Others

ETX0282 is an orally available, broad spectrum inhibitor of class A and C β-lactamases. Entasis is developing ETX0282 in combination with cefpodoxime proxetil, an orally available cephalosporin approved for treatment of a variety of bacterial infections.

Rebimastat 是基于巯基的第二代基质金属蛋白酶(MMP)抑制剂，具有潜在的抗肿瘤活性。利莫司他选择性抑制几种 MMPs (MMP 1、2、8、9和14)，从而诱导细胞外基质降解，抑制血管生成、肿瘤生长、侵袭和转移。

Etoloxamine HCl is the salt form of Etoloxamine free base, a histamine 1 receptor antagonist.

PEN-866 is a potential agent for controlling early stage tumor growth for non-small cell lung cancer (NSCLC). PEN-866 is a novel esterase-cleavable conjugate of an HSP90i and a topoisomerase I inhibitor, SN-38

Glutathione glycylethyl ester is a hydrophilic derivative of the protein tyrosine phosphatase inhibitor phenylarsine oxide (PAO). It inhibits angiogenesis and tumour growth.

CGP 40215 is a specific S-adenosylmethionine decarboxylase (AdoMetDC) inhibitor that was found to inhibit the growth of Leishmania donovani promastigotes

Azidothiorphan is a photoaffinity ligand for the active site of the neutral endopeptidase 24.11. After ultraviolet irradiation the inhibitor binds irreversibly to the enzyme, and photolabeling occurs at the active site. The competitive inhibitor thiorphan protects the endopeptidase from inactivation.

PF00349412 is a selective inhibitor of protozoan protein N-​myristoyltransferases. Inhibition of N-​myristoyltransferase has been validated pre-​clin. as a target for the treatment of fungal and trypanosome infections, using species-​specific inhibitors.

Deptropine citrate is a well-known H1-histamine receptor antagonist and muscarinic receptor antagonist. It is prescribed frequently for treatment of asthma. Recently deptropine has garnered interest as a potential treatment for breast cancer. In vitro studies have shown deptropine citrate has inhibitory effects on cell viability and mammosphere formation in Breast Cancer Stem Cells (BCSCs). However, it does not seem to inhibit the self-renewal capacity of the breast cancer cell line MDA-MB-231 when it is enriched with Cancer Stem Cells.

SC 23133 is an antimineralocorticoid that is known to induce a marked but reversible inhibition of aldosterone biosynthesis.

Asoxime dimethanesulfonate is an oxime reactivator used for counteracting intoxication by nerve agents. It is able to reactivate acetylcholinesterase (AChE) inhibited by cytotoxic nerve agents such as sarin or soman.

OBBA is a phospholipase A2 antagonist.

Acetoacetyl coenzyme A sodium 是重要内源性代谢物，在pH 7.5时其Km值达1.10 mM，主要用于磷酸转丁基酶 (PTB) 与poly-3-hydroxybutyrate (PHB) 的合成。

Tacrolimus anhydrous 8-epimer is a new l-pipecolic acid macrolide lactone, an important immunosuppressive drug that blocks T cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2.

VUF14480 is a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H₄ receptor. VUF14480 was shown to be a partial agonist of hH4 receptor-mediated G protein signalling and β-arrestin2 recruitment. VUF14480 bound covalently to the hH₄ receptor with submicromolar affinity. Serine substitution of C98(3.36) prevented this covalent interaction.

Trityl olmesartan medoxomil impurity II为Trityl olmesartan medoxomil的杂质，后者是Olmesartan medoxomil的中间体。

Methotrexate diethyl ester is an antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of tetrahydrofoltae dehydrogenase and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA.

ARRY-403, also known as AMG-151, is an orally available allosteric glucokinase (GK) activator developed for the treatment of type 2 diabetes mellitus (T2DM). ARRY-403 has many favorable physicochemical characteristics and ADME properties (low potential to cause drug–drug interactions (DDIs). ARRY-403 potently activates human glucokinase (GK) in vitro (EC50 = 79 nM at 5 mM glucose), with an S0.5 = 0.93 mM glucose (ARRY-403 at 5 mM) and Vmax = 134% compared to the no activator control. It possesses good in vitro drug-like properties (aqueous solubility, cell permeability, low low potential for drug-drug interactions, low predicted hepatic clearance), and selectivity against broad panels of receptors and enzymes.

ddTTP 是一类双脱氧核糖核苷酸 (ddNTPs)，可作为 DNA 聚合酶链延长抑制剂用于 DNA 测序。

alpha-Clopenthixol dihydrochloride is a thioxanthene with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors.

(R)-FTY-720 Vinylphosphonate is a sphingosine 1-phosphate type 1 (S1P1) receptor agonist and lacks anti-apoptotic activity.

GT-2394 is a histamine H3 receptor agonist.

Amsacrine Isothionate is an aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death.

L6H9 is a novel inhibitor of myeloid differentiation factor 2 (MD2), suppressing HG-induced expression of ACE and AT1 receptor and Angiotensin II (AngII) production in renal NRK‐52E cells, resulting in the decrease in fibrosis markers such as TGF-β and collagen IV.

LysoFos Glycerol 12 是一种有用的有机化合物，可用于生命科学领域的相关研究。其产品编号为 TF0073，CAS号为 1423237-43-7。

Estrogen receptor antagonist4 是一种有效的雌激素受体 (ER) 降解剂。雌激素信号系统在调节细胞生长、分化和凋亡 (apoptosis) 中发挥着重要作用。Estrogen receptor antagonist4 具有研究癌症疾病的潜力。

SC-50605 is a second-generation LTB4 receptor antagonist.

AG-012917 is a broad spectrum cyclin-​dependent kinase inhibitors with potential anticancer activity.

NTZ-24 is a novel potent STAT3 inhibitor.

Clonazoline is a coronary vasodilator that is an imidazoline sympathomimetic, an alpha-adrenoreceptor agonist. It was used as a nasal decongestant and vasoconstrictor.

Plagiochilin A Inhibits Cytokinetic Abscission and Induces Cell Death

MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cells. In addition, MRK003 caused an upregulation of pAkt, indicating crosstalk with the PI3K/Akt pathway.

Dinalbuphine sebacate is a long-lasting prodrug of nalbuphine, acting as a moderate-efficacy partial agonist or antagonist of the μ-opioid receptor and as a high-efficacy partial agonist of the κ-opioid receptor.

Motuporin is an inhibitor of type-1 and type-2A protein phosphatase catalytic subunits (PP-1c and PP-2Ac).

Monofluoromethylagmatine is an arginine decarboxylase inhibitor.

HA-117 is a dopamine receptor agonist.