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PARP1 degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (1) Autophagy (1) E3 Ligase Ligand-Linker Conjugates (5) EGFR (1) Endogenous Metabolite (3) PARP (14) PROTAC Linkers (3) PROTACs (9) Target Protein Ligand-Linker Conjugates (1)
By Research Areas:	Cancer (19) Inflammation/Immunology (1) Metabolic Disease (3)
Click Chemistry:	PROTAC Synthesis (1) Azide (3)

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Products

Isotope-Labeled Compounds

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-114324

PROTAC PARP1 degrader	PROTACs PARP	Cancer
PROTAC PARP1 degrader is a *PARP1* degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC₅₀ of 6.12 μM.

HY-114324A

rel-PROTAC PARP1 degrader	PROTACs PARP	Cancer
rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a *PARP1* degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC₅₀ of 6.12 μM.

HY-158045

*PROTAC PARP1* degrader-1**	PROTACs PARP	Inflammation/Immunology Cancer
PROTAC PARP1 degrader-1 (Compound CN0) is a PROTAC degrader of *PARP1. PROTAC PARP1* degrader-1 activates the cGAS/STING immunity pathway and eventually enhances T cell killing of tumor cells. PROTAC PARP1 degrader-1 inhibits DNA damage repair, resulting in highly efficient accumulation of cytosolic DNA fragments (Blue: CRBN ligand, Black: linker; Pink: PARP1 inhibitor) .

HY-130644

iRucaparib-AP6 1 Publications Verification	PROTACs PARP	Cancer
iRucaparib-AP6 is a highly efficient and specific PROTAC PARP1 degrader. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1 .

HY-130652

Pomalidomide 4'-PEG3-azide	E3 Ligase Ligand-Linker Conjugates	Cancer
Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient *PARP1*?degrader based on Rucaparib by using the PROTAC approach . Pomalidomide 4'-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-113432

Nudifloramide 2PY	Endogenous Metabolite PARP	Metabolic Disease
Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .

HY-170620

*PROTAC PARP1* degrader-4**	PROTACs PARP	Cancer
PROTAC PARP1 degrader-4 (Compound 180055) is a selective *PARP1* PROTAC degrader (DC₅₀ in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PROTAC PARP1 degrader-4 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PROTAC PARP1 degrader-4 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787)) .

HY-168722

*PROTAC PARP1* degrader-3**	PARP PROTACs	Cancer
PROTAC PARP1 degrader-3 (Compound C6) is a PROTAC degrader for *PARP1* with a DC₅₀ of 58.14 nM. PROTAC PARP1 degrader-3 exhibits cytotoxicity in cancer cell SW-620 and LOVO with IC₅₀ of 1.63 μM and 2.84 μM. PROTAC PARP1 degrader-3 exhibits a synergistic effect with SN-38 (HY-13704) in BRCA-mutated colon cancer cell with a combination index (CI) of 0.487. (Blue: Ligand for E3 ligase Cereblon (HY-23095); Pink: Ligand for target protein (HY-10619); Black: Linker (HY-16872))

HY-164306

*PROTAC PARP1* degrader-2**	PROTACs PARP	Cancer
PROTAC PARP1 degrader-2 (Compound 72) is a PROTAC degrader for *PARP* with a DC₅₀<10 nM in MDA-MB-231 cell. PROTAC PARP1 degrader-2 inhibits the cell viability of MDA-MB-436 with an IC₅₀ <100 nM. (Blue: ligand for target protein (HY-160937); Pink: ligand for E3 ligase (HY-W998262))

HY-147101

SK-575-NEG	PARP	Cancer
SK-575-NEG (compound 28), a methylation counterpart of SK-575, is synthesized by methylation of the amino group of piperidine-2,6-dione in SK-575 as an control compound. SK-575-NEG is strongly bound to *PARP1, with an IC₅₀* of 2.64 nM. SK-575-NEG was completely ineffective in inducing PARP1 degradation in MDA-MB-436 and Capan-1 cells at concentrations up to 1 μM .

HY-W998262

Pomalidomide 5-piperidylamine	E3 Ligase Ligand-Linker Conjugates	Cancer
Pomalidomide 5-piperidylamine is the conjugate of an E3 ligase ligand and a linker. Pomalidomide 5-piperidylamine can be used for synthesis of PROTAC PARP1 degrader-2 (HY-164306) .

HY-168723

Piperidine-C-Pip-C2-Pip-C2-OH	PROTAC Linkers	Cancer
Piperidine-C-Pip-C2-Pip-C2-OH is a PROTAC Linker that can be used to synthesize the PROTAC PARP1 degrader-3 (HY-168722) for tumor research .

