brca1-in-1

BRCA1-IN-1 is a novel small-molecule-like inhibitor of BRCA1 with an IC50 of 0.53 μM and a Ki of 0.71 μM.

BRCA1-IN-2 is a cell membrane-crossing BRCA1 protein-protein interaction (PPI) inhibitor with antitumor activity that acts by disrupting the interaction of BRCA1 (BRCT)2 with proteins.

PARP1-IN-30 is a specific and effective PARP1 inhibitor with cytotoxic properties. It precisely inhibits PARP1 in tumor cells lacking breast cancer 1 protein (BRCA1) or BRCA2. PARP1-IN-30 holds potential for use in cancer research.

(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.

PARP-1/Proteasome-IN-1 (compound 42i) is a dual inhibitor of PARP-1 and the proteasome, demonstrating significant inhibitory effects on breast cancer. By downregulating the expression of BRCA1 and RAD51, it impairs homologous recombination repair and induces apoptosis (cellular death).

Dicycloplatin is an inducer of DNA damage. It activates doubly phosphorylated checkpoint kinase 2 (CHK2), breast cancer 1 (BRCA1), and triply phosphorylated p53 to induce DNA damage. Dicycloplatin can cause cell cycle arrest, inhibit proliferation, and trigger apoptosis in prostate cancer PC3 cells and lung cancer NCI/H446 cells. It is applicable for research in the field of cancer.

EXO1-IN-1 (Compound F684) is a potent and selective inhibitor of exonuclease 1 (EXO1) with an IC50 of 15.7 μM. It inhibits DNA end resection, promotes the accumulation of DNA double-strand breaks, and induces S-phase polyadenylation, thereby disrupting DNA repair pathways in homologous recombination-deficient (HRD) cancer cells. This selectivity effectively targets and kills tumor cells with homologous recombination gene defects, such as BRCA1/2 mutations. EXO1-IN-1 holds promise for researching cancers with homologous recombination deficiencies, including BRCA-related tumors.

Theophylline-platinum(IV) prodrug-1 is a PARP-1 inhibitor. It enhances DNA damage, ROS generation, mitochondrial dysfunction, apoptosis, and S-phase arrest in SKOV3-BRCA1-KD cells while reducing invasion and metastasis. Additionally, it exhibits strong antitumor activity in SKOV3-BRCA1-KD xenograft tumor models. This compound is used for ovarian cancer research.

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.

LCS-1 is a selective superoxide dismutase 1 (SOD1) inhibitor and pyridazin-3-one derivative that displays trypanocidal activity at high concentrations.LCS-1 inhibits superoxide dismutase 1 inducing ROS-dependent death and degrading PARP and BRCA1 in glioma cells.

SC10914 is a highly potent PARP inhibitor (PARP1 IC50 = 7.87 nM) with potent anti-proliferative activity against human BRCA deficient tumor cells (MDA-MB-436, BRCA1 deficient, IC50 = 4.03 nM, Capan-1 BRCA2 deficient, IC50 = 11.66 nM) and PTEN deficient tumor cells (HGC-27,PTEN deficient, IC50 = 0.35 μM). SC10914 showed potent anti-tumor activity in BRCA1/2 mutant tumor models and better pharmacokinetics profile has the potential to be selected as the clinical candidate for the treatment of treatment of BRCA1/2 deficient cancers.

BAP1-IN-1 is an inhibitor of the catalytic activity of BRCA1-associated protein 1 (BAP1), which is related to cancer and can be used to study cancer.

PARP1-IN-15 (Compound 6) is a PARP1 inhibitor that also inhibits tankyrase (TNKS) and promotes DNA double-strand breaks, leading to tumor cell apoptosis. It exhibits anti-cancer activity in triple-negative breast cancer (TNBC) cells and patient-derived organoids, making it useful for TNBC research, including cases with or without BRCA1 mutations [1].

PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor with an IC50 of 0.6 ± 0.1 nM, displaying antiproliferative effects on MDA-MB-436 (BRCA1 −/−) and Capan-1 (BRCA2 −/−) cells, with IC50 values below 0.3 nM [1].

TG2-179-1 is a BRCA1-associated protein 1 (BAP1) inhibitor with potential anticancer activity. TG2-179-1 exhibits potent cytotoxic activity against colon cancer cells and induces apoptosis. TG2-179-1 can be used in colon cancer research. TG2-179-1 is a BRCA1-associated protein 1 (BAP1) inhibitor with potential anticancer activity.