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PARP-1 Inhibitor

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By Targets:	PARP (140) Adenosine Receptor (1) Akt (1) Apoptosis (33) Aurora Kinase (1) Autophagy (6) c-Met/HGFR (1) Caspase (4) CDK (3) DNA/RNA Synthesis (2) Endogenous Metabolite (3) Epigenetic Reader Domain (3) Fluorescent Dye (1) HDAC (4) Histone Methyltransferase (1) Influenza Virus (1) Isotope-Labeled Compounds (2) Microtubule/Tubulin (6) Mitophagy (4) PI3K (2) Poly(ADP-ribose) Glycohydrolase (PARG) (1) PPAR (1) PROTACs (5) Proteasome (1) Reactive Oxygen Species (1) Topoisomerase (3)
By Research Areas:	Cancer (127) Cardiovascular Disease (4) Infection (1) Inflammation/Immunology (10) Metabolic Disease (2) Neurological Disease (8)
Click Chemistry:	Alkynes (1)

148

Inhibitors & Agonists

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Products

Isotope-Labeled Compounds

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Targets Recommended: PARP

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-164475

PARP1-IN-29	PARP	Cancer
PARP1-IN-29 is an orally active *PARP-1* inhibitor with an IC₅₀ value of 6.3 nM. PARP1-IN-29, after being labeled with [18F], can be used for positron emission tomography (PET) imaging, specifically targeting *PARP-1* in tumors. PARP1-IN-29 is applicable in the fields of oncology and imaging research, particularly for detecting *PARP-1* activity in cancer .

HY-132297A

PARP1-IN-5 dihydrochloride 1 Publications Verification	PARP	Cancer
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective *PARP-1* inhibitor (IC₅₀ =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer .

HY-34386

6(5H)-Phenanthridinone	PARP	Inflammation/Immunology Cancer
6(5H)-Phenanthridinone is a potent *PARP-1* inhibitor and immunomodulator. 6(5H)-Phenanthridinone inhibits cell proliferation and can be used in cancer research .

HY-169299

TOPOI/PARP-1-IN-2	PARP Topoisomerase Apoptosis	Cancer
TOPOI/PARP-1-IN-2 (compound 6c) is a dual *PARP-1* and topoisomerase 1 (TOPO-1) inhibitor with IC₅₀s of 32.2 nM and 46.2 nM, respectively. TOPOI/PARP-1-IN-2 shows a selectivity for PARP-1 over PARP-2. TOPOI/PARP-1-IN-2 disrupts the cell cycle at the S phase and induces apoptosis in NCI-60 cancer cell lines .

HY-159612

PARP1-IN-28	PARP	Cancer
PARP1-IN-28 (compound 1) is a *PARP1* inhibitor. PARP1-IN-28 can be used in the study of cancer .

HY-157137

PARP1-IN-17	PARP Caspase Apoptosis	Cancer
PARP1-IN-17 is a *PARP-1* inhibitor (IC₅₀ = 19.24 nM for *PARP-1* and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity .

HY-168094

PARP1-IN-30	PARP	Cancer
PARP1-IN-30 is a specific and potent *PARP1* inhibitor with cytotoxicity. PARP1-IN-30 allows precise inhibition of *PARP1* in tumor cells with breast cancer 1 protein (BRCA1) or BRCA2 deficiencies. PARP1-IN-30 is promising for research of cancers .

HY-155246

PARP1-IN-15	Apoptosis PARP	Cancer
PARP1-IN-15 (Compound 6) is a *PARP1* inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations .

HY-162114

PARP1-IN-18	PARP	Cancer
PARP1-IN-18 (compound 25) is a potent *PARP1* inhibitor with an IC₅₀ value of 2.7 nM. PARP1-IN-18 has anticancer effects .

HY-132297

PARP1-IN-5	PARP	Cancer
PARP1-IN-5 is a low toxicity, orally active, potent and selective *PARP-1* inhibitor (IC₅₀ =14.7 nM). PARP1-IN-5 can be used for the research of cancer .

