(Rac)-Apremilast D5 ((Rac)-CC-10004 D5) is a deuterium labeled (R)-Apremilast. (R)-Apremilast ((R)-CC-10004) is a enantiomer of Apremilast[1].
2,2′,4,5,5′-Pentachlorobiphenyl-3′,4′,6′-d3 is the deuterium labeled 2,2′,4,5,5′-Pentachlorobiphenyl[1].
2'',4''-Di-O-(E-p-Coumaroyl)afzelin (compound 36) is a compound isolated from Epimedium sagittatum[1].
[Leu31,Pro34]- Neuropeptide Y (porcine), a Neuropeptide Y (NPY) analog, is a selective NPY Y1 receptor agonist. [Leu31,Pro34]- Neuropeptide Y (porcine) exhibits anxiolytic effects[1][2].
23-Nor-6-oxopristimerol is a phenolic dinor-triterpene[1].
CP-465022 hydrochloride is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes[1][2].
Bis-propargyl-PEG8 (compound 16e) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
HG106 is a potent SLC7A11 inhibitor. HG106 markedly decreased cystine uptake and intracellular glutathione biosynthesis. HG106 can be used for the research of KRAS-mutant lung adenocarcinoma[1].
Syk Inhibitor II dihydrochloride dihydrate is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride dihydrate inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride dihydrate shows less potent against other kinases and has anti-allergic effect[1].
EN884 is a BRD4 degrader via a SKP1- and proteasome-dependent manner. EN884 can be used in synthetic proteolysis targeting chimeras (PROTACs)[1].
Nicotinamide Hydrochloride is a form of vitamin B3 or niacin that inhibits sirtuin 2 (SIRT2) activity in vitro, with an EC50 of 2 μM. Nicotinamide Hydrochloride inhibits up to 90% melanoma cell number and increases cellular NAD+, ATP, ROS levels. Nicotinamide Hydrochloride inhibts tumor growth in vivo and improves survival of melanoma-bearing mice, which can be used for the research of skin cancers such as melanoma[1].
(Rac)-Levomepromazine-d3 ((Rac)-Methotrimeprazine-d3) hydrochloride is a labelled racemic Methotrimeprazine, which is a phenothiazine which has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors[1][2].
Isobutyl-deoxynyboquinone (IB-DNQ) is a selective substrate for NAD(P)H:quinone oxidoreductase (NQO1), produces ROS, and induces cytotoxicity in cancer cells in an NQO1-dependent manner; has improved solubility and biocompatibility in comparison with DNQ; a superior drug candidate for evaluating anticancer activities and tolerability in vivo.
2-Nitrobenzoic acid-d4 is the deuterium labeled 2-Nitrobenzoic acid[1].
p-Hydroxybenzaldehyde is a one of the major components in Dendrocalamus asper bamboo shoots, with antagonistic effect on GABAA receptor of the α1β2γ2S subtype at high concentrations.
PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs.IC50 value: 9 nMTarget: c-Metin vitro: PHA-665752 significantly inhibits c-Met kinase activity with Ki of 4 nM, and exhibits >50-fold selectivity for c-Met compared with various tyrosine and serine-threonine kinases. PHA-665752 potently inhibits the HGF-stimulated c-Met autophosphorylation with IC50 of 25-50 nM. PHA-665752 also significantly blocks HGF- and c-Met-dependent functions such as cell motility and cell proliferation with IC50 of 40-50 nM and 18-42 nM, respectively. In addition, PHA-665752 potently inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream of c-Met such as Gab-1, ERK, Akt, STAT3, PLC-γ, and FAK in multiple tumor cell lines [1]. PHA-665752 inhibits cell growth in TPR-MET-transformed BaF3 cells with IC50 of <60 nM, and inhibits constitutive cell motility and migration by 92.5% at 0.2 μM. Inhibition of c-Met by PHA665752 (0.2 μM) also induces cell apoptosis of 33.1% and G1 cell cycle arrest with cells in G1 phase increasing from 42.4% to 77.0%. PHA665752 can cooperate with rapamycin to inhibit cell growth of TPR-MET-transformed BaF3 cells and non-small cell lung cancer H441 cells [2].in vivo: Administration of PHA-665752 induces a dose-dependent tumor growth inhibition of S114 xenografts by 20 %, 39% and 68%, at dose of 7.5, 15, and 30 mg/kg/day, respectively [1]. PHA665752 treatment significantly reduces the tumor growth of NCI-H69, NCI-H441 and A549 in mouse xenografts by 99%, 75%, and 59%, respectively. PHA665752 also significantly inhibits angiogenesis by >85%, due to decreasing the production of vascular endothelial growth factor and increasing the production of the angiogenesis inhibitor thrombospondin-1 [3].
EC144 is a potent and selective inhibitor of heat shock protein 90 (Hsp90) with an IC50 of 1.1 nM. EC144 inhibits tumor growth and causes partial tumor regressions. EC144 has the potential for the research of cancer diseases[1].
D159687 is a selective PDE4D inhibitor[1].
4-(2-Carboxyphenyl)-7-diethylamino-2-(7-diethylamino-2-oxochroman-3-yl)-chromylium perchlorate is a carboxyl functionalized organic fluorescent dye (λex~650 nm, λem~690 nm)[1].
YS-363 is a potent, selective, and orally active EGFR inhibitor, with IC50s of 0.96 nM and 0.67 nM for wild-type and L858R mutant forms of EGFR, respectively. YS-363 can induce G0/G1 cell cycle arrest and apoptosis[1].
DDP-38003 dihydrochloride is an novel, orally available inhibitor of histone lysine-specific demethylase 1A (KDM1A/LSD1) with an IC50 of 84 nM.
4-Nitrophenyl Laurate is a class of 4-nitrophenyl ester, which can be used as enzyme substrate[1].
Dapoxetine HCl is a short-acting novel selective serotonin reuptake inhibitor(SSRI).Target: SSRIDapoxetine hydrochloride is a short-acting novel selective serotonin reuptake inhibitor marketed for the treatment of premature ejaculation in men. Premature ejaculation (PE) is the most common male sexual disorder, estimated to affect up to 30% of men. Dapoxetine is the only drug with regulatory approval for such an indication. The treatment of PE consists of primarily off-label use of oral selective serotonin reuptake inhibitors (SSRIs) via either on-demand or daily delivery.
trans-4-Nitrocinnamoyl chloride is used as derivatization reagent[1].
1-(β-D-Xylofuranosyl)uracil is a uridine analog. Uridine has potential antiepileptic effects, and its analogs can be used to study anticonvulsant and anxiolytic activities, as well as to develop new antihypertensive agents[1].
20,26-Dihydroxyecdysone is a predominant ecdysteroid metabolite[1].
CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities[1].
Litifilimab is a humanized IgG1-κ antibody targeting to C-type lectin domain family 4 member C (CLEC4C). Litifilimab can be used for cutaneous lupus erythematosus (CLE) study[1][2].
N6-Bz-5'-O-DMTr-3'-deoxyadenosine-2'-O-CED-phosphoramidite 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].
G4RGDSP, Integrin-binding peptide is a cell integrin-binding peptide that targets integrin receptors. G4RGDSP, integrin-binding peptide is coupled to alginate to increase the viability of cells in the scaffold. G4RGDSP, integrin-binding peptide can be used as an extrudable carrier for chondrocyte delivery for the study of 3D printing technology[1][2]