2. PROTAC MAPK/ERK Pathway Epigenetics Cell Cycle/DNA Damage
  3. PROTACs Mixed Lineage Kinase PARP
  4. PROTAC MLKL Degrader-3

PROTAC MLKL Degrader-3 is a MLKL PROTAC degrader with DC50 values of 248.9 nM (Hepa1-6) and 271.3 nM (HepG2), respectively. PROTAC MLKL Degrader-3 induces proteasome- and cereblon-dependent MLKL degradation via ubiquitination. PROTAC MLKL Degrader-3 reduces intratumoral MLKL levels and inhibits tumor growth in mice. PROTAC MLKL Degrader-3 can be used in the research of hepatocellular carcinoma.
(Pink: Mixed Lineage Kinase ligand (HY-182344); Blue: Cereblon ligand (HY-14658); Black: linker).

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

PROTAC MLKL Degrader-3

PROTAC MLKL Degrader-3 Chemical Structure

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 MLKL Degrader-3 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 PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC MLKL Degrader-3 is a MLKL PROTAC degrader with DC50 values of 248.9 nM (Hepa1-6) and 271.3 nM (HepG2), respectively. PROTAC MLKL Degrader-3 induces proteasome- and cereblon-dependent MLKL degradation via ubiquitination. PROTAC MLKL Degrader-3 reduces intratumoral MLKL levels and inhibits tumor growth in mice. PROTAC MLKL Degrader-3 can be used in the research of hepatocellular carcinoma[1]. (Pink: Mixed Lineage Kinase ligand (HY-182344); Blue: Cereblon ligand (HY-14658); Black: linker).

In Vitro

PROTAC MLKL Degrader-3 (compound C116) (1 nM-20000 nM, 0.5 μM-1 μM; 2 h-96 h) potently and rapidly degrades MLKL in murine Hepa1-6 and human HepG2 HCC cells, with DC50 values of 248.9 nM and 271.3 nM respectively, and maximal degradation exceeding 90% for both cell lines[1].
PROTAC MLKL Degrader-3 (C116) (1 μM; 4 h) selectively degrades MLKL in murine Hepa1-6 HCC cells without significantly affecting other proteins in the proteome[1].
PROTAC MLKL Degrader-3 (C116) (6 h) mediates MLKL degradation in a proteasome- and CRBN-dependent manner via enhancing MLKL ubiquitination in murine Hepa1-6 and human HEK293T cells[1].
PROTAC MLKL Degrader-3 (C116) (1 μM-10 μM; 24 h pretreatment, followed by 20 h PA stimulation) potentiates PA-induced parthanatos and subsequent cytotoxicity in murine Hepa1-6 and human HepG2 HCC cells, with this effect dependent on parthanatos signaling[1].
PROTAC MLKL Degrader-3 (C116) degrades MLKL across diverse murine and human cancer cell lines, including colorectal, triple-negative breast, and lung cancer cells[1].

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

PROTAC MLKL Degrader-3 Related Antibodies

Western Blot Analysis[1]

Cell Line: murine Hepa1-6 HCC cells, human HepG2 HCC cells
Concentration: 1 μM, 10 μM (24 h); 1 nM-20000 nM (24 h); 0.5 μM, 1 μM (2 h, 4 h, 6 h, 12 h, 24 h, 48 h, 72 h, 96 h)
Incubation Time: 24 h (1 μM, 10 μM, 1 nM-20000 nM); 2 h-96 h (0.5 μM, 1 μM)
Result: Reduced MLKL levels to 9.6% in Hepa1-6 cells and 18.7% in HepG2 cells at 1 μM for 24 h.
Reduced MLKL levels to 2.5% in Hepa1-6 cells and 11.7% in HepG2 cells at 10 μM for 24 h.
Induced concentration-dependent degradation with DC50 values of 248.9 nM in Hepa1-6 cells and 271.3 nM in HepG2 cells, and maximal percent degradation (Dₘₐₓ) of 99.3% in Hepa1-6 cells and 91.2% in HepG2 cells.
Induced over 90% MLKL reduction as early as 2 h at 1 μM, with robust degradation maintained for 48 h and recovery observed by 96 h.
Parmacokinetics
Species Dose Route T1/2 AUC
Mice[1] 10 mg/kg i.p. 5.5 h 1519 ng·h/mL
In Vivo

PROTAC MLKL Degrader-3 (compound C116) (10 mg/kg; i.p.; daily) significantly reduces intratumoral MLKL levels and inhibits orthotopic HCC tumor growth in male C57BL/6 mice, with good tolerability[1].

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

Animal Model: C57BL/6 (male, 5 weeks old, orthotopic liver tumor model via surgical implantation of Hepa1−6-luc cells)[1]
Dosage: 10 mg/kg
Administration: i.p.; daily; study duration
Result: Significantly inhibited orthotopic HCC tumor growth, as measured by reduced total bioluminescent flux.
Significantly reduced intratumoral MLKL levels in treated mice.
Showed good tolerability, with no induced weight loss in treated mice.
Molecular Weight

1026.02

Formula

C49H47F4N11O8S
SMILES

NC1=C(C2=C(C=N1)C3=CN(N=C3)C4CCN(CC4)C(C5CCN(C6=CC=C(C(N(C7C(NC(CC7)=O)=O)C8=O)=O)C8=C6)CC5)=O)C(C9=CC(OC(C%10=CC=C(C=C%10)F)C)=C(C=C9F)NS(=O)(C(F)F)=O)=NN2C
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 MLKL Degrader-3 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 MLKL Degrader-3PROTAC MLKL Degrader3PROTAC MLKL Degrader 3PROTACsMixed Lineage KinasePARPMLKspoly ADP ribose polymeraseproteasomecereblonpoly(ADP-ribose) polymerHepG2parthanatosmixed lineage kinase domain-like pseudokinasehepatocellular carcinomaHepa1-6MLKLapoptosis-inducing factorInhibitorinhibitorinhibit

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 MLKL Degrader-3
Cat. No.:
HY-182343
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.