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Cat. No.: HY-189701

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PROTAC FGFR4 degrader-1

PROTAC FGFR4 degrader-1 is a selective FGFR4 PROTAC degrader with DC₅₀ = 0.84 μM. PROTAC FGFR4 degrader-1 is obtained by coupling the FGFR4 covalent inhibitor H3B-6527 (HY-100491) with a VHL E3 ubiquitin ligase ligand via an alkyl linker, and achieves FGFR4 degradation through the ubiquitin-proteasome system. PROTAC FGFR4 degrader-1 can induce apoptosis in hepatocellular carcinoma cells and inhibit FGFR4-driven proliferation of hepatocellular carcinoma cells. PROTAC FGFR4 degrader-1 can downregulate RNA polymerase and aminoacyl-tRNA biosynthesis while upregulating DNA replication. PROTAC FGFR4 degrader-1 can be used for research on hepatocellular carcinoma.
(Pink: FGFR4 ligand (HY-189702); Blue: VHL ligand (HY-173435); Black: linker).

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

Formula: C₅₂H₆₂Cl₂N₁₂O₈S
Molecular Weight:1086.10

Storage:

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

PROTAC FGFR4 degrader-1 Chemical Structure

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Amount: USD 0.00

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC FGFR4 degrader-1 is a selective FGFR4 PROTAC degrader with DC₅₀ = 0.84 μM. PROTAC FGFR4 degrader-1 is obtained by coupling the FGFR4 covalent inhibitor H3B-6527 (HY-100491) with a VHL E3 ubiquitin ligase ligand via an alkyl linker, and achieves FGFR4 degradation through the ubiquitin-proteasome system. PROTAC FGFR4 degrader-1 can induce apoptosis in hepatocellular carcinoma cells and inhibit FGFR4-driven proliferation of hepatocellular carcinoma cells. PROTAC FGFR4 degrader-1 can downregulate RNA polymerase and aminoacyl-tRNA biosynthesis while upregulating DNA replication. PROTAC FGFR4 degrader-1 can be used for research on hepatocellular carcinoma^[1]. (Pink: FGFR4 ligand (HY-189702); Blue: VHL ligand (HY-173435); Black: linker).

IC₅₀ & Target

^[1]

FGFR4

0.84 μM (DC₅₀)

p38 MAPK

MEK

All PROTACs Isoforms :

All p38 MAPK Isoforms :

All MEK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Huh-7	DC₅₀	3.12 μM	FGFR4 degradation in human Huh7 hepatocellular carcinoma cells assessed by Western blot after 48 hrs incubation. FGFR4 degradation in human Huh7 hepatocellular carcinoma cells assessed by Western blot after 48 hrs incubation.	42743606
Huh-7	IC50	42.60 μM	Antiproliferative activity against human Huh-7 hepatocellular carcinoma cells assessed as viability reduction incubated 48 hrs by CCK-8 assay. Antiproliferative activity against human Huh-7 hepatocellular carcinoma cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.	42743606
BaF3	IC50	0.066 μM	Antiproliferative activity against Ba/F3-FGFR4 cells assessed as viability reduction incubated 48 hrs by CCK-8 assay. Antiproliferative activity against Ba/F3-FGFR4 cells assessed as viability reduction incubated 48 hrs by CCK-8 assay.	42743606

In Vitro

OthersAnti-cancerApoptosis

Others

PROTAC FGFR4 degrader-1 (compound V1) inhibits FGFR4 kinase activity in a cell-free FGFR4 kinase assay with an IC₅₀ of 26.4 nM; moreover, it covalently binds recombinant FGFR4 as a 1:1 adduct^[1].
PROTAC FGFR4 degrader-1 (0.07-20 μM; 48 h) degrades FGFR4 in JHH-7 cells with a DC₅₀ of 0.84 μM and a D_max of 80%; in Huh7 cells, the DC₅₀ is 3.12 μM and the D_max is 74%^[1].

Anti-cancer

PROTAC FGFR4 degrader-1 (1.25 μM; 0.5-72 h) persistently degrades FGFR4 in JHH-7 cells^[1].
PROTAC FGFR4 degrader-1 (0.3-1.25 μM; 6 h) selectively degrades FGFR4 rather than FGFR3 in MCF-7 cells^[1].
PROTAC FGFR4 degrader-1 (3 μM; 24 h) reduced FGFR4 immunofluorescence in JHH-7 cells^[1].
PROTAC FGFR4 degrader-1 (1.25-3 μM; washout 24-48 h) maintained FGFR4 degradation in JHH-7 cells within 48 h after washout^[1].
PROTAC FGFR4 degrader-1 (2.5 μM; 1 h)-induced FGFR4 degradation in JHH-7 cells can be rescued by excess H3B-6527 or VHL ligand, supporting ternary complex dependence; it can also be blocked by proteasome and neddylation inhibitors^[1].
PROTAC FGFR4 degrader-1 inhibits FGFR4-driven proliferation of JHH-7, Huh7, and Ba/F3-FGFR4 cells with IC₅₀ values of 16.31, 42.60, and 0.066 μM, respectively, whereas its IC₅₀ against L02 cells is >100 μM^[1].
PROTAC FGFR4 degrader-1 (2.5 μM) inhibits FGFR4 autophosphorylation and downstream MAPK/MEK phosphorylation in JHH-7 cells^[1].

