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PARP1 degrader

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By Targets:	PARP (27) Androgen Receptor (1) Apoptosis (3) Autophagy (2) Caspase (1) DNA/RNA Synthesis (2) Drug Derivative (1) Drug Intermediate (1) E3 Ligase Ligand-Linker Conjugates (5) EGFR (1) Endogenous Metabolite (4) HSP (1) Hsp-targeting Chimeras (1) HyT (2) Isotope-Labeled Compounds (1) Ligands for E3 Ligase (1) Ligands for Target Protein for PROTAC (2) PD-1/PD-L1 (1) PROTAC Linkers (3) PROTACs (15) Reference Standards (1) Target Protein Ligand-Linker Conjugates (1)
By Research Areas:	Cancer (30) Metabolic Disease (4) Neurological Disease (1)
Click Chemistry:	PROTAC Synthesis (2) Azide (3)

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Products

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: PARP

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-139156

SK-575 5 Publications Verification	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-158045

*PROTAC PARP1* degrader-1**	PROTACs PARP	Cancer
PROTAC PARP1 degrader-1 is a *PARP1* PROTAC degrader with a DC₅₀ value of 252.5 nM. PROTAC PARP1 degrader-1, combined with Daunorubicin (HY-13062A), induces the accumulation of cytoplasmic DNA fragments, activates the cGAS/STING innate immune pathway, and remodels the tumor microenvironment. PROTAC PARP1 degrader-1 can be used in research related to breast cancer .

HY-114324

PROTAC PARP1 degrader	PROTACs PARP	Cancer
PROTAC PARP1 degrader is a *PARP1* degrader based on MDM2 E3 ligand. PROTAC PARP1 degrader induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader consists of E3 ubiquitinase ligand MDM2 ligand (HY-128836), blue part; target protein ligand PAPR1 ligand (HY-171543), pink part; PROTAC linker N3-PEG4-C2-NH2 (HY-128834), black part .

HY-130644

iRucaparib-AP6 2 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-170620

PARP1 PROTAC 180055 1 Publications Verification	PROTACs PARP	Cancer
PARP1 PROTAC 180055 (Compound 180055) is a selective *PARP1* PROTAC degrader (DC₅₀ in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PARP1 PROTAC 180055 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PARP1 PROTAC 180055 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-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-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-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 .

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-113432R

Nudifloramide (Standard) 2PY (Standard)	Reference Standards 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-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-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-130647

Vrucaparib-TP4	PROTACs PARP	Cancer
Vrucaparib-TP4 (Compound 9) is a *PARP1* PROTAC-type degrader. Vrucaparib-TP4 promotes the ubiquitination and degradation of PARP1. Vrucaparib-TP4 can be used in the research of tumors .

HY-160937

AZD-9574-acid	Ligands for Target Protein for PROTAC PARP	Cancer
AZD-9574-acid (Compound 70D) is a *PARP-1* ligand. AZD-9574-acid serves as a Ligand for Target Protein for PROTAC for the synthesis of PARP-1 PROTAC degraders. AZD-9574-acid is applicable to cancer research .

HY-178496

DDO3602	Hsp-targeting Chimeras PARP HSP	Cancer
DDO3602 is a PARP1 HEMTAC degradation agent mediated by HSP90. DDO3602 has good anti-tumor activity and tumor selectivity. DDO3602 induces G2/M phase arrest, DNA damage, and inhibits cell migration by degrading PARP1 in MCF-7 cells (IC₅₀ = 187 nM). DDO3602 can be used for research on cancer such as breast cancer. (Pink: PARP1 Ligand (HY-75706); Blue: HSP90 Ligand (HY-179203); Black: Linker (HY-W015300))

HY-130645

iRucaparib-TP3	PARP	Neurological Disease Cancer
iRucaparib-TP3 is a selective *PARP1* degrader (DC₅₀=36 nM). iRucaparib-TP3 is promising for research of oncology (e.g., BRCA-mutated cancers) and neurodegenerative diseases .

HY-181460

PARP1 degrader-2	HyT PARP	Cancer
PARP1 degrader-2 (Compound 11e) is a potent, selective *PARP1* HYT degrader (DC₅₀: 2.16 μM). PARP1 degrader-2 selectively binds to and degrades PARP1 but not PARP2. PARP1 degrader-2 mediates the degradation of PARP1 via the ubiquitin-proteasome system (UPS). PARP1 degrader-2 exhibits anticancer activity against triple-negative breast cancer and colon cancer (hydrophobic tag: (HY-W022007); PARP1 ligand: (HY-75706); Linker: (HY-W015300)) .

