PARP
poly ADP ribose polymerase
PARP is a family of proteins involved in a number of cellular processes involving mainly DNA repair and programmed cell death. The PARP family comprises 17 members. They have all very different structures and functions in the cell. PARP1, PARP2, VPARP (PARP4), Tankyrase-1 and -2 (PARP-5a or TNKS, and PARP-5b or TNKS2) have a confirmed PARP activity. Others include PARP3, PARP6, TIPARP (or PARP7), PARP8, PARP9, PARP10, PARP11, PARP12, PARP14, PARP15, and PARP16. PARP is found in the cell’s nucleus. The main role is to detect and signal single-strand DNA breaks (SSB) to the enzymatic machinery involved in the SSB repair.
PARP Isoform Specific Products
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PARP
(303)
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PARP1
(209)
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PARP2
(83)
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PARP3
(23)
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PARP4
(11)
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TNKS1/
PARP5A (41)View all products
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TNKS2/
PARP5B (38)View all products
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PARP7
(25)
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PARP10
(20)
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PARP14
(17)
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PARP15
(14)
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PARP12
(4)
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PARP16
(3)
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All Product Categories
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PARP Inhibitors
(459)
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PARP Agonists
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PARP Activators
(111)
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PARP Modulators
(12)
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PARP Inducers
(20)
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PARP Degraders
(24)
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PARP Substrate
(1)
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PARP Ligands
(4)
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PARP Related Products (693)
Related Products (693)
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Antibodies (11)
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PARP Isoform Comparison
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Desethylamiodarone-d4 hydrochloride
0 ImagesCat. No.: HY-130353SCAS No.: 1189960-80-2Synonyms: N-Desethylamiodarone-d4 hydrochloride; LB 33020-d4 hydrochlorideDesethylamiodarone-d4 hydrochloride (N-Desethylamiodarone-d4 hydrochloride; LB 33020-d4 hydrochloride) is the deuterated-labeled Desethylamiodarone hydrochloride (HY-130353). Desethylamiodarone hydrochloride (N-Desethylamiodarone hydrochloride; LB 33020 hydrochloride) is the major active metabolite of Amiodarone (HY-14187) generated via CYP3A4 metabolism. Desethylamiodarone hydrochloride downregulates p‑Akt, p‑Bad and Bcl‑2, upregulates Bax, promotes mitochondrial release of cytochrome c, activates caspase‑3 and cleaves PARP‑1, thereby inducing cell cycle arrest and apoptosis. Desethylamiodarone hydrochloride can be used in cervical cancer-related research.
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PARP1-IN-43
0 ImagesCat. No.: HY-175482CAS No.: 3066798-40-8PARP1-IN-43 (Compound 5350) is a blood-brain barrier (BBB) permeable PARP1 inhibitor, with an IC50 of 5 nM. PARP1-IN-43 can be used for the study of homologous recombination (HR)-deficient central nerve system (CNS) cancers.
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Anticancer agent 64
0 ImagesCat. No.: HY-147514CAS No.: 2387902-92-1Anticancer agent 64 (compound 5m) shows cytotoxic activity in CCRF-CEM cells, with IC50 of 2.4 μM. Anticancer agent 64 shows good anticancer activity through apoptosis induction. Anticancer agent 64 induces caspase 3 and 7 activation and PARP cleavage. Anticancer agent 64 induces significant effect of mitochondria depolarization.
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4,4′-Secalonic acid D
0 ImagesCat. No.: HY-N15380CAS No.: 2265910-52-74,4′-Secalonic acid D (Compound 12) is a PARP1 inhibitor. 4,4′-Secalonic acid D induces the accumulation of ROS and DNA damage, activates the caspase-3/GSDME pathway, and triggers apoptosis and pyroptosis of tumor cells by inhibiting PARP1. 4,4′-Secalonic acid D has anti-tumor activity.
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Cimicifugic acid A
0 ImagesCat. No.: HY-N17665CAS No.: 205114-65-4Cimicifugic acid A is a cytotoxic caffeic acid derivative that can be isolated from the rhizomes of Cimicifuga heracleifolia. Cimicifugic acid A shows cytotoxic activity against cancer cells, and increases expression of cleaved PARP, thereby exhibiting pro-apoptotic activity. Cimicifugic acid A can be used for colon cancer research.
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PROTAC BET Degrader-15
0 ImagesCat. No.: HY-181729PROTAC BET Degrader-15 is a BET PROTAC degrader with DC50 values of <0.10 nM, <0.01 nM, and <0.01 nM against BRD2, BRD3, and BRD4, respectively. PROTAC BET Degrader-15 induces significant G2/M phase cell cycle arrest and triggers apoptosis. PROTAC BET Degrader-15 causes marked downregulation of c-Myc, accompanied by upregulation of the cell cycle inhibitory protein p21, downregulation of CDK6, and an increase in the apoptosis marker cleaved PARP. PROTAC BET Degrader-15 is applicable to the research of hematologic malignancies and lung cancer.
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Anticancer agent 358
0 ImagesCat. No.: HY-187679CAS No.: 3087062-38-9Anticancer agent 358 is a PARP inhibitor with antiproliferative activity against lung cancer cells and low toxicity to normal hepatocytes. Anticancer agent 358 binds to the active site of PARP via hydrogen bonds and π-π interactions with key residues, thereby promoting the accumulation of DNA damage. Anticancer agent 358 induces DNA damage, apoptosis, and autophagy in lung cancer cells. Anticancer agent 358 can be used for the research of non-small cell lung cancer.