Anti-cancer

Apoptosis

PROTAC FGFR4 degrader-1 (12.5-25.0 μM; 48 h) induces concentration-dependent apoptosis in JHH-7 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

Huh7 and JHH-7 HCC cells
Concentration:

0.5, 5 μM (degradation)
0.07, 0.15, 0.3, 0.6, 1.3, 2.5, 5, 10, 20 μM (JHH-7 HCC cells)
0.3, 0.6, 1.3, 2.5, 5, 10, 20 μM (Huh7 cells)
Incubation Time:

48 h
Result:

Degraded FGFR4 in JHH-7 cells with DC₅₀ 0.84 μM and D_max 80%, and in Huh7 cells with DC₅₀ 3.12 μM and D_max 74%.

Western Blot Analysis^[1]

Cell Line:

JHH-7 cells
Concentration:

1.25 μM
Incubation Time:

0.5, 1, 2, 4, 8, 12, 24, 48, 72 h
Result:

Continuously degraded FGFR4 in JHH-7 cells.

Western Blot Analysis^[1]

Cell Line:

MCF-7 breast cancer cells
Concentration:

0.3, 1.25 μM
Incubation Time:

6 h
Result:

Selectively degraded FGFR4 while largely sparing FGFR3 in MCF-7 cells.

Immunofluorescence^[1]

Cell Line:

JHH-7 cells
Concentration:

3 μM
Incubation Time:

24 h
Result:

Showed that fluorescence intensity of FGFR4 both on the membrane and in the cytoplasm in JHH-7 cells was dramatically decreased.

Western Blot Analysis^[1]

Cell Line:

JHH-7 cells
Concentration:

1.25, 3 μM
Incubation Time:

24 h; washout 24 and 48 h
Result:

Maintained FGFR4 degradation efficacy for 48 h post-washout in JHH-7 cells at 1.25 and 3 μM.

Western Blot Analysis^[1]

Cell Line:

JHH-7 cells
Concentration:

2.5 μM
10 μM (H3B-6527); 10 μM (VHL ligand) prior exposure
Incubation Time:

1 h
2 h (prior exposure)
Result:

Prior exposure to saturating concentrations of either H3B-6527 or VHL ligand rescued FGFR4 degradation.

Western Blot Analysis^[1]

Cell Line:

JHH-7 cells
Concentration:

1.25 μM
1 μM (MG-132 (HY-13259)); 1 μM (MLN-4924 (HY-70062)) prior exposure
Incubation Time:

1 h
2 h (prior exposure)
Result:

FGFR4 degradation induced by compound V1 was completely blocked by both MG-132 and MLN-4924.

Apoptosis Analysis^[1]

Cell Line:

JHH-7 cells
Concentration:

12.5 and 25.0 μM
Incubation Time:

48 h
Result:

Total apoptosis rates reached 38.56% and 47.31%, respectively.

Related Protocols :

Parmacokinetics

Species	Dose	Route	C_max	T_1/2	T_max	MRT_0-inf	MRT_0-t	AUC_0-t	AUC_0-inf	CL	V_dss
Mice^[1]	1 mg/kg	i.v.	17,200 ng/mL	1.82 h	0.083 h	0.221 h	0.193 h	1570 ng·h/mL	1570 ng·h/mL	10.6 mL/min/kg	0.141 L/kg

Chemical Information

Molecular Weight 1086.10
Formula C₅₂H₆₂Cl₂N₁₂O₈S
SMILES

O=C([C@H]1N(C([C@H](NC(CN2CCN(C3=CC=C(NC4=NC=NC(N(C)C(NC5=C(Cl)C(OC)=CC(OC)=C5Cl)=O)=C4)C(NC(C=C)=O)=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)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

Handling Instructions (2659 KB)

References

[1]. Li Y, et al. Design, synthesis, and biological evaluation of the first fibroblast growth factor receptor 4 PROTAC degrader. Bioorganic chemistry. 2026 Sep 09;182:110495.

Calculators

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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

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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PROTAC FGFR4 degrader-1

All PROTACs Isoforms

All p38 MAPK Isoforms

All MEK Isoforms

Biological Activity

Description

IC50 & Target

Cellular Effect

In Vitro

Parmacokinetics

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs