Art. -Nr.: HY-179717

WZS0347

Name: WZS0347
Brand: MedChemExpress
SKU: HY-179717
Price: 845.00 USD
Availability: InStock
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WZS0347 is a MITF PROTAC degrader. WZS0347 effectively reduces MITF protein levels in various melanoma cell lines. WZS0347 induces MITF degradation via the cereblon-dependent ubiquitin-proteasome pathway, downregulates the expression of downstream target genes of MITF, and inhibits the colony formation and migration abilities of cancer cells. WZS0347 can be used in melanoma-related research.
(Pink: Microphthalmia Associated Transcription Factor (MITF) ligand (HY-179718); Blue: Cereblon ligand (HY-131717); Black: linker (HY-22391)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.06%
Formel: C₄₁H₄₂N₈O₉
Molecular Weight:790.82

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

WZS0347 Chemical Structure

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

WZS0347 is a MITF PROTAC degrader. WZS0347 effectively reduces MITF protein levels in various melanoma cell lines. WZS0347 induces MITF degradation via the cereblon-dependent ubiquitin-proteasome pathway, downregulates the expression of downstream target genes of MITF, and inhibits the colony formation and migration abilities of cancer cells. WZS0347 can be used in melanoma-related research^[1]. (Pink: Microphthalmia Associated Transcription Factor (MITF) ligand (HY-179718); Blue: Cereblon ligand (HY-131717); Black: linker (HY-22391)).

IC₅₀ & Target^[1]

Cereblon

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

WZS0347 (0.1-1 μM; 48 h) potently induces MITF degradation in B16F10 mouse melanoma cells^[1].
WZS0347 (10 nM-10000 nM; 24 h) induces concentration-dependent degradation of MITF in B16F10 mouse melanoma cells^[1].
WZS0347 (1 μM; 1-24 h) induces time-dependent degradation of MITF in B16F10 mouse melanoma cells^[1].
WZS0347 (1 nM-1000 nM; 12 h) induces MITF degradation in human melanoma A375 cells in a concentration-dependent manner^[1].
WZS0347 (1 nM-1000 nM; 24 h) induces concentration-dependent degradation of MITF in GAK human melanoma cells^[1].
WZS0347 (1 μM; 24 h) induces MITF degradation in B16F10 mouse melanoma cells through binding to MITF, as pretreatment with the MITF ligand TT-012 (HY-156483) reverses this degradation effect^[1].
WZS0347 (1 μM; 24 h)-induced MITF degradation in B16F10 mouse melanoma cells is dependent on CRBN, as pretreatment with the CRBN ligand Lenalidomide (HY-A0003) reverses this degradation process^[1].
WZS0347 (1 μM; 24 h) induces proteasome-dependent degradation of MITF in B16F10 mouse melanoma cells, as pretreatment with a proteasome inhibitor abrogates this degradation^[1].
WZS0347 (1 μM; 0-24 h) shortens the half-life of MITF protein in B16F10 mouse melanoma cells, reducing the basal half-life from 12 h^[1].
WZS0347 (0.3 μM) downregulates the mRNA levels of MITF and its downstream target genes TYR and Trpm1 in B16F10 mouse melanoma cells^[1].
WZS0347 (100 nM-1000 nM; 5 days) inhibits colony formation of B16F10 mouse melanoma cells in a dose-dependent manner^[1].
WZS0347 (0.5-1 μM; 24 h) inhibits the migration of B16F10 mouse melanoma cells and A375 human melanoma cells in a dose-dependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:

B16F10 mouse melanoma cells
Concentration:

0.1 μM, 1 μM
Incubation Time:

48 h
Result:

Induced 78% MITF degradation at 0.1 μM after 48 h.
Induced 80% MITF degradation at 1 μM after 48 h.

Western Blot Analysis^[1]

Cell Line:

B16F10 mouse melanoma cells
Concentration:

10 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM, 10000 nM
Incubation Time:

24 h
Result:

Caused concentration-dependent reduction of MITF protein levels over 24 h.

Western Blot Analysis^[1]

Cell Line:

B16F10 mouse melanoma cells
Concentration:

1 μM
Incubation Time:

1 h, 2 h, 4 h, 12 h, 24 h
Result:

Caused significant MITF depletion starting at 12 h of treatment.

