nbc

NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor with an IC50 of 574 nM. It acts independently of Ca 2+ and inhibits Nigericin-induced inflammasome activation in THP-1 cells, as well as Imiquimod-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs) [1].

Potent NLRP3 inflammasome inhibitor (IC50 = 60-80 nM). Inhibits nigericin- and ATP-induced IL-1β release. Baldwin et al (2017) Boron-Based Inhibitors of the NLRP3 Inflammasome. Cell Chem.Biol. 24 1321 PMID:28943355 |Redondo-Castro et al (2018) Development of a characterised tool kit for the interrogation of NLRP3 inflammasome-dependent responses. Sci.Rep. 8 5667 PMID:29618797

NBC functions as an antioxidant and antiozonant. When applied topically at a concentration of 35% in a powder form, it offers protection to P. vulgaris leaves from ozone-induced bronzing. Additionally, NBC does not exhibit mutagenic properties in S. typhimurium according to the Ames test.

S0859 is an N-cyanosulphonamide that blocks the sodium/bicarbonate cotransporter (NBC, also known as SLC4A7), which regulates intracellular pH.

Anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic compound that targets mitochondrial DNA G-quadruplexes (mtG4). Under white light exposure, it exhibits an IC50 of 0.42 μM against 4T1 cells. Anti-TNBC agent-8 tightly binds to mtG4, leading to the production of substantial reactive oxygen species (ROS) under illumination. This results in the loss of mitochondrial membrane potential (MMP), reduced ATP production, elevated ROS levels, and significant apoptosis in triple-negative breast cancer (TNBC) cells, thus demonstrating its tumor growth inhibitory activity. Anti-TNBC agent-8 is applicable for research in TNBC.

Anti-TNBC agent-9 (Compound 3as) is an anticancer agent used for treating triple-negative breast cancer (TNBC). It exhibits significant inhibitory activity against MDA-MB-453 cells, with an IC50 value of 8.5 μM. Anti-TNBC agent-9 impedes tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. Additionally, it inhibits tumor cell proliferation by inducing apoptosis, achieved through the increased expression of pro-apoptotic protein BAX and decreased expression of anti-apoptotic protein BCL-2.

Anti-TNBC agent-4 (compound 7) exhibits strong inhibitory activity against various TNBC cells, with an IC50 range of 0.37 to 1.52 μM. It inhibits IKKβ-mediated phosphorylation of IκB and p65, and induces apoptosis in TNBC cells.

Anti-TNBC agent-5 (compound 10C) is an inhibitor of triple-negative breast cancer (TNBC) that exhibits favorable stability and pharmacokinetic properties. It demonstrates antiproliferative activity across various cancer cell types. Additionally, in the MDA-MB-231 xenograft model, anti-TNBC agent-5 effectively suppresses TNBC lung metastasis activity. This compound is useful for cancer research.

Anti-TNBC agent-6 (compound pt-3) is an effective agent against triple-negative breast cancer (TNBC). It exhibits cytotoxic activity and induces autophagy (autophagy) and ferroptosis (ferroptosis). Additionally, anti-TNBC agent-6 enhances intracellular ROS accumulation and demonstrates antitumor activity, offering potential for breast cancer research.

anti-TNBC agent-7 (Compound 13c) exhibits anticancer activity and functions as a molecular probe to identify and regulate the signaling of the USP21/JAK2/STAT3 axis. It demonstrates nanomolar cytotoxicity against MDA-MB-231 and HCC-1806 cancer cells, effectively combating triple-negative breast cancer (TNBC).

Anti-TNBC agent-10 is an agent targeting triple-negative breast cancer (TNBC). It demonstrates potent anti-TNBC activity against BT549 cells with an IC50 of 0.018 μM and remains active in MDA-MB-231 cells with an IC50 of 4.16 μM. In mice with subcutaneous MDA-MB-231 TNBC xenografts, it shows significant antitumor efficacy. Anti-TNBC agent-10 is applicable in TNBC studies.

anti-TNBC agent-1 is a highly effective compound specifically targeting and combating triple-negative breast cancer (TNBC), demonstrating remarkable potency against various breast cancer cell types with IC50 values ranging from 0.20 μM to 0.27 μM. Its mechanism of action involves inducing apoptosis in SUM-159 cells through the mitochondria pathway and causing G1 phase arrest in these cells.

CNBCA, a selective and potent competitive inhibitor of the SHP2 enzyme, exhibits an IC50 value of 0.87 μM. It binds to the full-length SHP2, effectively inhibiting its enzyme activity, as well as impeding pAkt and pERK1/2. Furthermore, CNBCA suppresses the proliferation of BT474 and MDA-MB468 cells, indicating potential utility in breast cancer research [1].

SBP-7455 potently inhibited ULK1/2 enzymatic activity in vitro and in cells, reduced the viability of TNBC cells and had oral bioavailability in mice.

Rasarfin inhibits Ras and ARF6.

AGX51 is an antagonist of inhibitor of DNA binding (ID) proteins. AGX51 treatment lead to pan-Id degradation, cell cycle arrest, and cell death.

Mevociclib (SY-1365) is a highly selective covalent inhibitor of CDK7, possessing therapeutic potential in both hematological and solid tumors.

MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).

BMS-986158 is a highly effective BET inhibitor, demonstrating IC50 values of 6.6 nM in NCI-H211 small cell lung cancer (SCLC) cells and 5 nM in MDA-MB231 triple negative breast cancer (TNBC) cells.

Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent, inducing cell apoptosis and inhibiting the growth of TNBC cancer cell lines (IC50s: 10 nM - 20 nM).

β-catenin/BCL9 PPI-IN-1 (compound B4) is an effective inhibitor of the interaction between β-catenin and B-cell lymphoma 9 proteins (β-catenin/BCL9 PPI), with an IC50 value of 2.25 μM.

GSK2801 is an effective, specific and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd: 136 nM) and BAZ2B(Kd: 257 nM) bromodomains.

TD52 is an orally active inhibitor of cancerous inhibitor of PP2A (CIP2A). TD52 is an Erlotinib derivative and indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter.

Insulin β Chain Peptide (15-23), also referred to as INS, is an insulin-derived peptide specifically recognized by islet-associated T cells. The tetramer of Insulin β Chain Peptide (15-23) effectively stained the INS-reactive CTL clone G9C8; however, neither this tetramer nor the negative control tetramer (TUM) stained splenic CD8+ T cells from NOD or 8.3-TCRαβ transgenic NOD mice.