HY-113432R

Nudifloramide (Standard) 2PY (Standard)	Endogenous Metabolite PARP	Metabolic Disease
Nudifloramide (Standard) is the analytical standard of Nudifloramide. This product is intended for research and analytical applications. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .

HY-113432S

Nudifloramide-d3	Endogenous Metabolite PARP	Metabolic Disease
Nudifloramide-d₃ (2PY-d3) is the deuterium labeled Nudifloramide. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro[1].

HY-168724

Thalidomide-piperidine-C-Pip-C2-Pip-C2-OH	PARP E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide-piperidine-C-Pip-C2-Pip-C2-OH (Compound C6) is a conjugate of the linker and E3 ligase ligand, that can be used in synthesis of PROTAC PARP1 degrader-30 (HY-168722) .

HY-139156

SK-575	PROTACs PARP	Cancer
SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of *PARP1, with an IC₅₀* of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations .

HY-120918

NH2-PEG7	PROTAC Linkers	Cancer
NH2-PEG7 is a PROTAC linker, which refers to the PEG composition. NH2-PEG7 can be used in the synthesis of the PROTAC PARP1 degrader iRucaparib-AP6 .

HY-130648

Thalidomide-NH-PEG7	E3 Ligase Ligand-Linker Conjugates Autophagy Apoptosis	Cancer
Thalidomide-NH-PEG7 is a synthesized E3 ligase ligand-linker conjugate for ADC. Thalidomide-NH-PEG7 can be connected to the ligand for protein by a linker to form PROTAC iRucaparib-AP6, a highly specific PARP1 degrader .

HY-W021401

Amino-PEG3-C2-Azido	PROTAC Linkers	Cancer
Amino-PEG3-C2-Azido is a PEG-based PROTAC linker can be used in the synthesis of the PARP1 degrader iRucaparib-TP3 (HY-130645) . Amino-PEG3-C2-Azido is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-130654

(S,R,S)-AHPC-C2-PEG4-N3 VH032-C2-PEG4-N3	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC₅₀) of 82 nM . (S,R,S)-AHPC-C2-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-141481

DP-C-4	PROTACs EGFR PARP	Cancer
DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and *PARP* .

HY-141486

(Rac)-PROTAC PARP/EGFR ligand 1	Target Protein Ligand-Linker Conjugates	Cancer
(Rac)-PROTAC PARP/EGFR ligand 1 incorporates a ligand for PARP and EGFR , and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). (Rac)-PROTAC PARP/EGFR ligand 1 can be used in the synthesis of DP-C-4, which is CRBN-based dual PROTAC for simultaneous degradation of EGFR and PARP .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-113432

Nudifloramide 2PY	Alkaloids Structural Classification Other disease Classification of Application Fields Source classification Disease markers Pyridine Alkaloids Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite PARP
Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .

HY-113432R

Nudifloramide (Standard) 2PY (Standard)	Structural Classification Natural Products Source classification Endogenous metabolite	Endogenous Metabolite PARP
Nudifloramide (Standard) is the analytical standard of Nudifloramide. This product is intended for research and analytical applications. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .

Cat. No.	Product Name	Chemical Structure

HY-113432S

Nudifloramide-d3
Nudifloramide-d₃ (2PY-d3) is the deuterium labeled Nudifloramide. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro[1].

Cat. No.	Product Name		Classification

HY-130652

Pomalidomide 4'-PEG3-azide		Azide
Pomalidomide 4'-PEG3-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide-based cereblon ligand and a linker. Pomalidomide 4'-PEG3-azide can be used for the synthesis of iRucaparib-TP3 (Compound 3). iRucaparib-TP3 is a highly efficient *PARP1*?degrader based on Rucaparib by using the PROTAC approach . Pomalidomide 4'-PEG3-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-W021401

Amino-PEG3-C2-Azido		PROTAC Synthesis Azide
Amino-PEG3-C2-Azido is a PEG-based PROTAC linker can be used in the synthesis of the PARP1 degrader iRucaparib-TP3 (HY-130645) . Amino-PEG3-C2-Azido is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

HY-130654

(S,R,S)-AHPC-C2-PEG4-N3 VH032-C2-PEG4-N3		Azide
(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC₅₀) of 82 nM . (S,R,S)-AHPC-C2-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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PARP1 degrader

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Isotope-Labeled Compounds

Click Chemistry

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