Galunisertib (LY2157299) is a selective TGF-β receptor inhibitor with an IC50 of 56 nM.
Diamthazole (Dimazole) hydrochloride is an antifungal agent. Diamthazole hydrochloride can be used for the research of infection[1].
Hsp90-IN-17 (Example 5) hydrochloride is an HSP90 inhibitor that can be used in the study of proliferative diseases, such as cancer and neurodegenerative diseases[1].
Pikromycin is a macrolide antibiotic that has been found in S. venezuelae and active against E. coli, S. aureus and B. subtilis[1].
RGW2938 is a phosphodiesterase inhibitor.
VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS). VLX600 causes mitochondrial dysfunction and induces a strong shift to glycolysis. VLX600 displays selective cytotoxic activity against malignant cell and induces autophagy. Anticancer activity[1][2].
Simtuzumab (AB 0024; GS 6624) is a monoclonal antibody directed against Lysyl oxidase like-2 (LOXL2). Simtuzumab can be used for the research of primary sclerosing cholangitis (PSC)[1].
ALW-II-41-27 is a Eph family tyrosine kinase inhibitor with an IC50 of 11 nM for Eph2.
Bromo-PEG2-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Macrocarpal D is a potent antibacterial agent. Macrocarpal D is a phloroglucinol dialdehyde diterpene derivatives that can be found in the leaves of Eucalyptus macrocarpa[1].
RORγt agonist 2 is a potent agonist of RORγt. RORγt agonist 2 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 2 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136339A1, compound 17)[1].
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive[1][2].
CTEP is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors.
MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6[1].
Sodium orthovanadate is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue.
[Tyr1]-Somatostatin-14 could binds to SSTR2[1].
Neochamaejasmin B is a biflavanone compound. Neochamaejasmin B is isolated from Stellera chamaejasme L. (Thymelaeaceae). Neochamaejasmin B has the cis-trans geometry at the C-2/C-3 and C-2″/C-3″ positions[1].
Neobyakangelicol is a natural product from Baizhi[1].
Dimesna is an protective agent used to decrease urotoxicity.IC50 value:Target:in vitro: Dimesna modulates paclitaxel-induced hyperpolymerization of MTP in a dose-dependent manner, and mesna, an in vivo metabolite of Dimesna, protects against time-dependent cisplatin-induced inactivation of MTP. [1] Dimesna -mediated prevention or mitigation of cisplatin-induced nephrotoxicity may involve aminopeptidase N (APN) inhibition by certain Dimesna -derived esna-disulfide heteroconjugates and appears correlated to the presence of a glycinate moiety and/or an anionic group. Two general mechanisms for Dimesna -mediated nephroprotection of cisplatin-induced nephrotoxicity involving the gamma-glutamyl transpeptidase (GGT), APN and cysteine-conjugated-β-lyase (CCBL) nephrotoxigenic pathway are proposed which acting in a concerted and/or synergistic manner, and thereby prevent or mitigate cisplatin-induced renal toxicity. [2] Mesna and its dimer, Dimesna, are coadministered for mitigation of ifosfamide- and cisplatin-induced toxicities, respectively. Dimesna is selectively reduced to mesna in the kidney, producing its protective effects. In vitro screens of uptake and efflux transporters reveal renal organic anion transporters OAT1, OAT3, and OAT4 are responsible for kidney-specific uptake of Dimesna. Uptake of Dimesna by OAT1, OAT3, and OAT4 is determined to be saturable with KM of 636 μM, 390 μM and 590 μM, respectively. [3]in vivo: Tumors of urinary bladder induced by cyclophosphamide (CP) in rats can be significantly reduced by Dimesna administration in a dose-related manner. [4]
Lipoamido-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Ethyl eosin is a fluorescent dye with an absorption peak at 527 nm and an absorption shoulder at 487 nm[1].
SB-206606, a stereoisomer of BRL 37344, is a potentially specific, beta 3-adrenergic receptor (β3-AR) ligand. The affinity of [3H]SB 206606 is 76 times higher for the β3-AR than for the beta 1/beta 2-adrenergic receptors[1].
Z-His-OH is a histidine derivative[1].
WAY-649123 is an active molecule.
PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction[1].
Balsalazide sodium hydrate could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
(Rac)-BINAP is the inactive isomer of (R)-BINAP (HY-W017757), and can be used as an experimental control. (R)-BINAP is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Benzylbenzofuran derivative-1 (Compound 8), a benzylbenzofuran derivative, can be isolated from Silene conoidea[1].
Spexin is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin exhibits no significant activity at galanin receptor 1. Spexin is an endogenous satiety-inducing peptide; Spexin inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin attenuates LH secretion in goldfish. Spexin exhibits anxiolytic effects in vivo.
Zardaverine is a newly developed dual-selective PDE3/4 inhibitor with IC50 values of 0.5 uM and 0.8 uM respectively. IC50 value: 0.5 uM (PDE3); 0.8 uM (PDE4)Target: PDE3; PDE4Zardaverine inhibited the cyclic GMP-inhibitable PDE III from human platelets and the rolipram-inhibitable PDE IV from canine trachea and human polymorphonuclear (PMN) cells with IC50-values of 0.58, 0.79 and 0.17 μM, respectively. The pyridazinone derivative affected the calmodulin-stimulated PDE I, the cyclic GMP-stimulated PDE II and the cyclic GMP-specific PDE V only marginally at concentrations up to 100μM. Zardaverine inhibits the ADP-induced aggregation of human platelets with an IC50 of 1.6 μM. This inhibition was synergistically increased by activators of adenylate cyclase such as PGE1 and forskolin. In human PMN cells, Zardaverine inhibited the zymosan-induced superoxide anion generation with an IC50 of 0.40 μM. Again, this effect was increased by activators of adenylate cyclase. Zardaverine acted in synergy with the adenylate cyclase activators prostaglandin E2 and CG 4203, a prostacyclin analog, and super-additive effects of combinations were observed. Zardaverine and dexamethasone prevent bronchial eosinophilia and neutrophilia with similar dosage of 30 microM/kg orally, suggesting that this PDE III/IV inhibitor may be useful for both, bronchorelaxation and reduction of inflammation in asthma therapy.