Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.

Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease[1][2].

mCAP is the first cap analog for the molecular biology toolbox. MCAP inserts in the correct orientation to enhance translation with a 50% chance. The other 50% of molecules can’t be a substrate for efficient translation, reducing the specific activity of the transcript. mCAP can be incorporated in a transcription by including a mixture of the cap analog and GTP (usually at a 4:1 ratio). Approximately 80% of synthesized mRNA will possess a 5’ cap, while the remaining 20% will possess a 5’ triphosphate.

CL2A-SN38 is a SN38 derivative with a peptide-linker which can easily react with antibody to form an antibody-drug conjugate (ADC). CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .

CL2-SN-38 is a cleavable linker-based antibody-drug conjugate (ADC) containing the topoisomerase I inhibitor SN-38 (Item No. 15632) and a maleimidocaproyl linker.1 CL2-SN-38 has been linked to tumor-selective human monoclonal antibodies, such as anti-CEACAM5 (hMN-14) to target SN-38 to tumor sites and improve its solubility. CL2-SN-38 linked to hMN-14 binds (Kd = 1.4 nM) and is cytotoxic to LoVo human colon adenocarcinoma cells (IC50 = 5.3 nM). CL2-SN-38 linked to hMN-14 increases survival in a colon carcinoma mouse model of lung metastasis.

LY-3502970 (Orforglipron) is a potent, selective, orally active non-peptide agonist of glucagon-like peptide-1 (GLP-1) receptor.LY3502970 is a partial agonist, biased toward G protein activation over β-arrestin recruitment at the GLP-1R.

KRCT-6j is a potent and selective TYRO3 inhibitor, 300-fold selectivity for TYRO3 over both AXL and MerTK.KRCT-6j selectively inhibited the proliferation of TYRO3-overexpressing Ba/F3 cells, also suppressed csEV-stimulated cell migration of LNCaP-SL cells in a concentration-dependent manner.KRCT-6j diminished csEV-induced membrane localization of F-actin, reversed the increased expression and nuclear localization of YAP stimulated by csEVs.KRCT-6j significantly inhibited tumor growth in xenografts implanted with GR-H1993 cells when combined with gefitinib.

S-2765(FXa substrate,Z-D-Arg-Gly-Arg-pNA Dihydrochloride) is specific to activated factor X (FXa),short peptide covalently bound to pNA (4-nitroaniline).

DOPA-NA is an anionic lipid that can be used to prepare liposomes, micelles and artificial membranes.

DOPS-NA is a ubstitute for Phosphoserine/phosphatidylserine. DOPS-NA can be used in lipid mixtures with DOPC and DOPE as effective nontoxic and nonviral DNA vectors.

NADI-351 is a specific small-molecule inhibitor of Notch1 transcriptional complexes with IC50 of 8.8 uM in cellualr reporter assays.NADI-351 inhibited OE33 cell growth in single dose MTT assays (EC50= 10 uM) and, more potently, in multi-dose colony formation assays (EC50=1.3 uM)NADI-351 is 15 times more potent than IMR-1 in an NTC AlphaScreen assay.NADI-351 selectively disrupted Notch1 transcription complexes, inhibited recruitment of Notch1 to the NTC (Notch Ternary Complex) and to the HES1 promoter, and reduced Notch1 recruitment to target genes.NADI-351 inhibits tumor growth in Notch-dependent cancers and does not exert gastrointestinal toxicity associated with goblet cell metaplasia.NADI-351 selectively inhibits stem-like esophageal adenocarcinoma (EAC) cell populations.

(R)-YNT-3708 is a potent, selective orexin 1 receptor (OX1R) agonist with EC50 of 7.48 nM and Emax 101%, 22-fold selectivity over OX2R (IC50=168 nM).

DSPC was used as the helper lipid for LNP

CVT-10216 is a potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2) (IC50 values are 29 and 1300 nM for ALDH2 and ALDH1, respectively).

RBI2 (Ribosome biogenesis inhibitor 2) is a small molecule inhibitor of ribosome biogenesis inhibitor, potently inhibits pre-rRNA levels in A375 with IC50 of 169 nM.

