2. PROTAC Metabolic Enzyme/Protease Stem Cell/Wnt JAK/STAT Signaling
  3. PROTACs Phosphatase STAT
  4. PD-305

PD-305 is a selective PTPN2 PROTAC degrader, with DC50 values of 0.25 nM and 5.11 nM against PTPN2 and PTPN1, respectively. PD-305 enhances IFN-γ-induced STAT1 phosphorylation, inhibits the proliferation of IFN-γ-stimulated colorectal cancer cells, promotes CD8+ T cell activation, enhances the tumor-killing activity of T cells, and suppresses tumor growth in mouse models. PD-305 can be used for the research of colorectal cancer.
(Pink: PTPN2 ligand (HY-184259); Blue: Cereblon ligand (HY-184258); Black: linker).

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

PD-305

PD-305 Chemical Structure

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PD-305 Related Antibodies

Top Publications Citing Use of Products

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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STAT3 STAT5 STAT6 STAT1

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Description

PD-305 is a selective PTPN2 PROTAC degrader, with DC50 values of 0.25 nM and 5.11 nM against PTPN2 and PTPN1, respectively. PD-305 enhances IFN-γ-induced STAT1 phosphorylation, inhibits the proliferation of IFN-γ-stimulated colorectal cancer cells, promotes CD8+ T cell activation, enhances the tumor-killing activity of T cells, and suppresses tumor growth in mouse models. PD-305 can be used for the research of colorectal cancer[1]. (Pink: PTPN2 ligand (HY-184259); Blue: Cereblon ligand (HY-184258); Black: linker).

IC50 & Target[1]

PTPN2

0.25 nM (DC50)

PTPN1

5.11 nM (DC50)

Cereblon

 

STAT1

 

STAT5

 

In Vitro

PD-305 (0.001-10000 nM; up to 24 h) induces time- and concentration-dependent PTPN2 degradation in transfected HEK293T cells, and causes prolonged PTPN2 downregulation that persists for 24 h after compound removal[1].
PD-305 (1-10000 nM; 24 h) enhances IFN-γ-induced STAT1 phosphorylation in HT-29 human colorectal cancer cells at nanomolar concentrations via PTPN2 degradation[1].
PD-305 (various concentrations; 72 h) potently inhibits the proliferation of IFN-γ-stimulated HT-29 human colorectal cancer cells with an IC50 of 11.95 nM, nearly 80-fold more potent than AC484[1].
PD-305 (0.2-20 μM; 0-24 h) enhances T-cell receptor signaling via increased LCK phosphorylation and promotes cytokine-induced STAT5 phosphorylation in Jurkat cells through PTPN2 degradation[1].

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

PD-305 Related Antibodies

Western Blot Analysis[1]

Cell Line: Jurkat cell line
Concentration: 1 μM (pretreatment for α-CD3 stimulation); 0.2, 2 and 20 μM (incubation with IFN-γ or IL-2)
Incubation Time: 24 h (pretreatment; incubation with IFN-γ or IL-2); 0-20 min (α-CD3 stimulation)
Result: Upregulated α-CD3-stimulated LCK phosphorylation in Jurkat cells.
Promoted IFN-γ- and IL-2-induced STAT5 phosphorylation, which correlated with reduced PTPN2 protein levels.
In Vivo

PD-305 (50 mg/kg; i.v.; single dose) induces nearly complete, subtype-selective in vivo PTPN2 degradation in MC38 tumor-bearing C57BL/6 mice and promotes CD8+ T cell activation[1].
PD-305 (10-25 mg/kg; i.p.; every other day; 20 days) significantly reduces MC38 tumor volume and weight in C57BL/6 mice without affecting body weight[1].

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

Animal Model: C57BL/6 (female, 6-8 weeks old, 18-22 g, subcutaneously injected with 1 × 105 MC38 cells)[1]
Dosage: 50 mg/kg
Administration: i.v.; single dose
Result: Induced almost complete PTPN2 degradation in tumor tissues, with remaining PTPN2 levels near 0% of vehicle control.
Induced modest degradation of PTPN1, with remaining PTPN1 levels ~60% of vehicle control.
Increased the proportion of CD69-positive CD8+ T cells in vivo to ~35% at 24 hours post-injection.
Animal Model: C57BL/6 (female, 6-8 weeks old, 18-22 g, subcutaneously injected with 1 × 105 MC38 cells)[1]
Dosage: 10 mg/kg; 25 mg/kg
Administration: i.p.; every other day; 20 days
Result: Significantly suppressed MC38 tumor growth compared to vehicle control.
Reduced mean tumor weight to ~1.3 g (10 mg/kg) and ~1.1 g (25 mg/kg) at day 21, compared to ~2.0 g in vehicle-treated mice.
Caused no significant changes in body weight relative to vehicle.
Molecular Weight

910.89

Formula

C43H42F4N6O10S
SMILES

O=C(N1CCC(C#CC2=C(C)C=C(O)C(N3CC(NS3(=O)=O)=O)=C2F)C1)C(C4)CC4N(CC5)CCC5C6=C(C=CC=C7C8=O)C7=C(N8C9CCC(NC9=O)=O)C=C6.O=C(O)C(F)(F)F
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
References
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PD-305 Related Classifications

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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:

PD-305PD305PD 305PROTACsPhosphataseSTATMC38 tumorHT-29 human colorectal cancer cellsC57BL/6 micecolorectal cancerCD8+ T cellJurkat cellsCRBNPTPN1PTPN2HEK293T cellsInhibitorinhibitorinhibit

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