cfa

BAY-1797 is an orally active and selective P2X4 antagonist (IC50: 211 nM against human P2X4) with anti-nociceptive and anti-inflammatory effects. BAY-1797 displays no or very weak activity on the other P2X ion channels.

Complete Freund's adjuvant (CFA) is an emulsified immunostimulant containing mineral oil and heat-killed mycobacteria, capable of inducing Th1 responses and enhancing immune reactions. It is frequently employed in establishing rat models of rheumatoid arthritis and persistent inflammatory pain.

GYY4137 (GYY 4137 morpholine salt) is a novel water-soluble and slow releasing H2S donor with vasodilator and antihypertensive activity. GYY4137 also exhibits anti-inflammatory and anticancer activity.

tCFA15, a trimethyl cyclohexenonic long-chain fatty alcohol with a 15-carbon atom side chain, may regulate Notch signaling and promote neuronal differentiation.

PacFA Ceramide is a 15-carbon light-activatable and clickable fatty acid. It is applicable for analyzing protein-lipid interactions in live cells.

pacFA L-carnitine is an acylcarnitine lipid.

Palmatine chloride an isoquinoline alkaloid, is an important medicinal herbal extract with diverse pharmacological and biological properties.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that suppresses HDAC1 activity and induces HDAC2 degradation, exhibiting oral bioavailability. Valproic Acid activates Notch1 signalling and inhibits the proliferation of small cell lung carcinoma cells, making it applicable for research into epilepsy and bipolar disorder.

RJW100 is a compound that acts as a potent agonist of liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1), exhibiting pEC50 values of 6.6 and 7.5, respectively. Additionally, RJW100 induces robust activation of the miR-200c (miRNA-200c, microRNA-200c) promoter.

Dihydro-5-azacytidine FA (DHAC) is a pyrimidine analog that has antitumor activity, inhibits cell growth, inhibits DNA methylation, and may be used in the study of malignant mesothelioma.

(Iso)-RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC 50 s of 6.4 and 7.2, respectively.

Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

Valproic acid sodium salt (Sodium Valproate) is the sodium salt form of valproic acid with anti-epileptic activity. Valproic acid sodium salt is converted into its active form, valproate ion, in blood. Although the mechanism of action remains to be elucidated, Valproic acid sodium salt increases concentrations of gamma-aminobutyric acid (GABA) in the brain, probably due to inhibition of the enzymes responsible for the catabolism of GABA. This potentiates the synaptic actions of GABA. Valproic acid sodium salt may also affect potassium channels, thereby creating a direct membrane-stabilizing effect.

3-(3,4-Dimethoxyphenyl)propanoic acid (3,4-Dimethoxyhydrocinnamic acid) is an orally active short-chain fatty acid (SCFAs) that promotes γ-globin gene expression and erythropoiesis in vivo, making it useful in treating beta hemoglobinopathies and other anemias.

Vardenafil hydrochloride trihydrate (BAY38-9456) is a new type PDE inhibitor with IC50 of 0.7 and 180 nM for PDE5 and PDE1, respectively.

1. Palmatine (Burasaine) is an inhibitor of dopamine generation. 2. Palmatine could potentially be developed for the treatment of flavivirus infections. 3. Palmatine has been used in the treatment of jaundice, dysentery, hypertension, inflammation, and liver-related diseases.

Divalproex Sodium (Valproate semisodium) binds to and inhibits gamma-aminobutyric acid (GABA) transaminase and its anticonvulsant activity may be exerted by increasing brain concentration of GABA and by inhibiting enzymes that catabolize GABA or block the reuptake of GABA into glia and nerve endings. It also is an HDAC inhibitor, Comprised of sodium valproate and valproic acid with anticonvulsant and antiepileptic activities. Divalproex may also work by suppressing repetitive neuronal firing through the inhibition of voltage-sensitive sodium channels.

AC 45594 (4-Heptyloxyphenol) is an agonist of steroidogenic factor 1 (SF-1) ( IC50 : 50-100 nM)

Vardenafil hydrochloride is a New Phosphodiesterase Type 5(PDE5) Inhibitor, in the Treatment of Erectile Dysfunction in Men With Diabetes

PROTAC FAK degrader 1 is a selective and potent degrader of focal adhesion kinase (Fak) with an IC50 of 6.5 nM.

TFMB-(R)-2-HG is a cell membrane-permeable (R)-2-HG, an oncogenic factor in acute myeloid leukemia. It impairs SCF ER-Hoxb8 cell differentiation in response to estrogen withdrawal.

PROTACFAKdegrader 2 (Compound F2) is a PROTAC degrader targeting focal adhesion kinase (FAK), with DC50 values for total FAK and phosphorylated p-FAK of 27.72 nM and 60.1 nM, respectively. It inhibits the viability of cancer cell lines 4T1, MDA-MB-231, MDA-MB-468, and MDA-MB-435, with IC50 values ranging from 0.73 to 5.84 μM. Additionally, PROTACFAKdegrader 2 counteracts multidrug resistance (MDR) by inhibiting the AKT and ERK signaling pathways. In HCT/8 xenograft mouse models, it demonstrates anti-tumor efficacy.

PROTACFAKdegrader 3 is a selective FAK PROTAC degrader (DC50 = 1.08 nM). It induces FAK degradation through the ubiquitin-proteasome system and its interaction with FAK and CRBN. By inhibiting FAK's non-catalytic activity, PROTACFAKdegrader 3 enhances MHC-I gene transcription and tumor cell surface expression, leading to increased antigen presentation and activation of cytotoxic CD8 T cells. Its ability to promote MHC-I expression and boost T cell activation strengthens its antitumor efficacy in vivo. PROTACFAKdegrader 3 is applicable to cancer research targeting FAK degradation, including studies on ovarian cancer and hepatocellular carcinoma.

SID 7969543 is a selective SF-1 inhibitor with potential anticancer activity, inhibits SF-1-triggered luciferase expression and can be used for cancer research.