no cytotoxicity

Flibanserin (Girosa) is a serotonergic antidepressant used to treat hypoactive sexual desire disorder. Flibanserin has been associated with a low rate of minor serum aminotransferase elevations during treatment but has not been linked to instances of clinically apparent acute liver injury.

Tau-aggregation and neuroinflammation-IN-1 is a potent inhibitor of tau protein aggregates, showing significant inhibitory activity against AcPHF6 and full-length tau protein aggregates. It has anti-inflammatory activity, reduces NO release, exhibits low cytotoxicity against LSP-stimulated BV2 cells, and reverses okadaic acid-induced memory impairment in rats.

Compound 27b, also known as hURAT1 inhibitor 1, is an isomarine-derived, orally active inhibitor that targets both hURAT1 and GLUT9 with IC50 values of 0.16 μM and 4.47 μM, respectively. This compound exhibits significant anti-hyperuricemia effects and has demonstrated potent uric acid-lowering activity in a hyperuricemia mouse model at a dose of 10 mg kg. Importantly, Compound 27b displays no notable in vitro cytotoxicity or in vivo hepatotoxicity, and possesses favorable pharmacokinetic (PK) characteristics.

MC1, an effective NLRP3 inhibitor, exhibits a KD value of 19.3 nM and is devoid of cytotoxicity. This compound enhances cognitive function without causing adverse effects and exhibits no hepatotoxicity. MC1 holds potential for research in Alzheimer's disease.

Antifungalagent 122 (compound 201), a potent and broad-spectrum antifungal agent, prevents the phase shift in fungi and the formation of fungal biofilms. This compound effectively inhibits the enzymatic activity of CYP3A4-M and CYP3A4-T, with IC50 values of 2.11 and 4.53 µM, respectively. Notably, Antifungalagent 122 exhibits no cytotoxicity.

Anticanceragent 263 (compound 7) is an effective anticancer agent. It binds with the G-quadruplex DNA (G4) sequence 22-mer Pu22 (a c-Myc DNA analog). As a structural modulator, Anticanceragent 263 significantly enhances the formation of protein α-helices and has the capacity to form a supramolecular network. Furthermore, Anticanceragent 263 exhibits no cytotoxicity.

PB01 is a DPP-4 inhibitor with an IC50 of 15.66 nM. It effectively suppresses high glucose-induced ROS generation and mitochondrial superoxide production while significantly reducing the cellular expression of DPP-4. Additionally, PB01 notably lowers blood glucose levels in diabetic mice. It demonstrates excellent safety, exhibiting almost no cytotoxicity at a concentration of 100 μM. PB01 holds promise for research in the diabetes field.

α-Glucosidase-IN-79 (Compound 4d9) is a non-competitive α-glucosidase inhibitor with an IC50 of 2.11 μM, demonstrating greater inhibitory potency than the existing α-glucosidase inhibitors Acarbose (IC50 of 327.0 μM) and HXH8r (IC50 of 15.32 μM). It exhibits no cytotoxicity on normal human liver cells (LO2) and shows good metabolic stability in rat plasma. α-Glucosidase-IN-79 holds promise for research in type 2 diabetes.

SLU-10906 (Compound 63) is an orally active inhibitor of Cryptosporidium. It demonstrates activity against the parasite in cell-based infection models with an EC50 of 0.19 μM and exhibits no cytotoxicity. SLU-10906 is a promising candidate for research in cryptosporidiosis.

PPARγ-IN-5 (Compound A3) is an inhibitor of PPARγ. In liver cells, it reduces lipid accumulation and shows no significant cytotoxicity in HepG2 cells at a concentration of 400 µM. PPARγ-IN-5 is applicable for research on non-alcoholic fatty liver disease.

SJPYT-310 is a selective PXR antagonist, exhibiting no noticeable cytotoxicity.

O6BTG-C8-αGlu is an O6-methylguanine-DNA methyltransferase (MGMT) inhibitor with an IC50 of 0.45 μM. At a concentration of 0.1 μM, it fully inhibits MGMT in HeLaS3 cells and demonstrates no cytotoxicity even at prolonged high doses (up to 20 μM). This compound is suitable for research on MGMT-related cancers.