HY-144338

PARP1/BRD4-IN-1	Epigenetic Reader Domain PARP Apoptosis DNA/RNA Synthesis	Cancer
PARP1/BRD4-IN-1 is a potent and high selective *PARP1/BRD4* inhibitor (IC₅₀s of 49 and 202 nM in PARP1 and BRD4, respectively). PARP1/BRD4-IN-1 represses the expression and activity of PARP1 and BRD4 to synergistically inhibit the malignant growth of pancreatic cancer cells .

HY-149001

PARP1-IN-9	PARP	Cancer
PARP1-IN-9 (Compound 5c) is a PARP1 inhibitor with an IC₅₀ of 30.51 nM. PARP1-IN-9 induces cell apoptosis and shows anticancer activity. PARP1-IN-9 has higher potency than Olaparib (HY-10162) .

HY-158680

PARP1-IN-21	PARP	Cancer
PARP1-IN-21 (example 16) is a potent inhibitor of *PARP1, with the IC₅₀* of ＜ 10 nM .

HY-158681

PARP1-IN-22	PARP	Cancer
PARP1-IN-22 (compound 15) is a potent inhibitor of *PARP1, with the IC₅₀* of ＜ 10 nM .

HY-160417

PARP1-IN-19	PARP	Cancer
PARP1-IN-19 is a *PARP1* inhibitor with antitumor effects (CN107955001A; Embodiment 3) .

HY-142657

PARP1-IN-7	PARP	Cancer
PARP1-IN-7 is an inhibitor of poly(ADP-ribose) polymerase-1 (PARP1) as an anticancer agent.

HY-147886

PARP1-IN-11	PARP	Cancer
PARP1-IN-11 (compound 49) is a potent *PARP1* inhibitor with IC₅₀ value of 0.082 µM. PARP1-IN-11 shows complete inhibition of PARP2 and substantially inhibits PARP3, TNKS1 and TNKS2 .

HY-156298

PARP1-IN-16	PARP Apoptosis	Cancer
PARP1-IN-16 (compound 12a) is a potent *PARP1* inhibitor, with an IC₅₀ of 1.89 nM. PARP1-IN-16 can arrest the cell cycle in S phase and induce apoptosis in HCT-116 cells .

HY-153590

PARP-1-IN-4	PARP	Cancer
PARP-1-IN-4 is a *PARP-1* inhibitor. PARP-1-IN-4 has inhibitory activity against PARP-1 with IC₅₀ value of 302 μM. PARP-1-IN-4 can be used for the research of lung adenocarcinoma .

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-169170

PARP1/BRD4-IN-3	Apoptosis DNA/RNA Synthesis Epigenetic Reader Domain PARP	Cancer
PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and *PARP1* inhibitor with IC₅₀ values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy .

HY-150765

PARP1-IN-12	PARP Apoptosis	Cancer
PARP1-IN-12 is a potent *PARP1* inhibitor with an IC₅₀ of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells .

HY-147030

PARP1-IN-8	PARP	Cancer
PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated *PARP1* inhibitor, with an IC₅₀ of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549 .

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-150613

PARP1/BRD4-IN-2	Epigenetic Reader Domain PARP Apoptosis	Cancer
PARP1/BRD4-IN-2 is a potent and selective *PARP1* and BRD4 inhibitor with IC₅₀ values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .

HY-147027

PARP-1-IN-2	PARP Caspase Apoptosis	Cancer
PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated *PARP1* inhibitor, with an IC₅₀ of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis .

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-149003

PARP1-IN-10	PARP Apoptosis	Cancer
PARP1-IN-10 (compound 12c) is a no-cytotoxicity and potent *PARP1* inhibitor with an IC₅₀ value of 50.62 nM in vitro. PARP1-IN-10 causes cell cycle arrest at G2/M phase and apoptosis, and enhances the cytotoxicity of temozolomide (TMZ) .

HY-161372

PARP1/c-Met-IN-1	PARP c-Met/HGFR Apoptosis	Cancer
PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for *PARP1* and c-Met, with IC₅₀s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice .

