2. PROTAC NF-κB Vitamin D Related/Nuclear Receptor Apoptosis
  3. PROTACs IKK Nuclear Hormone Receptor 4A/NR4A Caspase Necroptosis
  4. PROTAC IKKβ/NR4A1 degrader-1

PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand (HY-13067); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-79577).

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

PROTAC IKKβ/NR4A1 degrader-1

PROTAC IKKβ/NR4A1 degrader-1 Chemical Structure

CAS No. : 2826215-20-5

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PROTAC IKKβ/NR4A1 degrader-1 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All IKK Isoform Specific Products:

View All Isoforms
IKK-α IKK-β IKK IKKε TBK1

View All Nuclear Hormone Receptor 4A/NR4A Isoform Specific Products:

View All Isoforms
Nur77/NR4A1 Nurr1/NR4A2

View All Caspase Isoform Specific Products:

View All Isoforms
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC IKKβ/NR4A1 degrader-1 is a highly efficient and effective dual-PROTAC degrader targeting IKKβ and NR4A1. PROTAC IKKβ/NR4A1 degrader-1 can increase the levels of caspase 3 and cleaved caspase 3 proteins, while the necroptosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis. PROTAC IKKβ/NR4A1 degrader-1 can be used for the study of Acute myeloid leukemia (AML). Red: IKKβ/NR4A1 ligand (HY-13067); Blue: E3 ligase CRBN ligand (HY-14658); Black: Linker (HY-79577)[1].

IC50 & Target

IKKβ

 

Caspase-3

 

Nur77/NR4A1

 

In Vitro

PROTAC IKKβ/NR4A1 degrader-1 (Compound A9) (48 h) shows strong AML cell killing activity in Monomac-6 (IC50 = 0.32 µM), NB-4 (IC50 = 0.23 µM), U-937 (IC50 = 0.36 µM), Molm-13 (IC50 = 0.23 µM), and HL-60 cells (IC50 = 0.54 µM)[1].
PROTAC IKKβ/NR4A1 degrader-1 (0.5-1 µM) dose-dependently increases the levels of caspase 3 and cleaved caspase 3 proteins in NB-4, Monomac-6, and Molm-13 cells, while the necrosis marker RIP kinase remained unchanged, indicating that it can induce apoptosis[1].
PROTAC IKKβ/NR4A1 degrader-1 (0-1 µM) results in a dose-dependent decrease in IKKβ and NR4A1 protein levels in NB-4, Monomac-6, and Molm-13 cells[1].
PROTAC IKKβ/NR4A1 degrader-1 (0.5 μM, 16 h)-mediated degradation of IKKβ and NR4A1 can be reversed by the proteasome inhibitor MG132 (HY-13259), the E3 ligase competitor Pomalidomide (HY-10984), or the neddylation inhibitor Pevonedistat (MLN4924) (HY-70062) in A375 melanoma cells, while PROTAC IKKβ/NR4A1 degrader-1 NC has no degradation activity[1].
PROTAC IKKβ/NR4A1 degrader-1 (10 μM, 3 h) promotes the formation of a ternary complex in HEK293T cells, evidenced by co-immunoprecipitation of IKKβ with exogenous Flag-CRBN and of CRBN with Flag-NR4A1[1].
PROTAC IKKβ/NR4A1 degrader-1 (0.25-1 μM, 48 h) exhibits reduced efficacy in IKKβ or NR4A1 knockout cells[1].
PROTAC IKKβ/NR4A1 degrader-1 (0.125-0.25 μM, 72 h) results in overlap of the NF-κB signaling pathway in Molm-13 and Monomac-6 cells with the enrichment pathway in AML cells with high NR4A1 expression[1].

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

PROTAC IKKβ/NR4A1 degrader-1 Related Antibodies
In Vivo

PROTAC IKKβ/NR4A1 degrader-1 (Compound A9) (2-4 mg/kg, i.p., once every 3 days) effectively attenuates AML disease progression in mouse models of AML[1].

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

Animal Model: C57BL6/J mice were irradiated with 6.5 Gy X-ray and 24 h later 2x104 GFP-tagged KMT2A::MLLT3 AML cells/mouse were injected intravenously[1].
Dosage: The initial four-dose regimen is 4 mg/kg, with all subsequent doses decreasing to 2 mg/kg
Administration: I.p., once every 3 days
Result: AML cell growth slowed significantly.
Showed a trend of prolonged survival, but compared with the control group, it did not reach statistical significance.
No significant difference in the neutrophil count in their blood.
Molecular Weight

805.01

Formula

C48H60N4O7
CAS No.
SMILES

[H][C@@]12C[C@](C(NCCCCCCNC3=CC=CC4=C3C(N(C4=O)C5CCC(NC5=O)=O)=O)=O)(CC[C@@]1(CC[C@@]6(C7=CC=C8C([C@@]7(CC[C@]62C)C)=CC(C(O)=C8C)=O)C)C)C
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
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PROTAC IKKβ/NR4A1 degrader-1 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

PROTAC IKKβ/NR4A1 degrader-12826215-20-5PROTACsIKKNuclear Hormone Receptor 4A/NR4ACaspaseNecroptosisIκB kinaseI kappa B kinase Nuclear Hormone Receptor 4ANerve Growth Factor IB-like ReceptorIKKβNR4A1Acute Myeloid LeukemiaAMLKMT2A::MLLT3MLL-AF9Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PROTAC IKKβ/NR4A1 degrader-1
Cat. No.:
HY-179112
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.