HB3089 (HB-3089) is a novel potent, highly specific STING agonist, dose-dependently activates interferon-stimulated gene (ISG) signaling in THP1-Dual reporter cells with EC50 of 1-10 uM.

246C10 is a synthesized ionizable lipid. 246C10 can be formulated into lipid nanoparticles (LNPs) with dioleoylphosphatidylethanolamine (DOPE), cholesterol, and C16-PEG2000 ceramide (PEG-lipid) as well as mRNA. The lipid nanoparticle formulations can be used for mRNA delivery. To obtain iLNPs that could specifically target liver sinusoidal endothelial cells (LSECs), six different ionizable lipids (241C10 to 246C10) were synthesized by an epoxide ring-opening reaction with piperazine- or piperidine-containing amines. Biodistribution and gene regulation of various iLNPs were assessed in vivo, and the results showed that the 246C10 iLNPs (containing piperazine amine) had the highest luciferase expression in the liver. When further analyzing the 246C10 iLNPs transfection efficiency in different types of liver cells, it was found that tdTomato fluorescence was mainly concentrated in hepatocytes, not in LSECs. Figure 6f shows that 80% of hepatocytes are fluorescent, 40% of LSECs are fluorescent, and 20% of Kupffer cells are fluorescent. Due to the mannose receptor on LSECs, mannose-PEG lipid was introduced into 246C10 iLNPs to alter the distribution of iLNPs in different liver cells. As shown in Figure 6g, tdTomato fluorescence distribution was 15% of hepatocytes, 70% of LSECs, and 15% of Kupffer cells, significantly improved the ability of iLNPs to actively target LSECs. In contrast, this work indirectly shows that the iLNPs with piperazine head lipid are more able to deliver mRNA to the liver and translate the target protein than the iLNPs with piperidine head lipid. It is worth mentioning that the preparation buffer of 246C10 iLNPs could influence the encapsulation efficiency of mRNA. With the addition of sodium chloride in the citrate buffer, the encapsulation efficiency of CRISPR-Cas9 mRNA and sgRNA was increased. These iLNPs were able to treat hemophilia safely, without causing hepatotoxicity, the immune response induced by Cas9 and off-target editing.

FTT5 is a lipid-like compound for efficient delivery of long mRNAs in vivo.

Neurounina-1 is a small molecule Na+/Ca2+ exchanger (NCX) activator, stimulates NCX1 and NCX2 activities with EC50 of 1.1-2.7 nM, does not affect NCX3 activity.Neurounina-1 (10 nM) reduced cell death of primary cortical neurons exposed to oxygen-glucose deprivation followed by reoxygenation, also reduced γ-aminobutyric acid (GABA) release, enhanced GABA(A) currents, and inhibited both glutamate release and N-methyl-d-aspartate receptors in vitro.Neurounina-1 effectively protects against stroke damage in vivo.

KZR-8445 (KZR8445) is a cyclic depsipeptide, client-selective Sec61 inhibitor with IC50 of 100 nM, targets the Sec61 translocon and selectively modulate Sec61-mediated protein biogenesis.

RAP-103 is an orally active, stabilized pentapeptide analog of DAPTA (D-ala-peptide T-amide), and multi-chemokine receptor antagonist.

Homoorientin is a potent inhibitor of COX-2 with an IC50 value of 39 μM.

Nanvuranlat (JPH203) is a potent, selective L-type amino acid transporter 1 (LAT1, SLC7A5) inhibitor with IC50 of 60 nM (leucine uptake inhibition), but not LAT2.

IBS007125 is a small molecule inhibitor of c-Maf, inhibits multiple myeloma proliferation by targeting cMaf transcriptional activity.

YSK 05 is a pH-sensitive cationic lipid. YSK 05 improves the intracellular trafficking of non-viral vectors. YSK 05-MEND shows significantly good gene silencing activity and hemolytic activity. YSK 05 overcomes the suppression of endosomal escape by PEGylation. YSK 05 effectively enhances siRNA delivery both in vitro and in vivo.

