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Cat. No.: HY-181967

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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.

Formula: C₅₅H₆₉FN₈O₇S
Molecular Weight:1005.25

Storage:

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

PROTAC PARP1 degrader-5 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Classifications
Bioz

Biological Activity

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)

All PROTACs Isoforms :

All PARP Isoforms :

All DNA/RNA Synthesis Isoforms :

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.

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

Chemical Information

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

Handling Instructions (2659 KB)

References

[1]. Liu Y, et al. PROTAC-based synthetic lethality strategy endogenously activates systemic STING to boost antitumor immunity. Sci Adv. 2026;12(9):eado7448. [Content Brief]

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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.

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100 mg

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

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PROTAC PARP1 degrader-5

All PROTACs Isoforms

All PARP Isoforms

All DNA/RNA Synthesis Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC PARP1 degrader-5 Related Classifications

HY-181967 Related Classifications