parp-1-in-2

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-IN-23 (Compound I16) is an orally bioavailable, selective inhibitor of PARP-1, exhibiting an IC50 of 12.38 nM. This compound demonstrates efficacy in inhibiting tumor growth in vivo.

PARP1-IN-27 (Compound 9B) serves as an inhibitor of both PARP1 and PARP2, exhibiting IC 50 values of 2.53 nM and 6.45 nM, respectively, in SUM149PT cells. This compound effectively suppresses the proliferation of BRCA-mutated cancer cell lines such as SUM149PT, HCC1937, and Capan-1, with respective IC 50 values of 0.62, 1.91, and 4.26 μM. Additionally, PARP1-IN-27 exacerbates DNA double-strand breaks, enhances ROS production, causes G2/M phase cell cycle arrest, and triggers apoptosis in SUM149PT cells.

PARP1-IN-29 is an orally active PARP-1 inhibitor with an IC50 of 6.3 nM. When labeled with [18F], PARP1-IN-29 can be utilized for positron emission tomography (PET) imaging, specifically targeting PARP-1 in tumors. This compound is useful in oncology and imaging studies, particularly for detecting PARP-1 activity in cancer.

PARP1-IN-22 (compound 15) acts as a highly effective PARP1 inhibitor, demonstrating an IC 50 value of less than 10 nM.

PARP1-IN-21 (example 16) serves as a highly effective PARP1 inhibitor, exhibiting an IC50 value of less than 10 nM.

PARP1-IN-20 (compound 19A10) serves as a highly effective inhibitor of PARP1, demonstrating an IC50 value of 4.62 nM, but exhibits a relatively minimal PARP-trapping effect when compared with Veliparib, where it shows an IC50 (MDA-MB-436) greater than 100 μM.

PARP1-IN-28 (compound 1) is a PARP1 inhibitor.

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.

PARP1-IN-8 (N-(3-chlorophenyl)-3-(1-oxo-4-phenylphthalazin-2(1H)-yl)propanamide) is an effective inhibito of PARP1 (IC50 = 97 nM).

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

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.

PARP1-IN-37 (Compound 8) is an orally active and selective inhibitor of poly (ADP-ribose) polymerases 1 and 2 (PARP1/2), with an IC50 value of 24 nM for PARP1. It inhibits PARP activity in cells with an EC50 value of 3.7 μM and holds potential for research on BRCA-mutated tumors, such as breast and ovarian cancers.

PIM-1/HDAC-IN-2 is a potent dual inhibitor of PIM/HDAC, exhibiting an IC50 value of 0.11 μM. It synergistically impedes cell proliferation through the inhibition of PIM1 kinase and the selective suppression of HDAC6. This compound effectively induces PARP cleavage, causing cell cycle arrest in the G1 phase and reducing S phase cells. PIM-1/HDAC-IN-2 demonstrates significant anticancer activity in the MV4-11 tumor xenograft model, with minimal toxicity.

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]