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Art. -Nr.: HY-170595

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PROTAC LZK degrader 1

PROTAC LZK degrader 1 is an LZK (MAP3K13) PROTAC degrader. PROTAC LZK degrader 1 binds LZK with a K_d of 35 nM and recruits VHL E3 ubiquitin ligase to induce ubiquitin-proteasome dependent degradation of LZK in MAP3K13-amplified HNSCC cells. PROTAC LZK degrader 1 eliminates both kinase-dependent c-MYC stabilization and kinase-independent GOF p53 accumulation downstream of LZK, suppresses colony formation of LZK-amplified head and neck squamous cell carcinoma (HNSCC) cells. PROTAC LZK degrader 1 can be used for research on LZK-driven HNSCC.
(Pink: MAP3K13/LZK ligand (HY-170596); Blue: VHL ligand (HY-112078); Black: linker (HY-W019543)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2763268-64-8
Formel: C₅₁H₆₄F₂N₁₀O₅S
Molecular Weight:967.18

Speicherung:

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

Data Sheet (276 KB)

PROTAC LZK degrader 1 Chemical Structure

CAS. Nr.: 2763268-64-8

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protokoll (2)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PROTAC LZK degrader 1 is an LZK (MAP3K13) PROTAC degrader. PROTAC LZK degrader 1 binds LZK with a K_d of 35 nM and recruits VHL E3 ubiquitin ligase to induce ubiquitin-proteasome dependent degradation of LZK in MAP3K13-amplified HNSCC cells. PROTAC LZK degrader 1 eliminates both kinase-dependent c-MYC stabilization and kinase-independent GOF p53 accumulation downstream of LZK, suppresses colony formation of LZK-amplified head and neck squamous cell carcinoma (HNSCC) cells. PROTAC LZK degrader 1 can be used for research on LZK-driven HNSCC^[1]. (Pink: MAP3K13/LZK ligand (HY-170596); Blue: VHL ligand (HY-112078); Black: linker (HY-W019543)).

IC₅₀ & Target

^[1]

VHL	MAP3K13/LZK 35 nM (Kd)

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In Vitro

PROTAC LZK degrader 1 (compound 21A) (0.1-10 μM; 24-48 h) binds LZK with a K_d of 35 nM and induces concentration-dependent LZK degradation in Doxycycline (DOX) (HY-N0565)-inducible LZK-overexpressing CAL33 HNSCC cells^[1].
PROTAC LZK degrader 1 (1 μM; 0-48 h) achieves sustained LZK protein depletion over time, accompanied by reduced JNK phosphorylation^[1].
PROTAC LZK degrader 1 (1 μM; 24 h) exerts LZK degradation activity dependent on both proteasome and NEDD8 neddylation pathways, and fully abolishes LZK-degrading activity when co-treated with proteasome inhibitor MG-132 (HY-13259) and NEDD8-activating enzyme inhibitor MLN4924 (HY-70062)^[1].
PROTAC LZK degrader 1 (1 μM; 48 h) downregulates c-MYC and GOF p53 expression in CAL33 cells harboring MAP3K13 amplification^[1].
PROTAC LZK degrader 1 (1-2.5 μM) suppresses colony formation of LZK-amplified CAL33, BICR56, Detroit562 HNSCC cell lines, with minimal toxicity to LZK-wildtype BICR22 and BEAS-2B cells at 1 μM; higher concentration (2.5 μM) induces off-target cytotoxicity in control cells^[1].
PROTAC LZK degrader 1 exerts anti-clonogenic activity via LZK degradation, whereas its cis-epimer only binds LZK without inducing LZK degradation or anti-tumor colony-suppressive function^[1].
PROTAC LZK degrader 1 (100 nM) displays high selectivity toward LZK/DLK across a kinome panel covering over 450 kinases and exhibits negligible off-target kinase inhibitory effects^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Western Blot Analysis^[1]

View Protocol

Cell Line:

Dox-inducible CAL33 (LZK WT) HNSCC cells
Concentration:

0.1, 0.25, 0.5, 1, 2.5, 10 μM
Incubation Time:

24 h
Result:

Showed a K_d of 35 nM.
Dose-dependently degraded LZK and reduced phospho-JNK level.

Western Blot Analysis^[1]

View Protocol

Cell Line:

Dox-inducible CAL33 (LZK WT) HNSCC cells
Concentration:

1 μM
Incubation Time:

0, 16, 24, 48 h
Result:

Induced time-dependent sustained LZK degradation and suppresses JNK phosphorylation.

Western Blot Analysis^[1]

View Protocol

Cell Line:

Dox-inducible CAL33 (LZK WT) HNSCC cells
Concentration:

1 μM
Incubation Time:

24 h
Result:

Losed LZK-degrading capacity upon co-treatment with proteasome inhibitor or NEDD8 inhibitor.

Western Blot Analysis^[1]

View Protocol

Cell Line:

CAL33 HNSCC cells
Concentration:

1 μM, 2.5 Μm
Incubation Time:

48 h
Result:

Downregulates c-MYC and GOF p53 protein expression.

In Vivo

PROTAC LZK degrader 1 (compound 21A) (50 mg/kg; i.p.; single dose) exhibits low cell permeability and uneven tissue distribution, with measurable drug concentrations detected in plasma, liver, kidney, lung and brain across sampling time points ranging from 0.083 h to 48 h in female NSG mice^[1].

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

Animal Model:

In vivo pharmacokinetic study in female NSG mice (17-25 g)^[1]
Dosage:

50 mg/kg
Administration:

i.p.; single dose
Result:

Showed limited cell permeability, uneven distribution in plasma, liver, kidney, lung and brain tissues.

Chemical Information

CAS. Nr. 2763268-64-8
Molecular Weight 967.18
Formel C₅₁H₆₄F₂N₁₀O₅S
SMILES

FC(CC1)(F)CN1C2=CC(C3CCN(C(CCCCCCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)C[C@@H](O)C4)=O)=O)=O)CC3)=CC(NC7=CC(C#N)=CC=N7)=N2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Protokoll

All Cell Biology

Soft Agar Colony Formation Assay
Soft agar colony formation assay measures anchorage-independent growth, in which transformed or tumorigenic cells proliferate as colonies in a semisolid agar matrix while many non-transformed adherent cells fail to proliferate without attachment; classic studies showed that growth in semisolid medium correlates with tumorigenicity in nude mice, and later protocol papers describe the method as a stringent in vitro assay for malignant transformation. The readout is the number, size, morphology, or signal intensity of colonies formed within agar after incubation; published formats include manual colony counting after staining, 96-well or 384-well quantitative formats, DNA-binding dye detection, MTT/tetrazolium-based detection, digital image analysis, and PCR-based marker detection from soft agar cultures.
Colony Formation (Clonogenic) Assay
The clonogenic (colony formation) assay measures the ability of a single cell to retain reproductive viability and form a macroscopic colony, typically defined as a cluster derived from one progenitor cell after a defined growth period. This assay is widely used to evaluate cell survival after exposure to ionizing radiation or cytotoxic treatments and is considered a standard method in radiation biology for generating dose-response relationships of reproductive cell death. Colony formation reflects long-term proliferative capacity rather than short-term metabolic activity, and survival is quantified by comparing treated versus untreated conditions based on colony number and derived survival fractions.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Funk AL, et al. Targeting GOF p53 and c-MYC through LZK Inhibition or Degradation Suppresses Head and Neck Tumor Growth. bioRxiv [Preprint]. 2024 Nov 20:2024.11.19.623840. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protokoll
Reinheit & Dokumentation
Verweise

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PROTAC LZK degrader 1

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