SH5-07 (SH5 07; SH-507; SH5-07), a structural analog of BP-1-102, is a novel, potent and hydroxamic acid-based STAT3 inhibitor with potential antitumor activity. It shows potent anti-proliferative activity in vitro and high in vivo antitumor efficacy against human glioma and breast cancer models. SH5-07 dose-dependently inhibits Stat3 activity with an IC50 of 3.9±0.6 μM in […]

ALG1001 has been discontinued due to commercial reasons. ALG1001 TFA, the trifluoroacetic acid salt of ALG1001 (also known as Luminate, developed by Allegro Ophthalmics), is small peptide that acts as an inhibitor of angiogenesis and a modulator of integrin α2ß1, αV-ß 3, αV-ß 5. ALG-1001 is a first-in-class integrin peptide therapy which met the primary […]

L-755,507 is identified as a potent and selective β3 adrenergic receptor partial agonist with EC50 of 0.43 nM, it displayed > 1000-fold selective over β1- and β2-adrenoceptors (EC50 values are 0.43, 580 and > 10000 nM for activation of cloned human β3-, β1- and β2-adrenoceptors respectively). It is also recently identified to enhance CRISPR-mediated homology-directed […]

Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NFkB. DEM induces upregulation of GSH(L-c-glutamyl-L-cysteinyl-glycine) metabolism, and the downregulation of pathways of cancer, chemokine signaling, cytokine-cytokine receptor, and focal adhesion in transformed cells. DEM appears to modify microenvironment of transformed cells thereby restraining tumor cell growth.

SGE-516, a synthetic neuroactive steroid, is a potent positive allosteric modulator of both synaptic and extrasynaptic GABAA receptors. Neuroactive steroids (NASs) have been shown to impact central nervous system (CNS) function through positive allosteric modulation of the GABA(A) receptor (GABA(A)-R). SGE-516 treatment protected against hyperthermia-induced seizures, reduced spontaneous seizure frequency and prolonged survival in the […]

CFI400945 (CFI-400945) fumarate is a potent, selective, and orally bioavailable PLK4 (polo-like kinase 4) inhibitor with IC50 value of 2.8 ±1.4 nM and potential antineoplastic activity. CFI-400945 selectively inhibits PLK4, which results in the disruption of mitosis and the induction of apoptosis. PLK4 inhibition also prevents cell division and inhibits proliferation of PLK4-overexpressing tumor cells. […]

SNG1153 is a synthetic ER-α36 modulator which shows promising activities in various in vitro and in vivo models. SNG-1153 is the 2nd generation small molecule for cancer therapy developed by Shenogen Pharma Group. SNG-1153 has inhibitory effects on TKI-resistant CML cells. SNG1153 shows significant inhibition at low micromolar concentrations in ER-α36 overexpressed cell lines including […]

Prucalopride HCl (formerly known as R93877; R-108512; Resolor; Resotran; trade name: Motegrity), the hydrochloride salt of prucalopride which is a novel enterokinetic compound and is the first representative of the benzofuran class, is a novel selective, high affinity 5-HT (serotonin) receptor agonist for 5-HT4A and 5-HT4B receptor with anti-constipation effects. It inhibits 5-HT4A and 5-HT4B […]

Cyantraniliprole (also known as HGW-86), an anthranilic diamide analog, is a novel and potent second-generation insecticide which is able to deter insect feeding and reduce disease transmission. Cyantraniliprol is a valuable tool for managing Frankliniella occidentalis (Pergande) and also is as effective as abamectin in deterring potato psyllid feeding and could significantly reduce transmission of […]

Lanabecestat camsylate (formerly known as AZD-3293; LY3314814), the camsylate salt of Lanabecestat, is a BACE inhibitor that inhibits beta-secretase 1 cleaving enzyme (BACE) with a Ki of 0.4 nM. AZD3293 displayed significant dose- and time-dependent reductions in plasma, cerebrospinal fluid, and brain concentrations of Aβ40, Aβ42, and sAβPPβ. The in vitro potency of AZD3293 was […]