Melan-A/MART-1 analog ([Leu27]-Melan-A, MART-1 (26-35)) is a biological active peptide. (This Melan-A (26-35) analog, Leu substituted for Ala at position 27, shows better HLA-A*0201 binding properties as well as better immunogenicity and antigenicity than the natural Melan-A (26-35).Pyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
Gossypol, a natural product isolated from cottonseeds and roots, binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
(1R)-α-Pinene is a volatile monoterpene with antimicrobial activities. (1R)-α-Pinene reduces Bacillus cereus population growth, and exhibits repellent effects[1][2].
ABEI is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM[1].
Vanylglycol-d3 is the deuterium labeled Vanylglycol[1].
Eftozanermin alfa (ABBV-621) is a second-generation tumor necrosis factor-related apoptosis-inducing ligand receptor (TRAIL-R) agonist. Eftozanermin alfa induces apoptosis in tumor cells by activation of death receptors 4/5. Eftozanermin alfa can be used for the research of multiple solid and heme malignancies[1][2].
Cyclopyrimorate, a highly effective bleaching herbicide for weed control in rice fields, targets homogentisate solanesyltransferase (HST). HST is a downstream enzyme of 4-hydroxyphenylpyruvate dioxygenase in the plastoquinone (PQ) biosynthesis pathway[1][2].
113-O16B is a disulfide bond-containing ionizable cationic lipidoid. 113-O16B has been used in the generation of lipid nanoparticles (LNPs) for the delivery of mRNA[1].
Lirilumab (IPH2102) is an anti-KIR monoclonal antibody, and shows antitumor activity. Lirilumab can be used in Leukemia, squamous cell carcinoma of the head and neck (SCCHN) research[1][2].
Adenosine-2′-13C is the 13C labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiolo
Atipamezole hydrochloride is a synthetic α2-adrenoceptor antagonist with a Ki of 1.6 nM.
Cebranopadol ((1α,4α)stereoisomer) is a stereoisomer of cebranopadol. Cebranopadol is a potent agonist activity on ORL-1.
13-cis-N-[4-(Ethoxycarbonyl)phenyl]retinamide is a derivative of Retinoic acid.
Ethyl cinnamate-d4 is the deuterium labeled Ethyl cinnamate[1]. Ethyl cinnamate is a fragrance ingredient used in many fragrance compounds. Ethyl cinnamate is a food flavor and additive for cosmetic products. Ethyl cinnamate is also an excellent clearing reagent for mammalian tissues[2][3].
N-Acetyl-L-proline is aproline derivatives.
HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2(IC50=23.3 nM) and the G2019S mutant(IC50=3.2 nM)IC50 Value: 23.3 nM (WT LRRK2); 3.2 nM (LRRK2 G2019S) [1]Target: LRRK2HG-10-102-01 maintains the ability to potently inhibit the biochemical activity of wild-type and G2019S mutant LRRK2. HG-10-102-01 exhibited biochemical IC50s of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. At a concentration of 10 μM, HG-10-102-01 only inhibited the kinase activities of MLK1 and MNK2 to greater than 80% of the DMSO control. Dose-response analysis revealed inhibition of MLK1 with an IC50 2.1 μM and MNK2 with an IC50 0.6 μM. KinomeScan analysis against a near comprehensive panel of 451 kinases at a concentration of 1 μM resulted in no interactions detected with kinases other than G2019S LRRK2 with the exception of one mutant form of c-Kit (L576P) demonstrating the outstanding selectivity of this inhibitor.HG-10-102-01 significantly inhibited phosphorylation of wildtype LRRK2 and LRRK2[G2019S] mutant at Ser910 and Ser935 at 0.3-1.0 μM in cell culture, which is approximately the same potency as LRRK2-IN-1 (1). HG-10-102-01 is relatively insensitive to the A2016T mutation which suggests that this mutant will not be useful to validate whether the pharmacological effects of the compound are LRRK2-dependent.HG-10-102-01 can inhibit phosphorylation of Ser910 and Ser935 of LRRK2 in brain and peripheral tissues following intraperitoneal doses of 50 mg/kg. Further optimization of this chemo-type especially in regards to in vivo half-life will be reported in due course [1].