Pyrcoumin is a competitive inhibitor of dCTP pyrophosphatase 1 (dCTPP1, IC50=3.3 uM), inhibits Wnt signaling with IC50 of 8.4 uM in SuperTOPFlash reporter gene assays.

A potent and selective Histamine H3 receptor antagonist with Ki of 0.1-5.8 nM (human, rat H3).

Maltopentaose is the shortest chain oligosaccharide that can be classified as maltodextrin and is also used in a study to investigate glycation and phosphorylation of α-lactalbumin.

Trabikibart (CSL311), a βc (CSF2RB)-specific, fully human monoclonal antibody, binds to a unique epitope that is specific to the cytokine-binding site of the human βc receptor. Trabikibart has picomolar binding affinity for the human βc receptor. Trabikibart is a potent inhibitor of the combined effects of IL-3, GM-CSF and IL-5 on the survival of eosinophils. Trabikibart has the potential for chronic inflammatory diseases research.

Fluorescein-5-maleimide is a fluorescent thiol-reactive dye used to conjugate fluorescein to proteins (excitation: 494 nm, emission: 519 nm).

GSK137 is a potent, small-molecule BCL6 inhibitor binding to BCL6 BTB-POZ domain, displaces peptides derived from the human SMRT co-repressor from the BCL6 BTB-POZ domain in a TR-FRET assay with a pIC50 of 8.0.

Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.

MitoBloCK 1 is a small molecule inhibitor that blocks the import of substrates that use the TIM22 import pathway, but not TIM23 or the Mia40/Erv1 translocation pathways.

Potent and selective nociceptin opioid receptor (NOP) agonist

AC3573 (AC-3573) is a potent, specific small molecule inhibitor of HER3.AC3573 abrogates HER2–HER3 signalling in cells and is more specific for HER3, inhibits NRG (heregulin)-induced HER3 phosphorylation with IC50 of 10 uM, abrogates the formation of the active HER2-HER3 heterodimer, inhibits oncogenic downstream signalling in SK-BR-3 breast cancer cells.

Galvestine-1 is a potent small-molecule inhibitor of monogalactosyldiacylglycerol (MGDG) synthase that competitively binds to the diacylglycerol substrate site with an IC50 of 10 μM. This bioactive compound demonstrates excellent plant mobility, being efficiently absorbed through roots and systemically distributed via xylem transport to mesophyll tissues. In Arabidopsis thaliana, Galvestine-1 treatment leads to significant reduction of MGDG content and disrupts chloroplast development, likely through impairment of thylakoid membrane biogenesis. These unique properties establish Galvestine-1 as a valuable chemical tool for investigating MGDG-dependent processes and studying lipid homeostasis mechanisms in plants.

AC-003 is a novel, orally administered small-molecule inhibitor targeting receptor-interacting protein kinase 1 (RIPK1), demonstrating therapeutic potential for the treatment of idiopathic pulmonary fibrosis (IPF).

TM5441 is a novel orrally active TAP-1 antagonist.

A potent, selective, orally active orexin-2 receptor (OX2R) antagonist with pKi of 8.0 and 8.1 for human and rat OX2R, respectively.

IODVA1 is a small molecule with cellular inhibitory activity against several transformed cell lines including Ras-driven cells, targets Rac activation and signaling instead of Ras; IODVA1 inhibits ST8814 cell proliferation with GI50 of 1 uM, similar results were observed with MCF7, MDA-MB-231, and T47D cells with estimated GI50s <1 uM. IODVA1 significantly decreases number of colonies of the breast cancer cells in soft agar at 1 and 3 uM. IODVA1 probably does not bind Ras and that its mechanism of action is likely Ras-independent, inhibits lamellipodia and circular dorsal ruffle (CDR) formation in MDA-MB-231 cells and decreases Rac activation. IODVA1 inhibits Rac activation and downstream signaling leading to inhibition of lamellipodia and CDR formation; IODVA1 inhibits cell-substratum and cell-cell interactions, does not target kinases, and reduces tumor burden of solid tumors in vivo.