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PARP1-IN-39
0 ImagesCat. No.: HY-174446CAS No.: 3054988-47-2
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Stigmast-5-en-3-ol
0 ImagesStigmast-5-en-3-ol induces cancer cell apoptosis and inhibits proliferation by increasing the production of Bax, Caspase-9, p53, and PARP cleavage and reducing Bcl-xl expression. Stigmast-5-en-3-ol exhibits potent inhibitory activity against glucoamylase and α-amylase and possesses high antioxidant activity. Stigmast-5-en-3-ol can be used in the research of diseases such as leukemia, breast cancer, type 2 diabetes, and obesity.
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PARP1-IN-52
0 ImagesCat. No.: HY-181158PARP1-IN-52 is a poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor that forms stable interactions with the PARP-1 active site. PARP1-IN-52 exerts anticancer activity against breast cancer cells. PARP1-IN-52 can be used for the research of breast cancer.
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PC8
0 ImagesCat. No.: HY-181999PC8 is a selective dual inhibitor of PARP1/CDK6, with an IC50 of 0.126 μM for PARP1 and 0.197 μM for CDK6. PC8 does not alter PARP1 expression, but reduces the expression of its downstream target PAR. PC8 inhibits the canonical Wnt/β-catenin signaling pathway. PC8 induces intracellular ROS accumulation and exacerbates DNA damage. PC8 inhibits the proliferation of triple-negative breast cancer (TNBC) cells. PC8 can be used for the research of triple-negative breast cancer.
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Lss-11
0 ImagesCat. No.: HY-183143CAS No.: 1392014-36-6Lss-11 is a topoisomerase inhibitor. LSS-11 enhances cell death in cancer cells by inducing apoptosis through increasing the DR5 protein level and PARP1 cleavage. LSS-11 dose-dependently reduces STAT3 phosphorylation, downregulates its target genes MDR1 and MRP1, reduces P-gp protein expressionwithout affecting P-gp transport function. Lss-11 is a chemosensitizer and shows synergistic anticancer effect with Paclitaxel (HY-B0015). Lss-11 can be used for the research of paclitaxel-resistant lung cancer.
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Antitumor agent-169
0 ImagesCat. No.: HY-162643Antitumor agent-169 (Compound B3) is a dual inhibitor PD-1/PD-L1 interaction and PARP7, with IC50s of 0.426 μM and 2.50 nM. Antitumor agent-169 exhibits an affinity to human PD-L1, with Ki of 20.2 nM. Antitumor agent-169 restores the T cell function, increases IFN-γ secretion. Antitumor agent-169 inhibits cell viability of MDA-MB-231 and Jurkat T, exhibits antitumor efficacy against melanoma in mouse model and good pharmacokinetic characteristics.
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PROTAC PARP1 degrader-5
0 ImagesCat. No.: HY-181967PROTAC 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.
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TNKS 22
0 ImagesCat. No.: HY-12601CAS No.: 1507362-00-6Synonyms: TNKS-IN-22TNKS 22 (compound 22) is an orally active and selective tankyrase inhibitor. TNKS 22 inhibits TNKS1 and TNKS2 with IC50s of 0.1 and 4.1 nM, respectively.
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TNKS-IN-4
0 ImagesCat. No.: HY-12602CAS No.: 1507362-06-2TNKS-IN-4 (compound 49) is an orally active tankyrase (TNKS) inhibitor with IC50 values of 0.1 nM and 7.6nM for TNKS1 and TNKS2, respectively. TNKS-IN-4 can be used for study of APC-mutant colorectal cancer.
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INH2BP
0 ImagesCat. No.: HY-136778CAS No.: 137881-27-7INH2BP is a poly(ADP-ribose) polymerase (PARP) inhibitor with antioxidant and anti-apoptotic activities. INH2BP reduces the production of intracellular reactive oxygen species (ROS), modulates the expression of apoptosis-related proteins such as Bax, Bcl-2 and cleaved caspase-3 and enhances cell survival through the activation of the ERK1/2 and p38 MAPK signaling pathways. INH2BP is promising for research of cardiovascular diseases.
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STK899704
0 ImagesCat. No.: HY-120339CAS No.: 1578247-29-6STK899704 is a tubulin polymerization inhibitor. STK899704 exhibits broad-spectrum inhibitory activity against various cancer cell lines with IC50 values ranging from 0.2 to 1.0 μM. STK899704 disrupts the mitotic spindle structure, inducing G2/M phase cell cycle arrest. STK899704 inhibits the migration ability of HT29 cells by downregulating the FAK-MEK-ERK signaling pathway, thereby suppressing the expression and activity of MMP-2 and MMP-9. STK899704 activates caspase-3/7/8/9, leading to PARP cleavage and inducing apoptosis. STK899704 induces cellular senescence through the p53 pathway. STK899704 can be used in research on skin cancer, lung cancer, colon cancer, and other cancers.
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KCL-440
0 ImagesCat. No.: HY-15050CAS No.: 651029-09-3KCL-440 is a CNS-penetrated PARP inhibitor, with an IC50 of 68 nM. KCL-440 has strong inhibition of PARP-1.
