Landogrozumab (LY2495655) is an humanized anti-myostatin monoclonal antibody. Landogrozumab effectively improves muscle volume, hand grip strength and function. Landogrozumab can be used for the research of muscle wasting disease[1].
N-Acetyl-2-carboxybenzenesulfonamide is an orally active COX-1 and COX-2 inhibitor with IC50s of 0.06 μM and 0.25 μM, respectively. N-Acetyl-2-carboxybenzenesulfonamide shows anti-inflammatory activity[1].
L82-G17 is an uncompetitive DNA ligase I (Lig I)-selective inhibitor. L82-G17 inhibits the third step of the ligation reaction, phosphodiester bond formation. L82-G17can be used as a probe of the catalytic activity[1].
L-690330 is a competitive inhibitor of inositol monophosphatase (IMPase) with a Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively, exhibits 10-fold more sensitive than mouse and rat IMPase[1].
Netarsudil hydrochloride is a ROCK, and norepinephrine transporter inhibitor. Target: ROCKin vitro: AR-13324 is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes.[1] AR-13324 is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter.[2]in vivo: AR-13324 produces statistically significant lowering of episcleral venous pressure (EVP) in Dutch Belted (DB) rabbits. [3]
4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis[1][2][3].
Fmoc-Glu-AMC is a glutamic acid derivative[1].
Fmoc-aminooxy-PEG4-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
5'-DMT-3'-TBDMS-Bz-rA is a nucleoside with protective and modification effects.
Myxin is a di-N-oxide phenazine produced by Lysobacter antibioticus OH13. Myxin is toxic to many microorganisms and tumor cells[1].
Tamibarotene is a retinoic acid receptor α/β (RARα/β) agonist, showing high selectivity over RARγ.
APOL1-IN-1 is a apolipoprotein L1 (APOL1) inhibitor extracted from patent WO2020131807A1 compound 87. APOL1-IN-1 can be used for the research of focal segmental glomerulosclerosis (FSGS) and non-diabetic kidney disease (NDKD)[1].
Makisterone A, a 28-carbon moulting hormone, has been identified as the major free pupal ecdysteroid in the honey bee, Apis mellifera[1].
Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties[1].
Imidacloprid-d4 is the deuterium labeled Imidacloprid[1]. Imidacloprid is an effective and widely used neonicotinoid pesticide to control pests of cereals, vegetables, tea and cotton[2].
Val-Lys(Boc)-PAB is a ADC linker. Val-Lys(Boc)-PAB was used to prepare camptothecin peptide conjugates as antitumor agents (WO 2019195665). It was used as a non-linear self-immolative linker for reducing hydrophobicity of antibody-drug conjugates for cancer therapy (WO 2018069375).
ConB-1 is a potent and selective ALK inhibitor with low toxicity to normal cells[1].
BAY-678 racemate is a racemate of BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
Triptorelin is a GnRH agaonist shown to inhibit estradiol-induced cancer cell proliferationIn vivo: (1) Triptorelin can improve the pregnancy rate by 12% to 15% in ewes6 and downregulate ovarian GnRHR-I expression of female rats, especially in late-growing follicles.(2) Triptorelin immunity blocked EET and UWT, inhibited uterine growth and development and enhance the expression levels s of ESR1, LHR, and FSHR proteins.
α-Synuclein inhibitor 4 (compound 3gh) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 0.98 μM and inhibition ratio at 30 μM of 91.2%[1].
Peginterferon beta-1a (Peginterferon β-1a) is the first pegylated interferon beta-1a molecule. Peginterferon beta-1a induces cancer cells Apoptosis and shows anti-tumor activities in nude mice models. Peginterferon beta-1a can be used for the research of cancer and multiple sclerosis (RMS)[1].
Poloxamer 407 is a nonionic surfactant that is 100% active and relatively non-toxic to cells at low concentrations, and frequently used with dye AM esters such as Indo-1 AM, Fura-2 AM, Calcein AM, Fluo-3 AM, Fluo-4 AM, Quest Fluo-8™ AM and Quest Rhod-4™ AM, etc. to improve their water solubility.
(+)-Pileamartine A is a complex alkaloid. (+)-Pileamartine A can be accessed via intramolecular Pd(0)-catalyzed alkene 1,2-aminoarylation reactions[1].
Pilsicainide (SUN 1165 free acid) is a potent sodium channel blocker and potent class Ic antiarrhythmic agent[1][2].
Paradol is a pungent phenolic substance found in ginger and other Zingiberaceae plants. Paradol is an effective inhibitor of tumor promotion in mouse skin carcinogenesis, binds to cyclooxygenase (COX)-2 active site.
UNC2881 is a potent and specific Mer kinase inhibitor; inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. IC50 value: 22 nM [1]Target: Mer kinase inhibitorTreatment with UNC2281 is also sufficient to block EGF-mediated stimulation of a chimeric receptor containing the intracellular domain of Mer fused to the extracellular domain of EGFR. In addition, UNC2881 potently inhibits collagen-induced platelet aggregation, suggesting that this class of inhibitors may have utility for prevention and/or treatment of pathologic thrombosis.
Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker), used to lower the pressure in the eye in treating conditions such as glaucoma.
(±)-HIP-A is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-A is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-A can be used in the study of neurological diseases[1].
Buserelin (INN) Acetate is a gonadotropin-releasing hormone agonist (GnRH agonist).target: GnRHIn vivo: Buserelin treatment reduced the number of neurons along the entire gastrointestinal tract, with increased relative numbers of CRF-immunoreactive submucosal and myenteric neurons in colon (p < 0.05 and p < 0.01, respectively).[1]Compared with controls, buserelin treatment caused loss of myenteric neurons in the ileum and colon (P<0.01), a thinner circular muscle layer in ileum (P<0.05) and longitudinal muscle layer in colon (P<0.05). Long term follow up of buserelin induced enteric neuropathy reveals reduced body weight, loss of myenteric neurons, thinning of muscle layers, and increased numbers of eosinophils and T lymphocytes in the gastrointestinal tract.[2] A marked enteric neuronal loss with modest effects on GI function is found after buserelin treatment. Increased feces fat content is suggested an early sign of dysfunction.[3]
Phellodendrine chloride is a plant alkaloid found in Phellodendron amurense. Phellodendrine chloride suppresses the proliferation of KRAS mutated pancreatic cancer cells through inhibition of nutrients uptake via macropinocytosis [1].