HY-155766

PARP1-IN-14	PARP Apoptosis	Cancer
PARP1-IN-14 (compound 19k) is a potent *PARP1* inhibitor, with an IC₅₀ of 0.6 ± 0.1 nM. PARP1-IN-14 exhibits antiproliferative effect against both MDA-MB-436 (BRCA1 ^−/−) and Capan-1 (BRCA2 ^−/−) cells with IC₅₀ values below 0.3 nM .

HY-108413

Talazoparib tosylate 65+ Cited Publications BMN 673ts	PARP	Cancer
Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available *PARP1/2* inhibitor with an IC₅₀ of 0.57 nM for PARP1.

HY-108632

BYK204165	PARP	Cancer
BYK204165 is a potent and selective *PARP1* inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC₅₀ of 7.35 (pK_i=7.05), and murine PARP-2 (mPARP-2) with a pIC₅₀ of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1 .

HY-149800

PARP-1-IN-3	PARP Apoptosis Caspase	Cancer
PARP-1-IN-3, a benzamide derivative, is a potent *PARP-1* inhibitor with IC₅₀ values of 0.25 nM and 2.34 nM for PARP-1 and PARP-2, respectively. PARP-1-IN-3 induces apoptosis and arrest cell cycle at G2/M phase. PARP-1-IN-3 can be used in research of cancer .

HY-164713

PARP1-IN-31	Others	Others
PARP1-IN-31 (compound 11f) is a phthalazinone-based compound, an anti-lung adenocarcinoma compound with inhibitory activity against PARP-1 (IC₅₀ value of 97 nM), inducing apoptosis and inhibiting cell proliferation in lung cancer cell lines.

HY-161934

PARP1-IN-27	PARP Reactive Oxygen Species Apoptosis	Cancer
PARP1-IN-27 (Compound 9B) is the inhibitor for *PARP1* and *PARP2, with IC₅₀* of 2.53 nM and 6.45 nM in cell SUM149PT. PARP1-IN-27 inhibits the proliferation of BRCA-mutated cancer cells SUM149PT, HCC1937 and Capan-1, with IC₅₀ of 0.62, 1.91 and 4.26 μM respectively. PARP1-IN-27 aggravates DNA double-strand breaks, increases ROS generation, arrests cell cycle at G2/M phase, and induces apoptosis in SUM149PT .

HY-163658

PARP-1-IN-23	PARP	Cancer
PARP-1-IN-23 (Compound I16 ) is an orally active and selective *PARP-1* inhibitor with the IC₅₀ of 12.38 nM. PARP-1-IN-23 inhibits tumor growth in vivo .

HY-164757

PARP-1-IN-32	Poly(ADP-ribose) Glycohydrolase (PARG)	Cancer
PARP-1-IN-32 (compound 15) is a poly (ADPribose) polymerase-1 (PARP-1) inhibitor. PARP-1-IN-32 can be used in cancer research .

HY-119653

AZ9482	PARP	Cancer
AZ9482 is a triple *PARP1/2/6* inhibitor, with IC₅₀ values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively .

HY-116218C

Amelparib hydrochloride JPI-289 hydrochloride	PARP	Cardiovascular Disease Neurological Disease
Amelparib (JPI-289) hydrochloride is a potent, orally active, and water-soluble inhibitor of *PARP-1. Amelparib hydrochloride inhibits* *PARP-1* activity (IC₅₀ = 18.5 nM) and cellular PAR formation (IC₅₀ = 10.7 nM). Amelparib hydrochloride is a potential neuroprotective agent. Amelparib hydrochloride has the potential for the research of acute ischaemic stroke .

HY-146336

PARP1/2/TNKS1/2-IN-1	PARP Apoptosis	Cancer
PARP1/2/TNKS1/2-IN-1 (Compound I-9) is a dual *PARP-1, PARP-2, TNKS1* and TNKS2 inhibitor with IC₅₀ values of 0.25 nM, 1.2 nM, 13.5 nM and 4.15 nM against PARP-1, PARP-2, TNKS1 and TNKS2, respectively. PARP1/2/TNKS1/2-IN-1 exhibits favorable synergistic antitumor efficacy and induces apoptosis .

