CP-868388 free base is a potent, selective and orally active PPARα agonist with a Ki value of 10.8 nM. CP-868388 free base has little or no affinity for PPARβ (Ki of 3.47 μM) and PPARγ. CP-868388 free base has hypolipidemic and anti-inflammatory actions[1].
Veltuzumab (IMMU-106) is a humanized anti-CD20 monoclonal antibody. Veltuzumab has low EC50 value of 0.08-0.09 μg/mL in the Daudi cell line. Veltuzumab can be used for the research of cancer including non-Hodgkin lymphoma (NHL)[1].
ETC-159 is a potent, orally available PORCN inhibitor. It inhibits β-catenin reporter activity with an IC50 of 2.9 nM.
9-(β-D-Xylofuranosyl)guanine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH with IC50s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.
Sanggenol P, a flavonoid, shows anti-HBV activity on HepG2.2.15 cell line in vitro[1].
Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide[1].
MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity[1][2].
NCT-504 is a selective allosteric inhibitor of PIP4Kγ, with an IC50 of 15.8 μM. NCT-504 is potential for the research of Huntington's disease[1].
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.
Lanreotide acetate (BIM 23014 acetate) is a somatostatin analogue with antineoplastic activity. Lanreotide acetate can be used for carcinoid syndrome[1][2].
β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol[1][2][3].
Darifenacin HBr(UK88525) is a selective M3 muscarinic receptor antagonist with pKi of 8.9.IC50 value: 8.9 (pKi) [1]Target: M3 receptorin vitro: Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced concentration-dependent contraction of the isolated bladder of rat [1]. Darifenacin produces a concentration dependent increase in R123 (P-gp probe) accumulation in MDCK cells. Darifenacin stimulates ATPase activity in P-gp membrane in a clear concentration dependent response manner with an estimated ED50 value of 1.6?μM. Darifenacin (100 nM) shows a significantly greater permeability for darifenacin in the basolateral to apical direction resulting in an efflux ratio in BBMEC monolayers of approximately 2.6 [2].in vivo: Darifenacin produces dose-dependent inhibition of amplitude of volume-induced bladder contractions(VIBCAMP), producing 35% inhibition at dose of 283.3 nmol/kg and maximal inhibition of approximately 50–55% [1]. Darifenacin (0.1 mg/kg i.v.) reduces bladder afferent activity in both Aδ and C fibers in female Sprague-Dawley rats, the decrease in afferent spikes in C fibers may be more pronounced than that in Aδ fibers [3].
ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively.
Microcystin-LY, a cyclic heptapeptide toxin from the cyanobacterium Microcystis aeruginosa[2], acts as an activator of the Nrf2 pathway to induce oxidative stress response, and the induction effect is most obvious at 3μM.[1].
MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.
Olanzapine D3 (LY170053 D3) is the deuterium labeled Olanzapine. Olanzapine is 5-HT2 and D1/D2 antagonist. Olanzapine is an antipsychotic agent with anticholinergic properties[1]. Olanzapine induces autophagy, mitochondrial damage and mitophagy in human SH-SY5Y neuronal cell line[2].
THP-PEG9-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Homo Sildenafil-d5 is the deuterium labeled Homo Sildenafil. Homo Sildenafil, an analog of Sildenafil, acts as a phosphodiesterase inhibitor[1][2].
GR 144053 trihydrochloride is a selective and non-peptic GPIIb/IIIa inhibitor (IC50=37 nM)[1].
SLF1081851 (16 d) is an effective Sphingolipid Transporter 2 (Spns2) (S1P transporter) inhibitor with an IC50 value of 1.93 μM (S1P), SLF1081851 inhibits SphK2 with an IC50 value of ≈ 30 μM (SphK2), and is at least 15-fold more selective for SphK2 than SphK1. SLF1081851 has the potential to investigate Spns2 biology and can be used for autoimmune encephalomyelitis (EAE) research[1].
Amantadine Hydrochloride is an antiviral and an antiparkinsonian drug.Target: Influenza VirusAmantadine is an antiviral that is used in the prophylactic or symptomatic treatment of influenza A. It is also used as an antiparkinsonian agent, to treat extrapyramidal reactions, and for postherpetic neuralgia. Amantadine binding of M2, based on studies of a peptide representing the M2 transmembrane segment in dodecylphosphocholine micelles. Amantadine competes with protons for binding to the deprotonated tetramer, thereby stabilizing the tetramer in a slightly altered conformation. This model accounts for the observed inhibition of proton flux by amantadine [1]. In contrast to most other described channel-blocking molecules, amantadine causes the channel gate of NMDA receptors to close more quickly. Amantadine binding inhibits current flow through NMDA receptor channels but show that its main inhibitory action at pharmaceutically relevant concentrations results from stabilization of closed states of the channel [2].
8-Bromo-ATP (8-Bromoadenosine 5'-triphosphate), an ATP analogue, is a purinergic P2X receptor agonist. 8-Bromo-ATP shows cytotoxic to multiple myeloma cells with an IC50 of 23.1 μM[1][2][3].
1-(Methyl-d3)piperazine is the deuterium labeled N-Methylpiperazine[1].
Stigmasterol glucoside is a sterol isolated from P. urinaria with high antioxidant and anti-inflammatory activities[1], act as an inhibitor of 5α-reductase with an IC50 of 27.2 µM[2].
N2-iso-Butyroyl-5’-O-(4,4’-dimethoxytrityl)-3’-O-methylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7)[1].
Hydrochlorothiazide is a diuretic drug of the thiazide class. Target: OthersHydrochlorothiazide belongs to thiazide class of diuretics. It reduces blood volume by acting on the kidneys to reduce sodium (Na) reabsorption in the distal convoluted tubule. The major site of action in the nephron appears on an electroneutral Na+-Cl? co-transporter by competing for the chloride site on the transporter. By impairing Na transport in the distal convoluted tubule, hydrochlorothiazide induces a natriuresis and concomitant water loss. Thiazides increase the reabsorption of calcium in this segment in a manner unrelated to sodium transport. Additionally, by other mechanisms, Hydrochlorothiazide is believed to lower peripheral vascular resistance [1].
3,6-Dichlorotrimellitic anhydride is the key precursor that is used for preparing a variety of dichlorinated fluoresceins and rhodamines such as TET and HEX. These chlorinated fluoresceins and rhodamines are widely used for labeling oligos and in DNA sequencing.
Boc-Lys(Fmoc)-OH is a lysine derivative[1].