1. Signaling Pathways
  2. Cell Cycle/DNA Damage
    Epigenetics
  3. PARP

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-116218C
    Amelparib hydrochloride
    Inhibitor 98.37%
    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.
    Amelparib hydrochloride
  • HY-B0960S
    Sulfabenzamide-d4
    99.74%
    Sulfabenzamide (N-Sulfanilylbenzamide)-d4 is the deuterium labeled Sulfabenzamide (HY-B0960). Sulfabenzamide is a sulfonamide antibacterial agent. Sulfabenzamide exhibit antibacterial activity against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 8739). Sulfabenzamide can promote autophagic cell autophagy in breast cancer cells through p53/ DRAM pathway. Sulfabenzamide increases caspase-3 activity, deactivates PARP1 and DNA-PK, downregulates AKT1 and AKT2. Sulfabenzamide can be used for the researches of breast cancer and bacterial infections.
    Sulfabenzamide-d<sub>4</sub>
  • HY-128853S
    Taurodeoxycholate-d6 sodium
    Activator 99.4%
    Taurodeoxycholate-d6 sodium salt is a bile salt-related anionic detergent. Taurodeoxycholate-d6 sodium salt is formed in the liver by conjugation of deoxycholate with Taurine (HY-B0351). Taurodeoxycholate-d6 sodium salt is used for isolation of membrane proteins including inner mitochondrial membrane proteins. Taurodeoxycholate-d6 (TDCA) exhibits anti-inflammatory and neuroprotective effects.
    Taurodeoxycholate-d<sub>6</sub> sodium
  • HY-142657
    PARP1-IN-7
    Inhibitor 99.80%
    PARP1-IN-7 is an inhibitor of poly(ADP-ribose) polymerase-1 (PARP1) as an anticancer agent.
    PARP1-IN-7
  • HY-102035
    PARP-2-IN-1
    Inhibitor 99.56%
    PARP-2-IN-1 is a potent and selective PARP-2 inhibitor with an IC50 of 11.5 nM.
    PARP-2-IN-1
  • HY-133124
    PARP/PI3K-IN-1
    Inhibitor 99.40%
    PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.
    PARP/PI3K-IN-1
  • HY-141481
    DP-C-4
    Inhibitor 98.15%
    DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP.
    DP-C-4
  • HY-23338
    TNKS-2-IN-1
    Inhibitor
    TNKS-2-IN-1 (Compound 13g) is a TNKS-2 inhibitor. TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM.
    TNKS-2-IN-1
  • HY-N16483
    Procyanidin B2-3'-O-gallate
    Procyanidin B2-3'-O-gallate is a mono-gallate ester that can be isolated from grape seed extract. Procyanidin B2-3'-O-gallate has anti-cancer efficacy and reduces the viability of prostate carcinoma LNCaP cells. Furthermore, Procyanidin B2-3'-O-gallate induces apoptosis, and causes caspases-9 and -3 and PARP cleavage, and down-regulates Bcl-2, Bcl-Xl and androgen receptor levels.
    Procyanidin B2-3'-O-gallate
  • HY-170935
    SRSF1-IN-1
    Activator
    SRSF1-IN-1 is a SRSF1 inhibitor. SRSF1-IN-1 inhibits SRSF1 expression, thereby modulating the splicing of Bcl-x pre-mRNA. SRSF1-IN-1 inhibits the proliferation of various cancer cells. SRSF1-IN-1 induces apoptosis in gastric cancer cells, reduces Bcl-xl expression, and upregulates cleaved PARP and caspase 3. SRSF1-IN-1 induces autophagy and promotes cell death. SRSF1-IN-1 exhibits anti-tumor activity in a mouse gastric cancer xenograft model. SRSF1-IN-1 can be used for the research of various cancers including liver cancer, gastric cancer, breast cancer, colon cancer, glioma, and melanoma.
    SRSF1-IN-1
  • HY-143338
    ART-IN-1
    Inhibitor 98.91%
    ART-IN-1 (compound 7) is a selective PARP inhibitor with IC50s of 19, 22, 2.4, >100, 1.1 µM for PARP2, TNKS2, PARP10, PARP14, PARP15, respectively.