HY-176128

BWA-6047	PROTACs Androgen Receptor Apoptosis PARP Caspase	Cancer
BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC₅₀ values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer .

HY-180276

PARP1 degrader 1	HyT PARP Drug Derivative Autophagy	Cancer
PARP1 degrader 1 (Compound 2c) is a comparatively potent *PARP1* HyT degrader (DC₅₀: 618 nM for intracellular PARP-1). PARP1 degrader 1 is also a HyT-Olaparib (HY-10162) conjugate. PARP1 degrader 1 induces UPR/autophagy, thus facilitating the degradation of PARP-1. PARP1 Degrader 1 can be used in the research of cancer .

HY-181967

*PROTAC PARP1* degrader-5**	PROTACs PARP DNA/RNA Synthesis PD-1/PD-L1	Cancer
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 .

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-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-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-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-173437

CW-2	PROTACs PARP DNA/RNA Synthesis	Cancer
CW-2 is a *PARP1* PROTAC degrader. CW-2 has potent antiproliferative effects against MDA-MB-231 cells (IC₅₀ = 0.72 μM) and CDDP-resistant cells (A549/CDDP: IC₅₀ = 3.52 μM). CW-2 has synergistic antitumor activity and enhanced membrane permeability. CW-2 exerts antitumor effects by inducing DNA damage, impairing DNA repair, and activating mitochondria-dependent apoptosis (Pink: PARP1 ligand (HY-173441); Blue: E3 CRBN ligand (HY-173439); Black: linker (HY-173440)) .

HY-W973851

2H-Indazole-7-carboxamide	Ligands for Target Protein for PROTAC PARP	Others
2H-Indazole-7-carboxamide is a PARP1 ligand and can be used for the synthesis of PROTACs, such as PROTAC PARP1 degrader-1 (HY-158045) .

HY-130646

iVeliparib-AP6	PROTACs PARP	Cancer
iVeliparib-AP6 is a proteolysis-targeting chimera (PROTAC) molecule designed based on Veliparib (HY-10129), which targets *PARP1/2. The DC₅₀s* of iVeliparib-AP6 for inducing the degradation of PARP1 and PARP2 are 36 nM and 63 nM, respectively, and its IC₅₀s are 69 nM and 21 nM, respectively. iVeliparib-AP6 contains a Veliparib-based PARP inhibitor warhead linked to a CRBN E3 ligase binder; it uses Thalidomide (HY-14658) as a ligand to recruit CRBN E3 ubiquitin ligase and exerts the PARP2 degradation mechanism .

HY-W022007

5-Norbornene-2-methylamine JBP	Ligands for E3 Ligase	Others
5-Norbornene-2-methylamine (JBP) is a hydrophobic tag. 5-Norbornene-2-methylamine can be used for the synthesis of HyT degraders, such as PARP1 degrader-2 (HY-181460) .

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 .

HY-113432S2

Nudifloramide-13C,d3 2PY-¹³C,d₃	Isotope-Labeled Compounds Endogenous Metabolite PARP	Metabolic Disease
Nudifloramide- ¹³C,d₃ (2PY- ¹³C,d₃) is the ¹³C- and deuterium labeled Nudifloramide (HY-113432). 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-185594

4-(Cyclohexylbuta-1,3-diyn-1-yl)benzoic acid	Drug Intermediate	Others
4-(Cyclohexylbuta-1,3-diyn-1-yl)benzoic acid is a Hyt hydrophobic group. 4-(Cyclohexylbuta-1,3-diyn-1-yl)benzoic acid can be used in the synthesis of PARP1 degrader 1 (HY-180276).

HY-183013

*PROTAC PARP2 degrader-1*	PROTACs PARP Apoptosis	Cancer
PROTAC PARP2 degrader-1 is an orally active *PARP2* PROTAC degrader with a DC₅₀ of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC₅₀ = 2.74 nM) and PARP2 (IC₅₀ = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-113432

Nudifloramide 2PY	Alkaloids Structural Classification Other disease Classification of Application Fields Disease markers Pyridine Alkaloids Metabolic Disease Endogenous metabolite Disease Research Fields Source Classification	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 Endogenous metabolite Source Classification	Reference Standards 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 .

HY-113432S2

Nudifloramide-13C,d3
Nudifloramide- ¹³C,d₃ (2PY- ¹³C,d₃) is the ¹³C- and deuterium labeled Nudifloramide (HY-113432). 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		Classification

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-130652

Pomalidomide 4'-PEG3-azide		PROTAC Synthesis 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-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

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