Activators & Inhibitors

Activity: Selective ALK1/2 inhibitor . Function/Pharmacology: MU1700 is a potent (IC50’s = 13 nM ALK1; 6 nM ALK2) and highly selective (selective against 369 kinases with only ALK6 (41 nM) being inhibited) ALK1/2 inhibitor. Much higher kinome selectivity than the typically used ALK 1/2 inhibitor LDN-193189. MU1700 exhibits favorable pharmacokinetic and bioavailability profiles for in vivo use. It showed excellent CNS penetration with brain concentrations exceeding that in plasma. Chemical Name: 6-(4-(Piperazin-1-yl)phenyl)-3-(quinoline-4-yl)furo[3,2-b]pyridine dihydrochloride

Activity: FTO inhibitor . Function/Pharmacology: FB23-2 is an inhibitor (IC50 = 2.6 µM) of the mRNA m6A demethylase fat-mass- and obesity-associated protein (FTO).1 Displays significant anti-proliferative activity in NB4 (IC50 = 0.8 µM) and MONOMAC6 (IC50 = 1.5 µM) cells. Selective against the RNA demethylase ALKB5. FB23-2 induced myeloid differentiation and apoptosis in acute myeloid leukemia cells. FB23-2 suppressed the proliferation and migration of hepatocellular carcinoma cells via suppressing the expression of the kinase ERBB3 and human tubulin beta class Iva (TUBB4A).2 Chemical Name: 2-[2,6-Dichloro-4-(3,5-dimethyl-1,2-oxazol-4-yl)anilino]-N-hydroxybenzamide

Activity: JSP-1 dual specificity phosphatase inhibitor . Function/Pharmacology: BML-260 is a potent inhibitor of the dual specificity phosphatase JSP-1 (IC50= 18 uM).1 It promotes the growth of cord blood and mobilizes peripheral blood hematopoietic stem and progenitor cells.2 It increases UCP1 expression in both brown and white adipocytes increasing mitochondrial activity and heat generation, an effect that is JSP-1 independent.3 Chemical Name: (Z)-4-(5-Benzylidene-4-oxo-2-thioxothiazolidin-3-yl)benzoic acid

Activity: EBI2 (GPR183) antagonist . Function/Pharmacology: ML401 is a potent antagonist of GPR183 (IC50 = 1.03 nM), also known as EBI2 or Epstein-Barr virus-induced gene 2. ML401 inhibited 7α,25-dihydroxycholesterol-induced RS11846 cell chemotaxis, IC50=6 nM.1 GPR183 is a key chemotactic receptor guiding B cell localization to appropriate microenvironments for activation and differentiation.2 It also regulates the homeostasis, localization and immunological function of splenic dendritic cells.3 Oxysterols have been shown to be endogenous ligands for GPR183 with 7α,25-dihydroxycholesterol being the most potent (Kd=450 pM).4 Chemical Name: (E)-3-(4-Bromophenyl)-1-(4-(4-chlorobenzyl)piperazin-1-yl)prop-2-en-1-one

Activity: FOXO1 inhibitor . Function/Pharmacology: AS1842856 potent and selective FOXO1 inhibitor, IC50s=33 nM and >1 mM for FOXO3a and 4.1 Oral administration to diabetic db/db mice leads to a reduction of fasting plasma glucose levels.1 Suppresses autophagy, FSP27 expression and adipocyte differentiation.2 AS1842856 is a highly useful tool for probing the involvement of FOXO1 in cellular processes.3-5 Chemical Name: 5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid

Activity: Nutrient additive for cell culture . Function/Pharmacology: Hypoxanthine is a natural purine analog and a breakdown product of adenosine.1 Together with aminopterin and thymidine, it is a component of HAT medium2, which is used to select clones during recombinant protein and antibody production, particularly important in bioprocessing. It is a biomarker of ischemia2,3, and it is used in malaria research as an essential nutrient for P. Falciparum4. It also can enable stem cell expansion.5 Chemical Name: 1,9-Dihydro-6H-purin-6-one; 6-Hydroxypurine

Activity: TRPM8 blocker . Function/Pharmacology: PBMC is a potent and selective blocker of TRPM8 channels. PBMC blocks both chemical and thermal activation of TRPM8.1 Reverses the menthol and cold-induced facilitation of the micturition reflex.2 PBMC represents a new lead for analgesic drugs based on blocking TRPM8.3 Water soluble and easier to handle version of PBMC (Cat# 10-1413). Chemical Name: (S)-1-Phenylethyl(2-aminoethyl)(4-(benzyloxy)-3-methoxybenzyl)carbamate hydrochloride