Pencycuron-d5 is the deuterium labeled H-DL-Abu-OH[1].
Enalaprilat (MK-422 anhydrous), the active metabolite of the oral prodrug Enalapril, is a potent, competitive and long-acting angiotensin-converting enzyme (ACE) inhibitor, with an IC50 of 1.94 nM. Enalaprilat can be used for the research of hypertension[1][2][3].
Stepronin (Prostenoglycine) is an orally active expectorant (inhalation administration is preferable to oral administration). Stepronin inhibits airway secretion in vitro by reducing Cl- secretion from epithelial cells and mucus glycoprotein secretion from submucosal glands[1].
ACT-777991 is an orally active and selective CXCR3 antagonist. ACT-777991 has microsomes and hepatocytes stability across animal models. ACT-777991 inhibits the migration of activated T cells toward CXCL11[1].
18:0 EPC chloride is a synthetic cationic phospholipid. 18:0 EPC chloride (at the critical synergistic concentrations of 2.34-2.93 μM) significantly improves the inactivation effect of eugenol against Escherichia coli[1].
Alkyne derivative of BDP FL, an analog of BODIPY? FL alkyne. BDP FL is a borondipyrromethene dye, a bright and photostable fluorophore which emits in fluorescein (FAM) channel. Unlike FAM, BDP FL is very photostable. Its brightness is similar to fluorescein. This alkyne can be conjugated with a number of azide-containing molecules by copper-catalyzed Click Chemistry
3-Methylanisole-d3 is the deuterium labeled 3-Methylanisole[1].
Trk-IN-3 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively[1]. Anti-hyperalgesic effect[1].
DL-Threonine methyl ester hydrochloride is a threonine derivative[1].
(Z)-Pseudoginsenoside Rh2 is the (Z) isoform of Pseudoginsenoside Rh2 (HY-125825), which is synthesized from Ginsenoside Rh2, possesses anti-cancer activitied[1].
Sodium Channel inhibitor 2 is a sodium channel blocker extracted from patent WO 2004011439 A2, compound 3c.
Quercetin-3,4-di-O-glucoside is a flavonoid that can be isolated from Allium cepa[1].
17β-Dihydroequilenin 3-sulfate-4,16,16-d3 (sodium) is the deuterium labeled 17β-Dihydroequilenin 3-sulfate-4,16,16.
ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
Calycosin (Cyclosin) is a natural active compound with anti-oxidative and anti-inflammation activity.IC50 value:Target: in vitro: calycosin had obvious anti-proliferation effects on SKOV3 cells in a dose- and time-dependent manner. calycosin up-regulated the Bax/Bcl-2 ratio and cleaved caspase-3, cleaved caspase-9 expression in a dose-dependent manner. In summary, calycosin might exert anti-growth and induce-apoptosis activity against ovarian cancer SKOV3 cells through activating caspases and Bcl-2 family proteins, therefore presenting as a promising therapeutic agent for the treatment of ovarian cancer [1]. Both calycosin and genistein inhibited proliferation and induced apoptosis in MCF-7 breast cancer cells, especially after treatment with calycosin. Treatment of MCF-7 cells with calycosin or genistein resulted in decreased phosphorylation of Akt, and decreased expression of its downstream target, HOTAIR [2]. incubation of calycosin resulted in enhanced expression ERβ in MCF-7 and T-47D cells, rather than MDA-231 and MDA-435 cells. Moreover, with the upregulation of ERβ, successive changes in downstream signaling pathways were found, including inactivation of insulin-like growth factor 1 receptor (IGF-1R), then stimulation of p38 MAPK and suppression of the serine/threonine kinase (Akt), and finally poly(ADP-ribose) polymerase 1 (PARP-1) cleavage [3].in vivo: calycosin stimulated a dramatic increase in uterine weight and downregulated the level of ERα protein in OVX mice [4].
Yukovanol is a flavanone, which can be isolated from the roots of some Citrus species[1].
Amiodarone is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM. Target: Potassium ChannelAmiodarone shows beta blocker-like and potassium channel blocker-like actions on the SA and AV nodes, increases the refractory period via sodium- and potassium-channel effects, and slows intra-cardiac conduction of the cardiac action potential, via sodium-channel effects. Amiodarone (2-butyl, 3-(4-diethylaminoethoxy, 3,5-diiodo, benzoyl) benzofuran hydrochloride), an anti-anginal drug which causes coronary dilatation and depresses myocardial oxygen consumption, was found to protect anaesthetized guinea-pigs against ouabain-induced ventricular fibrillation.2. A 5% (73.4 mM) solution of amiodarone had no local anaesthetic action on guinea-pig skin [1]. Amiodarone proved safe in patients with severe congestive heart failure and severe myocardial damage. Its clinical efficacy was related to its electrophysiologic properties and to two unique properties: its wide safety margin and its cumulative effect [2].
STING modulator-3 is a STING inhibitor. STING modulator-3 inhibits R232 STING with an Ki value of 43.1 nM in scintillation proximity assay. STING modulator-3 has no effect on IRF-3 activation or TNF-β induction in THP-1 cells[1].
WKYMVM is a potent N-formyl peptide receptor (FPR1) and FPRL1/2 agonist, also activates several leukocyte effector functions such as chemotaxis, mobilization of complement receptor-3, and activation of the NADPH oxidase[1][2].
Juniper camphor is a sesquiterpene compound isolated from camphor blue oil, the high-boiling fraction of camphor[1].
BRG1-IN-1 (Compound 11d) is a potent inhibitor of BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors[1].
Wilforlide B, a natural norditerpenoid, possesses anti-tumor activity in human cancer cells[1].
Bromo-PEG2-bromide is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].
Bleselumab (ASKP 1240) is a human anti-CD40 monoclonal antibody (mAb). Bleselumab binds to human CD40 with high affinity (Kd: 0.24 nM). Bleselumab inhibits immune responses by blocking the interaction of CD40 with its ligand CD40L. Bleselumab prevents organ transplant rejection[1].
eIF4A3-IN-6 is a potent inhibitor of eukaryotic initiation factor 4A (eIF4A), such as eIF4AI and eIF4AII. eIF4A3-IN-6 has the potential for the research of eIF4A dependent diseases, including the research of cancer (extracted from patent US20170145026A1)[1].
HDAC-IN-40 is a potent alkoxyamide-based HDAC inhibitor with Ki values of 60 nM and 30 nM for HDAC2 and HDAC6, respectively. HDAC-IN-40 had antitumor effects[1].
AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.
Irinotecan-d10 ((+)-Irinotecan-d10) hydrochloride is the deuterium labeled Irinotecan. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex[1][2].
Ifinatamab is monoclonal immunoglobulin G1-kappa with anti-human B7 homolog 3 protein (Human B7-H3). Ifinatamab is a glycoforme α immunomodulateur[1].
Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can attenuate cocaine-induced locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer[1][2][3][4].