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Cat. No.: HY-210438

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L013

L013 is an orally active and selective NRF2 PROTAC degrader. L013 directly binds to the NRF2 protein and promotes NRF2 ubiquitination and UPS-related degradation through a Cullin-dependent, CRBN-related process. L013 inhibits RNA polymerase II transcriptional elongation and downregulates NFE2L2 transcript levels. L013 selectively reduces NRF2 protein/mRNA and inhibits proliferation/colony formation in esophageal squamous cell carcinoma cells with NRF2 hyperactivation. L013 inhibits tumor growth in the KYSE150 esophageal squamous cell carcinoma xenograft mouse model and reduces intratumoral NRF2 and Ki-67 protein levels. L013 can be used for research on esophageal squamous cell carcinoma and lung squamous cell carcinoma.
(Pink: Keap1-Nrf2 ligand (HY-189822); Blue: Ligands for E3 Ligase ligand (HY-41547); Black: linker (HY-W574507)).

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Formule: C₄₂H₅₃ClN₁₂O₄
Masse moléculaire:825.40

Stockage:

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

L013 Chemical Structure

Stock

Quantité

Amount: USD 0.00

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

L013 is an orally active and selective NRF2 PROTAC degrader. L013 directly binds to the NRF2 protein and promotes NRF2 ubiquitination and UPS-related degradation through a Cullin-dependent, CRBN-related process. L013 inhibits RNA polymerase II transcriptional elongation and downregulates NFE2L2 transcript levels. L013 selectively reduces NRF2 protein/mRNA and inhibits proliferation/colony formation in esophageal squamous cell carcinoma cells with NRF2 hyperactivation. L013 inhibits tumor growth in the KYSE150 esophageal squamous cell carcinoma xenograft mouse model and reduces intratumoral NRF2 and Ki-67 protein levels. L013 can be used for research on esophageal squamous cell carcinoma and lung squamous cell carcinoma^[1]. (Pink: Keap1-Nrf2 ligand (HY-189822); Blue: Ligands for E3 Ligase ligand (HY-41547); Black: linker (HY-W574507)).

IC₅₀ & Target

^[1]

RNA Polymerase

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In Vitro

L013 binds recombinant full-length NRF2 (SPR K_d 62 μM, ITC K_d 23.4 μM, MST K_d 8.51 μM)^[1].
L013 decreases NFE2L2 mRNA and reduces pSer2 CTD occupancy/RNA Pol II CTD Ser2 phosphorylation in KYSE150 ESCC cells, consistent with impaired transcriptional elongation^[1].
L013 (1 nM-10 μM; 0-8 h) is a rapid and selective NRF2 degrader in KYSE150 and KYSE510 ESCC cells^[1].
L013 (500 nM-1 μM; 1-24 h) promotes NRF2 ubiquitination and enhances NRF2-CRBN binding in KYSE150 and KYSE510 ESCC cells, whereas UPS/proteasome inhibition only partially reverses L013-mediated NRF2 reduction^[1].
L013 inhibits the proliferation and colony formation of KYSE150 and KYSE510 ESCC cells with NRF2 hyperactivation in an NRF2-dependent manner^[1].
L013 (10 nM-1 μM; 48-72 h) inhibits organoid viability and degrades NRF2 in ESCC and LUSC organoids, with selective sensitivity in ESCC#3 and LUSC#1 with high NRF2 expression^[1].

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

Western Blot Analysis^[1]

Cell Line:

KYSE150 and KYSE510 ESCC cells
Concentration:

1 nM, 10 nM, 50 nM, 100 nM, 200 nM, 500 nM, 1 μM, 5 μM, 10 μM (dose-depend)
1 μM (time-depend)
Incubation Time:

8 h (dose-depend)
0, 1, 2, 4, 6, 8 h (time-depend)
Result:

Was a rapid and selective NRF2 degrader in KYSE150 and KYSE510 ESCC cells.

Parmacokinetics

Species	Dose	Route	CL_{_obs}	T_1/2	AUC_last	AUC_inf	MRT_{INF_obs}	T_max	C_max	F
Mice^[1]	1 mg/kg	i.v.	65.3 mL/min/kg	1.6 h	256.8 ng·h/mL	260.1 ng·h/mL	1.0 h	/	/	/
Mice^[1]	10 mg/kg	p.o.	/	/	9.9 ng·h/mL	/	/	2.1 h	8.7 ng/mL	0.4 %

In Vivo

L013 (10 mg/kg; oral gavage; every other day) suppresses tumor growth in esophageal squamous cell carcinoma KYSE150 xenografts in BALB/c nude mice, reducing tumor burden and decreasing NRF2 and Ki-67 levels^[1].

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

Animal Model:

BALB/c nude (male, 6-week-old, 1.5×10⁶ KYSE150 cells)^[1]
Dosage:

10 mg/kg
Administration:

oral gavage; every other day
Result:

Inhibited tumor growth in KYSE150 xenografts, with reduced tumor volume and tumor weight compared with vehicle control groups.
IHC showed reduced NRF2 and Ki-67 levels in L013-treated xenografts.

Related Protocols :

Chemical Information

Masse moléculaire 825.40
Formule C₄₂H₅₃ClN₁₂O₄
SMILES

CN(N=C1)C(CC2CC2)=C1C3=NC(N[C@H](CC4)CC[C@@H]4NCC5=CN(N=N5)CCCCCCCCNC6=CC=CC(C(N7C8CCC(NC8=O)=O)=O)=C6C7=O)=NC=C3Cl
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Yu X, et al. L013 promotes NRF2 degradation in NRFA-subtype esophageal squamous cell carcinoma. Cell reports. Medicine. 2026 Sep 11.

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Calculateur de dilution

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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.

Bioz

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MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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L013

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