    ART-IN-1
  • HY-168979
    Itareparib
    Inhibitor
    Itareparib is the inhibitor for PARP and exhibits antineoplastic activity.
    Itareparib
  • HY-N6651
    Isocryptotanshinone
    Inhibitor ≥98.0%
    Isocryptotanshinone is a dual STAT3 and PTP1B (IC50 = 56.1 μM) inhibitor. Isocryptotanshinone inhibits STAT3 by binding to the STAT3 SH2 domain to block phosphorylation and nuclear translocation[1][2]. Isocryptotanshinone exerts its anti-proliferative effect via the induction of cell cycle arrest, apoptosis, and pro-death autophagy, through the regulation of STAT3, AKT/mTOR and MAPK signaling pathways. Isocryptotanshinone suppresses the xenograft gastric cancer (GC) tumor growth in BALB/c nude mice. Isocryptotanshinone can be used for cancer research, such as lung cancer, breast cancer and GC.
    Isocryptotanshinone
  • HY-173349
    TDI-012804
    Inhibitor
    TDI-012804 is a TNKS2 inhibitor that selectively inhibits intracellular endogenous TNKS2 protein. TDI-012804 increases the expression of AXIN1 protein in cells that are heterozygous (Tnks1HET) and completely knocks out (Tnks1KO) for TNKS1. TDI-012804 inhibits the proliferation of ApcQ1405X/Tnks1KO organoids (EC50 of 59.1 nM) and is selectively toxic to Tnks1KO AKP-G12D and AKP-G13D organoids.
    TDI-012804
  • HY-13305
    MK-2048
    Activator 99.01%
    MK-2048 is a HIV-1 and HIV-1 integrase inhibitor. MK-2048 shows selective activity against HTLV-1-infected cells and retained potency against HIV-1 variants. MK-2048 induces apoptosis, inhibits cell growth, reduces proviral loads, and blocks HTLV-1 transmission and immortalization. MK-2048 can be used for the research of HIV-1 infection.
    MK-2048
  • HY-149086
    BPA-B9
    Activator 98.50%
    BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis.
    BPA-B9
  • HY-D1236
    Fluorescent brightener 71
    Inhibitor
    Fluorescent brightener 71 (FB71) is an inhibitor targeting deubiquitinases UCHL5 and USP14, as well as a CD40 ligand. Fluorescent brightener 71 blocks enzymatic activity, induces apoptosis, inhibits cell growth and triggers reactive oxygen species production. Meanwhile, Fluorescent brightener 71 upregulates the expression of oxidative stress-related genes gpx-4 and sod-4, and reversibly increases the protein levels of UCHL5 and USP14 through a feedback response. Fluorescent brightener 71 inhibits the growth, movement and reproductive capacity of Caenorhabditis elegans, and also exhibits concentration-dependent toxic effects. Fluorescent brightener 71 can be applied to scientific research in related fields such as breast cancer.
    Fluorescent brightener 71
  • HY-183013
    PROTAC PARP2 degrader-1
    Degrader
    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.
    PROTAC PARP2 degrader-1
  • HY-117208
    TLSC702
    Inhibitor
    TLSC702 is a human glyoxalase I (hGLO I) inhibitor with an IC50 of 2.0 μM. TLSC702 inhibits the activity of human glyoxalase I, thereby leading to the accumulation of methylglyoxal and its derived advanced glycation end products. TLSC702 inhibits tumor cell proliferation, induces apoptotic morphological changes, internucleosomal DNA fragmentation and PARP cleavage in tumor cells. TLSC702 can be used in research related to leukemia and lung cancer.
    TLSC702
  • HY-10162S3
    Olaparib-d4-1
    Inhibitor 98.59%
    Olaparib-d4-1 (AZD2281-d4-1) is the deuterium labeled Olaparib (HY-10162). 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.
    Olaparib-d<sub>4</sub>-1
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