2. PROTAC Epigenetics Cell Cycle/DNA Damage Immunology/Inflammation
  3. PROTACs PARP DNA/RNA Synthesis PD-1/PD-L1
  4. PROTAC PARP1 degrader-5

PROTAC PARP1 degrader-5 is a PARP1 PROTAC degrader with a DC50 of 0.12 μM. PROTAC PARP1 degrader-5 hijacks the ubiquitin-proteasome system via catalytic ternary complex formation to drive sustained PARP1 degradation. PROTAC PARP1 degrader-5 induces DNA damage, drives marginal cytosolic double-stranded DNA accumulation in tumor cells, and up-regulates PD-L1 surface expression in tumor cells. PROTAC PARP1 degrader-5 shows tumor growth inhibition activity in murine melanoma models when encapsulated in lipid nanoparticles. PROTAC PARP1 degrader-5 can be used for the research of cancer, such as melanoma.
(Pink: PARP-1 ligand (HY-10162); Blue: VHL ligand (HY-112078); Black: linker (HY-W012241)).

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

PROTAC PARP1 degrader-5

PROTAC PARP1 degrader-5 Chemical Structure

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PROTAC PARP1 degrader-5 Related Antibodies

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Description

PROTAC PARP1 degrader-5 is a PARP1 PROTAC degrader with a DC50 of 0.12 μM. PROTAC PARP1 degrader-5 hijacks the ubiquitin-proteasome system via catalytic ternary complex formation to drive sustained PARP1 degradation. PROTAC PARP1 degrader-5 induces DNA damage, drives marginal cytosolic double-stranded DNA accumulation in tumor cells, and up-regulates PD-L1 surface expression in tumor cells. PROTAC PARP1 degrader-5 shows tumor growth inhibition activity in murine melanoma models when encapsulated in lipid nanoparticles. PROTAC PARP1 degrader-5 can be used for the research of cancer, such as melanoma[1]. (Pink: PARP-1 ligand (HY-10162); Blue: VHL ligand (HY-112078); Black: linker (HY-W012241)).

IC50 & Target[1]

VHL

 

PARP1

0.12 μM (DC50)

In Vitro

PROTAC PARP1 degrader-5 (Compound PROP) (0.01-25 μM; 12-24 h) potently degrades PARP1 protein in B16F10 cells with a DC50 of 0.12 μM[1].
PROTAC PARP1 degrader-5 (1 μM; 24 h) reduces PARP1 fluorescence intensity in B16F10 cells[1].
PROTAC PARP1 degrader-5 (1 μM; 24 h) induces minimal DNA damage and induces a 3.7-fold increase in cytosolic dsDNA levels in B16F10 cells[1].
PROTAC PARP1 degrader-5 (1 μM; 12 h) up-regulates PD-L1 expression in B16F10, 4T1, H22, KPC, and CT26 cells, causing a 1.7-fold increase in B16F10 cells[1].
PROTAC PARP1 degrader-5 (1 μM) increases the proportion of mature BMDCs to 41.9%[1].
PROTAC PARP1 degrader-5 (1 μM; 24 h) induces cGAMP production in co-cultured DC2.4 and THP-1 cells[1].
PROTAC PARP1 degrader-5 (The lipid nanoparticle-encapsulated PROP) (0.01-25 μM; 24 h) exhibits cytotoxicity in H22 and CT26 cells with IC50 values of 18.6 μM and 13.1 μM, respectively and educes colony-forming[1].

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

PROTAC PARP1 degrader-5 Related Antibodies

Western Blot Analysis[1]

Cell Line: B16F10
Concentration: 0.01, 0.1, 1, 10, 25 μM
Incubation Time: 12 h; 24 h
Result: Induced PARP1 protein degradation with a half-maximal degradation concentration of 0.12 μM.
Reduced PARP1 protein levels to 21.8% of PBS-treated controls after 24 h of treatment.

Immunofluorescence[1]

Cell Line: B16F10
Concentration: 1 μM
Incubation Time: 24 h
Result: Resulted in a marked reduction of PARP1-specific fluorescence signals compared to PBS-treated controls.
In Vivo

PROTAC PARP1 degrader-5 (The lipid nanoparticle-encapsulated PROP) (12 mg/kg; i.v.; daily; 5 days) delays B16F10 melanoma growth, reduces lung metastasis, induces PD-L1 up-regulation in tumor tissue, and extends median survival to 40 days in female C57BL/6J mice[1].
PROTAC PARP1 degrader-5 (The lipid nanoparticle-encapsulated PROP) (12 mg/kg; i.v.; daily; 5 days) fails to robustly suppress CT26 colon carcinoma and 4T1 breast cancer growth in female BALB/cJ mice compared to the combination formulation[1].

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

Animal Model: C57BL/6J (female, 6 to 8 weeks old, subcutaneous injection B16F10 cells)[1]
Dosage: 10 mg/kg (delivered via LNP@PROₚ formulation)
Administration: i.v.; daily; 5 consecutive days
Result: Delayed tumor growth but did not achieve robust suppression compared to combination formulation.
Extended median survival to up to 40 days, with no mice surviving to 60 days.
Induced a 1.3±0.2-fold up-regulation of PD-L1 in tumor tissue versus PBS controls.
Inhibited lung metastasis
Molecular Weight

1005.25

Formula

C55H69FN8O7S
SMILES

O=C(N[C@@H](C(C)(C)C)C(N1C[C@@H](C[C@H]1C(N[C@H](C2=CC=C(C=C2)C3=C(N=CS3)C)C)=O)O)=O)CCCCCCCCCCC(N4CCN(C(C5=C(F)C=CC(CC6=NNC(C7=C6C=CC=C7)=O)=C5)=O)CC4)=O
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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PROTAC PARP1 degrader-5 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:

PROTAC PARP1 degrader-5PROTACsPARPDNA/RNA SynthesisPD-1/PD-L1poly ADP ribose polymerase PD-1/Programmed death-ligand 1melanomabone marrow-derived dendritic cellsubiquitin-proteasome systemlipid nanoparticlesBRD4cancer cell linesPARP1murine melanoma modelsprogrammed death-ligand 1base excision repairInhibitorinhibitorinhibit

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