lung diseases

HCH6-1 is a competitive Formyl peptide receptor 1 (FPR1) antagonist.

AZD8309 is a potent, orally available antagonist of the chemokine receptor CXCR2 that regulates neutrophil transport, significantly reduces MPO in the pancreas and lung, and decreases trypsin and elastase activity in the pancreas.AZD8309 can be used to study a range of inflammatory diseases.

S-Y048 is an Oxoeicosanoid (OXE) receptor antagonist that inhibits allergen-induced eosinophil infiltration into the skin of experimentally sensitized rhesus monkeys to house dust mites and inhibits lung inflammation caused by aerosolized allergen challenge. S-Y048 can be used to study asthma and other eosinophilic diseases.

Chromomycin A3 is an antibiotic produced by Streptomyces sp that binds to gc-rich DNA sequences in the presence of divalent cations and inhibits DNA replication and transcription; it is also used as a fluorescent DNA stain and assay; and it has anticancer activity against diseases such as Hodgkin's, lung adenocarcinomas, melanomas, and breast cancer.

FTY720 (S)-Phosphate is the active stereoisomeric phosphate derivative of FTY720 that acts as a potent modulator of sphingosine-1-phosphate (S1P) receptors. FTY720 (S)-Phosphate binds to S1P receptor subtypes S1P1, S1P3, S1P4, and S1P5 with Ki values of 2.1, 5.9, 23, and 2.2 nM respectively, causing receptor internalization on lymphocytes， preventing S1P-mediated lymphocyte egress from lymphoid tissues. FTY720 (S)-Phosphate also enhances endothelial barrier integrity, stimulates transporters such as Abcb1 and Abcc1, and inhibits cytosolic phospholipase A2 activity, highlighting its multifunctional pharmacological properties, making it an compound of interest in the research of diseases including multiple sclerosis, autoimmune diseases and cancer.

MS8511 hydrochloride is a selective G9a/GLP inhibitor with IC50 values of 100 nM and 140 nM respectively, exhibiting covalent and irreversible characteristics. MS8511 reduces intracellular H3K9me2 levels and enhances anti-proliferative activity, making it suitable for investigating multiple cancers.

SR-302 is a potent and selective inhibitor of DDR/p38, with IC50 values of 0.125 μM for p38α, 0.023 μM for DDR1, and 0.018 μM for DDR2. It is utilized in research related to fibrotic diseases, such as kidney and lung fibrosis, atherosclerosis, and various types of cancer.

P2Y14R antagonist 3 (compound A) is an orally active P2Y14R antagonist with an IC50 of 23.60 nM and a Kd of 7.26 μM. It mitigates lung injury in mice induced by Lipopolysaccharides (LPS) and can be utilized in the study of inflammatory diseases.

PDE4-IN-26 (Compound A5) is an orally active, highly selective inhibitor of PDE4. It exhibits anti-inflammatory properties by inhibiting p38 MAPK phosphorylation. In mouse models of acute lung injury and chronic obstructive pulmonary disease, PDE4-IN-26 reduces lung inflammation, damage, and fibrosis, while promoting sputum secretion and alleviating cough. It is useful for researching lung injury-related diseases.

(Iso)-TRPV4 antagonist 5 are potent, selective, and orally active transient receptor potential vanilloid 4 (TRPV4) channel blockers for the treatment of pulmonary edema and respiratory diseases. This compound was discovered through optimization of a spirocarbamate lead designed to reduce interstitial lung fluid. Research on its derivatives and related compounds primarily focuses on improving metabolic stability, reducing lipophilicity to enhance clearance, and increasing potency.

CDD-2789 is a highly selective small molecule inhibitor that targets Activin receptor type 1 (ALK2, also known as ACVR1). It effectively blocks the BMP and activin A-induced downstream phosphorylation reactions by inhibiting the ALK2/ALK1-mediated SMAD1/5 signaling pathway. In the NanoBRET cell model, CDD-2789 demonstrates an inhibitory activity with an IC50 value of 0.54 µM for ALK2. This compound holds potential for research in ALK2-related diseases, including brainstem glioma (DIPG), ependymoma, endometrial cancer, melanoma, non-small cell lung cancer, colorectal cancer, and pancreatic cancer.

c-Kit-IN-9 (Compound D9) is an inhibitor of c-Kit. It suppresses inflammation in J774A.1, RAW264.7, MPMs cells, and lung tissue by blocking LPS-induced NF-κB pathway activation. Additionally, c-Kit-IN-9 demonstrates effective anti-inflammatory activity in mouse models of acute lung injury and sepsis. It is useful for research on acute lung injury and related inflammatory diseases.

