2. PROTAC Immunology/Inflammation
  3. PROTACs AP-1
  4. FOSL1 degrader 1

FOSL1 degrader 1 is a FOSL1 PROTAC degrader with a DC50 of 2.3 μM. FOSL1 degrader 1 induces proteasomal degradation of FOSL1. FOSL1 degrader 1 eliminates cancer stem cells in head and neck squamous cell carcinoma. FOSL1 degrader 1 suppresses head and neck squamous cell carcinoma tumorigenesis. FOSL1 degrader 1 can be used for the research of head and neck squamous cell carcinoma.
(Pink: FOSL1 ligand (HY-12270); Blue: Cereblon ligand (HY-10984); Black: linker (HY-130200)).

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

FOSL1 degrader 1

FOSL1 degrader 1 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

FOSL1 degrader 1 Related Antibodies

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  • Biological Activity

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Description

FOSL1 degrader 1 is a FOSL1 PROTAC degrader with a DC50 of 2.3 μM. FOSL1 degrader 1 induces proteasomal degradation of FOSL1. FOSL1 degrader 1 eliminates cancer stem cells in head and neck squamous cell carcinoma. FOSL1 degrader 1 suppresses head and neck squamous cell carcinoma tumorigenesis. FOSL1 degrader 1 can be used for the research of head and neck squamous cell carcinoma[1]. (Pink: FOSL1 ligand (HY-12270); Blue: Cereblon ligand (HY-10984); Black: linker (HY-130200)).

IC50 & Target[1]

FOSL1

2.3 μM (DC50)

In Vitro

FOSL1 degrader 1 (compound 4) (range; 24 h) potently inhibits AP-1 luciferase activity in UM-SCC1-AP-1-luc cells with an IC50 of 26.4 μM[1].
FOSL1 degrader 1 (0.005-50 μM; 16 h) potently and selectively induces proteasome-dependent FOSL1 degradation in UM-SCC1 cells, with a DC50 of 2.3 μM, and reduces JUN expression as a downstream effect of FOSL1 degradation[1].
FOSL1 degrader 1 (15 μM; 16 h) significantly suppresses the expression of FOSL1 target genes (FOSL1, BMI1, SNAI2) in UM-SCC1 cells[1].
FOSL1 degrader 1 (48 h) has minimal toxicity to non-malignant TIGK cells, with an ED50 of 1087 μM[1].
FOSL1 degrader 1 (2 weeks) potently suppresses the self-renewal of ALDHhigh/CD44high UM-SCC1 cancer stem cells, with an ED50 of 0.18 μM[1].

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

FOSL1 degrader 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: UM-SCC1 cells
Concentration: 0.005 μM, 0.015 μM, 0.05 μM, 0.15 μM, 0.5 μM, 1.5 μM, 5 μM, 15 μM, 50 μM
Incubation Time: 16
Result: Led to down-regulation of FOSL.
The expression of JUN, the major JUN family member in HNSCC, was also dramatically decreased after a 16h treatment.

RT-PCR[1]

Cell Line: UM-SCC1 cells
Concentration: 15 μM
Incubation Time: 16 h
Result: The expression of FOSL1 target genes, including SNAI2, FOSL1 itself, and the functional HNSCC CSC marker, BMI1, was significantly inhibited.
In Vivo

FOSL1 degrader 1 (compound 4) (2-21 mg/kg; i.p.; every other day; 30 days) suppresses HNSCC tumor growth in a dose-dependent manner, while maintaining minimal impact on mouse body weight[1].
FOSL1 degrader 1 (compound 4) (21 mg/kg; i.p.; daily; 5 days) potently eliminates active FOSL1 and Bmi1+ CSCs in HNSCC tumors[1].
FOSL1 degrader 1 (compound 4) (21 mg/kg; i.p.; 3 doses on days 11, 13, 15 post-inoculation) significantly prolongs median overall survival by 43.8% in HNSCC orthotopic xenograft mice compared to vehicle control[1].

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

Animal Model: Bmi1CreER;RosatdTomato (6-week-old at study initiation; HNSCC induced via 4NQO)[1]
Dosage: 2 mg/kg; 7 mg/kg; 21 mg/kg
Administration: i.p.; every other day; 30 days
Result: Significantly inhibited HNSCC tumor growth relative to vehicle control across all three doses.
Showed dose-dependent suppression of Tomato+ (Bmi1+ CSC-derived) cells and Fosl1 protein expression in tumor tissues.
Caused no significant impact on mouse body weight over the 30-day period.
Animal Model: Bmi1CreER;RosatdTomato (tumor-bearing; HNSCC induced via 4NQO)[1]
Dosage: 21 mg/kg
Administration: i.p.; daily; 5 days
Result: Reduced Bmi1+ CSC numbers per mm2 of tumor tissue.
Achieved near-complete elimination of phospho-Fosl1 staining in tumor tissues, indicating effective degradation of active FOSL1.
Animal Model: NOD-scid-Gamma (NSG) (HNSCC orthotopic xenograft via UM-SCC1 cell inoculation)[1]
Dosage: 7 mg/kg; 21 mg/kg
Administration: i.p.; 3 doses on days 11, 13, 15 post-inoculation
Result: Extended median overall survival to 23 days in the 21 mg/kg group, representing a 43.8% increase relative to vehicle control.
Showed no significant difference in median survival (16 days) between 7 mg/kg group and vehicle control.
Molecular Weight

1124.19

Formula

C58H69N5O18
Appearance

Solid

Color

White to yellow

SMILES

O=C1CCC(N2C(C(C(NCCOCCOCCOCCOCCOCCOCCOCCNC(CCC3=C(OCC4=CC(ON=C5O)=C5C=C4)C=CC(C(C6=C(O)C=C(OC7CCCC7)C=C6)=O)=C3)=O)=CC=C8)=C8C2=O)=O)C(N1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (88.95 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.8895 mL 4.4476 mL 8.8953 mL
5 mM 0.1779 mL 0.8895 mL 1.7791 mL
View the Complete Stock Solution Preparation Table

* 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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 (stored under nitrogen). 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 0.8895 mL 4.4476 mL 8.8953 mL 22.2382 mL
5 mM 0.1779 mL 0.8895 mL 1.7791 mL 4.4476 mL
10 mM 0.0890 mL 0.4448 mL 0.8895 mL 2.2238 mL
15 mM 0.0593 mL 0.2965 mL 0.5930 mL 1.4825 mL
20 mM 0.0445 mL 0.2224 mL 0.4448 mL 1.1119 mL
25 mM 0.0356 mL 0.1779 mL 0.3558 mL 0.8895 mL
30 mM 0.0297 mL 0.1483 mL 0.2965 mL 0.7413 mL
40 mM 0.0222 mL 0.1112 mL 0.2224 mL 0.5560 mL
50 mM 0.0178 mL 0.0890 mL 0.1779 mL 0.4448 mL
60 mM 0.0148 mL 0.0741 mL 0.1483 mL 0.3706 mL
80 mM 0.0111 mL 0.0556 mL 0.1112 mL 0.2780 mL
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FOSL1 degrader 1 Related Classifications

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:

FOSL1 degrader 1PROTACsAP-1Activator Protein 1proteasomal degradationBMI1FOSL1head and neck squamous cell carcinomaUM-SCC1 cellscancer stem cellsJUNAP-1 luciferase activityUM-SCC1-AP-1-luc cellsSNAI2Inhibitorinhibitorinhibit

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