Nonadecanedioic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Croverin is a diterpenoid compound isolated from the aerial parts of Croton laui[1].
1,2-Di-O-isopropylidene-5-O-(4-methylbenzoyl)-α-D-xylofuranose is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
EBOV-IN-1 (com 3.47) is an adamantane dipeptide piperazine and an inhibitor of Ebola virus (EBOV). EBOV-IN-1 targets Niemann-Pick C1 (NPC1) and inhibits its binding to the EBOV glycoprotein (GP) that activates and mediates viral penetration into host cells, thereby inhibiting EBOV infection. EBOV-IN-1 inhibits pseudotyped EBOV infection with an IC50 of 13 nM[1].
Ulefnersen is a RNA-binding protein fused-in sarcoma (FUS) synthesis reducer[1]. Ulefnersen can be used in Amyotrophic Lateral Sclerosis (ALS) research[2].
AMI-1 is a potent, cell-permeable compound which inhibits protein arginine N-methyltransferases (PRMTs), including human PRMT1 (IC50 = 8.8μM) and yeast-Hmt1p (IC50 = 3.0μM), by blocking peptide-substrate binding.IC50 value: 8.8μM (human PRMT1), 3.0μM (yeast-Hmt1p)Target: human PRMT1, yeast-Hmt1pin vitro: AMI-1 suppresses the transcriptional coactivator activity of PRMT1 and PRMT4 and it inhibits HIV-1 RT polymerase (IC50 = 5.0μM). PRMT1 methylates histone H4, and is essential for other subsequent histone modifications.[1] AMI-1 is the most active nonpeptidic inhibitor reported to be selective against PRMT1. AMI-1 is a selective PRMT inhibitor with a bisanionic structure that is related to compounds known to generate pleiotropic interactions with many proteins, should be further optimized before exploring additional binding pockets. [2]in vivo: AMI-1 is administered intranasally to chronic AIPI rats to determine PRMT effects on asthmatic parameters. AMI-1 inhibited the expression of COX2 in TGF-β-stimulated cells. AMI-1 administered to AIPI rats reduced COX2 production and humoral immune response, and it abrogated mucus secretion and collagen generation.[1]
(2,4-Dichloro-3,5-dimethoxyphenyl) methyl 6-O-β-D-glucopyranosyl-β-D-glucopyranoside is an anticancer agent that inhibits the proliferation of lung cancer A549 cells (IC50=29 μΜ). (2,4-Dichloro-3,5-dimethoxyphenyl) methyl 6-O-β-D-glucopyranosyl-β-D-glucopyranoside can be obtained from Lilium regale and can be used in cancer research[1].
Apronal (Allylisopropylacetylurea, Apronalide) is a hypnotic and sedative drug that has been withdrawn in several countries due to side effects.
Febuxostat n-butyl isomer is an impurity of Febuxostat. Febuxostat is selective xanthine oxidase inhibitor with a Ki of 0.6 nM[1].
Penicillin V-d5 (Phenoxymethylpenicillin-d5) is the deuterium labeled Penicillin V. Penicillin V (Phenoxymethylpenicillin) is an orally active antibiotic. Penicillin V inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis[1][2][3][4].
S32826 is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 inhibits LPA release from adipocytes[1].
15-Azido-pentadecanoic acid is a click chemistry reagent containing an azide group. Azido Palmitic Acid can be used to identify and characterize post-translationally palmitylated proteins with using a simple and robust two-step labeling and detection technique[1].
8-Prenyldaidzein is an isoflavonoid, that can be isolated from Bituminaria morisiana. 8-Prenyldaidzein shows antioxidant activity[1].