PARP Inhibitor

Olaparib-d₄-2 is the deuterium labeled Olaparib (HY-10162). Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC₅₀s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator. Olaparib cannot cross the intact blood-brain barrier (BBB).

PARP1-IN-12 is a potent PARP1 inhibitor with an IC₅₀ of 2.99 nM. PARP1-IN-12 exhibits antiproliferative activity, can induce cell apoptosis and cause cycle arrest at G2/M phase. PARP1-IN-12 also can induce DNA double strand breaks (DSBs) in BRCA-deficient cells.

LT-626 is a potent PARP inhibitor with an IC₅₀ of 1.60 nM. LT-626 inhibits cellular PAR synthesis with an EC₅₀ of 17.9 nM and shows enhanced cytotoxicity in colorectal cancer cells harboring MRE11 mutations. LT-626 exhibits synergistic effects with Cisplatin (HY-17394), Oxaliplatin (HY-17371), and SN-38 (HY-13704) in colorectal cancer cells. LT-626 can be used for colorectal research.

TNKS-2-IN-4 (Compound 17) is a selective TNKS-2 inhibitor with an IC₅₀ of 19 nM. TNKS-2-IN-4 exhibits anticancer activity against colorectal cancer.

PP-048 is a selective dual inhibitor of Polθ/PARP1, with IC₅₀ values of 4.9 nM and 6.8 nM for the Polθ helicase/ATPase domain and PARP1, respectively. PP-048 impairs the compensatory DNA repair capacity of homologous recombination-deficient cells by simultaneously inhibiting the DNA repair functions associated with Polθ and PARP1, thereby exacerbating DNA double-strand damage and inducing apoptosis. PP-048 exhibits more potent selective antiproliferative activity against HR-deficient cancer cells. PP-048 can be used in studies related to Polθ/PARP1 dual-target inhibition, synthetic lethality, DNA damage repair, and HR-deficient triple-negative breast cancer.

L-2286 is an orally active PARP-1 inhibitor. L-2286 alleviates carotid artery remodeling, oxidative stress and inflammation in spontaneously hypertensive rats, protects neurons in the dorsal hippocampus, and reduces pyramidal cell loss and gliosis without affecting blood pressure. L-2286 can be used in research related to hypertension.

RBN010860 (example 150) is a potent PARP7 inhibitor with an IC₅₀ of <0.1 μM. RBN010860 can be used for the study of cancer.

CEP-6800 is an inhibitor of PARP-1 with chemopotentiating ability. CEP-6800 attenuates irinotecan (HY-16562)- and Temozolomide (HY-17364)-induced poly(ADP-ribose) accumulation in LoVo as well as HT29 xenografts. CEP-6800 can suppress Calu-6 tumor growth. CEP-6800 can be studied in anti-cancer research.

MAHS-3 is a thymidylate synthase (TS) and dihydrofolate reductase (DHFR) inhibitor, with IC₅₀ values of 5.279 μM and 52.60 μM against human targets, respectively. MAHS-3 exhibits broad-spectrum antiproliferative activity against cancer cells, induces cell cycle arrest, activates endogenous caspase-dependent apoptosis, reduces MMP levels, inhibits cell migration, increases intracellular NO levels, and promotes autophagy activity. MAHS-3 can be used in cancer-related research.

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

PARP1-IN-35 (compound T26) is a selective, orally active, cross -the blood-brain barrierPARP1 inhibitor with IC₅₀ values of 0.2, 122 nM for PARP1, PARP2, respectively. PARP1-IN-35 shows antiproliferative activity and anticancer activity. PARP1-IN-35 has the potential for the research of breast cancer.

Anisomelic acid is a human papillomavirus HPV16 E6 and HPV E7 depletor. Anisomelic acid directly interacts with HPV16 E6, promotes its ubiquitination and proteasomal degradation by recruiting E3 ubiquitin ligase, downregulates E6 and facilitates E7 degradation. Anisomelic acid induces endogenous mitochondrial apoptosis, activates caspase-3, causes cleavage of PARP, and triggers p53-independent endogenous apoptosis by depleting cIAP2. Anisomelic acid can be used in research related to HPV-positive cancers and cervical cancer.

TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC₅₀ value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4%.

ARCher-142 (compound S8) is a potent tankyrase inhibitor. ARCher-142 selectively binds to ARC4 with potency of 8 µM.

Solanesol (Standard) is the analytical standard of Solanesol (HY-N0576). This product is intended for research and analytical applications. Solanesol is an orally active aliphatic terpene alcohol. Solanesol is mainly found in tobacco and other Solanaceae plants. Solanesol induces HO-1 and Hsp70 expression, activates p38 and Akt signaling pathways, and inhibits Apoptosis (reduces caspase-3 and PARP cleavage). Solanesol has antioxidant, anti-inflammatory, and neuroprotective activities. Solanesol can be used in the research of Huntington's disease, alcoholic liver disease, chronic inflammatory pain, anxiety, Alzheimer's disease, and bipolar disorder.

PARP1/NAMPT-IN-2 (Compound 13j) is a dual PARP/NAMPT inhibitor with IC₅₀ values of 0.8 nM and 18 nM for PARP1 and NAMPT, respectively. PARP1/NAMPT-IN-2 can inhibit the proliferation, migration and induce apoptosis of breast cancer cells. PARP1/NAMPT-IN-2 can be used for the research of triple-negative breast cancer.

CEP-9722, the proagent of CEP-8983, is a selective and orally active PARP-1 and PARP-2 inhibitor with IC₅₀s of 20 nM and 6 nM, respectively. CEP-9722 has anticancer effects.

PARP7-IN-21 (compound 128) is a potent inhibitor of PARP7, with the IC₅₀ of ＜ 10 nM.

CDK9/PARP-IN-1 (compound 37) is a CDK9/PARP inhibitor. CDK9/PARP-IN-1 inhibits CDK9 and PARP1 with IC₅₀s of 118 and 107 nM, respectively. CDK9/PARP-IN-1 exhibits broad-spectrum antiproliferative effects across multiple cancer cell lines.

PARP10-IN-4 (compound 12Z) is a potent PARP10 inhibitor with a pIC₅₀ of 7.95. also shows inhibitory activity against TNKS1, TNKS2, and PARP11 with pIC₅₀ values of 6.95, 7.03, and 7.01, respectively.