PARP Inhibitor

PARP1-IN-36 (compound 11) is a 4-carboxamido-isoindolinone derivative and a selective PARP-1 inhibitor with a K_d < 0.01 μM. PARP1-IN-36 can be utilized in cancer, cardiovascular diseases, nervous system injury and inflammation research.

Fucosterol (Standard) is the analytical standard of Fucosterol. This product is intended for research and analytical applications. Fucosterol is a sterol isolated from algae, seaweed or diatoms. Fucosterol exhibits various biological activities, including antioxidant, anti-adipogenic, blood cholesterol reducing, anti-diabetic and anti-cancer activities. Fucosterol regulates adipogenesis via inhibition of PPARα and C/EBPα expression and can be used for anti-obesity agents development research.

Parp2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Parp2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

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

HER2-IN-23 is a selective HER2 inhibitor. HER2-IN-23 reduces in total HER2 expression rather than in phosphorylated HER2 (p-HER2). HER2-IN-23 reduces cyclin D1 level and stimulates PARP cleavage. HER2-IN-23 can be used for the study of HER2-positive breast cancer.

VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC₅₀s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC₅₀: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent.

NU 1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor with a K_i of 6 nM. NU 1085 shows strong cytotoxicity to cancer cells (LC₅₀ = 83-94 μM) and can enhance the anticancer effect of Temozolomide (HY-17364). NU 1085 can be used for the research of cancer, such as lung cancer.

Picolinamide (Standard) is the analytical standard of Picolinamide. This product is intended for research and analytical applications. Picolinamide (2-Picolinamide) is an inhibitor of Poly(ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.

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

ADP-ribose/PARP-IN-1 (Compound Ex.16) is a conjugated compound. ADP-ribose/PARP-IN-1 contains disease targeting moieties, PARP inhibitor moieties, cleavable linkers, chelators. ADP-ribose/PARP-IN-1 targets specific targets through the disease targeting moiety and selectively delivers PARP inhibitors to tumor cells. The cleavable linker of ADP-ribose/PARP-IN-1 releases the PARP inhibitor under appropriate conditions, inhibiting PARP to prevent DNA damage repair, while the radionuclide carried by the chelator exerts a killing effect. ADP-ribose/PARP-IN-1 can be used in the research of prostate cancer.

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).

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.

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.

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.

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.

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.

Antitumor agent-104 (Compound 9) is an antitumor agent by inhibiting DNA damage repair in tumors. Antitumor agent-104 inhibits PARP1 enzymatic activity and the PAR protein level. Antitumor agent-104 also inhibits the expression of CDK12.