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.

ODM-203 (ODM203) is a potent, selective, dual inhibitor of FGFR and VEGFR tyrosine kinases with approximately equal potency towards recombinant FGFR1, 2, 3 and 4, as well as VEGFR1, 2 and 3 (IC50=5-35 nM).

Deferasirox (Exjade)

Elagolix is a Gonadotropin-Releasing Hormone (GnRH) Antagonist.

Balixafortide(POL 6326) is a novel potent, selective, peptidic CXCR4 antagonist that interferes with the tumor-protective microenvironment and sensitizes tumor cells to chemotherapy.

CP-31398 is a small molecule p53 reactivator that protects p53 from thermal denaturation, not only reactivates mutant p53 but also induces stabilization of wild type p53.

PF-3450074 (PF74) is a small molecule HIV capsid protein, destabilized the viral capsid in vitro.

SNAP-94847 is a selective, high-affinity, and competitive MCH1 receptor (MCH1-R) antagonist with Ki of 1.69 nM.

PWT143 (ME-401), is an orally bioavailable inhibitor of the delta isoform of phosphatidylinositide 3-kinase (PI3K), with potential antineoplastic activity.

GDC-0623 is a potent, ATP-uncompetitive inhibitors of MEK1(Ki=0.13 nM, +ATP).

>98%,Standard References

A potent and selective antagonist of CXCR4 with IC50 of 13 nM in a CXCR4 125I-SDF inhibition binding assay.

NAB-14 is a potent, selective negative allosteric modulator of GluN2C/2D-containing NMDA receptors with IC50 of 580 nM, >800-fold selective over GluN2A/GluN2 receptors; inhibits triheteromeric (GluN1/GluN2A/GluN2C) NMDARs with modestly reduced potency and efficacy compared to diheteromeric (GluN1/GluN2C/GluN2C) receptors; inhibits GluN2D-mediated synaptic currents in rat subthalamic neurons and mouse hippocampal interneurons, but has no effect on synaptic transmission in hippocampal pyramidal neurons.

PF-915275 is a potent and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) (Ki ＜ 1 nM) with good preclinical pharmacokinetic properties.IC50 value: ＜ 1 nM (Ki)[2]Target: 11βHSD1in vitro: PF-915275 maintains potency in our cellular assay against human 11βHSD1 (HEK293, EC50 = 5 nM) and is selective against human 11βHSD2 (HEK293, 1.5% inhibition 10 μM). PF-915275 displays only weak affinity for the rodent choline transporter (Ki = 9.6 μM) and the hamster melatonin MT3 receptor (Ki = 9.6 μM) in the Cerep Bioprint screening panel. PF-915275 has good in vitro pharmacokinetic properties. In particular, PF-915275 is categorized as a low clearance compound (liver microsome assays) with high permeability (Caco2 assay). [2]in vivo: As a prelude to in vivo studies with PF-915275, the rat pharmacokinetic properties of this compound were determined. PF-915275 has an excellent pharmacokinetic profile characterized by low clearance, long half-life and good oral bioavailability. [2]

Delafloxacin meglumine (ABT492 meglumine; RX-3341 meglumine; WQ-3034 meglumine) is a broad-spectrum fluoroquinolone antibiotic. Delafloxacin has a broad spectrum of activity that includes drug-resistant Staphylococcus aureus, Streptococcus pneumoniae, and