NF-κB/HIF-1α-IN-1 (compound 9c) effectively inhibits the NF-κB activation pathway and demonstrates selective antifibrotic activity. This compound exhibits no significant cytotoxicity in NCI tumor cell lines. In rat models, NF-κB/HIF-1α-IN-1 successfully ameliorates liver fibrosis, suppresses the expression levels of NF-κB and HIF-1α, and induces Nrf2.

AChE-IN-87 is an AChE inhibitor with an IC50 of 0.05 μM and a Ki of 16.93 nM. It exhibits no cytotoxicity toward 3T3 cells and is suitable for Alzheimer's disease (AD) research.

BTK-IN-28 (compound PID-4) is a potent BTK inhibitor with anti-cancer properties. It effectively inhibits BTK and downstream signaling cascades, selectively suppressing the proliferation of Burkitt's lymphoma RAMOS cells, while exhibiting no significant cytotoxicity towards non-tumor cells.

TLR7 agonist18 (Compound 21a) is a selective Toll-like receptor 7 (TLR7) agonist with an EC50 of 7.8 μM. It demonstrates no cytotoxicity in an HEK293 cell line co-transfected with the hTLR7 gene and can induce the secretion of several cytokines, including IL-1β, IL-12p70, IL-8, and TNF-α. This compound is useful in research related to vaccines, asthma, allergies, and cancer treatment.

OX2R-IN-2 (compound 63c) is an agonist of the type 2 orexin receptor (OX2R) with an EC50 value of 339 nM. It can cross the blood-brain barrier and exhibits no cytotoxicity.

IDD-8E is an effective anti-pseudomonal agent (MIC = 4.4 µM) with no cytotoxicity. It demonstrates significant killing of Pseudomonas and disruption of its biofilm. IDD-8E targets the ATP-binding pocket of WaaP and also inhibits other ESKAPE pathogens.

The compound effectively and directly inhibits JAK2 tyrosine kinase autophosphorylation and specifically inhibits ligand-dependent JAK2 activation. It has no cytotoxicity at 100 μM. A 16-hour treatment with compound (1 μM) decreases JAK2 tyrosine autophos

A 30312 is a fused indole, which overcomes multidrug resistance in P388/Adr cells in vitro. It potentiates the cytotoxicity of the antitumor drugs Adriamycin, vincristine and vinblastine in multidrug-resistant cells with no effect on drug-sensitive parent P388 cells.

CL385319 is a potent inhibitor of H5N1 avian influenza A virus infection by blocking viral entry. CL-385319 is effective in inhibiting infection of highly pathogenic H5N1 influenza A virus in Madin-Darby Canine Kidney (MDCK) cells with an IC50 of 27.03±2.

I-XW-053 sodium inhibits the replication of a diverse panel of primary HIV-1 isolates in Peripheral blood mononuclear cell with no appreciable cytotoxicity.

rac-1,2-bis-Palmitoyl-3-chloropropanediol is a 3-monochloropropane-1,2-diol (3-MCPD) ester.1It has been found as a contaminant in edible olive oils, with the lowest and highest concentrations in extra virgin and olive pomace oils, respectively.rac-1,2-bis-Palmitoyl-3-chloropropanediol has also been found in cottonseed and palm oils, as well as in shortening.2It induces renal tubular necrosis and a decrease in spermatids, but no gross pathological changes, in mice.3 1.Hung, W.-C., Peng, G.-J., Tsai, W.-J., et al.Identification of 3-MCPD esters to verify the adulteration of extra virgin olive oilFood Addit. Contam. Part B Surveill.10(3)233-239(2017) 2.MacMahon, S., Begley, T.H., and Diachenko, G.W.Occurrence of 3-MCPD and glycidyl esters in edible oils in the United StatesFood Addit. Contam. Part A. Chem. Anal. Control Expo. Risk Assess.30(12)2081-2092(2013) 3.Liu, M., Gao, B.-Y., Qin, F., et al.Acute oral toxicity of 3-MCPD mono- and di-palmitic esters in Swiss mice and their cytotoxicity in NRK-52E rat kidney cellsFood Chem. Toxicol.50(10)3785-3791(2012)

High affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM). Exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). Exhibits >4500-fold selectivity for PCAF over BRD4. Also exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC). Moustakim et al (2017) Discovery of a PCAF bromodomain chemical probe. Angew.Chem.Int.Ed. 56 827 PMID:27966810