remodeling

SB 204741 is a selective 5-HT2B antagonist with high affinity and pKi value of 7.1.

JQ-1 (carboxylic acid) is a cell-permeable BRD4 inhibitor with IC50s of 77 nM for BRD4(1) and 33 nM for BRD4(2)

Rho-Kinase-IN-1 is an inhibitor of ROCK with Kis of 30.5 nM and 3.9 nM for ROCK1 and ROCK2, respectively. Rho-Kinase-IN-1 can be used in studies about excessive cell proliferation, remodeling, edema and inflammation diseases.

N-Oleoyl-L-Serine (N-Oleoylserine) is an endogenous long-chain fatty acid amide that is a lipid modulator of bone remodeling and stimulates osteoclast apoptosis which can be used to study osteoporosis. N-Oleoyl-L-Serine showed high activity in an osteoblast proliferation assay.N-Oleoyl-L-Serine promotes osteoclast apoptosis by inhibiting Erk1 2 phosphorylation and expression of nuclear κB ligand (RANKL) receptor activator in bone marrow stromal cells and osteoblasts, which attenuates osteoclast populations.

GS-6201 (CVT-6883) is a selective antagonist of the adenosine A2B receptor, demonstrating high affinity and selectivity with a Ki of 22 nM for human adenosine A2B receptors.

5-Hydroxy-1-methylhydantoin (HD-003) is an antioxidant potentially for the treatment of renal failure. A creatinine metabolite, 5-Hydroxy-1-methylhydantoin , a hydroxyl radical scavenger, has previously been shown to confer renoprotection by inhibiting the progression of chronic kidney disease in rats. 5-Hydroxy-1-methylhydantoin is a novel anti-oxidant drug completely suppressed the expression of B2-kinin receptors (B2KR) in response to high glucose (25 mM) stimulation in VSMC and was also shown to attenuate the effects of BK on VSMC remodeling. 5-Hydroxy-1-methylhydantoin inhibited the BK-induced increase in MAPK phosphorylation and attenuated the increase in connective tissue growth factor (CTGF) protein levels in VSMC. These findings suggest that 5-Hydroxy-1-methylhydantoin may confer vascular protection against high glucose concentrations and BK-stimulation to ameliorate vascular injury and remodeling through its anti-oxidant properties.

ATP (Adenosine triphosphate) provides cellular energy, participates in overall energy balance, and maintains intracellular homeostasis. ATP can act as an extracellular signaling molecule through interactions with specific purinergic receptors to mediate a variety of processes including neurotransmission, inflammation, apoptosis, and bone remodeling.

XRK3F2 is an inhibitor of the p62-ZZ domain, blunts MM-induced Runx2 suppression in vitro, and induces new bone formation and remodeling in the presence of tumor in vivo.

GFB-8438 is a potent and subtype selective inhibitor of TRPC5(IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively).

Myoseverin, an inducer of the reversible fission of multinucleated myotubes into mononucleated fragments, affecting the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with

MMP-9-IN-6 is an MMP-9 inhibitor with an IC50 value of 50 μM and good anti-ulcer efficacy.MMP-9-IN-6 has potential anti-tumor activity and can be used to study tissue remodeling, wound repair and atherosclerosis.

TH5427 hydrochloride is a potent and selective inhibitor of NUDT5 with an IC50 of 29 nM. It demonstrates a remarkable 690-fold selectivity towards NUDT5 compared to MTH1. Moreover, TH5427 hydrochloride effectively inhibits progestin-dependent, PAR-derived nuclear ATP synthesis in breast cancer cells, thereby impeding chromatin remodeling, gene regulation, and ultimately suppressing proliferation.

SMARCA2-IN-8 (Compound 13) is an orally effective inhibitor targeting the SWI SNF chromatin remodeling complexes SMARCA2 (also known as Brahma homolog, BRM) and SMARCA4 (also known as Brahma-related gene 1, BRG1), with IC50 values of 5 nM and 6 nM respectively. This compound inhibits the proliferation of SMARCA2-mutant SKMEL5 cancer cells with an AAC50 of 5 nM and downregulates the expression of the SMARCA2-dependent gene KRT80, showing an AAC50 of 10 nM. Additionally, SMARCA2-IN-8 demonstrates antitumor efficacy and favorable pharmacokinetic properties in mice.

