Aspartame acesulfame is a methyl ester of a dipeptide. Aspartame acesulfame can be used as a synthetic nonnutritive sweetener. Aspartame acesulfame is composed of phenylalanine (50%), aspartic acid (40%) and methanol (10%)[1][2].
Glycyrrhizin-6'-methylester is a natural product that can be isolated from licorice (Glycyrrhiza glabra)[1].
PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant).IC50 value: 4.8 nM [1]Target: in vitro: Being more selective than staurosporine or PF-02341066, PF-04217903 displays >1000-fold selectivity for c-Met over a panel of 208 kinases, although more susceptible to oncogenic mutations of c-Met that attenuate potency than PF-02341066. In addition to WT c-Met, PF-04217903 displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I with IC50 of 3.1 nM, 6.4 nM, and 6.7 nM, respectively, but has no inhibitory activity against c-Met-Y1230C with IC50 of >10 μM [1]. PF-04217903 in combination with sunitinib significantly inhibits endothelial cells, but not the tumor cells B16F1, Tib6, EL4, and LLC [2] PF-04217903 significantly inhibits the clonogenic growth of LXFA 526L and LXFA 1647L with IC50 values of 16 nM, and 13 nM, respectively, yielding an additive effect when in combination with cetuximab [3]. in vivo: Although unable to inhibit tumor growth in the sunitinib-sensitive B16F1 and Tib6 tumor models, the combination of PF-04217903 and sunitinib significantly inhibits tumor growth in sunitinib-resistant EL4, and LLC tumor models compared with sunitinib or PF-04217903 alone by significantly blocking vascular expansion, indicating a functional role for HGF/c-Met axis in the sunitinib-resistant tumors [2].
Illudin M is a cytotoxic fungal sesquiterpene that can be isolated from the culture medium of Omphalotus olearius mushrooms. Illudin M can alkylate DNA. Illudin M has anti-tumor activities[1][2].
Cycloartenyl ferulate (Cycloartenol ferulate) is one of the typical triterpene alcohols and possesses several biological activities including anti-oxidative activity, antiallergic activity, anti-inflammatory and anticancer activities[1].
Hypoxanthine-13C5,15N4 is a 15N-labeled and 13C-labled Dansyl chloride.
Pizotifen is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
BnO-PEG1-CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
DMT-2'O-Methyl-rU Phosphoramidite (2'-O-Me-U Phosphoramidite) is a 2'-O-Me derivative, and can be used for oligonucleotide synthesis[1][2].
TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8[1].
Glyoxalase I inhibitor (free base) is a potent Glyoxalase I (GLO1) inhibitor, candidate for anticancer agents.
(RS)-S-Adenosyl-L-methionine-d3(S-methyl-d3) Tetra(p-toluenesulfonate) Salt is the deuterium labeled (RS)-S-Adenosyl-L-methionine Tetra(p-toluenesulfonate) Salt[1].
(β-Asp5)-Delta-Sleep Inducing Peptide (DSIP-isoD) is a synthetic polypeptide that can be partially hydrolyzed by NaOH or SDS. (β-Asp5)-Delta-Sleep Inducing Peptide can be used to study the catalytic activity of mitochondrial protein L-isoaspartyl (D-aspartyl) methyltransferase (PIMT)[1].
19-Hydroxybaccatin III is a compound isolated from the leaves and twigs of Taxus sumatrana[1].
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively.
Ammelide-13C3 is the 13C3 labeled Ammelide.
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs)[1][2].
Danshensu, an active ingredient of Salvia miltiorrhiza, shows wide cardiovascular benefit by activating Nrf2 signaling pathway.
Peripheral Myelin Protein P2 (53-78), bovine is derived from bovine peripheral myelin P2 protein amino acid residues 53-78. Peripheral Myelin Protein P2 (53-78), bovine is a T cell epitope for the induction of experimental autoimmune neuritis (EAN) in Lewis rats[1].
2-nonyl-3-hydroxy-4-Quinolone (C9-PQS) is a quinolone compound produced by P. aeruginosa and other related bacterias. 2-nonyl-3-hydroxy-4-Quinolone is a quorum sensing (QS) signal molecule that controls the expression of many virulence genes as a function of cell population density[1].
L-Asparaginase (L-ASNase), a hydrolase that catalyzes the conversion of L-asparagine, used in acute lymphoblastic leukemia treatment. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis[1].
tert-Butylamine-d9 Hydrobromide is the deuterium labeled tert-Butylamine Hydrobromide[1].
C12-SPM is a lipid nanoparticle that mediates siRNA delivery. C12-SPM has no significant cytotoxicity and can be used for research on hepatoviral diseases[1].
BMS-5 is a potent LIMK inhibitor with IC50s of 7 nM and 8 nM for LIMK1 and LIMK2, respectively.
Lib2-1, a macrocyclic peptide, is an IL-17C/IL-17RE interaction inhibitor. Lib2-1 can be used for autoimmune and inflammatory diseases research[1].
Azido-PEG1-C1-Boc is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Benzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease.Target: mAChRBenzotropine is a centrally-acting, antimuscarinic agent used as an adjunct in the treatment of Parkinson's disease. It may also be used to treat extrapyramidal reactions, such as dystonia and Parkinsonism, caused by antipsychotics. Symptoms of Parkinson's disease and extrapyramidal reactions arise from decreases in dopaminergic activity which creates an imbalance between dopaminergic and cholinergic activity. Anticholinergic therapy is thought to aid in restoring this balance leading to relief of symptoms. In addition to its anticholinergic effects, benztropine also inhibits the reuptake of dopamine at nerve terminals via the dopamine transporter. Benzotropine also produces antagonistic effects at the histamine H1 receptor [1, 2].Benztropine (BZT) and its analogues inhibit dopamine uptake and bind with moderate to high affinity to the dopamine transporter (DAT). BZT analogues also exhibit varied binding affinities for muscarinic M(1) and histamine H(1) receptors. The BZT analogues showed a wide range of histamine H(1) receptor (K(i)=16-37,600 nM) and DAT (K(i)=8.5-6370 nM) binding affinities [3].
8-Allylthioadenosine is an adenosine analog. Adenosine analogs mostly act as smooth muscle vasodilators and have also been shown to inhibit cancer progression. Its popular products are adenosine phosphate, Acadesine (HY-13417), Clofarabine (HY-A0005), Fludarabine phosphate (HY-B0028) and Vidarabine (HY-B0277)[1].
SCH 23390 hydrochloride is a potent dopamine receptor D1 antagonist with Ki values of 0.2 and 0.3 nM for the D1 and D5.
(8R,8'R)-Matairesinol 4,4'-di-O-β-D-glucopyranoside (MDG) is a natural product isolated from Trachelospermum asiaticum[1].