a 002

Varespladib methyl (LY333013), a bioavailable prodrug of Varespladib, is a selective group II secretory phospholipase A2 inhibitor.

Triciribine phosphate (VD 002) is a highly selective AKT inhibitor that induces cell cycle arrest and cysteinyl asparagin-dependent apoptosis, inhibits neovascularization, and can be used in the study of leukemia.

Ralaniten (EPI-002) is a potent, specific, and orally active antagonist of the androgen receptor N-terminal structural domain (AR-NTD), inhibiting AR transcriptional activity with an IC50 value of 7.4 μM. Ralaniten exhibits anticancer activity and is used to study desmoplasia-resistant prostate cancer (CRPC).

ATX-002 is a property-tunable lipid for RNA drug delivery.

8-M-PDOT (AH-002) is a selective and potent melatonin MT2 receptor agonist that also inhibits MT1 receptors. 8-M-PDOT exhibits anxiolytic activity and can be used to study MT2-induced neuropathic pain.

The S-enantiomer of BET-BAY 002, referred to as BET-BAY 002 S enantiomer, is a potent inhibitor of BET (Bromodomain and Extra-Terminal motif proteins).

BET-BAY 002 is an effective BET inhibitor and exhibits efficacy in a multiple myeloma model.

20-HEDE (WIT 002) is an antagonist of 20-hydroxyeicosatetraenoic acid (20-HETE).

BSJ-05-002 serves as a FAK PROTAC.

Hydroxy tipelukast (Compound MN-002), a metabolite of Compound MN-001, is an orally active phenoxyalkyl carboxylic acid. It inhibits hepatic steatosis, lobular inflammation, hepatocellular ballooning, and liver fibrosis, while also reducing hepatic hydroxyproline levels. Hydroxy tipelukast is a promising candidate for the study of nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH).

SPP-002 is a sulfate ester analogue that acts as a potential Sialyltransferase (ST) inhibitor. It selectively inhibits N-glycan sialylation with at least an order of magnitude greater potency compared to the unmodified parent lithocholic acid (LCA). By inhibiting the integrin/FAK/paxillin signaling pathway, SPP-002 reduces tumor cell migration and invasion. It is applicable in research on tumor metastasis.

Cantrixil (TRX-E-002-1) is a second-generation super-benzopyran (SBP) compound, derived from TRX-E-002. It elicits an increase in phosphorylated c-Jun levels, leading to caspase-mediated apoptosis in ovarian cancer cells. Cantrixil exhibits potent pan anti-cancer activity against various cancer phenotypes.

ZLc-002 is a selective small-molecule inhibitor of nNOS-Capon coupling. ZLc-002 suppresses inflammatory nociception and chemotherapy-induced neuropathic pain. ZLc-002 can be used in anxiety disorder and inflammation research[1] [2] [3].

OG-L002 is an effective and selective LSD1 inhibitor (IC50: 20 nM), showing 69- and 36-fold selectivity over MAO-A and MAO-B, respectively.

IST5-002 (N6-Benzyladenosine-5'-phosphate) is a selective Stat5a/b inhibitor with anticancer activity that inhibits the transcriptional activity of Stat5a/b and induces apoptosis and death of prostate cancer cells and chronic myelogenous leukemia (CML) cells, which can be used for cancer research.

PRMT5-IN-18 (Compound 002) is a potent inhibitor of PRMT5, useful in studying PRMT5-mediated diseases such as tumors.

Gusacitinib, also known as ASN-002 and EN-3351, is a potent dual inhibitor of SYK/JAK kinases. ASN002 showed strong antitumor activity in both hematological and solid tumor xenograft models. ASN002 strongly suppressed the SYK and JAK family kinase signaling pathways as measured in pLAT and pSTAT assays, respectively. When profiled in a panel of 178 cell lines, ASN002 showed strong anti-proliferative activity in many lymphoid/leukemia cell lines, including SU-DHL-6, SU-DHL-4, OCI-LY10, H929 and Pfeiffer.

(Rac)-ZLc-002 is a compound that inhibits the interaction between neuronal nitric oxide synthase (nNOS) and the nitric oxide synthase 1 adaptor protein (NOS1AP), effectively reducing inflammatory pain and chemotherapy-induced neuropathic discomfort. Additionally, it enhances the efficacy of Paclitaxel in decreasing tumor cell viability [1] [2].

SC209, an ADC cytotoxin and metabolite of STRO-002 [1] [2], is utilized in the synthesis of anti-EGFR antibody-drug conjugate ADC.

Prasinezumab is a monoclonal antibody that selectively binds aggregated α-synuclein. Prasinezumab is under investigation as a disease-modifying therapeutic candidate for early-stage Parkinson’s disease, where it is being evaluated for its ability to interfere with pathogenic α-synuclein aggregation and progression of neurodegeneration.

Quisovalimab (AVTX-002; AEVI 002; SAR 252067), a human monoclonal antibody targeting LIGHT, a tumor necrosis factor (TNF)-related cytokine (TNFSF14), is crucial for managing acute respiratory distress syndrome (ARDS) and cytokine release syndrome (CRS) in COVID-19 and has potential applications in treating ARDS related to COVID-19, subject to ongoing research [1].

α-MSH (MSH, amide) is amide stimulates melanocortin 1 receptor that results in the activation of adenylyl cyclase.

Visugromab (CTL-002) is a monoclonal antibody that targets and neutralises GDF-15. Visugromab exhibits synergistic anticancer activity with the anti-PD1 antibody Nivolumab, making it suitable for PD-1/PD-L1 recurrent/refractory metastatic solid tumours.

ABX-002 (MA-JD21) is a TR-β selective, CNS-penetrant TR-β agonist prodrug, utilized for research on major depressive disorder (MDD) [1].