parp 2 in 1

PARP-2-IN-1 is a potent and selective inhibitor of PARP-2 (IC50 of 11.5 nM).

PARP-1-IN-2 is a potent PARP1 inhibitor that crosses the blood-brain barrier (IC50: 149 nM).PARP-1-IN-2 showed significant antiproliferative activity against the human lung adenocarcinoma epithelial cell line A549 in cellular assays.PARP-1-IN-2 induced apoptosis in A549 cells.

TOPOI PARP-1-IN-2 (compound 6c) serves as a dual inhibitor targeting both PARP-1 and topoisomerase 1 (TOPO-1), with IC50 values of 32.2 nM and 46.2 nM, respectively. This compound exhibits greater selectivity for PARP-1 over PARP-2. Additionally, TOPOI PARP-1-IN-2 disrupts the S phase of the cell cycle and induces apoptosis in the NCI-60 cancer cell lines.

PARP-1- 2-IN-1 is a potent inhibitor of PARP-1 (IC50: 0.51 nM) and PARP-2 (IC50: 23.11 nM).

PARP-2 1-IN-2, an enantiomer of Veliparib, serves as a potent inhibitor of PARP, demonstrating inhibition constants (Kis) of 2 nM for PARP-2 and 5 nM for PARP-1. This compound exhibits a half-maximal effective concentration (EC50) of 3 nM in cell-based assays evaluating PARP activity [1].

PARP-1 2-IN-2-IN-1 (Compound 12e) effectively inhibits PARP1 2 and CDK12 with IC50 values of 34 nM, 30 nM, and 285 nM respectively, impairing DNA damage repair and inducing cell cycle arrest and apoptosis. This compound also hampers the proliferation of TNBC cells and the growth of TNBC xenograft tumors [1].

PARP-1 2 7-IN-1 (compound 86) is a highly effective inhibitor of PARP-1 2 7, demonstrating an IC50 value of less than 10 nM .

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax Bcl-2, activating caspases as well as cleaving PARP.

PARP1 2 TNKS1 2-IN-1 is a multi-target inhibitor of PARP-1, PARP-2, TNKS1, and TNKS2, with potential anti-tumor activity that induces apoptosis.

TNKS-2-IN-1 is a TNKS-2 inhibitor.TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM, respectively.TNKS-2-IN-1 has antimicrobial activity against E. coli and S. aureus.TNKS-2-IN-1 inhibits the release of IL-1β from the NLRP3 inflammasome (IC50: 5 μM) by inhibiting IL-1β release from ATP-stimulated J1A.774 cells.

PARP-1-IN-3 is a potent PARP-1 inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 0.25 nM and 2.34 nM, respectively.PARP-1-IN-3 has potential anti-inflammatory activity, induces apoptosis, and arrests the cell cycle in the G2 M phase.PARP-1-IN-3 may be useful for the study of cancer-related diseases. cancer-related diseases.

PARP PI3K-IN-1 is a novel dual poly (ADP-ribose) polymerase (PARP) and phosphatidylinositol 3-kinase (PI3K) dual inhibitor with anticancer, antitumour and antiproliferative activities for the study of breast, pancreatic and lung cancers.

PARP7-IN-16 free base is the freebase form of PARP7-IN-16. As a selective oral inhibitor of PARP-1 2 7, it demonstrates IC50 values of 0.94, 0.87, and 0.21 nM, respectively. This compound is utilized in the research of breast and prostate cancer.

AZ9482 is a selective and potent inhibitor of PARP featuring an amide linkage to a 2-piperazinyl-3-cyano-pyridine. AZ9482 exhibits very potent activity of centrosome declustering with EC50 of < 18 nM in HeLa cells.

1. Dehydrocorydaline(DHC) not only inhibits antibody-mediated allergic reactions but also influences cell-mediated allergic reactions, and the inhibitory effect of Corydalis Tuber on allergic reactions may be partially attributed to DHC. 2. Dehydrocorydal

1. Cucurbitacin IIA (Dihydrocucurbitacin Q1) can induce apoptosis and enhance autophagy , contributes to the anti-inflammatory activity of Cucurbitacin IIA against inflammation-related diseases. 2. Cucurbitacin IIA is a novel class of anti-cancer drug in suppression of cancer cell expansion by disrupting the actin cytoskeleton and directing the cell to undergo PARP-mediated apoptosis through the inhibition of survivin downstream of JAK2 STAT3.

PARP EZH2-IN-1 is a novel dual inhibitor targeting PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM), showing promising potential for treating triple-negative breast cancer with wild-type BRCA.

1. 5,7-Dihydroxychromone (5,7-Dihydroxy-4H-Chromen-4-One) isolated from DME is one of the active compounds that may contribute to regulate blood glucose levels. 2. 5,7-Dihydroxychromone exerts neuroprotective effect against 6-OHDA-induced oxidative stress and apoptosis by activating Nrf2 ARE signal . 3. 5,7-Dihydroxychromone induces the translocation of Nrf2 to the nucleus and increases Nrf2 ARE binding activity which results in the up-regulation of the expression of Nrf2-dependent antioxidant genes, including HO-1, NQO1, and GCLc.

Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4].

Rucaparib (AG014699) acetate is a highly effective oral inhibitor of PARP proteins, specifically targeting PARP-1, PARP-2, and PARP-3, with a Ki value of 1.4 nM for PARP1. Additionally, it exhibits inhibitory action on hexose-6-phosphate dehydrogenase (H6PD) to a moderate extent. Rucaparib acetate shows promise in the field of research for castration-resistant prostate cancer (CRPC). [1] [2] [3] [4]

Rucaparib (AG014699) tartrate is an orally active inhibitor of PARP proteins (PARP-1, PARP-2, and PARP-3) and acts on PARP-1 (Ki: 1.4 nM). It is also a hexose hexaphosphate dehydrogenase (H6PD) inhibitor and has potential for use in the study of destructive resistant prostate cancer (CRPC).

Rucaparib (AG014699) camsylate is an orally active inhibitor of PARP proteins (PARP-1, PARP-2, and PARP-3) with a Ki=1.4 nM for PARP-1, and also inhibits hexose hexaphosphate dehydrogenase (H6PD). Rucaparib camsylate has potential for investigation in debulking resistant prostate cancer (CRPC) studies.

AZ6102 is a potent TNKS1 2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.

JPI 547, also known as NOV 1402, is an oral inhibitor of PARP 1 2 and Tankyrase 1 2. JPI-547 demonstrated anti-tumor activity in BRCA-deficient xenograft models as a single-agent and in combination with chemotherapy and immune checkpoint inhibitors.