NMS-P937 (NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Phase 1.

Ectoine is an inhibitor of protein misfolding. It acts by significantly down-regulating Syp, Mapk3 and Tnfα and up-regulating Vegf in rat's hippocampus, prohibiting insulin amyloid formation in vitro.

Sarsasapogenin is a steroidal sapogenin, that is the aglycosidic portion of a plant saponin.

Bakuchiol is a phytoestrogen isolated from the seeds of Psoralea corylifolia L; has anti-tumor effects.

Naringenin is the predominant flavanone in grapefruit; displays strong anti-inflammatory and antioxidant activities. Naringenin has anti-dengue virus (DENV) activity.

Cytochalasin H is a potent inhibitor of actin incorporation into filaments,a cell-permeable fungal toxin used in actin polymerization studies and cytological research.

D3263 is a novel, orally bioavailable small molecule Trp-p8 agonist.

D-64131 is a novel inhibitor of Tubulin polymerization that competitively binds with [(3)H]colchicine to αβ-Tubulin.

Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells.

Ginsenoside Rg1 is one of the major active components of ginseng. Ginsenoside Rg1 displays promising effects by reducing cerebral Aβ levels. Ginsenoside Rg1 also reduces NF-κB nuclear translocation.

Nifurtimox is a 5-nitrofuran and is used to treat diseases caused by trypanosomes including Chagas disease and sleeping sickness. It is given by mouth and not by injection. Nifurtimox is now in a Phase II clinical trial for the treatment of pediatric neuroblastoma and medulloblastoma. Nifurtimox decreased cell viability in a concentration-dependent manner. Nifurtimox also suppressed basal and TrkB-mediated Akt phosphorylation, and the cytotoxicity of nifurtimox was attenuated by a tyrosine hydroxylase inhibitor (alpha-methyl-tyrosine). Nifurtimox killed catecholaminergic, but not cholinergic, autonomic neurons in culture. In vivo xenograft models showed inhibition of tumor growth with a histologic decrease in proliferation and increase in apoptosis. These results suggest that nifurtimox induces cell death in neuroblastoma . Therefore, further studies are warranted to develop nifurtimox as a promising new treatment for neuroblastoma.

DS-6930 (DS 6930, DS6930) is a novel potent, selective PPARγ agonist with EC50 of 41 nM, Emax-68%; significantly recruits several cofactors, such as RIP140 and PGC1, in cofactor recruitment assays; demonstrateshigh PPARγ agonist potency with robust plasma glucose reduction, maintains diminished PPARγ-related adverse effects upon toxicological evaluation in vivo, and demonstrated no hepatotoxicity.

8-Hydroxy-efavirenz is the primary metabolite of the antiretroviral drug Efavirenz, stimulates the glycolytic flux in cultured rat astrocytes.

AZD 4205 (AZD4205) is a potent, selective JAK1 inhibitor IC50 of 73 nM and Ki of 2.8 nM, shows high selectivity against JAK2 and JAK3 with IC50 of 13,233 nM and >30,000 nM respectively; shows potent inhibition of p-STAT3 in a cell based assay of JAK1 activity with an IC50 of 128 nM and excellent selectivity across the kinome; reduces residual disease and prolongs the benefit of Osimertinib in lung cancer patients with EGFR activating mutations both in vitro and in vivo.

Daidzin is a potent, selective aldehyde dehydrogenase 2 (ALDH2,IC50 = 80 nM) inhibitor, which has antiallergic anti-oxidant, anti-carcinogenic, antithrombotic,and anti-atherosclerotic activities

Cimicoxib, aslo known as UR-8880, is a non-steroidal anti-inflammatory drug (NSAID) used in veterinary medicine to treat dogs for pain and inflammation associated with osteoarthritis and for the management of pain and inflammation associated with surgery. It acts as a COX-2 inhibitor.

Dasotraline(SEP-225289) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.

Datelliptium chloride is a DNA-intercalating agent derived from ellipticine, with anti-tumor activities.

Decursin is an anticancer agent, with potential anti-inflammatory activity.

Vericiguat (BAY 1021189) is a novel potent, selective, orally available soluble guanylate cyclase (sGC) stimulator (MEC=0.3 uM), stimulating sGC NO-independently and in synergy with NO.

UAMC-3203 is a novel potent, drug-like ferroptosis inhibitor with IC50 of 12 nM, inhibit erastin-induced ferroptotic cell death more potently than Ferrostatin-1.

25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells.

TPT-172, also known as R33 (described in Mecozzi et al' s paper), is a thiophene thiourea derivative with molecule weight 172 in free base form. There is no formal name yet, we temporally call this molecule as TPT-172.

Regorafenib hydrochloride (BAY73-4506) is a potent, orally active multikinase inhibitor that potently inhibits endothelial cell kinases in biochemical and cellular kinase phosphorylation assays with nanomolar range (IC50=3-200 nM).

CK1-IN-1, is a casein kinase 1 (CK1) inhibitor. PUN51207 was reported in patent WO2015119579A1, compound 1c, has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.

Eprotirome, also known as KB-2115, is a liver-selective thyroid hormone receptor agonist that has been shown to lower plasma LDL cholesterol concentrations in previous phase 1 and 2 studies of patients with dyslipidaemia. KB2115 lowers plasma LDL cholesterol and stimulates bile acid synthesis without cardiac effects in humans.

(-)-Cotinine is a major metabolite of nicotine in humans, it is a minor alkaloid found in tobacco plants.

AT-1002, a 6-mer synthetic peptide, is a tight junction regulator and absorption enhancer.

Defensamide, also known as MHP and methyl caprooyl tyrosinate, is an activator of sphingosine kinase (SPHK1), and significantly stimulates CAMP mRNA and protein production in KC.

KL001 (KL-001) is a small molecule that specifically interacts with cryptochrome (CRY) and small molecule modulator of the circadian clock.