maturation

Betamethasone (NSC-39470), a glucocorticoid steroid, has immunosuppressive and anti-inflammatory properties.

Allethrin induces oxidative stress, apoptosis and calcium release. Allethrin, a pyrethroid insecticide is a major mosquito repellent agent.

Cyclofenil is an estrogen antagonist, has anti-dengue-virus activity

Jagged-1 (188-204) TFA(219127-21-6 free base) is a fragment of the JAG-1 protein. JAG-1 is Notch ligand, a peptide that is the most conspicuously expressed ligand in skin. JAG-1 induces epidermal maturation. Exposing submerged keratinocytes monolayers to JAG-1 with elevated calcium concentration produces stratification with loricrin expression and NF-alphaB activation.

Cavosonstat (N91115) is an orally active S-nitrosoglutathione reductase (GSNOR) inhibitor that promotes cystic fibrosis transmembrane conductance regulator (CFTR) maturation and plasma membrane stabilization. As a CFTR stabilizer, Cavosonstat can be used to study cystic fibrosis.

BDCRB inhibits herpesvirus DNA maturation. BDCRB causes the HCMV terminase to skip the normal cleavage site and to continue to package DNA until a second cleavage site is encountered 30 kb further along the concatemer.

Acetyl-L-carnitine hydrochloride (Acetyl L-carnitine hydrochloride) is a nutritional supplement composed of the hydrochloride salt form of the acetylated form of the endogenously produced L-carnitine, with potential neuroprotective, cognitive-enhancing, anti-depressive and immunomodulating activities. It may also relieve peripheral neuropathy induced by chemotherapy, diabetes or other diseases. In addition, acetyl-L-carnitine may modulate the immune response by increasing T-lymphocytes maturation and may downregulate pro-inflammatory cytokines in response to viruses, such as SARS-CoV-2. It may also disrupt the ACE2 signaling pathway and inhibit the production of reactive oxygen species (ROS).

Lumacaftor (VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein. It enhances F508del-CFTR protein maturation in FRT cells (EC50: 100 nM).

Vacuolin-1 is a cell-permeable inhibitor of Ca2+ dependent fusion of lysosomes to the cell membrane. It acts by inhibiting release of lysosomal content.vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation

BMS641 (BMS-209641) is a selective and potent RARβ agonist with high affinity for RARβ, which synergistically activates RARβ and RARgamma to induce cellular maturation into specialized neuronal subtypes.

GSK3532795 is a potent, orally active, second-generation HIV-1 maturation inhibitor (EC50s: 10.2, 1.9, 2.7, and 13 nM for HIV-1 WT(human serum), HIV-1 WT, HIV-1 V370A, and HIV-1 ΔV370).

Reslizumab (Sch 55700) is a humanized immunoglobulin G (IgG)4 κ monoclonal antibody that binds to human interleukin 5, thereby decreasing eosinophil production and survival.Reslizumab improves lung function, induces a decrease in eosinophil production and maturation, and may be used in the study of asthma.

GSK2838232, a novel human immunodeficiency virus (HIV) maturation inhibitor, inhibits HIV reverse transcriptase activity across a broad panel of HIV-1 isolates.

9-cis-Retinal is a retinoid with Kd of 8 nM and 5 nM for cellular retinol binding protein-I (CRBP-1) and CRBP-II, respectively. 9-cis-Retinal accelerates the differentiation and maturation of rod photoreceptors in retinal organoids, reduces the toxicity of unliganded opsins, and can be used to study congenital stationary night blindness caused by G90D rhodopsin.

1Z105, an orally active TLR4 MD2 ligand, facilitates dendritic cell maturation and antigen presentation, thereby preventing arthritis.

PfCLK3-IN-1 (Compound 4) serves as a covalent inhibitor of the malaria parasite CLK3 (Pf CLK3) under alkaline conditions, with a pEC50 of 7.1. It inhibits the maturation of gametocytes during the sexual stage of the parasite, thereby hindering transmission. Additionally, PfCLK3-IN-1 effectively suppresses the Dd2-B2 clone of the malaria parasite, exhibiting an IC50 of 239.5 nM.

Lipid N2-3L is an ionizable cationic lipid with a pKa of 8.99, utilized in the formation of supramolecular lipid nanoparticles (SMLNPs) for enclosing mRNA in both in vitro and in vivo applications. Lipid N2-3L-containing SMLNPs accumulate at the injection site and draining lymph nodes in mice, featuring a luciferase reporter gene. Additionally, SMLNPs made with Lipid N2-3L that encapsulate ovalbumin mRNA and the Toll-like receptor 7 8 (TLR7 8) agonist R-848 serve as adjuvants. These enhance dendritic cell maturation and antigen presentation, reducing tumor volume and increasing survival rates in MC-38-OVA colon cancer mouse models.

GSK3532795 (also known as BMS-955176) is a potent oral second-generation HIV-1 maturation inhibitor (MI) that has advanced to phase IIb clinical trials. This compound exhibits broad coverage against polymorphic viruses (EC50 < 15 nM, covering common polymorphisms representing 96.5% of HIV-1 subtype B) and demonstrates favorable pharmacokinetic properties in preclinical species.

MK256 is a novel CDK8 inhibitor that demonstrates potent antitumor activity against AML by inhibiting the STAT pathway. It induces differentiation and maturation while inhibiting proliferation in AML cell lines. MK256 decreases the phosphorylation of STAT1(S727) and STAT5(S726) and reduces mRNA expression of MCL-1 and CCL2 in these cells. Its efficacy is validated in the MOLM-14 xenograft model, showing phosphorylation inhibition of STAT1(S727) and STAT5(S726) post-treatment. Pharmacokinetic studies in the MOLM-14 model reveal a dose-dependent inhibition of the STAT pathway. Both in vitro and in vivo studies confirm that MK256 effectively downregulates the STAT pathway.

ARN23765 is an F508del-CFTR corrector with an EC50 of 38 pM in human bronchial epithelial cells. It enhances the maturation and function of F508del-CFTR at the cell membrane, influencing ion transport and secretion, thereby addressing the pathological mechanisms of cystic fibrosis (CF).

VB-85247 is a STING agonist that, by activating the STING pathway, induces the upregulation of inflammatory cytokines IFNα/β, TNFα, IL6, and CXCL10, as well as the maturation and activation of dendritic cells. It can lead to the regression of tumors within the bladder and is applicable in bladder cancer research.

Mozenavir (DMP 450) is an orally active and highly selective inhibitor of HIV-1 protease with a Ki of 0.3 nM. It disrupts the cleavage and processing of viral polyproteins, thereby inhibiting the replication and maturation of HIV-1. Mozenavir shows potential for research into HIV infections.

Maribavir (GW257406X) is an orally available benzimidazole riboside compound with activity against cytomegalovirus (CMV). Maribavir is a selective ATP competitor of the viral UL97 kinase, which is involved in viral nuclear maturation events, such as viral DNA assembly and movement of viral capsids from the nucleus of infected cells. Maribavir has activity against strains of CMV that are resistant to standard anti-CMV agents.

Psora 4 (5-(4-Phenylbutoxy)psoralen) is a selective and potent Kv1.3 blocker, a caloric restriction mimetic with immunosuppressive activity that enhances neural progenitor cell differentiation and maturation.