Nrf2 antioxidant pathway, upregulates autophagy-related and HSP70 family proteins, and shows no significant effect on off-target proteins IKKβ and SLC30A1^[1].
The DC₅₀ values of NBE5 for Keap1 degradation in HCT116 and RKO cells were 0.82 μM and 1.72 μM, respectively; furthermore, at a concentration of 1 μM, the maximum degradation rate of Keap1 in BEAS-2B cells reached 92.5%^[1].

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

Cell Viability Assay^[1]

Cell Line:

HCT116 and RKO cell
Concentration:

2.0 μM
Incubation Time:

6-18 h
Result:

Mediated Keap1 degradation, increased nuclear Nrf2, upregulated downstream antioxidant enzyme protein.

In Vivo

NBE5 (5-20 mg/kg; p.o.; once daily; 10 days) dose-dependently relieves symptoms of DSS-induced acute colitis in male C57BL/6J mice, including reduced weight loss, increased colon length, lower Disease Activity Index scores, and decreased colonic Keap1 levels and inflammation^[1].

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

Animal Model:

C57BL/6J (male)^[1]
Dosage:

5 mg/kg; 20 mg/kg
Administration:

p.o.; once daily; 10 days
Result:

Reduced weight loss compared to DSS-only treated mice.
Increased colon length compared to DSS-only treated mice.
Lowered Disease Activity Index scores compared to DSS-only treated mice.
Significantly reduced Keap1 intensity in colon tissues compared to DSS-only treated mice.
Potently decreased colonic inflammation and reversed histopathological changes of the colon compared to DSS-only treated mice.

Chemical Information

분자량 780.13
화학식 C₅₀H₇₃N₃O₄
SMILES

O=C(NCC1C(C2)C=CC2C1)CCCCCCCCCCNC([C@](CC3)(CCC(C)(C4)C)[C@]4([H])[C@](C(C=C5[C@]6(CC[C@]7([H])[C@@]5(C=C(C(C7(C)C)=O)C#N)C)C)=O)([H])[C@@]36C)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. Li Z, et al. Discovery of novel Keap1-targeting hydrophobic tag (HyT) tethering degraders with potent Nrf2 activation activity. Eur J Med Chem. 2026;308:118700. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

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NBE5

All HSP Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

NBE5 Related Classifications

HY-181907 Related Classifications