parp1-in-5

PARP1-IN-5 is a potent, selective, orally active, low-toxicity PARP-1 inhibitor with an IC50 value of 14.7 nM. PARP1-IN-5 can be used in cancer research.

PARP1-IN-5 dihydrochloride is an orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.

1, 5-Isoquinolinediol is an inhibitor of poly(ADP-ribose) synthetase (PARP1; IC50: 0.39 μM). The poly(ADP-ribose) polymerases (PARPs) form a family of enzymes with roles in DNA repair and apoptosis. 1, 5-Isoquinolinediol has been used to study the role of

(rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is an orally active inhibitor of PARP1/2, with Ki values of 1.2 nM and 0.87 nM, respectively. It inhibits cellular PARylation at an EC50 of 2.51 nM. This compound leads to the accumulation of DNA damage and suppresses the proliferation of BRCA1/2-mutated MX-1 and Capan-1 cells, with IC50 values of 0.3 nM and 5 nM, respectively. Additionally, (rac)-Talazoparib exhibits antitumor activity in mouse models.

TNKS-2-IN-3 (Compound 5) is a selective and competitive inhibitor of Tankyrase 2 (TNKS2), with an IC50 value of 0.3 nM. It exhibits over 20-fold selectivity for TNKS2 compared to TNKS1 and more than 100-fold selectivity over PARP1/2. By inhibiting TNKS2-mediated ADP ribosylation, TNKS-2-IN-3 stabilizes axin and suppresses the Wnt/β-catenin pathway, demonstrating antiproliferative activity in colorectal cancer cells. TNKS-2-IN-3 holds potential for research in solid tumors with aberrant Wnt pathway activation, such as colorectal cancer.

PARP1-IN-43 (Compound 5350) is a PARP1 inhibitor with an IC50 of 5 nM that can cross the blood-brain barrier (BBB). It is useful for studying homologous recombination (HR) deficient cancers within the central nervous system (CNS).

Phosphoramide mustard cyclohexanamine is the active metabolite of cyclophosphamide, an alkylating agent that cross-links DNA strands, organizes cell division and causes cell death, and has antitumor activity.

5-Hydroxymethyl-2'-deoxycytidine is an oxidized derivative of 5-methyl-2'-deoxycytidine (5-mdC) in DNA, causing DNA damage reactions, chromosomal aberrations, replication fork damage, and loss of cell viability.5-Hydroxymethyl-2'-deoxycytidine is an oxidized derivative of 5-methyl-2'-deoxycytidine in DNA. Hydroxymethyl-2'-deoxycytidine replication fork instability is associated with the presence of poly(ADP-ribose) polymerase 1 (PARP1) on chromatin.

AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.

5-Hydroxy Lansoprazole Sulfide is an inhibitor of fatty acid synthase (FASN). FASN, which is responsible for de-novo synthesis of lipids, has been found to be overexpressed in cancerous tissue. 5-Hydroxy Lansoprazole Sulfide specifically inhibits enoyl reductase, and was found to more effectively inhibit FASN function than lansoprazole and was also more efficient at regulating NHEJ repair of oxidative DNA damage via PARP1.

Pomalidomide 5-piperidylamine serves as a conjugate of a linker and an E3 ligase ligand. This compound is utilized in the synthesis of PROTACPARP1 degrader-2.

Venadaparib (NOV140101) (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib is insensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSBs) and can be used in solid tumor research.

Olaparib (Standard) is a reference standard for research and analysis in studies involving Olaparib. Olaparib (KU0059436) is a small molecule inhibitor of PARP1/PARP2 (IC50=5/1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.