parp-7

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.

Compound A5b, also known as JMJD3 HDAC-IN-1, is a dual inhibitor that targets both JMJD3 (Jumonji domain-containing protein demethylase 3) and HADC1 (histone deacetylase, IC50 = 16 nM). It induces hypermethylation of histone H3K27 and hyperacetylation of H3K9, while also promoting apoptosis through the cleavage of caspase-7 and PARP. This compound has demonstrated the ability to effectively inhibit cancer cell cloning, migration, and invasion [1].

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.

VEGFR PARP-IN-1 (Compound 14b) is a dual inhibitor of VEGFR and PARP with IC50 values of 191 nM and 60.9 nM, respectively. It impairs DNA damage repair pathways, promotes apoptosis, and halts cells in the G2 M phase. This compound demonstrates considerable antiproliferative activity against BRCA wild-type breast cancer cells, with IC50 values of 4.1 μM for MDA-MB-231 cells and 3.5 μM for MCF-7 cells, indicating its potential as an antitumor and anti-metastasis agent [1].

5,7,4'-Trimethoxyflavone (4',5,7-Trimethoxyflavone) is isolated from Kaempferia parviflora (KP) which is a medicinal plant from Thailand.

DLC-50 is a dual inhibitor of PARP-1 and HDAC-1, exhibiting IC50 values of 1.2 nM and 31 nM respectively. It hinders the proliferation of cancer cells such as MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 values of 0.3 μM, 2.7 μM, and 2.41 μM respectively. Additionally, DLC-50 induces apoptosis in MDA-MB-231 cells and causes cell cycle arrest at the G2 phase.

Anticancer agent 137 (8q), a potent PI3k inhibitor, exhibits broad-spectrum anticancer activity by inducing G2 M cell cycle arrest and apoptosis. It increases levels of cleaved PARP, and caspases 3 and 7, making it useful in cancer research [1].

PARP7-IN-16 (compound 36) is a potent, selective, and orally active inhibitor of PARP-1 2 7, with IC50 values of 0.94, 0.87, and 0.21 nM, respectively, and holds potential applications in breast and prostate cancer research [1].

ME0328 is a potent, selective PARP inhibitor with an IC50 of 0.89 μM for PARP3, showing approximately 7-fold selectivity over PARP1.

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

Dehydrocavidine (Dehydrocorydaline) has antitumor activity, it inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax Bcl-2, activating caspases as well as cleaving PARP.

OUL245, a 7-Hydroxy derivative, selectively inhibits PARP2 with an IC50 of 44 nM. Additionally, it exhibits inhibition against other PARP and TNKS enzymes, displaying IC50 values ranging from 2.9 to 8.8 μM.

RBN-2397 is a potent, selective and orally active accross species NAD+ competitive PARP7 inhibitor with IC50 less than 3 nM.

MAPK-IN-3 (Compound 4a) is an antiproliferative agent demonstrating significant inhibitory effects on KYSE 30, HCT 116, and HGC 27 cell lines, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. This compound arrests the cell cycle via a p53-dependent mechanism and induces apoptosis through a p53-independent pathway. It reduces the expression of cell cycle-related proteins, such as Cyclin D1 and Cyclin B1, while increasing pro-apoptotic proteins like cleaved PARP, cleaved caspase-7, and cleaved caspase-9. MAPK-IN-3 also decreases anti-apoptotic proteins such as Bcl-2, elevates ROS levels in KYSE 30 cells, and enhances the expression of ROS-related MAPK pathway members, including p-ERK, p-p38, and p-JNK.

Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid exhibiting anti-inflammatory and anti-cancer activities and can enhance the activation of p38 MAPK.

PAWI-2 functions as both a p53 activator and a Wnt inhibitor. It suppresses β3-KRAS signaling independently of KRAS and selectively inhibits the phosphorylation of TBK1. Additionally, PAWI-2 triggers apoptosis (activation of caspase-3 7) and induces PARP cleavage. It facilitates the translocation of retinoblastoma protein into the nucleus, leading to G2 M cell cycle arrest. PAWI-2 reverses the cancer stem cell-like properties of KRAS-dependent human pancreatic cancer stem cells (hPCSC) and overcomes drug resistance. Moreover, it inhibits the growth of hPCSC tumors in an orthotopic xenograft mouse model.

Aviculin, a lignan glycoside, exhibits significant anticancer properties, particularly in inhibiting the metabolic activity of MCF-7 cells to below 50%, with an IC 50 value of 75.47 μM. It promotes apoptosis in breast cancer cells via the intrinsic apoptosis pathway, enhancing the expression of initiator caspase-9, executioner caspase-7, and poly (ADP-ribose) polymerase (PARP). Furthermore, Aviculin leads to an increased Bax Bcl-2 ratio, underlying its potential as an effective anticancer agent.

Anticancer agent 64 (compound 5m) exhibits potent cytotoxicity against CCRF-CEM cells with an IC50 value of 2.4 μM, induces apoptosis by activating caspase 3 and 7 and causing PARP cleavage, and significantly disrupts mitochondrial membrane potential, thereby contributing to its anticancer efficacy [1].

ART-IN-1 (compound 7) is a selective inhibitor of PARP with IC50 values of 19 μM for PARP2, 22 μM for TNKS2, 2.4 μM for PARP10, >100 μM for PARP14, and 1.1 μM for PARP15 [1].