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Pathways Recommended:	PROTAC

Results for "

PROTAC PARP1 degrader

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Ligands for Target Protein for PROTAC (2) PARP (19) PROTAC Linkers (3) Androgen Receptor (1) Apoptosis (3) Autophagy (1) Caspase (1) DNA/RNA Synthesis (2) E3 Ligase Ligand-Linker Conjugates (5) EGFR (1) PD-1/PD-L1 (1) PROTACs (15) Target Protein Ligand-Linker Conjugates (1)
By Research Areas:	Cancer (26)
Click Chemistry:	PROTAC Synthesis (2) Azide (3)

Inhibitors & Agonists

Click Chemistry

Targets Recommended: PROTAC-Linker Conjugates for PAC PROTAC Linkers PARP Ligands for Target Protein for PROTAC

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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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		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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