Western Blot Analysis^[1]

Cell Line:

A375 human melanoma cells
Concentration:

1 nM, 3 nM, 7 nM, 15 nM, 30 nM, 62 nM, 125 nM, 250 nM, 500 nM, 1000 nM
Incubation Time:

12 h
Result:

Caused concentration-dependent reduction of MITF protein levels over 12 h.

Western Blot Analysis^[1]

Cell Line:

GAK human melanoma cells
Concentration:

1 nM, 3 nM, 7 nM, 15 nM, 30 nM, 62 nM, 125 nM, 250 nM, 500 nM, 1000 nM
Incubation Time:

24 h
Result:

Caused concentration-dependent reduction of MITF protein levels over 24 h.

Western Blot Analysis^[1]

Cell Line:

B16F10 mouse melanoma cells
Concentration:

1 μM TT-012 (HY-156483) (pre-incubation), 1 μM this compound
Incubation Time:

2 h (TT-012 pre-incubation), 24 h (this compound)
Result:

Reversed MITF degradation when cells were pretreated with TT-012.

Western Blot Analysis^[1]

Cell Line:

B16F10 mouse melanoma cells
Concentration:

1 μM Lenalidomide (HY-A0003) (pre-incubation), 1 μM this compound
Incubation Time:

2 h (lenalidomide pre-incubation), 24 h (this compound)
Result:

Reversed MITF degradation when cells were pretreated with lenalidomide.

Western Blot Analysis^[1]

Cell Line:

B16F10 mouse melanoma cells
Concentration:

1 μM
Incubation Time:

2 h (proteasome inhibitor pre-incubation), 24 h (this compound)
Result:

Abolished MITF degradation when cells were pretreated with proteasome inhibitor.

Western Blot Analysis^[1]

Cell Line:

B16F10 mouse melanoma cells
Concentration:

1 μM Cycloheximide (HY-12320) + 1 μM this compound
Incubation Time:

0 h, 1 h, 2 h, 4 h, 12 h, 24 h
Result:

Significantly shortened MITF's basal half-life from 12 h.

Cell Proliferation Assay^[1]

Cell Line:

B16F10 mouse melanoma cells
Concentration:

100 nM, 300 nM, 1000 nM
Incubation Time:

5 days
Result:

Caused dose-dependent suppression of colony formation over 5 days.

Cell Migration Assay ^[1]

Cell Line:

B16F10 mouse melanoma cells, A375 human melanoma cells
Concentration:

0.5 μM, 1 μM
Incubation Time:

24 h
Result:

Suppressed cell migration in both B16F10 and A375 cells in a dose-dependent manner over 24 h.

Chemical Information

Appearance Solid
Molecular Weight 790.82
Formel C₄₁H₄₂N₈O₉
Color White to yellow
SMILES

O=C(NCCCCCCCNC1=CC(NC(/C=C/C2=CC=CO2)=O)=NC(NC(/C=C/C3=CC=CO3)=O)=C1)CNC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (126.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2645 mL

6.3226 mL

12.6451 mL

5 mM

0.2529 mL

1.2645 mL

2.5290 mL

10 mM

0.1265 mL

0.6323 mL

1.2645 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.16 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.16 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Shen W, et al. Discovery of a first-in-class degrader for microphthalmia-associated transcription factor (MITF). European journal of medicinal chemistry. 2026 Jan 15;302(Pt 3):118367. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2645 mL	6.3226 mL	12.6451 mL	31.6128 mL
	5 mM	0.2529 mL	1.2645 mL	2.5290 mL	6.3226 mL
	10 mM	0.1265 mL	0.6323 mL	1.2645 mL	3.1613 mL
	15 mM	0.0843 mL	0.4215 mL	0.8430 mL	2.1075 mL
	20 mM	0.0632 mL	0.3161 mL	0.6323 mL	1.5806 mL
	25 mM	0.0506 mL	0.2529 mL	0.5058 mL	1.2645 mL
	30 mM	0.0422 mL	0.2108 mL	0.4215 mL	1.0538 mL
	40 mM	0.0316 mL	0.1581 mL	0.3161 mL	0.7903 mL
	50 mM	0.0253 mL	0.1265 mL	0.2529 mL	0.6323 mL
	60 mM	0.0211 mL	0.1054 mL	0.2108 mL	0.5269 mL
	80 mM	0.0158 mL	0.0790 mL	0.1581 mL	0.3952 mL
	100 mM	0.0126 mL	0.0632 mL	0.1265 mL	0.3161 mL

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WZS0347

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

WZS0347 Related Classifications

HY-179717 Related Classifications

Bioz