PARP 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.

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.

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.

6(5H)-Phenanthridinone is a potent PARP-1 inhibitor and immunomodulator. 6(5H)-Phenanthridinone inhibits cell proliferation and can be used in cancer research.

PARP-1-IN-4 is a PARP-1 inhibitor. PARP-1-IN-4 has inhibitory activity against PARP-1 with IC₅₀ value of 302 μM. PARP-1-IN-4 can be used for the research of lung adenocarcinoma.

ARTD3/PARP3-IN-1 is an unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3.

Rucaparib (Standard) is the analytical standard of Rucaparib. This product is intended for research and analytical applications. Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research.

LS-75 is a PARP-1 inhibitor with blood-brain permeability and IC₅₀ value of 18 μM. LS-75 has neuroprotective activity.

AKT-IN-28 is an Akt allosteric inhibitor, a derivative of Shikonin (HY-N0822). AKT-IN-28 effectively binds to the allosteric site of Akt through hydrophobic and hydrogen interactions with Kd of 2.07 μM. AKT-IN-28 significantly inhibits Akt activity, induces cell apoptosis, arrests cell cycle in G2/M phase, and suppresses proliferation, migration and metabolism of KRAS mutant colorectal cancer cells.

FGFR-IN-28 is a FGFR inhibitor with inhibitory activity against multiple subtypes of the FGFR family, with an IC₅₀ of 4.4 nM against FGFR4. FGFR-IN-28 inhibits kinase activity and phosphorylation processes, and blocks the downstream MAPK and AKT signaling pathways. FGFR-IN-28 induces cellular DNA damage, cell cycle arrest, apoptosis and ferroptosis, and reduces the adhesion, invasion and metastasis abilities of cancer cells. FGFR-IN-28 exhibits anti-tumor activity in in vitro experiments on colon cancer cells, and inhibits tumor growth in colon cancer xenograft models. FGFR-IN-28 can be used in colon cancer-related research.

TP-110 is a proteasome inhibitor. TP-110 specifically inhibits the protease-like activity of the 20S proteasome, but does not affect the trypsin-like or peptidyl-glutamyl peptide hydrolysis activity. TP-110 inhibits the NF-κB pathway, activates caspase-8, -9, and -3, and causes PARP cleavage, significantly reducing the levels of cIAP-1 and XIAP. TP-110 causes cell cycle arrest at the G2/M phase and promotes apoptosis of cancer cells. TP-110 can be used in cancer research of prostate cancer and multiple myeloma, etc.

Anticancer 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.

Apoptosis inducer 45 is an apoptosis inducer. Apoptosis inducer 45 is cytotoxically active against the MCF-7 cell line. Apoptosis inducer 45 elicits MCF-7 cell apoptosis via the mitochondrial pathway (increases the Bax/Bcl-2 ratio) by activating cleavage of caspase-9, thereby inducing the fragmentation of DNA repair protein PARP. Apoptosis inducer 45 also can induce caspase-8 cleavage, subsequently initiating cleavage of caspase-3 and its downstream protein PARP to culminate in the extrinsic apoptosis. Apoptosis inducer 45 can be used in the research of breast cancer.

GPS167 is a CLK kinase inhibitor that potently and selectively inhibits recombinant human CLK1, CLK2 and CLK4. By inhibiting CLK-mediated phosphorylation of SRSF10, GPS167 upregulates the protein-binding ability of CLK1 and CLK4 with SRSF10, downregulates oncogenic BCLAF1-L and upregulates tumor-suppressive BCLAF1-S, regulates alternative splicing of genes such as MDM2 and MDM4, stabilizes p53 protein and induces DNA damage, ultimately triggering tumor cell apoptosis. GPS167 can block the epithelial-mesenchymal transition process of tumors, activate intracellular double-stranded RNA-mediated antiviral immune responses, and produce synergistic cytotoxicity when combined with microtubule-targeting drugs. GPS167 can be used in research related to various cancers including colorectal cancer.

Nudifloramide-d₆ (2PY-d₆) is deuterium-labeled Nudifloramide (HY-113432).

Anticancer agent 71 (Compound 4b) is a potent anticancer agent and induces apoptosis. Anticancer agent 71 arrests cell cycle at G2/M phase and induces apoptosis through upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression levels. Anticancer agent 71 shows antiproliferative activity.

2-Methylquinazolin-4-ol (Standard) is the analytical standard of 2-Methylquinazolin-4-ol. This product is intended for research and analytical applications. 2-Methylquinazolin-4-ol is a potent competitive poly(ADP-ribose) synthetase inhibitor, with a Ki of 1.1 μM. 2-Methylquinazolin-4-ol mammalian aspartate transcarbamylase (ATCase) inhibitor, with 0.20 mM[1][2].

PARP7-IN-19 (compound 5a) is an inhibitor of PARP7 ( IC₅₀ ≤10nM). PARP7-IN-19 can be used in the research area of tumors.

PARP1-IN-38 (compound ent-6_P) is a potent PARP1 inhibitor with an IC₅₀ of 10 μM. PARP1-IN-38 shows selective cytotoxic activity in BRCA mutant cancer cells

Lerzeparib is an (ADP-ribose) polymerase (PARP) inhibitor, with antineoplastic activity.