PAA-38 is a highly potent selective inhibitor targeting bacterial prolyl-tRNA synthetase (ProRS). PAA-38 againsts Pseudomonas aeruginosa ProRS (PaProRS) with a Kd value of 0.399 nM and an IC50 value of 4.97 nM. PAA-38 againsts human cytoplasmic ProRSs (HsProRS) with an IC50 value of 35.5 nM. PAA-38 demonstrates an in vitro antibacterial activity of minimum inhibitory concentration (MIC) = 4-8 μg/mL.

ACA22 is a small molecule KRAS inhibitor, inhibits KRAS-mediated signal transduction in cells expressing wild type (WT) and G12D mutant KRAS.

QCA276 is a novel potent BET proteins inhibitor with IC50/Ki of 10/.3 nM, QCA276 is the BET ligand for PROTAC QCA570.

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

TFAX 488,SE dilithium, an amine reactive green fluorescent dye, is insensitive to pH in the range 4-10. TFAX 488,SE dilithium forms bright and photostable conjugates with proteins and antibodies. TFAX 488,SE dilithium is suitable for use in flow cytometry, two-photon excitation microscopy (TPE), and super resolution microscopy techniques, such as dSTORM, SIM and STED. Excitation maximum=495 nm; emission maximum=515 nm; extinction coefficient=73,000 M-1cm-1; quantum yield=0.92.

ACA-14 is a small molecule direct inhibitor of KRAS, impedes the interaction of KRAS with its effector Raf and reduces both intrinsic and SOS-mediated nucleotide exchange rates.

A potent, long lasting 5-HT(1B/1D) receptor agonist as a antimigraine agent..

MC-GGFG-DX8951 is a drug-linker conjugate for ADC with antitumor activity by using DX8951 (DNA topoisomerase I inhibitor), linked via the protease cleavable MC-GGFG linker.

JP-11646 is a novel potent, selective, non-ATP competitive Pim2 inhibitor with IC50 of 0.5/1/24 nM for Pim2/3/1, respectively; shows less potency for other kinases in a kinase selectivity panel; exhibits 4-760-fold greater suppression of MM proliferation and viability than ATP-competitive PIM inhibitors; significant reduces tumor burden and increases median survival in xenogeneic myeloma murine models.

Rhodamine 123 is a chemical compound and a dye.

DN200434 (DN-200434) is a highly potent (functional IC50=6 nM, binding IC50=40 nM), selective, biocompatible and orally available ERRγ inverse agonist.DN200434 binds to key ERRγ binding pocket residues through four-way interactions.DN200434 effectively upregulated iodide-handling genes and restored radioiodine avidity in ATC tumor lesions.DN200434 enhanced ATC tumor radioiodine therapy susceptibility, markedly inhibiting tumor growth.DN200434 shows higher potency than GSK5182.

OG 488, acid, a fluorescent pH indicator, has many applications in biochemistry and neurosciences.

HCQ-2 NHS is a dark quencher with no native emission due to the polyaromatic-azo backbone and a terminal NHS ester. UBHQ-2 NHS has a wide and intense quenching range from 560-670 nm, which makes it useful as an acceptor in fluorescence resonance energy transfer (FRET) applications in conjunction with orange to far-red emitting dyes. The NHS ester can be applied to label the primary amines (-NH2) of proteins, amine-modified oligonucleotides, and other amine-containing molecules.

5-FAM SE is a single isomer, it is one of the most popular green fluorescent reagents used for labeling peptides, proteins and nucleotides.

Fluorescein isothiocyanate(FITC) is a derivative of fluorescein used in wide-ranging applications including flow cytometry.

JZL184 is a strong and selective inhibitor of Monoglyceride Lipase

YO-01027 (Dibenzazepine, DBZ) is a dipeptidic g-secretase inhibitor with IC50 of 2.6 and 2.9 nM for APPL and Notch, respectively.

8-Hydroxy-DPAT hydrobromide (8-OH-DPAT hydrobromide) is a potent and selective 5-HT1A agonist with a pIC50 of 8.19. 8-Hydroxy-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site.

CeMMEC13 is a potent inhibitor of TAF1 (2) bromodomain, with an IC50 of 2.1 μM.

E-64c is a synthetic analog of E-64, a potent and irreversible cysteine protease inhibitor isolated from Aspergillus japonicus.