SMARCA2-IN-1 (Compound I-19) serves as an inhibitor of the SWI SNF chromatin remodeling complex SMARCA2, exhibiting an IC50 value greater than 1000 nM in H1299 cells.

Enrasentan (also known as SB-217242) is a dual receptor endothelin antagonist with a higher affinity for the ET(A) receptor. In animal models of hypertension and cardiac hypertrophy, this compound reduces blood pressure, prevents cardiac hypertrophy, and preserves myocardial function. Enrasentan enhances survival rates, limits left ventricular remodeling, and maintains myocardial performance in hypertensive cardiac hypertrophy and dysfunction.

MDL-100240 is a dual inhibitor of angiotensin-converting enzyme (ACE) and neprilysin with a balanced activity. MDL 100240 shows an impressive effectiveness both in preventing and in regressing hypertension-induced vascular remodeling and cardiac hypertrop

1-O-Hexadecyl-2-eicosapentaenoyl-sn-glycero-3-PC is a compound that results from the incorporation of eicosapentaenoic acid (EPA) into lyso-PAF C-16, a process demonstrated in neutrophils from monkeys and humans consuming a diet rich in fish oils. Furthermore, it functions as a precursor for PAF C-16 synthesis via the remodeling pathway.

(-)-Praeruptorin A has anti-inflammatory, anti-contractile and anti-hyperplasia activities, it exerts distinct relaxant effects on isolated rat aorta rings dependent on endothelium and nitric oxide synthesis;it also can significantly suppress airway inflammation and airway remodeling induced by ovalbumin challenge, and is a potential candidate for the treatment of asthma. (-)-Praeruptorin A resensitizes Pgp-mediated MDR (Pgp-MDR) cancer cells to cancer drugs.

Nanatinostat, also known as Tractinostat, CHR-3996 and VRx-3996, is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor cell apoptosis. This agent may upregulate HSP70 and downregulate anti-apoptotic Bcl-2 proteins more substantially than some first-generation HDAC inhibitors. HDACs, upregulated in many tumor cell types, are a family of metalloenzymes responsible for the deacetylation of chromatin histone proteins.

FT-1101 is an orally bioavailable, potent and selective BET inhibitor. FT-1101 binds to the acetylated lysine recognition motifs in the bromodomain sites of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to the inhibition of tumor cell growth. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth.

WQ-C-401 is an orally active inhibitor of the platelet-derived growth factor receptor (PDGFR). It inhibits cell proliferation by blocking PDGFR auto-phosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRαY849 and 5.8 nM for PDGFRβY1021. Additionally, WQ-C-401 suppresses the proliferation and migration of PASMCs by inhibiting PDGF-BB-induced phosphorylation of ERK1 2, reduces collagen I synthesis, and increases α-SMA expression, thereby preventing pulmonary vascular remodeling. This compound shows promise for research in the field of pulmonary arterial hypertension.

Mivebresib (ABBV-075), also known as ABBV-075, is a potent BET inhibitor (bromodomain (BRD)-containing protein) with potential antineoplastic activity. Upon administration, the bromodomain inhibitor ABBV-075 binds to the acetyl-lysine binding site in the BRD of certain BRD-containing protein(s), thereby preventing the interaction between those proteins and acetylated histones. This disrupts chromatin remodeling, prevents the expression of certain growth-promoting genes, and leads to an inhibition of cell growth in susceptible tumors. Also a potent inhibitor of MYC and the TMPRSS2-ETS fusion proteins.

MDL3, a novel inhibitor of PDE4B and PDE5A, demonstrates resilience against liver damage and inflammation while inhibiting pathological remodeling of adipose tissue.

SMARCA2-IN-4 (Compound 26) is an inhibitor of the SWI SNF chromatin remodeling complex SMARCA, specifically targeting its bromodomain. This compound exhibits high affinity for PB1(5), SMARCA2B, and SMARCA4, with dissociation constants (Kd) of 124, 262, and 417 nM, respectively.