Ionizable Lipid Products

Bexin-1 is a specific inhibitor that targets Munc13-4, a protein critical for regulated exocytosis, particularly in secretory cells such as immune cells (e.g., cytotoxic T lymphocytes, mast cells) and neuroendocrine cells. Munc13-4 plays a key role in vesicle priming and fusion with the plasma membrane, a process essential for the release of secretory granules containing hormones, neurotransmitters, or immune mediators.

Org 274179-0 is a highly potent, allosteric antagonist of the thyroid-stimulating hormone receptor (TSH receptor), inhibits bTSH-, hTSH- and M22-mediated CRE-luciferase transactivation in the CHO cell line.

PF-07328948 is a first-in-class branched-chain ketoacid dehydrogenase kinase (BDK) inhibitor with IC50 of 15 nM and shows a high degree selectivity over a number of kinases and other off-targets. PF-07328948 is the first known selective BDK inhibitor candidate to be examined in clinical studies.

PT-2385 is a selective HIF-2α antagonist with a Ki of less than 50 nM.

NH-23-C2 (Caspase-2 inhibitor NH-23-C2) is a potent, selective and cell-permeable endogenous caspase-2 inhibitor, does not block caspase-3 or caspase-8.NH-23-C2 displays off-reactivity with cysteine and threonine proteases (cathepsins B, L, V, S).HCT116 cells were preincubated with NH-23-C2 inhibitor, MDM-2 cleavage was inhibited in a concentration-dependent manner (IC50 =3.11 μM).NH-23-C2 selectively block caspase-2 activity and caspase-2-mediated MDM-2 cleavage.

PZ09 (PKC-zeta inhibitor 9, PKC-ζ inhibitor PZ9) is a potent, isoform selective PKC-zeta (PKC-ζ) inhibitor with IC50 of 5.18 nM, displays excellent selectivity (>200-fold) over other PKC isoforms with exception of PKC-i (10-fold). PZ09 also shows high selectivity for CDK-2 (>200-fold), as well as a broader range of other kinases (<50% inhibition at 10 uM). PZ09 is a small-molecule inhibitor, the first tool to successfully interrogate aPKC signaling in cells.

Artemisitene is an antimalarial agent and the oxidized form of Artemisinin. Artemisinin precursors are the important basic substances for biosynthesis of Artemisinin, including Artemisinic acid, Artemisinin B, Artemisitene, etc.

E722-2648 (Compound C-1) is a novel specific and competitive small molecule β-catenin/BCL9 interaction inhibitor with ITC KD of 1.05 uM and IC50 of 9 uM, blocks oncogenic Wnt signaling and disrupts cholesterol homeostasis in colorectal cancer.E722-2648 (Compound C-1) inhibited β-catenin/BCL9 complexes at concentrations as low as 1 uM in BCL9-dependent CRC cell lines, Colo320 and HCT116.E722-2648 (Compound C-1) inhibited the expression of bona fide downstream Wnt/β-catenin target genes, AXIN2 and CD44, in the β-catenin/BCL9-dependent CRC cell lines.E722-2648 (Compound C-1) disrupted cholesterol homeostasis via increased cholesterol esterification and lipid droplet accumulation.E722-2648 (Compound C-1) demonstrated antitumorigenic activity in CRC cell lines and xenograft mouse models.

DG-172 is a novel PPARβ/δ-selective ligand showing high binding affinity (IC50= 27 nM) and potent inverse agonistic properties; inhibits agonist-induced activity of PPARβ/δ, enhances transcriptional corepressor recruitment; down-regulates transcription of the PPARβ/δ target gene Angptl4 in mouse myoblasts (IC50= 9.5 nM); orally bioactive.

Rhobo6 is a fluorescent glycan-binding probe optimized for live-cell imaging and in vivo tracking of glycoconjugates. It exhibits pH-dependent binding (pKa ~5-7), high photostability, and minimal cytotoxicity. Compatible with mammalian cells, zebrafish, plant tissues, and mouse models.

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

MRT-6160 represents a groundbreaking molecular glue degrader designed to selectively target VAV1, achieving its proteasomal degradation with a DC50 value of 7 nM. This innovative compound showcases its unique mechanism and therapeutic potential.

SKLB-03176 (SKLB03176) is a potent, selective, covalent EZH2 inhibitor with IC50 of 47 nM, covalently binds to the SAM pocket of EZH2.SKLB-03176 showed good inhibitory activity against mutations EZH2 Y641F, EZH2 Y641N, and EZH2A677G at 200 nM concentration.SKLB-03176 exhibited weak activity against other targets, such as 5 histone methyltransferases and more than 30 kinases, >50-fold selective for EZH2 over the highly homologous H3K27 methyltransferase EZH1 (IC50=2.45 uM).SKLB-03176 inhibited the activity of a variety of EZH2 mutants and significantly inhibited the expression of H3K27Me3 in cells.SKLB-03176 showed no cytotoxicity to normal cells.

KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.

Fluorofurimazine is an advanced furimazine derivative with enhanced aqueous solubility, allowing for greater signal output compared to furimazine in bioluminescence imaging. This compound supports higher substrate concentrations and delivers improved sensitivity for in vivo optical imaging applications.

Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM. Gandotinib (LY2784544) also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.

DesMEM AZD4694（AZD4694 Precursor 1）is the precursor of 18F AZD4694 for the synthesis of 18F AZD4694, an amyloid-β imaging ligand with high affinity for amyloid-β plaques.

Cephalofurimazine (CFz) is a NanoLuc substrate optimized for enhanced brain performance. When paired with Antares luciferase, it generates over 20 times more signal from the brain compared to the traditional combination of D-luciferin and firefly luciferase.

PF-07220060 is a potent CDK4/CDK6 inhibitor with a Ki of 0.6 nM and 13.9 nM for CDK4/Cyclin D1 and CDK6/Cyclin D3, respectively.

J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA is used for the relief of mechanical allodynia and mechanical hyperalg