5-A-RU (5-Amino-6-(D-ribitylamino)uracil), a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules that are derived fromBencycloquidium Bromide is a muscarinic M3 antagonist. Bencycloquidium bromide inhibits nasal hypersecretion in a rat model of allergic rhinitis. Bencycloquidium Bromide showed high affinity toward the M(3) receptor in Chinese hamster ovary (CHO) cells (M(1) pKi=7.86, M(2) pKi=7.21, M(3) pKi=8.21); pA(2)=8.85, 8.71 and 8.57 in methacholine-induced contraction of trachea, ileum and urinary bladder, 8.19 in methacholine-induced bradycardia of right atrium in vitro, respectively.This compound is unstable in powder form and other related salt forms are recommened.
Bencycloquidium Bromide is a muscarinic M3 antagonist. Bencycloquidium bromide inhibits nasal hypersecretion in a rat model of allergic rhinitis. Bencycloquidium Bromide showed high affinity toward the M(3) receptor in Chinese hamster ovary (CHO) cells (M(1) pKi=7.86, M(2) pKi=7.21, M(3) pKi=8.21); pA(2)=8.85, 8.71 and 8.57 in methacholine-induced contraction of trachea, ileum and urinary bladder, 8.19 in methacholine-induced bradycardia of right atrium in vitro, respectively.This compound is unstable in powder form and other related salt forms are recommened.
NU1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitors have been developed that potentiate the cytotoxicity of ionizing radiation and anticancer drugs. The biological effects of NU1085 [Ki = 6 nM], in combination with temozolomide (TM) or topotecan (TP) have been studied in 12 human tumor cell lines (lung, colon, ovary, and breast cancer). Cells were treated with increasing concentrations of TM or TP + - NU1085 (10 microM) for 72 h.
Chlormadinone (free base) is a synthetic steroid hormone and antagonist at androgen and estrogen receptors used to treat BPH and polycystic ovary syndrome. It also promotes osteoblast differentiation and Ca deposition in bone marrow stem cells.
J-104132 is a potetn and selective endothelin A B receptor antagonist (Ki: cloned human ETA = 0.034 nM; cloned human ETB = 0.104 nM) . In vitro, J-104132 is a potent antagonist of ET-1-induced accumulation of [3H]inositol phosphates in Chinese hamster ova
Pericosine A is a fungal metabolite that has been found inP. byssoidesand has anticancer activity.1It inhibits the growth of a variety of cancer cells, including breast, colon, lung, ovary, stomach, and prostate cell lines (GI50s = 0.05-24.55 μM) and increases survival in a P388 mouse xenograft model when administered at a dose of 25 mg/kg. Pericosine A inhibits EGFR by 40 to 70% when used at a concentration of 100 μg/ml. It also reacts with organosulfur compounds in skunk spray to form stable thioethers as odorless products.2 1.Yamada, T., Iritani, M., Ohishi, H., et al.Pericosines, antitumour metabolites from the sea hare-derived fungus Periconia byssoides. Structures and biological activitiesOrg. Biomol. Chem.5(24)3979-3986(2007) 2.Du, L., Munteanu, C., King, J.B., et al.An electrophilic natural product provides a safe and robust odor neutralization approach to counteract malodorous organosulfur metabolites encountered in skunk sprayJ. Nat. Prod.82(7)1989-1999(2019)
The extracellular signal-regulated kinase (ERK) signal transduction pathway regulates a diverse array of cellular processes. These processes include cell survival, proliferation, motility, and differentiation and are constitutively activated in cancers involving lung, colon, pancreas, kidney, and ovary. CAY10561 is a potent, ATP-competitive inhibitor of ERK2 (Ki = 2 nM). This compound is highly selective for ERK2 compared to other kinases such as PKA (Ki = 0.39 μM) and JNK3 (Ki = 4 μM). CAY10561 inhibits proliferation of COLO 205 cells with an IC50 value of 0.54 μM.
Streptonigrin is an aminoquinone antitumor and antibacterial antibiotic produced by Streptomyces flocculus. Streptonigrin inhibits β-Catenin/Tcf signaling and shows cytotoxicity in β-catenin-activated cells. Streptonigrin induces delayed chromosomal instability involving interstitial telomeric sequences in Chinese hamster ovary cells. Note: Streptonigrin from natural resource is (-)-rotation, has CAS#3930-19-6 and is a R-isomer.
Albizziin is amino acid analog which acts as a competitive inhibitor of asparagine synthetase with respect to glutamine. Albizziin has been used to isolate mutants of Chinese hamster ovary cells with alterations in levels of the target enzyme. Several classes of mutations can be distinguished on the basis of cross-resistance to beta-aspartyl hydroxamate, another amino acid analog. Studies on asparagine synthetase indicate that resistance to albizziin may be due to altered regulation of asparagine synthetase, structural mutations of the enzyme, and gene amplification.