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Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. [1] Osunprotafib (ABBV-CLS-484) stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function and enhances T cell anti-tumor immunity by enhancing JAK-STAT signaling and reducing T cell dysfunction. [2]

T-448 is a specific, orally active, and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) with an IC50 of 22 nM.

CINPA1 (CINPA 1) is a selective inhibitor of constitutive androstane receptor (CAR) with an IC50 of 70 nM for CAR-mediated transcription. CINPA1 can be used in studies about CAR function.

AMG-0347 (UNII-CD7L9290QR) is a small molecule inhibitor targeting TRPA1(transient receptor potential ankyrin 1) ion channels, a receptor found in sensory neurons and involved in the detection of pain and environmental stimuli. AMG-0347 acts by blocking the function of TRPA1 and has analgesic effects.

TCIP 1 is a small molecule in the category of transcriptional epigenetic covalent inhibitor probes (TCIPs) that forms covalent bonds with molecules targeting BCL6 and BRD4. This compound facilitates cell death gene expression by directing endogenous cancer drivers or transcription factors to the promoters of these genes. Additionally, TCIP 1 exhibits a gain-of-function mechanism, displaying both cell and tissue specificity, and it establishes a ternary complex with BCL6 and BRD4. It counteracts BCL6's inhibitory effect on apoptosis gene expression, leading to the activation of apoptosis. Furthermore, TCIP 1 markedly suppresses MYC oncogene expression and curtails the proliferation of diffuse large B-cell lymphoma (DLBCL) [1].

1-Decanol inhibits various bacteria and fungi, including Candida albicans, Penicillium, Aspergillus niger, Bacillus subtilis, Propionibacterium, and others.

(-)-Epicatechin gallate ((-)-Epicatechin 3-O-gallate) is one of the catechin isomers and a potent antioxidant that can modulate a wide range of membrane proteins. Its bilayer-modifying potency was tested using gramicidin A (gA) channels as probes. All the catechins alter gA channel function and modify bilayer properties, with a 500-fold range in potency. The gallate group causes current block, as evident by brief downward current transitions.

Lifitegrast (SAR 1118) is an antagonist of lymphocyte function-associated antigen-1.

1. trans-Cinnamaldehyde (Phenylacrolein) exhibits excellent anti-inflammatory activities and antidepressant-like effects in stressed mid-aged rats as a COX-2 inhibitor. 2. Cinnamic aldehyde induces apoptosis of CML cells in vitro, down-regulation of the expression and function of BCR-ABL may be one of its most important anti-leukemia mechanisms. 3. Cinnamic aldehyde and cinnamic acid are cardioprotective in a rat model of ischemic myocardial injury, the mechanism is related to anti-oxidative and anti-inflammatory properties.

Sarpogrelate hydrochloride (MCI-9042) , a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate hydrochloride was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate hydrochloride lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate hydrochloride -induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

Collagenase Type I is a proteolytic enzyme that primarily targets collagen and is able to break down peptide bonds in collagen. Collagenase is used as a potential therapeutic option to break up the herniated disc material, thereby reducing compression of nearby nerves. Collagenase may aid in the breakdown and reorganization of excessive scar tissue, potentially improving tissue function and appearance. Collagenase has the potential to treat intervertebral disc herniation, keloid, fat mass, lipoma, as well as Peyronie's disease and palmar fibromatosis.

1-Thioglycerol (alpha-Thioglycerol) is an antioxidant thioglycerol that scavenges free radicals and reduces oxidative stress as a media component, and is used as a matrix in fast atom bombardment mass spectrometry (FAB-MS) and liquid secondary ion mass spectrometry (LSIMS).

1-Nonanol (Nonan-1-ol) is a fragrance with antifungal activity that acts by disrupting cell membrane integrity and mitochondrial function.

UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy.

Salubrinal, a phosphatases (PP1) inhibitor(IC50=1.7 μM), exhibits function on the eukaryotic translation initiation factor 2 subunit (eIF2α).

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

BMS-688521 BMS-688521 is an orally active and potent inhibitor of LFA-1 ICAM interaction, a small molecule antagonist of leukocyte function-associated antigen-1 (LFA-1), with potential anti-inflammatory activity.

MIRA-1 (WRN Helicase Inhibitor) is a restorer of wild-type p53 conformation cellular function and selectively inhibits Werner syndrome WRN helicase activity with an IC50 of 20 µM.

KR-32568 is a sodium hydrogen exchanger 1 (NHE-1) inhibitor (IC50: 230 nM) with potent cardioprotective effects. At a concentration of 10 μM, it restored cardiac systolic function in an isolated ischemic rat heart model. Additionally, KR-32568 (0.3 mg kg) reduced myocardial infarction size in a rat model of ischemia and reperfusion injury.

1-(3,4-dihydroxyphenyl)-2-(dimethylamino)ethan-1-one hydrochloride is a cholinergic agent that inhibits choline metabolism, which leads to increased levels of acetylcholine in the brain, which in turn enhances cognitive function and memory.

1-Methyl-6-oxo-1,6-dihydropyridine-3-carboxylic acid (Nudifloric Acid) from Cordyceps bassiana targets to block AP-1-mediated luciferase activity, implying an anti-inflammatory function.

Doxapram hydrochloride hydrate (Doxapram HCl) effectively inhibits the function of TASK-1, TASK-3, and TASK-1 TASK-3 heterodimeric channels, displaying EC50 values of 410 nM, 37 μM, and 9 μM, respectively.

Substance P Receptor Antagonist 1 has potential applications in treating gastrointestinal disorders, inflammatory diseases, respiratory conditions, and central nervous system disorders.