t 9

t9,t11,c15-CLNA is an isomer of conjugated linolenic acid (CLNA) produced by Lactobacillus plantarum ZS2058. It exhibits key activities including anti-inflammatory and antioxidant effects, as well as enhancement of intestinal barrier function. The regulatory mechanisms of t9,t11,c15-CLNA involve the upregulation of tight junction proteins, the inhibition of pro-inflammatory cytokines (such as TNF-α, IL-6), and the activation of antioxidant enzymes (such as SOD, CAT). t9,t11,c15-CLNA can be utilized in research on inflammatory bowel disease (like colitis).

T9 peptide (SKTFNTHPQSTP) is a muscle-targeting peptide that tightly binds to C2C12 myoblasts. When combined with oligonucleotides, T9 peptide enhances specificity towards the heart and quadriceps without similarly targeting the kidney, liver, or diaphragm.

CU-T12-9 is a potent TLR1/2 agonist(EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay). It acts by activating the NFkB pathway, upregulating proinflammatory cytokines, and enhancing TLR1 and TLR2 dimerization.CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.

EGFRT790M/L858R-IN-9 (Compound 8) is an inhibitor targeting the EGFR-L858R/T790M mutations. It effectively inhibits the phosphorylation of the EGFR-L858R/T790M mutant kinase, demonstrating an IC50 value of 0.0064 µM. Additionally, EGFRT790M/L858R-IN-9 can suppress the proliferation of non-small cell lung cancer (NSCLC) cells, making it useful for cancer research.

Acid-PEG9-t-butyl ester is a PROTAC linker from the PEG class, used for synthesizing PROTAC molecules.

c9,t11,c15-CLNA is an isomer of conjugated linolenic acid (CLNA) produced by Lactobacillus plantarum ZS2058. This compound demonstrates significant anti-colorectal cancer cell proliferation activity (IC50: 18.26 μM). It induces pyroptosis by activating the caspase-1-mediated classical pyroptosis pathway. c9,t11,c15-CLNA can be utilized in colorectal cancer research.

c9,t11-CLA is an active isomer of conjugated linoleic acid (CLA) known for its various physiological activities, including anti-cancer, anti-atherosclerosis, anti-obesity, anti-diabetic, and anti-hypertensive effects. Its primary regulatory mechanisms involve modulating cell signaling pathways and metabolic processes. c9,t11-CLA can be utilized in the development of functional foods, pharmaceuticals, and health-related research.

CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC MDA-MB-231 cells with an IC50 of 0.044 μM and inducing apoptosis. This compound diminishes CDK9 transcriptional activity and downregulates phosphorylation of RNA Pol II CTD ser2. In vivo, CDK9-Cyclin T1 PPI-IN-1 effectively impedes tumor growth in a TNBC 4T1 mouse model [1].

Bis-PEG9-t-butyl ester is a homofunctional, dual-substituted PEG derivative suitable for drug delivery. (Bis-PEG9-t-butyl ester) [Bis-PEG9-t-butyl ester] is employed in pharmaceutical applications for effective compound transport.

CCR1 antagonist 9 (compound 19e) is a selective CCR1 antagonist based on aziridine. It exhibits an IC50 of 6.8 nM for CCR1 inhibition in calcium flux assays and an IC50 of 30 μM for hERG.

GT 949 is a selective excitatory positive allosteric modulator of amino acid transporter-2 (EAAT2) with an EC50 of 0.26 nM.

1H-Benzimidazole-6-carboxylic acid is a GLP-1 receptor agonist.

Antitrypanosomal agent 9 is a potent compound with inhibitory activity against T. b. brucei, exhibiting an IC50 of 1.15 μM. It is utilized in research for human African trypanosomiasis (HAT).

Compound 2g (Anti-inflammatory agent 93) is an active compound that exhibits analgesic activity.

FXR agonist9 (compound 26) is a selective, orally active partial agonist of FXR with an EC50 of 0.09 µM (maximum efficacy of 75.13%). It ameliorates the pathological features of fatty liver disease in mice induced by HFD and CCl4-related metabolic dysfunction.

AR antagonist 9 is an orally active, selective androgen receptor (AR) antagonist that inhibits cancer by disrupting the formation of AR ligand-binding domain dimers, showing potential in overcoming drug resistance in prostate cancer (PCa). Its antagonistic activity against AR has an IC50 of 0.051 μM, comparable to Enzalutamide (IC50= 0.060 μM). This compound demonstrates superior inhibitory effects on ARF876L/T877A and ARW741C mutants compared to Enzalutamide. Additionally, AR antagonist 9 possesses favorable pharmacokinetic properties, with an oral bioavailability (F) of 66.24% in rats, and significantly inhibits tumor growth in LNCaP xenograft mouse models upon oral administration. AR antagonist 9 holds promise for research in overcoming PCa resistance.

CB2 receptor agonist 9 (Compound 33) is an orally active agonist of cannabinoid receptor 2 (CB2 receptor) with an EC50 of 16.2 nM. It inhibits the expression of TNF-α, IL-1β, and IL-6, demonstrating anti-inflammatory activity in a DSS-induced acute colitis model in mice.

Anti-inflammatory agent 94 (compound 4b) is an effective cannabinoid ligand with Ki values of 29 nM for CB2 and 8 nM for CB1. It is applicable in inflammation research.

Anticonvulsant agent 9 (compound 4f) is an activator of the α1β2γ2GABA_A receptor, with an EC50 value of 1.24 μM. It inhibits the inactivation of Nav1.2 channels and exhibits significant anticonvulsant activity.

Anti-inflammatory agent 95 (Compound 2e) is a compound with potent anti-inflammatory properties, showing significant inhibition of NO production in LPS-induced RAW 264.7 mouse macrophages, with an IC50 of 8.8 μM. It also effectively suppresses the secretion of TNF-α and IL-1β, achieving inhibition rates of 60% and greater than 90% at 100 μM, respectively. Anti-inflammatory agent 95 holds promise for research into inflammatory diseases.

Antidepressant agent 9 (Compound 24) is an orally active inhibitor of NMDAR and SERT, with IC50 values of 3.50 μM and 1044 nM, respectively. It exhibits good metabolic stability and plasma exposure, and demonstrates antidepressant-like effects in the forced swim test in mice.

Anti-inflammatory agent 96 (Compound 5) is a potent anti-inflammatory compound. It effectively reduces ear edema induced by TPA and paw edema caused by CFA.

Anti-inflammatory agent 97 (Compound 1l) is an anti-inflammatory compound and also inhibits oxidative stress. It can reduce colon shortening and alleviate inflammatory symptoms in a mouse model of ulcerative colitis induced by DSS. Additionally, it modulates the inflammation-associated TLR4/NF-κB signaling pathway and the oxidative stress-related Nrf2/HO-1 signaling pathway.

Neuroprotective agent 9 (compound 7) is a neuroprotective compound with promising potential for use in research on neuronal damage, including conditions such as stroke, brain injury, and neuropathic pain.