22-hydroxy mifepristone

22-Hydroxy Mifepristone (RU 42698) is an orally active hydroxylated alcohol metabolite that exhibits both anti-progestational and anti-glucocorticoid activities. This compound contains an alkyne group and is capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. Furthermore, 22-Hydroxy Mifepristone demonstrates a relative binding affinity of 48% to the human glucocorticoid receptor.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Liproxstatin-1 is a potent and selective inhibitor of ferroptosis (IC50=22 nM). Liproxstatin-1 protects cells from ferroptosis induced by ferroptosis inducers (e.g., Erastin, RSL3).

(-)-Epigallocatechin Gallate (EGCG) is a phenolic antioxidant polyphenol flavonoid found in plants such as green and black tea, which inhibits telomerase and DNA methyltransferase, blocks the activation of EGF receptors and HER-2 receptors, inhibits cellular oxidation, and prevents free radical damage to cells.

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4 5.2 nM). Lenvatinib has strong anti-tumor activity.

Rutin (Quercetin 3-O-rutinoside), a flavonoid, has a variety of biological activities including antiallergic, anti-inflammatory, antiproliferative, and anticarcinogenic properties.

Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.

Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.

Lipopolysaccharides (LPS), derived from Escherichia coli O55:B5, are essential components of the outer membrane of Gram-negative bacteria. Composed of lipid A, a core oligosaccharide, and an O-specific polysaccharide, LPS exhibits strong immunogenicity. It activates immune cells via the TLR4 receptor, induces chemotactic cell migration and cytokine secretion, and helps maintain the integrity of the bacterial outer membrane, protecting against bile salts and lipid-based antibiotics. LPS is commonly used to establish inflammatory models, including arthritis, chronic obstructive pulmonary disease (COPD), acute respiratory distress syndrome (ARDS), and gastrointestinal disease models.

Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.

Resmetirom (MGL-3196) is a THR-β agonist (EC50=0.21 μM), with high selectivity and oral activity. Resmetirom can be used in the research of non-cirrhotic and non-alcoholic steatohepatitis.

Avapritinib (BLU-285) is a selective, highly potent, and orally active inhibitor of KIT and PDGFRA activation loop mutant kinases, targeting KIT D816V (IC50:0.27 nM) and PDGFRA D842V (IC50:0.24 nM), and attenuates the transport functions of ABCB1 and ABCG2. It binds to the active conformation of the kinases and exhibits antitumor activity.

Ferrostatin-1 (Fer-1) is a potent and selective inhibitor of iron death. Ferrostatin-1 potently inhibits Erastin-induced iron death in HT-1080 cells with an EC50 of 60 nM. Ferrostatin-1 also exhibits antioxidant and antifungal activities.

Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki values of 0.160 nM, 24.9 nM and 0.920 nM, respectively. Fiduxosin can be used for the treatment of benign prostatic hyperplasia.

GNF4877 is a potent inhibitor of DYRK1A and GSK3β (IC50s: 6 nM and 16 nM, respectively), resulting in the blockade of nuclear export of nuclear factor of activated T-cells (NFATc) and increased β-cell proliferation.

Mutant IDH1-IN-2 is an inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with an IC50 of 16.6 nM in fluorescence biochemical assay and an IC50 of <22 nM in LS-MS biochemical assay.

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409 22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409 22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

PD-1-IN-22 is a potent inhibitor of the programmed cell death-1 (PD-1) programmed cell death-ligand 1 (PD-L1) interaction, with an IC50 of 92.3 nM.

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.

AZD-0284 is an inverse agonist of the nuclear receptor RORγ. In development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].

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.

SSR180711 hydrochloride (SSR-180711A HCl) is a selective Alpha7 nicotinic acetylcholine partial agonist for the study of neurodegenerative and cognitive disorders.

Safotibant (LF-22-0542) is a bradykinin B1 receptor antagonist with anti-inflammatory and analgesic activity for the topical treatment of diabetic macular edema.

(Iso)-MS4322 ((Iso)-YS43-22) is a selective and potent protein arginine methyltransferase 5 (PRMT5) degrader with potential anticancer activity that effectively reduces PRMT5 protein levels in MCF-7 cells and inhibits the growth of a wide range of cancer cells.