c-fos

Picrasidine I has antiosteoclastogenic effect by inhibiting inflammation induced activation of MAPKs, NF-κB and ROS generation followed by suppressing the gene expression of c-Fos and NFATc1 in osteoclast precursors.

C-Fos Lentiviral CDNA ORF Clone, Human, C-GFPSpark Tag is an ORF clone of the FOS plasmid, where Fos encodes a leucine zipper protein and forms the transcription factor complex AP-1, which regulates cell proliferation, differentiation, and transformation.

c-Fos-IN-1 (Compound P16) acts as a c-Jun inhibitor, effectively reducing the mRNA and protein levels of c-Fos. It also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. This compound demonstrates anticancer properties through the inhibition of the ERK/c-Fos/Jun pathway. c-Fos-IN-1 curbs the proliferation and migration of gastric cancer cells, with an IC50 of 2.31 μM for MGC-803 cells, causing cell cycle arrest at the G2/M phase and inducing apoptosis in cancer cells. Additionally, c-Fos-IN-1 hampers the growth of gastric cancer tumors.

Rabacfosadine (GS-9219) is a novel dual pre-drug of the acyclic nucleotide phosphonate PMEG to tumor lymphocytes for the study of lymphoma.

T-5224 is a selective inhibitor of the transcription factor c-Fos/activator protein (AP)-1 with anti-inflammatory effects. T-5224 specifically suppresses the DNA-binding activity of c-Fos/c-Jun, thereby inhibiting IL-1β-induced transcriptional upregulation of Mmp-3, Mmp-13, and Adamts-5, without affecting the binding activity of other transcription factors. T-5224 can be used in research on rheumatoid arthritis, osteoarthritis, and cartilage degeneration.

Fosteabine is an oral and prodrug analog of cytarabine. It is resistant to deoxycytidine deaminase.

Lenacapavir pacfosacil (Example 44) is an inhibitor of viral capsid and nucleocapsid, exhibiting antiviral properties. This compound is utilized in the study of retrovirus infections, including HIV infection.

Rabacfosadine succinate is the acyclic nucleoside phosphonate PMEG double prodrug.

Osemozotan HCl (Osemozotan hydrochloride) is a novel and selective 5-HT1A receptor agonist that reduces methamphetamine-induced c-Fos expression in the medial prefrontal cortex and striatum.Osemozotan HCl is used in the study of mechanical abnormalities of pain and depression.

Elgodipine significantly reduced the incidence and severity of exercise-induced angina pectoris systemically and was able to inhibit vascular smooth muscle proliferation through a mechanism independent of the expression of the transcription factors c-fos and c-jun. The Elgodipine-induced inhibition was voltage-dependent. Elgodipine is a potential compound for the treatment of angina pectoris.

Vitamin K2 (Menatetrenone) is a menaquinone compound and form of vitamin K2 with potential antineoplastic activity. Menatetrenone may act by modulating the signaling of certain tyrosine kinases, thereby affecting several transcription factors including c-myc and c-fos. This agent inhibits tumor cell growth by inducing apoptosis and cell cycle arrest.

Latanoprost acid is a selective agonist of prostanoid receptors and inhibits RANKL-induced osteoclastogenesis and function through the inhibition of c-fos/NFATc1 pathway. Latanoprost acid can be used in studies about lowering pressure inside the eyes.

JNK-1-IN-3 (Compound 9e) is a JNK1 inhibitor that downregulates JNK1 and phosphorylated JNK1, reduces c-Jun and c-Fos expression in tumours, and restores p53 activity. JNK-1-IN-3 exhibits potent antiproliferative activity against renal carcinoma and breast cancer cell lines.

Schizophyllan is an extracellular β-glucan synthesized by Schizophyllum commune. It improves mitochondrial function by activating the SIRT3 signaling pathway, thereby alleviating metabolic liver injury. Meanwhile, it inhibits JNK/p38 phosphorylation and downregulates the expression of PGC1β/PPARγ, c-Fos and NFATc1, thus suppressing osteoclast formation and promoting osteoblast differentiation. In addition, Schizophyllan enables targeted delivery of oligonucleotide drugs and antigens to antigen-presenting cells via Dectin-1-mediated recognition, showing broad application prospects in the treatment of inflammatory diseases and vaccine development.

