NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) (compound 39) is a potent APJ agonist, with a Ki of 0.6 nM. NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) can activate Gαi1 (EC50=0.8 nM) and recruit β-arrestin2 (EC50=31 nM). NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) exhibits prolonged cardiac effects.

AAK1-IN-2 TFA (compound (S)-31) is a potent, selective and brain-penetrant inhibitor of Adaptor Protein 2-Associated Kinase 1 (AAK1), with an IC50 of 5.8 nM. AAK1-IN-2 TFA can be used for the research of neuropathic pain.

PHGDH-IN-2 is a potent and NAD+ competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells.

GRPR antagonist-2 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 0.77 and 2.5 μM in HGC-27 and Pan02 cells, respectively). Anticancer activity.

GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity.

Anti-inflammatory agent 12 (Compound 2) is a pentacyclic triterpene compound. Anti-inflammatory agent 12 shows a significant bias in the LPS-induced inflammatory response with an IIC50 value of 2.22 μM. Anti-inflammatory agent 12 has the potential for the research of inflammation disease.

ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 cells.

Anticancer agent 33 (compound 3), a Squamocin and Bullatacin derivative, is a potent anticancer agent. Anticancer agent 33 shows high potency to inhibit 4T1 breast cancer cell line (A549, HeLa, HepG2 and MCF-7 cells) growth with IC50s of 1.9-5.4 µM.

AGL-0182-30 is a proprietary microtubule disrupting agent.

BOD-NH-NP is an activatable fluorescent probe for imaging endogenous nitric oxide via the eNOS enzymatic pathway.

Antitumor agent-47 (Compound 3e) is a silibinin derivative with an antitumor activity. Antitumor agent-47 shows cytotoxic activity against NCI-H1299 and HT29 cells with IC50 values of 8.07 µM and 6.27 µM, respectively.

Antitumor agent-49 (Compound 10) is a Harmine derivative-furoxan hybrids containing NO donor, with antitumor activities. Antitumor agent-49 shows cytotoxic activity against HepG2 cells with an IC50 of 1.79 µM. Antitumor agent-49 produces high levels of NO in vitro.

TS010 is a potent inhibitor of GLO-I with IC50 of 0.57 μM. TS010 has the potential for the research of cancer disease.

ChemR23-IN-3 is a potent thiazole-based ChemR23 inhibitor with an IC80 value of 12 nM.

17β-HSD1-IN-1 (Compound 1) is a highly selective 17β-HSD1 inhibitor with IC50s of 5.6 and 3155 nM for 17β-HSD1 and 17β-HSD2, respectively. 17β-HSD1-IN-1 can be used for the research of non-small cell lung cancer (NSCLC).

BSc5367 is a potent Nek1 inhibitor with an IC50 of 11.5 nM. NIMA-related protein kinase Nek1 is crucially involved in cell cycle regulation, DNA repair and microtubule regulation and dysfunctions of Nek1 play key roles in amyotrophic lateral sclerosis (ALS), polycystic kidney disease (PKD) and several types of radiotherapy resistant cancer.

PKN1/2-IN-1 is a potent, cell penetrant and selective PKN2 (PRK2) inhibitor (IC50=16 nM; Ki=8 nM).

Volanesorsen is an antisense oligonucleotide targeting Apolipoprotein C-III (APOC3) mRNA to treat patients with the familial chylomicronemia syndrome.

Anticancer agent 37 (compound 18), a sulfonylurea derivative, is a potent anticancer agent. Anticancer agent 37 inhibits HePG2 cell growth with an IC50 of 17.2 µg/mL.

Triton X-100 is a non-denaturing detergent that solubilizes lipid membranes. Triton X-100 is commonly used in laboratories and is applied to vaccines at different stages of the manufacturing process. Triton X-100 is listed as an excipient in certain vaccines including split virus influenza vaccines. Triton X-100 is a nonionic surfactant.

Custirsen is a highly specific antisense oligonucleotide that inhibits the production of clusterin , an antiapoptotic protein that is upregulated in response to chemotherapy and that confers treatment resistance.

SLEC-11 acts as a potential synthetic lethal lead for the treatment of gastric cancer. AL-GDa62 shows EC50 of 12.2 μM and 8.2 μM for isogenic mammary epithelial cells MCF10A-WT (wild-type) and MCF10A-CDH1-/-.

Diquat dibromide is a comprehensive herbicide commonly used in the cultivation of cotton, soybeans, and other crops to combat unwanted weeds. Diquat dibromide has an IC50 of 60 mg/L in the Allium root growth inhibition test.

Nangibotide TFA is a TREM-1 receptor inhibitor that can modulate innate immune response. Nangibotide TFA can reduce systemic and in situ inflammatory reaction in rodent models of myocardial ischaemia-reperfusion.

PAMP-12 is a potent MRGPRX2 (MrgX2) agonist (EC50=20-50 nM). PAMP-12 is an endogenous peptide that elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells.

Colchicine is a potent therapeutic tool against COVID-19. Colchicine is a tricyclic alkaloid that is extracted from the plant Colchicum autumnale. Colchicine acts as a potent inhibitor of tubulin polymerization.

Cinobufagin, a kind of Chinese materia medica with antitumor effect, is widely used in clinical practice, especially in anti-liver cancer. IC50 value: Target: In vitro: Cinobufagin inhibited proliferation of cancer cells at doses of 0.1, 1, or 10 μM after 2–4 days of culture. Cytotoxicity of cinobufagin on the DU145 and LNCaP cells was dose-dependent. Cinobufagin increased [Ca2+]i and apoptosis in cancer cells after a 24-hr culture as well as caspase 3 activities in DU145 and PC3 cells and caspase 9 activities in LNCaP cells [1]. Cinobufagin suppresses cell proliferation and causees apoptosis in prostate cancer cells via a sequence of apoptotic modulators, including Bax, cytochrome c and caspases [2].

>98%,Standard References

Lefamulin acetate is a pleuromutilin antibiotic that is being developed by Nabriva Therapeutics for the treatment of acute bacterial skin and skin-structure infections.

A potent GSK3β inhibitor with IC50 of 22 nM.