target 1

Target 1 has a wide range of applications in life science related research.

5-HT1A modulator 1 is a small molecule modulator, a high-affinity multi-target ligand with potent inhibitory activity against 5-HT1A receptor (IC50=2 nM), α1-adrenergic receptor (IC50=10 nM), and dopamine D2 receptor (IC50=40 nM). This compound is primarily used for research on neuropsychiatric disorders such as anxiety, depression, or schizophrenia.

JNK-IN-8 (JNK Inhibitor XVI) is an effective JNK inhibitor that inhibits JNK1, JNK2, and JNK3 with IC₅₀ values of 4.7, 18.7, and 1 nM, respectively. JNK-IN-8 offers the advantages of minimal off-target activity, sustained inhibition, and high specificity. JNK-IN-8 primarily acts by blocking the JNK/c-Jun signaling pathway, inhibiting the phosphorylation of the downstream transcription factor c-Jun, thereby regulating the expression of genes associated with inflammatory responses, apoptosis, and stress responses. JNK-IN-8 can be used in research on tumors, inflammation, and neurological diseases.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

Vepdegestrant (ARV-471) is a selective and highly potent estrogen receptor (ER, ESR1) PROTAC degrader with strong degrading activity against the ER protein. By directly degrading the ER protein rather than merely antagonizing its activity, vepdegestrant effectively inhibits the ER signaling pathway and demonstrates significant antitumor activity in ER-positive (ER⁺) breast cancer, with a DC50 value of approximately 2 nM. It is particularly effective against tumors harboring ESR1 mutations.

Torin 1 is an effective inhibitor of mTORC1/2 with (IC50: 2 nM/10 nM); has 1000-fold selectivity for mTOR than PI3K.

Trevogrumab (REGN-1033) is a fully human monoclonal antibody specifically designed to target and inhibit the activity of growth differentiation factor 8 (GDF8), which is also known as myostatin and functions as a negative regulator of muscle growth;Trevogrumab is currently under extensive research of sarcopenia, a complex condition characterized by progressive and generalized loss of skeletal muscle mass and function often associated with aging, wasting atrophy, various chronic diseases, and significant alterations in dietary and nutritional intake.

Somatostatin 1-28 acetate belongs to natural products, serving as a multi-target agonist with endocrine inhibitory activity. Somatostatin 1-28 acetate circulates in human plasma, accounting for approximately 46% of total somatostatin-like immunoreactivity, and can be used for studying hormone secretion regulatory mechanisms.

FASN-in-1 is an effective, specific inhibitor of fatty acid synthase (FASN), a compound specifically designed to target and inhibit the activity of the enzyme involved in fatty acid synthesis, potentially disrupting fatty acid production and affecting various cellular processes.

PROTAC BRD4 ligand-1 is a PROTAC and a BRD4-targeted inhibitor with BET inhibitory activity. This ligand is cell-permeable and is used for the synthesis of PROTAC GNE-987, possessing antitumor potential.

GNE-049 is a highly selective and potent inhibitor designed to target the CREB-binding protein (CBP) with high affinity, exhibiting an IC50 of 1.1 nM for the suppression of BRET and BRD4 activity, which consequently blocks prostate cancer cell proliferation in both in vitro and in vivo models.

Crebinostat is a potent histone deacetylase (HDAC) inhibitor, targeting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively. It increases the density of synapsin-1 punctae along dendrites in neurons in vitro, modulates chromatin-mediated neuroplasticity, and enhances memory in mice. Additionally, Crebinostat induces histone H3 and H4 acetylation and enhances the expression of Egr1, a cAMP-responsive element binding protein (CREB) target gene.

BMS-1166-n-piperidine-co-n-piperazine dihydrochloride, a resorcinol di-Ph ether scaffold-based programmed cell death-1 (PD-1)/programmed cell death ligand 1 (PD-L1) inhibitor, inhibits the PD-1/PD-L1 interaction with an IC50 of 39.2 nM. It contains the target protein PD-1/PD-L1 ligand and PROTAC linker, which can be used to synthesize PROTAC PD-1/PD-L1 degrader-1 and has anticancer activity. Additionally, it serves as a diluent for the preparation of tablets for direct compression.

P53R3 is a potent reactivator of p53, effectively restoring sequence-specific DNA binding to several p53 hot spot mutants, namely p53 R175H, p53 R248W, and p53 R273H. This compound exhibits p53-dependent antiproliferative effects with significantly higher specificity compared to PRIMA-1 and promotes the recruitment of both wild-type p53 and p53 M237I to various target gene promoters. Additionally, P53R3 markedly increases the mRNA, total protein, and cell surface expression of death receptor 5 (DR5), demonstrating its utility in cancer research.

MCT1-IN-3 is a monocarboxylate transporter 1 (MCT1) inhibitor, targeting solute carrier (SLC) monocarboxylate transporter 1 (MCT1; SLC16A1) for cancer treatment. MCT1-IN-3 (compound 24) showed the highest MCT1 transport inhibition with an IC50 value of 81.0 Nm and also exhibits significant inhibitory activity against the multidrug transporter ABCB1.

PARP1/2/TNKS1/2-IN-1 is a multi-target inhibitor of PARP-1, PARP-2, TNKS1, and TNKS2, with potential anti-tumor activity that induces apoptosis.

ML228 is a potent the Hypoxia Inducible Factor (HIF) pathway activator with EC50 of 1 μM. ML228 potently activates HIF in vitro as well as its downstream target VEGF.

Antimicrobial agent-22 (THI 6c) is a broad-spectrum, multi-target antibacterial with rapid bactericidal efficacy, effective anti-biofilm activity, and low cytotoxicity and hemolytic properties [1].

Triciferol acts as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR ( IC 50 =87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Triciferol also exhibits efficacious antiproliferative and cytotoxic activities in cancer cell models in vitro [1].

Verucopeptin is a pyranized cyclic peptide and an inhibitor of hypoxia-inducible factor 1 (HIF-1). It is an antibiotic effective against B16 melanoma, with anticancer activity, lowering the expression of HIF-1 target genes and HIF-1α protein levels. It can be used in cancer research.

MKC-1 (Ro-31-7453) is an orally bioavailable small-molecule bisindolylmaleimide cell cycle inhibitor with potential antineoplastic activity. MKC-1 and its metabolites inhibit tubulin polymerization, blocking mitotic spindle formation, which may result in apoptosis and tumor cell death.

5-Fluorouridine is a metabolite of 5-fluorouracil that inhibits rRNA synthesis in human colon cancer cells and exhibits antitumor and antiviral activity. 5-Fluorouridine exerts a cytotoxic effect on the growth of L1210 cells, with an IC₅₀ value of 2 nM. 5-Fluorouridine binds to poly-A RNA and exhibits antiproliferative activity. 5-Fluorouridine can be used in studies of nucleic acid metabolism, cancer chemotherapy, and viral replication mechanisms.

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1/2) with IC50 values of 77/33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

Methyl α-D-mannopyranoside (Methyl α-D-mannopyranoside) can be used as an intermediate for chemical sythesis and can target macrophages in anti-tuberculosis inhalation therapy[1].