NecroX-2 is a cell-permeable necrosis inhibitor with antioxidant properties. NecroX-2 selectively suppresses necrotic cell death triggered by oxidative stress. NecroX-2 does not confer protection against apoptosis induced by staurosporine or etoposide but shows protective effects under conditions such as cold shock, hypoxia, and oxidative stress in vitro.

Cannabidiolic acid methyl ester (HU-580) is an orally active analogue of cannabidiolic acid. It enhances the activation of 5-HT1A receptors and increases the expression of c-Fos and NeuN in specific hypothalamic nuclei in rats. Cannabidiolic acid methyl ester exhibits anti-nausea, anxiolytic, and anti-nociceptive effects.

NF-κB/MAPK-IN-2 (compound 14) is a potent inhibitor of NF-κB and MAPK pathways. It effectively reduces the protein expression levels of p-p65, p-IκB, p-p38, p-JNK, and p-ERK. This compound decreases the release of TNF-α and IL-6 induced by LPS and inhibits the nuclear translocation of p65 and c-Fos. NF-κB/MAPK-IN-2 shows potential for research in sepsis.

Methylcarbamyl PAF C-8 is resistant to degradation by PAF-AH and has a half-life of over 100 minutes in platelet-poor plasma, exhibiting platelet aggregation activity. In NRK-49 cells overexpressing PAF receptor, it induces the expression of c-myc, c-fos, and activates mitogen-activated protein kinase (MAPK). Furthermore, Methylcarbamyl PAF C-8 can induce G1 phase cell cycle arrest. This compound shows potential for research in cardiovascular and anti-cancer applications.

ATB-429 is a mesalazine derivative capable of releasing H2S, demonstrating significant analgesic and anti-inflammatory effects in an irritable bowel syndrome (IBS) model. By releasing hydrogen sulfide (H2S), ATB-429 modulates hypersensitivity induced by colorectal distension in healthy and post-colitis rats. It alleviates abdominal withdrawal responses and inhibits spinal c-Fos mRNA expression, indicating its potential to relieve pain associated with gastrointestinal inflammation. Furthermore, ATB-429 downregulates mRNA expression of colonic cyclooxygenase-2 (COX-2) and IL-1β, an effect not observed with mesalazine alone. The mechanism involves ATP-sensitive K+ (KATP) channels, evidenced by the reversal of ATB-429's effects with glibenclamide. These findings suggest that ATB-429 may offer therapeutic benefits for treating inflammatory pain-related bowel conditions.

RIPK1-IN-32 is an RIPK inhibitor with anti-inflammatory properties. It inhibits nitric oxide (NO) release, with an IC50 of 3.26 μM. Additionally, RIPK1-IN-32 disrupts the RIPK1/NF-κB/MAPK signaling pathway, preventing nuclear translocation of p65 and c-fos, leading to reduced expression of TNF-α and IL-6 and significantly alleviating acute liver injury related to sepsis. This compound is useful for studies on acute liver injury and sepsis.

Y1693 is an orally active RANKL inhibitor with a Kd value of 5.03 μM for hRANKL. Y1693 inhibits activation of the downstream c-fos/NFATc1 signaling pathway by blocking the interaction between RANKL and RANK. Y1693 significantly inhibits RANKL-induced osteoclast differentiation, F-actin ring formation, and bone resorptive activity while downregulating the mRNA and protein expression levels of TRAP, cathepsin K, c-fos, and NFATc1. Y1693 demonstrates no obvious cytotoxicity toward bone marrow-derived macrophages and osteoclast precursor cells and exhibits favorable ADME properties. Y1693 improves ovariectomy-induced osteoporosis in mice and reverses ligation-induced periodontal alveolar bone loss. Y1693 is applicable to research involving osteoporosis, osteoclast biology, and periodontal disease-associated bone remodeling mechanisms.

PCC0105005 is a dual-target CGRP Receptor antagonist (IC50 = 1.01 nM) and 5-HT1F Receptor partial agonist (EC50 = 77.91 nM). It demonstrates significant efficacy in rat models of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins while inhibiting the phosphorylation levels of ERK and CREB. This compound is useful for migraine research.

HHL-6 is a c-Fos and BDNF protein expression modulator.

RGH 1756 is an atypical antipsychotic with high affinity to dopamine D(3) receptors that leads to c-Fos induction in a unique pattern.