SNT-8370 is an orally active inhibitor of VAP-1 (IC50: 10 nM) and myeloperoxidase (MPO) (IC50: 17 nM), exhibiting 100-1000 times greater inhibitory potency on VAP-1 and MPO compared to other mammalian peroxidases. It effectively suppresses MPO-mediated LDL lipid peroxidation and reduces leukocyte infiltration in acute inflammatory lung injury models. SNT-8370 is an anti-inflammatory compound suitable for research on inflammatory diseases.

Spns2-IN-3 (compound 510) is an SPNS2 inhibitor with an IC50 value of 1.2 μM for hSPNS2. It is applicable in research on autoimmune diseases such as multiple sclerosis (MS) and inflammatory bowel disease (IBD), as well as fibrosis, muscle atrophy, metastasis, acute lung injury, rheumatoid arthritis, colitis, Alzheimer's disease, and other conditions linked to SPNS2 activity.

Dexamethasone acetate monohydrate is an adrenocortical steroid. It is used in the treatment of many conditions, including rheumatic problems, a number of skin diseases, asthma, severe allergies, chronic obstructive lung disease, brain swelling, croup, and antibiotics

GPR84agonist-2 (Compound 8e) is a highly selective GPR84 agonist with an EC50 value of 7.24 nM. It activates the Gαq signaling pathway, leading to the production of inositol triphosphate (IP3) and the release of calcium ions. This compound enhances the chemotaxis of neutrophils and the release of pro-inflammatory cytokines, making it a promising candidate for research into inflammatory diseases such as ulcerative colitis and acute lung injury.

Prallethrin is an airborne mosquito repellent and a non-fluorinated pyrethroid that targets lung surfactant proteins (SPs). It exhibits vapor toxicity and can bind to SPs through hydrogen bonding and hydrophobic interactions, impairing their function. Prallethrin is utilized in research concerning respiratory diseases, pathogenic infections, and malignant tumors.

MRT-23227 is a molecular glue degrader targeting cereblon (CRBN). It forms a ternary complex with CRBN and G3BP2, which activates the ubiquitin-proteasome system to degrade G3BP2. MRT-23227 shows potential for research in G3BP2-related cancers (such as breast cancer and lung cancer) and neurodegenerative diseases.

Mrt-5702D is a molecular glue degrader targeting cereblon (CRBN). It forms a ternary complex with CRBN and G3BP2, activating the ubiquitin-proteasome system to degrade G3BP2. Mrt-5702D holds potential for research in G3BP2-related cancers (such as breast cancer and lung cancer) and neurodegenerative diseases.

Linvemastat (Compound FC-4) is an orally active MMP-12 inhibitor with an IC50 of less than 10 nM and demonstrates high selectivity over MMP-1, -2, -3, -7, -9, -10, and -14. It significantly reduces lung fibrosis in a mouse model of bleomycin-induced unilateral pulmonary fibrosis and effectively alleviates kidney damage, interstitial inflammation, or fibrosis in a unilateral ureteral obstruction renal fibrosis model. Linvemastat is suitable for research into inflammatory diseases such as idiopathic pulmonary fibrosis (IPF), inflammatory bowel disease (IBD), and asthma.

Huib32 is a potent small-molecule USP32 inhibitor with an IC₅₀ of 21.2 nM and high selectivity over closely related deubiquitinases (DUBs) including USP8/10/16, UCHL1, and OTUB2. It inhibits USP32 via reversible covalent binding to the active site Cys743, thereby increasing substrate ubiquitination, altering endosomal morphology, and producing biological phenotypes similar to USP32 knockout. It can be used in research on breast cancer, ovarian cancer, lung cancer, Alzheimer’s disease, Parkinson’s disease, and other diseases.

ALK5-IN-85 (Compound 19) is an inhibitor of TGFβRI (ALK5) with an IC50 of less than 100 nM. It can be used for the treatment of respiratory diseases such as idiopathic pulmonary fibrosis, asthma, chronic obstructive pulmonary disease, and lung cancer, as well as for research on skin and ocular fibrotic diseases.

DCLK1-IN-6 (Compound 12n) is an inhibitor of doublecortin-like kinase 1 (DCLK1) with an IC50 value of 58 nM. It effectively suppresses DCLK1 enzyme activity and the inflammatory pathways it mediates. This compound exhibits noteworthy anti-inflammatory properties, significantly alleviating symptoms in acute lung injury (ALI) and sepsis mouse models. DCLK1-IN-6 is useful in research on acute inflammatory diseases.

BRM/BRG1 ATP-IN-7 (Compound Cpd69) functions as a selective dual inhibitor, effectively targeting BRM (SMARCA2) and BRG1 (SMARCA4) with IC50 values of 12 nM and 8 nM, respectively. It shows potential for research in BRM/BRG1-dependent cancers, such as non-small cell lung cancer and Ewing's sarcoma, as well as virus-associated diseases like HPV infection.