PARP Inhibitor

Anticancer agent 358 is a PARP inhibitor with antiproliferative activity against lung cancer cells and low toxicity to normal hepatocytes. Anticancer agent 358 binds to the active site of PARP via hydrogen bonds and π-π interactions with key residues, thereby promoting the accumulation of DNA damage. Anticancer agent 358 induces DNA damage, apoptosis, and autophagy in lung cancer cells. Anticancer agent 358 can be used for the research of non-small cell lung cancer.

PARP1-IN-39 is an inhibitor of PARP1 with an IC₅₀ of 0.22 nM. PARP1-IN-39 has an IC₅₀ of 1.57 nM in human breast cancer cells. PARP1-IN-39 can be studied in breast, ovarian, pancreatic, and prostate cancers associated with DNA repair deficiencies, such as BRCA1/2 mutations.

TNKS 22 (compound 22) is an orally active and selective tankyrase inhibitor. TNKS 22 inhibits TNKS1 and TNKS2 with IC₅₀s of 0.1 and 4.1 nM, respectively.

KCL-440 is a CNS-penetrated PARP inhibitor, with an IC₅₀ of 68 nM. KCL-440 has strong inhibition of PARP-1.

PARP-2-IN-2 (compound 27) is a PARP 2 inhibitor with an IC₅₀ value of 0.057 μM. PARP-2-IN-2 induces cell cycle arrest and apoptosis of MCF-7 breast cancer cells. PARP-2-IN-2 can be used for the research of cancer.

4-Aminonaphthalimide is a potent PARP inhibitor and potentiates the cytotoxicity of γ-radiation in cancer cells.

PARP7/HDACs-IN-1 (compound 9l) is a dual-target inhibitor targeting PARP7/HDAC with anti-tumor activity. PARP7/HDACs-IN-1 inhibits different subtypes of PARPs and HDACs with IC₅₀s of 83.3 nM (PARP1), 3.1 nM (PARP7), 35 nM (HDAC1), 30.3 nM (HDAC2), 35.4 nM (HDAC3), and 6.4 nM respectively. (HDAC6). br/.

Telapristone acetate (CDB-4124) is a potent progesterone receptor (PR) modulator. Telapristone acetate inhibits the proliferation of ovarian cancer cells by inducing cell cycle arrest and apoptosis. Telapristone effectively inhibits the occurrence and development of spontaneous and chemically induced mammary tumors in rats. Telapristone acetate can be used for breast and ovarian cancer research.

Parp1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Parp1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Senaparib hydrochloride (IMP4297 hydrochloride) is an oral, selective PARP1/2 inhibitor with potent anti-tumor activity. Senaparib hydrochloride shows antitumor activity against advanced ovarian cancer.

Parp14 Rat Pre-designed siRNA Set A contains three designed siRNAs for Parp14 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

PARP1-IN-28 (compound 1) is a PARP1 inhibitor. PARP1-IN-28 can be used in the study of cancer.

Cajanol is an isoflavanone that can be isolated from the roots of Cajanus cajan (L.) Millsp.. Cajanol inhibits cancer cell proliferation and induces cancer cell apoptosis. Cajanol promotes the expression of Bax, inhibits the expression of Bcl-2, activates caspase-9 and caspase-3, induces PARP cleavage, arrests the cell cycle at the G2/M phase, generates ROS, disrupts mitochondrial membrane potential and triggers cytochrome c release. Cajanol induces bacterial DNA damage, disrupts bacterial cell membranes, and exerts antibacterial activity in vitro. Cajanol reduces the expression of PI3K, inhibits the phosphorylation of Akt and NF-κB, downregulates the expression and transport function of P-gp, restores the sensitivity of drug-resistant cancer cells to Paclitaxel, and inhibits the growth of Paclitaxel-resistant metastatic ovarian tumors. Cajanol is applicable to research related to breast cancer, ovarian cancer and bacterial infections.

Parp3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Parp3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

PARP-1/Proteasome-IN-1 (compound 42i) is a dual PARP-1 and proteasome inhibitor with significant inhibitory effects on breast cancer. PARP-1/Proteasome-IN-1 can downregulate the expression of BRCA1 and RAD51 to inhibit homologous recombination repair function and induce apoptosis.

CHNQD-00824 is a Terphenyllin (HY-119821) derivative with potent anticancer effect. CHNQD-00824 inhibits the proliferation and migration of cancer cells via DNA damage. CHNQD-00824 triggers apoptosis and inhibits Doxycin Hydrochloride (DOX)-induced liver-specific enlargement in zebrafish embryos. CHNQD-00824 can be used for cancer research, such as liver and breast cancer.

PARP1/2-IN-4 (compound 3) is a PARP1/2 inhibitor.

TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC₅₀ of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9.TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis.TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells.TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells.TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay.TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA).TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells.TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells.TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines.TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer.

Rucaparib-d₃ (AG014699-d₃) is the deuterated -labeled Rucaparib (HY-10617A). Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a K_i 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.

5-AIQ hydrochloride is a PARP-1 inhibitor. 5-AIQ hydrochloride is an important functional group in various drugs. 5-AIQ hydrochloride reduces the tissue injury associated with ischemia-reperfusion of the liver, it can be used for the research of the research conditions associated with ischemia-reperfusion of the liver.