2. PROTAC Apoptosis Cell Cycle/DNA Damage
  3. PROTACs Apoptosis DNA/RNA Synthesis
  4. FPP29

FPP29 is a potent peptide-based FOXM1 PROTAC degrader. FPP29 induces ubiquitination and degradation of FOXM1. FPP29 inhibits FOXM1 via the ubiquitin-proteasome degradation pathway. FPP29 induces Apoptosis. FPP29 suppresses tumor growth in hepatocellular carcinoma xenograft models. FPP29 can be used in the research of hepatocellular carcinoma (cell-penetrating peptide: (HY-P0133); VHL ligase ligand: (HY-P11493); linker: (HY-W013664); FOXM1 ligand: (HY-P11494)).

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

Custom Peptide Synthesis

FPP29

FPP29 Chemical Structure

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Based on 1 publication(s) in Google Scholar

FPP29 Related Antibodies

Top Publications Citing Use of Products

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Description

FPP29 is a potent peptide-based FOXM1 PROTAC degrader. FPP29 induces ubiquitination and degradation of FOXM1. FPP29 inhibits FOXM1 via the ubiquitin-proteasome degradation pathway. FPP29 induces Apoptosis. FPP29 suppresses tumor growth in hepatocellular carcinoma xenograft models. FPP29 can be used in the research of hepatocellular carcinoma (cell-penetrating peptide: (HY-P0133); VHL ligase ligand: (HY-P11493); linker: (HY-W013664); FOXM1 ligand: (HY-P11494))[1].

IC50 & Target[1]

VHL

 

In Vitro

FPP29 (24 h) potently inhibits the viability of HCCLM3 cells, with an IC50 of 3.65 μM after 24 h of incubation[1].
FPP29 (4 μM; 24-48 h) significantly inhibits the migration ability of HCCLM3 cells[1].
FPP29 (2-8 μM; 24 h) induces dose-dependent apoptosis in HCCLM3 cells following 24 h of incubation at concentrations of 2 μM, 4 μM, and 8 μM[1].
FPP29 (2-8 μM; 6-48 h) downregulates the protein expression of FOXM1, cyclin B1 and CDC25B in HCCLM3 cells, and regulates epithelial-mesenchymal transition markers in a dose-dependent and time-dependent manner (upregulating E-cadherin and downregulating N-cadherin)[1].

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

FPP29 Related Antibodies

Cell Migration Assay [1]

Cell Line: human hepatocellular carcinoma HCCLM3 cells
Concentration: 4 μM
Incubation Time: 24 h, 48 h
Result: Significantly inhibited HCCLM3 cell migration at 24 h and 48 h compared to the control, with statistical significance.

Apoptosis Analysis[1]

Cell Line: human hepatocellular carcinoma HCCLM3 cells
Concentration: 2-8 μM
Incubation Time: 24 h
Result: Induced apoptosis in HCCLM3 cells in a dose-dependent manner; the number of yellow-green/orange apoptotic cells increased with increasing FPP29 concentrations.

Western Blot Analysis[1]

Cell Line: human hepatocellular carcinoma HCCLM3 cells
Concentration: 2-8 μM (24 h incubation); 4 μM (6 h, 12 h, 24 h, 48 h incubation)
Incubation Time: 24 h (dose-dependent); 6 h, 12 h, 24 h, 48 h (time-dependent)
Result: Reduced protein expression of FOXM1, cyclin B1, and CDC25B in both dose-dependent (0-8 μM, 24 h) and time-dependent (4 μM, 0-48 h) manners.
Increased E-cadherin protein expression and decreased N-cadherin protein expression in a dose-dependent manner (0-8 μM, 24 h).
Parmacokinetics
Species Dose Route Tmax T1/2
Mice[1] 20 mg/kg i.v. 0.25 h 1.04 h
In Vivo

FPP29 (7.5-15 mg/kg; intratumoral injection) inhibits hepatocellular carcinoma tumor growth in xenograft mice by downregulating FOXM1[1].

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

Animal Model: BALB/c nude mice (6-week-old male, subcutaneous xenograft model)[1]
Dosage: 7.5 mg/kg; 15 mg/kg
Administration: intra-tumoral injection
Result: Inhibited tumor growth by 55%.
Inhibited tumor growth by 75%.
Reduced tumor weight in a dose-dependent manner.
Downregulated FOXM1 protein levels in tumor tissues in a dose-dependent manner.
Increased tumor necrosis and inflammatory cell infiltration.
Reduced Ki-67-positive proliferating cells.
Significantly increased TUNEL-positive apoptotic cells.
Caused no significant changes in mouse body weight, major organ histopathology, liver function tests, or blood routine indices.
Molecular Weight

3267.72

Formula

C145H228N56O32
Appearance

Solid

Color

White to off-white

Sequence

Ala-Trp-Trp-Asn-Thr-Glu-Trp-Gly-Ser-Ala-Leu-Ala-Pro-Tyr-Ile-Pro-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg
Sequence Shortening

AWWNTEWGSALAPYIPRRRRRRRRR
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (7.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.3060 mL 1.5301 mL 3.0602 mL
5 mM 0.0612 mL 0.3060 mL 0.6120 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 (sealed storage, away from moisture). 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
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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 (sealed storage, away from moisture). 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 0.3060 mL 1.5301 mL 3.0602 mL 7.6506 mL
5 mM 0.0612 mL 0.3060 mL 0.6120 mL 1.5301 mL
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FPP29 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:

FPP29FPP 29FPP-29PROTACsApoptosisDNA/RNA SynthesisFOXM1epithelial-mesenchymal transitionVHL E3 ubiquitin ligaseapoptosishepatocellular carcinomaCDC25B293T cellscyclin B1HCCLM3 cellsubiquitin-proteasome systemInhibitorinhibitorinhibit

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