SB 222200 is a selective, reversible and competitive antagonist of human NK-3 receptor(Ki=4.4 nM) that effectively crosses the blood-brain barrier.IC50 Value: 4.4 nM ( Ki for hNK-3 receptor); 250 nM( Ki for hNK-2 receptor) [1]Target: NK3 Receptorin vitro: SB-222200 inhibited (125)I-[MePhe(7)]neurokinin B (NKB) binding to Chinese hamster ovary (CHO) cell membranes stably expressing the hNK-3 receptor (CHO-hNK-3R) with a K(i) = 4.4 nM and antagonized NKB-induced Ca(2+) mobilization in HEK 293 cells stably expressing the hNK-3 receptor (HEK 293-hNK-3R) with an IC(50) = 18.4 nM. SB-222200 was selective for hNK-3 receptors compared with hNK-1 (K(i) > 100,000 nM) and hNK-2 receptors (K(i) = 250 nM). n HEK 293 cells transiently expressing murine NK-3 receptors (HEK 293-mNK-3R), SB-222200 inhibited binding of (125)I-[MePhe(7)]NKB (K(i) = 174 nM) and antagonized NKB (1 nM)-induced calcium mobilization (IC(50) = 265 nM) [1].in vivo: In mice oral administration of SB-222200 produced dose-dependent inhibition of behavioral responses induced by i.p. or intracerebral ventricular administration of the NK-3 receptor-selective agonist, senktide, with ED(50) values of approximately 5 mg/kg. SB-222200effectively crossed the blood-brain barrier in the mouse and rat. The inhibitory effect of SB-222200 against senktide-induced behavioral responses in the mouse correlated significantly with brain, but not plasma, concentrations of the compound. Pharmacokinetic evaluation of SB-222200 in rat after oral administration (8 mg/kg) indicated sustained plasma concentrations (C(max) = about 400 ng/ml) and bioavailability of 46% [1].
(+)-Sparteine is a natural alkaloid acting as a ganglionic blocking agent. (+)-Sparteine competitively blocks nicotinic ACh receptor in the neurons.
Tubulin inhibitor 24 is a potent tubulin inhibitor. Tubulin inhibitor 24 inhibits tubulin polymerization. Tubulin inhibitor 24 induces cell cycle arrest at the G2/M phase in a concentration-dependent manner. Tubulin inhibitor 24 shows antitumor activity with no obvious toxicity[1].
GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis[1].
α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor)[1][2][3][4].
(tert-Butoxycarbonyl)-D-serine is a serine derivative[1].
L-Lactic acid-13C3 is a stable isotope labeled L-Lactic acid analog. L-Lactic acid-13C3 can be used for lactate metabolism research[1].
IU1-47 is a potent USP14 inhibitor with an IC50 of 0.6 μM. IU1-47 induces tau elimination in cultured neurons[1].
m-PEG3-Sulfone-PEG3-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Nimustine hydrochloride (ACNU) is a DNA cross-linking and DNA alkylating agent, which induces DNA replication blocking lesions and DNA double-strand breaks and inhibits DNA synthesis, commonly used in chemotherapy for glioblastomas[1][2][3].
PF-00956980 is a reversible pan-JAK inhibitor with IC50 values of 2.2, 23.1 and 59.9 μM for JAK1, JAK2 and JAK3, respectively. PF-00956980 can be used in the research of lung and skin inflammatory diseases[1].
Biotin-LC-LC-NHS is a SMCC cross-linking reagent that can be used to mark antibody and other small molecules, such as Paclitaxel[1][2].
Sulfabrom (N 3517; Sulfabromomethazine) is a long-acting veterinary medicine that is used for the treatment of coccidiosis and various bacterial infections in the poultry, swine and cattle.
Sofalcone, a gastric antiulcer agent in clinical use, is known to induce the expression of Heme oxygenase-1 (HO-1) in gastric epithelium.
Arachidonylcyclopropylamide (ACPA) is a potent and selective CB1 receptors agonist. Arachidonylcyclopropylamide inhibits forskolin-stimulated cAMP production in CHO cells transfected with human cannabinoid CB1 receptors (IC50=2 nM)[1].
STAT3-IN-5 is a potent STAT3 inhibitor. STAT3-IN-5 inhibits STAT3-Y705 phosphorylation with an EC50 value of 170 nM. STAT3-IN-5 inhibits cytokine induced JAK activation. STAT3-IN-5 induces apoptosis. STAT3-IN-5 can be used in research of cancer[1].
Pazufloxacin-d4 is deuterium labeled Pazufloxacin.
Bifemelane is a nootropic compound. Bifemelan causes the first peak by stimulating release from intracellular Ca2+ stores and the second by capacitive entry through store–operated Ca2+ channels. Bifemelane will be provided as a pharmacological tool for basic studies on astrocytes[1].
C6-Bis-phosphoramidic acid diethyl ester is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Rovanersen (WVE-120101) is an antisense oligonucleotide that can be used for huntington’s disease research[1].
AMG-076 is an orally bioavailable and selective MCHR1 antagonist. AMG-076 results in significant reduction in body weight gain in nonobese mice fed a high-fat diet and in high-fat diet-induced obese (DIO) mice[1].
Antibiotic-202 is an antibiotic compound, for treating bacterial infections. Target: AntibacterialAntibiotic-202 is useful for the treatment or prevention of bacteria infections.
PEG5-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
2-Propylheptanol is an intermediate and can be used for synthesizing a series of plasticizers by esterification with phthalic anhydride, trimellitic anhydride and adipic acid, etc[1].
3'-TBDMS-Bz-rA Phosphoramidite is a phosphorite monomer that can be used in the synthesis of oligonucleotides.
α-Amyrin acetate, a natural triterpenoid, has anti-inflammatory activity, antispasmodic profile and the relaxant effect[1][2].
LLL12 is a small molecule inhibitor of STAT3 that inhibits STAT3 phosphorylation. LLL12 enhanced the inhibitory effect of Cisplatin (HY-17394) and Paclitaxel (HY-B0015) on ovarian cancer cell formation, migration, and growth[1].
Cresyl Violet perchlorate is a red fluorescent stain, which can be used to stain neurons.
Myristoleic acid, a cytotoxic component in the extract from Serenoa repens, induces apoptosis and necrosis in human prostatic LNCaP cells[1].
Remodelin is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.IC50 value:Target: NAT10 inhibitorRemodelin can improve nuclear architecture, chromatin organization, and fitness of both human lamin A/C-depleted cells and HGPS-derived patient cells, and decrease markers of DNA damage in these cells. Using a combination of chemical, cellular, and genetic approaches, acetyl-transferase protein NAT10 was identified as the target of Remodelin that mediated nuclear shape rescue in laminopathic cells via microtubule reorganization. Down-regulation and mutations of the nuclear-architecture proteins lamin A and C cause misshapen nuclei and altered chromatin organization associated with cancer and laminopathies, including the premature-aging disease Hutchinson-Gilford progeria syndrome (HGPS). Remodelin is a useful chemical tool to study how NAT10 affects nuclear architecture and suggest alternative strategies for treating laminopathies and aging.