recruitment

NH-3 is a potent orally active thyroid hormone receptor (THR) antagonist which exhibits reversible behavior, demonstrated by an IC 50 of 55 nM. Derived from the selective thyromi-metic GC-1, NH-3 effectively inhibits the binding of thyroid hormones to their respective receptors, resulting in hindered cofactor recruitment.

Lenalidomide-Br (Compound 41), a derivative of Lenalidomide, acts as a ligand for cereblon (CRBN) - an E3 ubiquitin ligase involved in protein recruitment. This compound can be conjugated to a protein ligand via a linker to create PROTACs, such as the PROTAC STAT3 degrader SD-36.

AS-041164 is a selective and orally active PI3Kγ isoform inhibitor(IC50 of 70 nM), and shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). It has anti-inflammatory effects.

BLT-1 is a scavenger receptor BI (SR-BI)inhibitor.

SB-265610 (GSK-CXCR2) is a nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis (IC50s: 3.7 nM and 70 nM, respectively).

BMS-986122 (BMS 986122) is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM).

MLS1547 (MLS000051547) is a highly efficacious agonist of G protein-biased dopamine D2 receptor with a Ki of 1.2 μM. MLS1547 stimulates D2R G protein-mediated signaling with EC50 of 0.37 μM in a calcium mobilization assay.

SX-682 is an orally available allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor myeloid suppressor cell recruitment and enhances T cell activation and anti-tumor immunity, with the potential to treat castration-resistant prostate cancer.

WHI-P97 is a rationally designed potent inhibitor of JAK-3. IC50 value: Target: JAK3 Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal.

SAR247799 (S1P1 agonist 3) is a selective and G-protein-biased S1P1 agonist that activates downstream G-protein signaling pathways more preferentially than β-blocker proteins and internalized signaling pathways, activates S1P 1 on endothelial cells without causing receptor desensitization, and protects the endothelium without affecting lymphocyte populations, and can be used to study type 2 diabetes, endothelial dysfunction and vascular hyperpermeability.

Anti-Mouse Ly6G Antibody (1A8) is an anti-mouse Ly6G antibody that binds to Ly-6G on neutrophils and can be used for flow cytometry analysis and studies of neutrophil infiltration, recruitment and migration.

Leukotriene C4 (LTC4) is an arachidonate lipid mediator that regulates leukocyte recruitment and function at sites of inflammation.Leukotriene C4 is a mediator of bronchoconstriction, mucus hypersecretion, and eosinophilia, and has a mediating role in urticaria.

6'-GNTI dihydrochloride is a κ-opioid receptor (KOR) agonist that favors activation of G-protein-mediated signaling over recruitment of β-aspirin 2. 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons.

P53R3 is a potent reactivator of p53, effectively restoring sequence-specific DNA binding to several p53 hot spot mutants, namely p53 R175H, p53 R248W, and p53 R273H. This compound exhibits p53-dependent antiproliferative effects with significantly higher specificity compared to PRIMA-1 and promotes the recruitment of both wild-type p53 and p53 M237I to various target gene promoters. Additionally, P53R3 markedly increases the mRNA, total protein, and cell surface expression of death receptor 5 (DR5), demonstrating its utility in cancer research.

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1/2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

C004019 belongs to PROTACs and is a tau protein-targeted degrader (via recruitment of VHL E3 ligase) with blood-brain barrier permeability and selective tau degradation capability. This compound significantly reduces tau levels and improves cognitive function, and is used in research on Alzheimer's disease and related tauopathies.

GPR35 agonist 3 is a synthetic GPR35 agonist with an EC50 value of 1.4 μg in the β-arrestin recruitment assay.GPR35 agonist 3 is used in the study of cancer, type 2 diabetes, and cardiovascular disease.

Thalidomide 4-fluoride (E3 ligase Ligand 4) (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand. Thalidomide 4-fluoride can be used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.

(S,R,S)-AHPC (VH032-NH2) is a VH032-based ligand for recruiting the von Hippel-Lindau (VHL) protein, potentially useful for the targeted degradation of the androgen receptor.

Thalidomide-5-OH (2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione) is the Thalidomide-based cereblon ligand that used in the recruitment of CRBN protein. It can be connected to the ligand for protein by a linker to form PROTAC.

(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is utilized in the synthesis of ARV-771, a potent BET protein degrader. It selectively degrades BET protein in castration-resistant cells with a DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, it serves as the VHL ligand from (S,R,S)-AHPC for recruiting von Hippel-Lindau (VHL) protein.

Thalidomide-propargyl, a Thalidomide-derived Cereblon ligand, facilitates the recruitment of Cereblon. It can be attached to the protein ligand via a linker, producing IMiD-containing PROTACs.

Thalidomide-5-methyl is a Thalidomide-based cereblon (CRBN) ligand used for the recruitment of CRBN protein.

Neotuberostemonine (NTS) is one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, it has a significant protective effect on bleomycin (BLM)-induced pulmonary fibrosis through suppressing the recruitment and M2 polarization of macroph