HY-139879

PARP1-IN-6	PARP	Cancer
PARP1-IN-6 is a dual *tubulin/PARP-1* inhibitor with IC₅₀ values of 0.94 and 0.48 μM, respectively.

HY-163817

PARP1/2-IN-3	PARP	Cancer
PARP1/2-IN-3 (Compound 29) is an orally active inhibitor for *PARP 1* and PARP 2 with IC₅₀ of 0.2235 nM and <0.001 nM. PARP1/2-IN-3 inhibits the proliferation of Capan-1 wildtype, AZD2281 or BMN673 resistant cells with IC₅₀ of 1.82-9.98 nM. PARP1/2-IN-3 exhibits antitumor efficacy in mice .

HY-18954

NMS-P118 2 Publications Verification	PARP	Cancer
NMS-P118 is a potent, orally available, and highly selective *PARP-1* Inhibitor for cancer therapy.

HY-U00223

WD2000-012547	PARP	Cancer
WD2000-012547 is a selective poly(ADP-ribose)-polymerase (PARP-1) inhibitor with a pK_i of 8.221.

HY-161517

PARP1-IN-20	PARP	Cancer
PARP1-IN-20 (compound 19A10) is a potent inhibitor of *PARP1, with the IC₅₀* of 4.62 nM and has similar low *PARP*-Trapping effect compared with Veliparib (HY-10129), IC₅₀ (MDA-MB-436) >100 μM .

HY-145804

AZD-9574 1 Publications Verification	PPAR	Neurological Disease
AZD-9574 is a potent and brain penetrant *PARP1* inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs. AZD-9574 is an anti-cancer agent and can be used for HRD ⁺ breast cancer and advanced solid malignancies research .

HY-116218

Amelparib JPI-289 free base	PARP	Cardiovascular Disease Neurological Disease
Amelparib (JPI-289 free base) is a potent, orally active, and water-soluble inhibitor of *PARP-1. Amelparib inhibits* PARP-1 activity (IC₅₀=18.5 nM) and cellular PAR formation (IC₅₀=10.7 nM) in the nanomolar range. Amelparib is a potential neuroprotective agent. Amelparib has the potential for the research of acute ischaemic stroke .

HY-161288

UKTT15	PARP	Cancer
UKTT15 (compound 6) is an allosteric inhibitor of *PARP1* .

HY-14478

UPF 1069 1 Publications Verification	PARP	Cancer
UPF 1069 is a *PARP* inhibitor, with IC₅₀s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.

HY-16106

Talazoparib 65+ Cited Publications BMN-673; LT-673	PARP	Cancer
Talazoparib (BMN-673) is a highly potent, orally active *PARP1/2* inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with K_is of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity .

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 .

Cat. No.	Product Name	Chemical Structure

HY-16106S

Talazoparib-13C,d4
Talazoparib- ¹³C,d4 is ¹³C and deuterated labeled Talazoparib (HY-16106). Talazoparib is an orally active PARP 1/2 inhibitor with Ki values of 1.2 nM and 0.87 nM for inhibiting PARP1 and PARP2 enzymatic activities, respectively. Has anti-tumor activity.

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].

HY-10162S1

Olaparib-d8
Olaparib-d₈ is the deuterium labeled Olaparib (AZD2281). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].

HY-10162S3

Olaparib-d4-1
Olaparib-d₄-1 is the deuterium labeled Olaparib. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator[1][2][3][4].

HY-Z0283S

Benzamide-15N
Benzamide- ¹⁵N is a ¹⁵N-labeled Benzamide. Benzamide inhibits poly(ADP-ribose) polymerase (PARP)[1][2].

Cat. No.	Product Name		Classification

HY-145749

PARPYnD		Alkynes
PARPYnD is a *PARP* enzyme photoaffinity probe (AfBP) based on the triple *PARP1/2/6* inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC₅₀ of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells .

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PARP-1 Inhibitor

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